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Patel, Simmi, William J. McAuley, Michael T. Cook, Yi Sun, Shaheen Hamdy, and Fang Liu. "The Swallowing Characteristics of Thickeners, Jellies and Yoghurt Observed Using an In Vitro Model." Dysphagia 35, no. 4 (November 9, 2019): 685–95. http://dx.doi.org/10.1007/s00455-019-10074-1.
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Abstract Drinks and foods may be thickened to improve swallowing safety for dysphagia patients, but the resultant consistencies are not always palatable. Characterising alternative appetising foods is an important task. The study aims to characterise the in vitro swallowing behaviour of specifically formulated thickened dysphagia fluids containing xanthan gum and/or starch with standard jellies and yoghurt using a validated mechanical model, the “Cambridge Throat”. Observing from the side, the model throat can follow an experimental oral transit time (in vitro-OTT) and a bolus length (BL) at the juncture of the pharynx and larynx, to assess the velocity and cohesion of bolus flow. Our results showed that higher thickener concentration produced longer in vitro-OTT and shorter BL. At high concentration (spoon-thick), fluids thickened with starch-based thickener showed significantly longer in vitro-OTT than when xanthan gum-based thickener was used (84.5 s ± 34.5 s and 5.5 s ± 1.6 s, respectively, p < 0.05). In contrast, at low concentration (nectar-like), fluids containing xanthan gum-based thickener demonstrated shorter BL than those of starch-based thickener (6.4 mm ± 0.5 mm and 8.2 mm ± 0.8 mm, respectively, p < 0.05). The jellies and yoghurt had comparable in vitro-OTT and BL to thickeners at high concentrations (honey-like and spoon-thick), indicating similar swallowing characteristics. The in vitro results showed correlation with published in vivo data though the limitations of applying the in vitro swallowing test for dysphagia studies were noted. These findings contribute useful information for designing new thickening agents and selecting alternative and palatable safe-to-swallow foods.
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Chakder, S., G. J. Rosenthal, and S. Rattan. "In vivo and in vitro influence of human recombinant hemoglobin on esophageal function." American Journal of Physiology-Gastrointestinal and Liver Physiology 268, no. 3 (March 1, 1995): G443—G450. http://dx.doi.org/10.1152/ajpgi.1995.268.3.g443.
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The purpose of the present investigation was to examine the influence of a nitric oxide scavenger, hemoglobin (Hb), on esophageal function. Intraluminal pressures of anesthetized opossums were recorded from lower esophageal sphincter (LES) and 1, 5, and 9 cm above the LES. The influence of a representative Hb-based oxygen carrier was examined on swallowing-induced esophageal peristalsis and LES relaxation. In in vitro studies, LES relaxation and esophageal peristaltic contractions were induced by the activation of nonadrenergic noncholinergic (NANC) neurons by electrical field stimulation (EFS). Hb caused significant impairment in swallowing- and EFS-induced LES relaxation and a significant increase in the speed of esophageal peristalsis. In some experiments, swallowing caused simultaneous contractions in the esophagus following Hb administration. Although Hb completely blocked LES relaxation by NO and significantly attenuated that by NANC nerve stimulation, it had no significant effect on isoproterenol-induced LES relaxations. The data support the role of NO in LES relaxation and esophageal peristalsis. This esophageal model may be important in understanding the influence of NO inhibitors and scavengers in gastrointestinal motility.
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Malouh, Marwa A., Julie A. Y. Cichero, Yu Sun, Esther T. L. Lau, Lisa M. Nissen, and Kathryn J. Steadman. "Medication Lubricants for Oral Delivery of Drugs: Oral Processing Reduces Thickness, Changes Characteristics, and Improves Dissolution Profile." Pharmaceutics 16, no. 3 (March 18, 2024): 417. http://dx.doi.org/10.3390/pharmaceutics16030417.
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Swallowing oral solid dosage forms is challenging for those who have medication swallowing difficulties, including patients with dysphagia. One option is to mix the drug (whole or crushed) with a thick vehicle (medication lubricant). Previous in vitro studies consistently suggest that thick vehicles could impact the dissolution of solid dosage forms, potentially influencing their therapeutic effectiveness, but do not account for changes that happen during oral processing and swallowing. This study aims to investigate the potential impact of medication lubricants on drug release and examine the effect of oral processing. In vitro dissolution of whole and crushed paracetamol tablets mixed with five commercially available medication lubricants (two IDDSI level 2, two IDDSI level 3, and one IDDSI level 4) were tested with and without oral processing; a medication lubricant with/without paracetamol was placed in the mouth (five healthy volunteers), prepared for swallowing, but then expectorated and assessed for physical characteristics and drug release. Medication lubricants, both alone and mixed with crushed paracetamol tablets, showed a significant decrease in viscosity after oral processing. Without oral processing, IDDSI level 3 and 4 lubricants significantly delayed the dissolution of paracetamol tablets. After oral processing, particularly with crushed tablets, there was a substantial increase in the dissolution rate. These findings suggest that dissolution testing overestimates the impact of medication lubricants on drug dissolution. Therefore, using in vitro dissolution tests to predict the dissolution rate of medications mixed with thick vehicles is discouraged. It is essential to consider ways to incorporate the effects of the oral environment and oral processing on thick vehicles used for oral medication administration.
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Fujiso, Yo, Nicolas Perrin, Julian van der Giessen, Nihal Engin Vrana, Fabrice Neveu, and Virginie Woisard. "Swall-E: A robotic in-vitro simulation of human swallowing." PLOS ONE 13, no. 12 (December 19, 2018): e0208193. http://dx.doi.org/10.1371/journal.pone.0208193.
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Marconati, Marco, and Marco Ramaioli. "The role of extensional rheology in the oral phase of swallowing: an in vitro study." Food & Function 11, no. 5 (2020): 4363–75. http://dx.doi.org/10.1039/c9fo02327e.
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In vitro swallowing experiments suggest that thin, viscoelastic liquids with strong apparent extensional viscosity lead to fast transit, lower oral residues and a compact bolus leaving the oral cavity.
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Eremin, V. A., and E. V. Blynskaya. "Modern approaches to assessing the quality of orally disintegrating tablets." Farmacevticheskoe delo i tehnologija lekarstv (Pharmacy and Pharmaceutical Technology), no. 6 (December 19, 2023): 8–17. http://dx.doi.org/10.33920/med-13-2306-01.
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Orally disintegrating tablets (ODTs) are the preferred and accepted solid dosage forms by patients. These tablets disintegrate in the oral cavity within a short period, providing an advantage for individuals who have difficulty swallowing. Quality control of ODTs can be achieved through measures such as friability, porosity, hardness, wetting time, water absorption capacity, in vitro disintegration test, and dissolution test. This article summarizes the advantages and in vitro quality control tests of orally disintegrating tablets.
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Tafere, Chernet, Zewdu Yilma, Solomon Abrha, and Adane Yehualaw. "Formulation, in vitro characterization and optimization of taste-masked orally disintegrating co-trimoxazole tablet by direct compression." PLOS ONE 16, no. 3 (March 16, 2021): e0246648. http://dx.doi.org/10.1371/journal.pone.0246648.
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Introduction Orally disintegrating tablet (ODT) is a dosage form that overcomes the problem of swallowing which is prevalent in about 35% of the general population. Co-trimoxazole (CTX) is given for patients with HIV for the prophylaxis of opportunistic infection (OI), commonly for pneumocystis carinii pneumonia. It was reported that CTX was associated with a 25–46% reduction in mortality among individuals infected with HIV in sub-Saharan Africa. Esophageal candidiasis which usually comes along with HIV/AIDS is one of AIDS defining illness affecting up to 1 in 5 of people with AIDS. This opportunistic illness is manifested by painful or difficulty of swallowing. In this respect, CTX ODT offer the advantages of both liquid dosage forms in terms of easy swallowing thereby improve patient compliance and solid dosage forms in terms of dose uniformity, stability, lower production, and transportation costs. The objective of this study was to formulate, characterize and optimize CTX ODT which could overcome swallowing problem and improve patient compliance. Co-trimoxazole ODTs were prepared by direct compression technique using a semi synthetic super disintegrant (crospovidone) along with other excipients. Two taste masking techniques were employed, addition of sweetening agent, and solid dispersion by using a pH sensitive polymer, Eudragit E-100 at different ratios (1:1, 1:2 and 1:3). Taste masking was determined by comparing taste threshold value and in vitro drug release. Preliminary study was used to investigate the effect of crospovidone, compression force (CF) and Hydroxypropyl cellulose (HPC) on disintegration time, friability and wetting time (WT). Factorial design was used as it enables simultaneous evaluation of formulation variables and their interaction effect. From the preliminary study, the factors that were found significant were further optimized using central composite design. Design-Expert 8.0.7.1 software was employed to carry out the experimental design. The bitterness threshold concentration of Trimethoprim was found to be 150 μg/ml and the in vitro drug release of the three batches of drug to polymer ratio (F1:1, 1:2 and 1:3) was 2.80±0.05, 2.77±0.00 and 2.63±0.00 respectively. From the optimization study, the optimal concentration for the superdisintegrant was 8.60% w/w and a CF of 11.25 KN which gave a rapid disintegration and WT of 13.79 and 23.19 seconds respectively and a friability of 0.666%. Conclusion In this study, co-trimoxazole ODT was formulated successfully. Central composite design was effectively used to model and optimize friability, DT and WT. The method was found effective for estimating the effect of independent variables on the dependent variables by using polynomial equation and surface plots. Optimization of the response variables was possible by using both numerical and graphical optimization and the predicted optimal conditions were confirmed experimentally and were found to be in good agreement within 5% of the predicted responses. The results of the study showed that CTX ODT had significantly rapid disintegration, less than 1% friability and enhanced dissolution profiles. The successful formulation of CTX ODT can solve difficulty of swallowing of conventional tablets for some group of patients which are unable to swallow solid oral dosage form.
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Seifelnasr, Amr, Xiuhua Si, Peng Ding, and Jinxiang Xi. "Liquid Dynamics in the Upper Respiratory–Digestive System with Contracting Pharynx Motions and Varying Epiglottis Angles." Liquids 4, no. 2 (May 15, 2024): 415–31. http://dx.doi.org/10.3390/liquids4020022.
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Swallowing disorders, or dysphagia, can lead to bolus aspiration in the airway, causing serious adverse health effects. Current clinical interventions for dysphagia are mainly empirical and often based on symptoms rather than etiology, of which a thorough understanding is still lacking. However, it is challenging to study the swallowing process that involves sequential structural motions and is inaccessible to standard visualization instruments. This study proposed an in vitro method to visualize swallowing hydrodynamics and identify the fundamental mechanisms underlying overflow aspirations. An anatomically accurate pharynx–epiglottis model was developed from patient-specific CT images of 623 µm isotropic resolution. A compliant half-pharynx cast was prepared to incorporate dynamic structures and visualize the flow dynamics in the mid-sagittal plane. Three locations of frequent overflow aspiration were identified: the epiglottis base, cuneiform tubular recesses, and the interarytenoid notch. Water had a consistently higher aspiration risk than a 1% w/v methylcellulose (MC) solution. The contracting–relaxing pharynx and flapping epiglottis spread the liquid film, causing a delayed esophageal entry and increased vallecular residual, which was more pronounced with the MC solution. Dispensing the liquid too slowly resulted in water aspiration, whereas this was not observed with the MC solution. An incomplete epiglottis inversion, such as horizontal or down-tilt 45°, aggravated the aspiration risks of water. This study suggests that it is practical to use anatomically accurate respiratory–digestive models to study the swallowing process by incorporating varying physiological details.
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Pawar, Harshal Ashok, and Pooja Rasiklal Joshi. "Development and Evaluation of Taste Masked Granular Formulation of Satranidazole by Melt Granulation Technique." Journal of Pharmaceutics 2014 (February 12, 2014): 1–7. http://dx.doi.org/10.1155/2014/789676.
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Drugs from nitroimidazole category are generally bitter in taste. Oral formulation with bitter taste is not palatable. Geriatrics and pediatrics patients usually suffer from swallowing difficulties. Many other patients in some disease conditions avoid swallowing tablets. Satranidazole is a new nitro-imidazole derivative with bitter taste and is available in market as film coated tablet. The purpose of this research was to mask the bitter taste of Satranidazole by coating complexation with low melting point wax and Eudragit EPO. Different types of wax (glyceryl monostearate, stearic acid and cetyl alcohol) were tried for taste masking. The drug to stearic acid ratio 1 : 2 was found to be optimum on the basis of taste evaluation and in vitro release. The formulated granules were found to possess good flow property. FTIR studies confirmed that there was no interaction between drug and excipients. Scanning Electron Microscopy of drug and the optimized batch of granules was performed. The in vitro release of drug from granules was compared with marketed tablet formulation. The taste masked granules of optimized batch showed 87.65% release of drug in 1 hr which is comparable to that of marketed tablet formulation.
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Rekling, Jens C., and Jack L. Feldman. "Calcium-Dependent Plateau Potentials in Rostral Ambiguus Neurons in the Newborn Mouse Brain Stem In Vitro." Journal of Neurophysiology 78, no. 5 (November 1, 1997): 2483–92. http://dx.doi.org/10.1152/jn.1997.78.5.2483.
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Rekling, Jens C. and Jack L. Feldman. Calcium-dependent plateau potentials in rostral ambiguus neurons in the newborn mouse brain stem in vitro. J. Neurophysiol. 78: 2483–2492, 1997. The nucleus ambiguus contains vagal and glossopharyngeal motoneurons and preganglionic neurons involved in respiration, swallowing, vocalization, and control of heart beat. Here we show that the rostral compact formation's ambiguus neurons, which control the esophageal phase of swallowing, display calcium-dependent plateau potentials in response to tetanic orthodromic stimulation or current injection. Whole cell recordings were made from visualized neurons in the rostral nucleus ambiguus using a slice preparation from the newborn mouse. Biocytin-labeling revealed dendritic trees with pronounced rostrocaudal orientations confined to the nucleus ambiguus, a morphological profile matching that of vagal motoneurons projecting to the esophagus. Single-stimulus orthodromic activation, using an electrode placed in the dorsomedial slice near the nucleus tractus solitarius, evoked single excitatory postsynaptic potentials (EPSPs) or short trains of EPSPs (500 ms to 1 s). However, tetanic stimulation (5 pulses, 10 Hz) induced voltage-dependent afterdepolarizations or long-lasting plateau potentials (>1 min) with a constant firing pattern. Depolarizing or hyperpolarizing current pulses elicited voltage-dependent afterdepolarizations or plateau potentials lasting a few seconds to several minutes. Constant spike activity accompanied the long-lasting plateau potentials, which ended spontaneously or could be terminated by weak hyperpolarizing current pulses. Current-induced afterdepolarizations and plateau potentials were dependent on extracellularand intracellular Ca2+, as they were blocked completely by extracellular Co2+, Cd2+, or intracellular bis-( o-aminophenoxy)- N,N,N′,N′-tetraacetic acid (BAPTA). Orthodromically induced afterdepolarizations and plateau potentials were blocked by intracellular BAPTA. Afterdepolarizations and plateau potentials were completely blocked by substitution of extracellular Na+ with choline. Afterdepolarizations persisted in tetrodotoxin. We conclude that rostral ambiguus neurons have a Ca2+-activated inward current carried by Na+. Synaptic activation of this conductance may generate prolonged spike activity in these neurons during the esophageal phase of swallowing.
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Kogo, Mikihiko, Tadashi Yamanishi, Hidehiko Koizumi, and Tokuzo Matsuya. "Swallowing-like activity elicited in vitro in neonatal rat organ attached brainstem block preparation." Brain Research 955, no. 1-2 (November 2002): 24–33. http://dx.doi.org/10.1016/s0006-8993(02)03339-5.
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Drushel, R. F., D. M. Neustadter, L. L. Shallenberger, P. E. Crago, and H. J. Chiel. "The kinematics of swallowing in the buccal mass of Aplysia californica." Journal of Experimental Biology 200, no. 4 (February 1, 1997): 735–52. http://dx.doi.org/10.1242/jeb.200.4.735.
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Changes in the positions, shapes and movements of the feeding apparatus (buccal mass) of the marine mollusc Aplysia californica were studied in intact, transilluminated juveniles. The buccal mass assumes characteristic shapes as its internal structure, the radula/odontophore, moves anteriorly (protracts) or posteriorly (retracts). These shapes are especially distinctive when the radula/odontophore has protracted forwards fully, is close to its resting or neutral position, or has retracted backwards fully. We refer to the shapes that occur at full protraction, transition and full retraction as shape 1 (spherical), shape 2 (ovoid) and shape 3 (gamma-shaped), respectively. We introduce this shape nomenclature in order to avoid confusion with the existing terms protraction and retraction, which we reserve exclusively to describe the direction of movement of the radula/odontophore. The observed shape changes do not agree with those predicted on the basis of in vitro observations of a feeding head preparation, but are similar to shapes observed in vitro in the snail Lymnaea stagnalis. The buccal mass also rotates approximately 10 degrees dorsally during retraction, pivoting on the attachment to the mouth, before the subsequent protraction and return of the buccal mass to the transition shape. This rotation may be due to activation of the extrinsic muscles of the buccal mass. Plots of the buccal mass shape parameters eccentricity versus ellipticity create a two-dimensional shape space, which accurately quantifies the subtle transitions of shape between the different phases of the feeding cycle. Quantitative differences are observed between pure swallows and swallows with tearing behavior, but the qualitative shapes are similar. Hysteresis in the shape space plots of most swallows provides evidence for the hypothesis that protraction and retraction each have distinct 'active' and 'return' phases. The observed kinematic pattern imposes constraints on the internal structures of the buccal mass and may be used to infer the shape and positions of the radula and odontophore.
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Ershad, Abdul Latif, Ali Rajabi-Siahboomi, Shahrzad Missaghi, Daniel Kirby, and Afzal Rahman Mohammed. "Multi-Analytical Framework to Assess the In Vitro Swallowability of Solid Oral Dosage Forms Targeting Patient Acceptability and Adherence." Pharmaceutics 13, no. 3 (March 19, 2021): 411. http://dx.doi.org/10.3390/pharmaceutics13030411.
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A lack of effective intervention in addressing patient non-adherence and the acceptability of solid oral dosage forms combined with the clinical consequences of swallowing problems in an ageing world population highlight the need for developing methods to study the swallowability of tablets. Due to the absence of suitable techniques, this study developed various in vitro analytical tools to assess physical properties governing the swallowing process of tablets by mimicking static and dynamic stages of time-independent oral transitioning events. Non-anatomical models with oral mucosa-mimicking surfaces were developed to assess the swallowability of tablets; an SLA 3D printed in vitro oral apparatus derived the coefficient of sliding friction and a friction sledge for a modified tensometer measured the shear adhesion profile. Film coat hydration and in vitro wettability was evaluated using a high-speed recording camera that provided quantitative measurements of micro-thickness changes, simulating static in vivo tablet–mucosa oral processing stages with artificial saliva. In order to ascertain the discriminatory power and validate the multianalytical framework, a range of commonly available tablet coating solutions and new compositions developed in our lab were comparatively evaluated according to a quantitative swallowability index that describes the mathematical relationship between the critical physical forces governing swallowability. This study showed that the absence of a film coat significantly impeded the ease of tablet gliding properties and formed chalky residues caused by immediate tablet surface erosion. Novel gelatin- and λ-carrageenan-based film coats exhibited an enhanced lubricity, lesser resistance to tangential motion, and reduced stickiness than polyvinyl alcohol (PVA)–PEG graft copolymer, hydroxypropyl methylcellulose (HPMC), and PVA-coated tablets; however, Opadry® EZ possessed the lowest friction–adhesion profile at 1.53 a.u., with the lowest work of adhesion profile at 1.28 J/mm2. For the first time, the in vitro analytical framework in this study provides a fast, cost-effective, and repeatable swallowability ranking method to screen the in vitro swallowability of solid oral medicines in an effort to aid formulators and the pharmaceutical industry to develop easy-to-swallow formulations.
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Sherman, Ethan G., Patrick J. Antonelli, and Roger Tran-Son-Tay. "In vitro testing of tympanostomy tube occlusion." Otolaryngology–Head and Neck Surgery 141, no. 5 (November 2009): 598–602. http://dx.doi.org/10.1016/j.otohns.2009.08.019.
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Objective: Tympanostomy tubes (TTs) are commonly rendered nonfunctional by mucus plug formation. The purpose of this study was to determine whether an in vitro model could be developed to assess TT plug formation with results consistent with human trials. Study Design: An ear chamber was designed to mimic middle ear air and mucus flow conditions in post-TT otorrhea. TT occlusion was tested and correlated to published in vivo results. Methods: TTs that had previously been studied in vivo (Goode “T” and Reuter Bobbin collar buttons) were placed in the model chamber. Pooled, homogenized human middle ear mucus and an analog, egg white, were delivered at 80 μL per hour through the TTs. An air bolus was delivered every two minutes to simulate swallowing. Chamber pressure was monitored over 2.5 hours. Occlusion was determined by a pressure peak and visual confirmation. Results: Obstruction was found in 60 percent of the Reuter Bobbin and 40 percent of the Goode TTs using the mucus analog. These results are similar to those reported from previous in vivo studies. No plugging was reported for either TT using homogenized human ear mucus. Conclusions: The in vitro TT chamber simulates the in vivo environment and yields results consistent with in vivo observations. This model system may allow for rapid prototyping and evaluation of new TTs that may be less vulnerable to occlusion.
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Singh, Kehar, Gaikwad Dushyant Dadabhau, and Satbir Singh. "Formulation Design and Development of Fast Disintegrating Tablets of Losartan Potassium By Using Locast Bean Gum As Superdisintigrants." International Journal of Membrane Science and Technology 10, no. 5 (October 23, 2023): 1084–96. http://dx.doi.org/10.15379/ijmst.v10i5.3700.
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For patients who have trouble swallowing tablets, capsules, etc., fast dissolving drug delivery devices provide an option. Water is not necessary for the swallowing of fast dissolving pills because they dissolve instantly in the mouth. Using locust bean gum as a natural superdisintegrant, the present work set out to produce fast-dissolving tablets of losartan potassium. Perform pre formulation studies like partition coefficient, solubility and identification of drug. The influence of precompressional parameters like interaction studies and compatibility. Other tablet properties were examined, as well as the impact of formulation parameters on losartan potassium disintegration and in-vitro dissolution. The findings indicated that the 7.5% concentration of locust bean gum had good superdisintegrant qualities and produced quickly dissolving tablets. The best tablet formulation (F3) had a 20-second minimum disintegration time and a 30-minute maximum drug release of 98%. The locust bean gum was discovered to have a notable ability to be employed as a superdisintegrant, with a swelling index of 22. The DSC analysis and IR spectra demonstrated that there was no interaction of any type with the tablet's formulation ingredients. Accelerated short-term experiments on optimized formulation show no appreciable modifications to the formulation.
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Mahmood, Sura Zuhair, Hiba Sabah Sabry, Nora Zawar Yousif, and Zeina D. Salman. "OPTIMIZATION AND EVALUATION OF CHLORPHENIRAMINE MALEATE ORAL STRIP FOR PEDIATRIC USE." Asian Journal of Pharmaceutical and Clinical Research 11, no. 12 (December 7, 2018): 548. http://dx.doi.org/10.22159/ajpcr.2018.v11i12.28985.
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Objective: The goal of performing this study is to prepare an oral strip, especially designed for pediatric use that provides fast onset of action with ease of swallowing particularly for young individuals who suffer from difficulty of swallowing, in addition provides maximum therapeutic effectiveness by reducing the first pass effect.Materials and Methods: The oral strip was prepared by solvent casting technique through using different sole polymers (hydroxypropyl methylcellulose [HPMC] 15cp, HPMC 50cp, polyvinyl alcohol, and sodium carboxymethyl cellulose). Maltodextrin (MD) was added as the secondary polymer in different ratios to optimize the release parameters, and disintegration time (DT), three different plasticizers were employed (propylene glycol, dibutyl phthalate, and glycerin) to boost the film forming polymer characteristics.Results: From this study, it is obvious that F10 which composed of HPMC as a main polymer and MD as a secondary polymer in ratio 2:1, respectively, provides adequate physicochemical characteristics, in vivo/in vitro DT (40/36 s), respectively, nevertheless a satisfactory release parameters as (59.9%) released at 2 min and 80% of drug released at 14.8 min.Conclusion: The optimized formula is pretty encouraging to originate an oral strip that provides ease of administration, fast onset of action with wide acceptance for the pediatric population.
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Sharma, Deepak, Mankaran Singh, Dinesh Kumar, and Gurmeet Singh. "Formulation Development and Evaluation of Fast Disintegrating Tablet of Cetirizine Hydrochloride: A Novel Drug Delivery for Pediatrics and Geriatrics." Journal of Pharmaceutics 2014 (February 18, 2014): 1–8. http://dx.doi.org/10.1155/2014/808167.
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Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of Cetirizine Hydrochloride for allergic and respiratory disorders. As precision of dosing and patient's compliance become important prerequisite for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient’s acceptability. Hence, the present investigation was undertaken with a view to develop a fast disintegrating tablet of Cetirizine Hydrochloride which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as Sodium Starch Glycolate were optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug excipient compatibility and accelerated stability study. It was concluded that fast disintegrating tablets of Cetirizine Hydrochloride were formulated successfully with desired characteristics which disintegrated rapidly, provide rapid onset of action, and enhance the patient convenience and compliance.
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Sharma, Deepak. "Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate for Respiratory Disorders." ISRN Pharmaceutics 2013 (July 15, 2013): 1–8. http://dx.doi.org/10.1155/2013/674507.
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Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of salbutamol sulphate for respiratory disorders for pediatrics. As precision of dosing and patient's compliance become important prerequisites for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient’s acceptability. Hence, the present investigation were undertaken with a view to develop a fast disintegrating tablet of salbutamol sulphate which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as sodium starch glycolate was optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. It was concluded that fast disintegrating tablets of salbutamol sulphate were formulated successfully with desired characteristics which disintegrated rapidly; provided rapid onset of action; and enhanced the patient convenience and compliance.
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Satpute, Mangesh Machhindranath, and Nagesh Shivaji Tour. "Formulation and in vitro evaluation of fast dissolving tablets of metoprolol tartrate." Brazilian Journal of Pharmaceutical Sciences 49, no. 4 (December 2013): 783–92. http://dx.doi.org/10.1590/s1984-82502013000400018.
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The demand for fast dissolving tablets has been growing during the last decade, especially for elderly and children who have swallowing difficulties. In the present work, fast dissolving tablets of metoprolol tartrate, were prepared using sodium starch glycolate, sodium croscarmellose and crospovidone as superdisintegrants, by the direct compression method. The tablets prepared were evaluated for various parameters including weight variation, hardness, friability, in vitro dispersion time, drug-polymer interaction, drug content water absorption ratio, wetting time, in vitro drug release, FTIR and DSC studies. The tablets prepared by the direct compression method had a weight variation in the range of 145 mg to 152 mg, which is below ± 7.5%, a hardness of 3.6 kg/cm² to 4.5 kg/cm², percentage friability of 0.46% to 0.73%, in vitro dispersion time of 18 s to 125 s, drug content uniformity of between 98.12% and 100.03%, a water absorption ratio of 67% to 87%, wetting time of 32 sec. to 64 sec., and an in vitro drug release of 53.92% - 98.82% within 15 min. The IR spectral analysis and DSC study showed no drug interaction with formulation additives of the tablet, and the formulations indicated no significant changes in hardness, friability, drug content or in vitro drug release. Fast dissolving tablets of metoprolol tartrate have enhanced dissolution and will lead to improved bioavailability and more effective therapy.
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Hebert, Mello, Richard Moore, Eric Jen, and Scott Siegert. "Complete in vitro Dissolution of Valbenazine as Either Whole Capsules or Crushed Capsule Contents." CNS Spectrums 28, no. 2 (April 2023): 227. http://dx.doi.org/10.1017/s1092852923001499.
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AbstractIntroductionTardive dyskinesia (TD) is a persistent and potentially disabling movement disorder associated with exposure to antipsychotics and other dopamine receptor blocking agents. Three valbenazine capsule strengths (40 mg, 60 mg, 80 mg) are approved for the once-daily treatment of TD. However, some patients with TD, especially in elderly populations, have trouble swallowing due to orolingual movements. This study was conducted to evaluate two different dissolution methods for valbenazine: whole intact capsules versus crushed capsule contents.MethodsSamples were prepared using two commercial lots (Lot-A, Lot-B) for two doses (40 mg, 80 mg), with six replicate samples per lot and dose. The whole capsules were weighed, put into a sinker, and added to a dissolution bath containing 900 mL of 0.1N HCl at 37±0.5° Celsius. Testing on the crushed capsule contents commenced after opening the capsules, weighing and crushing the contents, and transferring the contents to the dissolution bath. Samples were collected (at 10, 15, 20, 30, 45, and 60 min) with a paddle speed of 50 rpm and analyzed using high performance liquid chromatography. Standards were prepared at nominal concentrations of 0.044 mg/mL (for 40 mg) and 0.089 mg/mL (for 80 mg).ResultsCapsules were opened easily by manual manipulation, and contents were crushed easily between spoons. Very rapid (>85% in 15 min) and complete drug release was observed in all samples, independent of capsule strength (40 mg, 80 mg) or preparation (whole intact capsule or crushed capsule contents). For 40-mg capsules, average percent release at first and last collection timepoints were as follows (whole vs crushed): 10 min (98.4% vs 98.6% [A], 93.7% vs 97.6% [B]); 60 min (102.3% vs 100.5% [A], 100.9% vs 100.6% [B]). Results for 80-mg capsules were as follows: 10 min (98.2% vs 99.6% [A], 99.4% vs 97.9% [B]); 60 min (102.0% vs 101.6% [A], 103.2% vs 100.9% [B]).ConclusionsCrushing the capsule contents did not impact the in vitro dissolution performance of valbenazine. Many patients with TD, particularly elderly patients, have difficulty swallowing and may benefit from alternative delivery methods for valbenazine, especially if other TD medications cannot be crushed. More research is needed to better understand if and how crushing the capsule contents of valbenazine affects their stability when mixed with food or delivered through a feeding tube.FundingNeurocrine Biosciences, Inc.
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Alpos, Marbie, Sze Ying Leong, Veronica Liesaputra, Candace E. Martin, and Indrawati Oey. "Understanding In Vivo Mastication Behaviour and In Vitro Starch and Protein Digestibility of Pulsed Electric Field-Treated Black Beans after Cooking." Foods 10, no. 11 (October 22, 2021): 2540. http://dx.doi.org/10.3390/foods10112540.
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The aim of this study was to understand (i) the in vivo mastication behaviour of cooked black beans (chewing duration, texture perception, oral bolus particle size, microstructure, and salivary α-amylase) and (ii) the in vitro digestibility of starch and protein of in vivo-generated black bean oral bolus under simulated gastrointestinal condition. The beans were pre-treated using pulsed electric field (PEF) with and without calcium chloride (CaCl2) addition prior to cooking. The surface response model based on least square was used to optimise PEF processing condition in order to achieve the same texture properties of cooked legumes except for chewiness. In vivo mastication behaviour of the participants (n = 17) was characterized for the particle size of the resulting bolus, their salivary α-amylase activity, and the total chewing duration before the bolus was deemed ready for swallowing. In vitro starch and protein digestibility of the masticated bolus generated in vivo by each participant along the gastrointestinal phase were then studied. This study found two distinct groups of chewers—fast and slow chewers who masticated all black bean beans, on average, for <25 and >29 s, respectively, to achieve a bolus ready for swallowing. Longer durations of chewing resulted in boluses with small-sized particles (majorly composed of a higher number of broken-down cotyledons (2–5 mm2 particle size), fewer seed coats (5–13 mm2 particle size)), and higher activity of α-amylase. Therefore, slow chewers consistently exhibited a higher in vitro digestibility of both the starch and protein of processed black beans compared to fast chewers. Despite such distinct difference in the nutritional implication for both groups of chewers, the in vivo masticated oral bolus generated by fast chewers revealed that the processing conditions involving the PEF and addition of CaCl2 of black beans appeared to significantly (p < 0.05) enhance the in vitro digestibility of protein (by two-fold compared to untreated samples) without stimulating a considerable increase in the starch digestibility. These findings clearly demonstrated that the food structure of cooked black beans created through PEF treatment combined with masticatory action has the potential to modulate a faster hydrolysis of protein during gastrointestinal digestion, thus offering an opportunity to upgrade the quality of legume protein intake in the daily diet.
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Almajidi, Yasser Q., Zainab H. Mahdi, and Nidhal K. Maraie. "PREPARATION AND IN VITRO EVALUATION OF MONTELUKAST SODIUM ORAL NANOEMULSION." International Journal of Applied Pharmaceutics 10, no. 5 (September 8, 2018): 49. http://dx.doi.org/10.22159/ijap.2018v10i5.28367.
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Objective: Oral nanoemulsion (NE) represent one of the newest technology to enhance intestinal drug permeability, bioavailability and facilitate swallowing of the oral dosage form.Methods: In this study, montelukast sodium (MS) nanoemulsions (NEs) were formulated by ultra-sonication using different surfactants (tween 20, tween 60 and tween 80) in different surfactant: co-surfactant (ethanol) ratios (Smix). The prepared NEs were evaluated for different parameters including droplet size (DS) using zetasizer as a function of ultra-sonication time, dispersibility, phase separation, conductivity, percent transmittance, optical transparency, in vitro release in addition to morphology using transmission electron microscopic (TEM).Results: The results revealed that F3 was the optimum formula having an average DS 32.95±2.8 nm after 5 min ultra-sonication assured by zetasizer and TEM, furthermore, a clear to bluish NE was formed after aqueous dilution with high conductivity (59.2±1.76 μs/cm) which indicated the formation of O/W NE. In addition, an optically clear NE was formed with (88.6±2.1) % transmittance with no sedimentation, creaming or separation after centrifugation signifying the formation of a stable NE. Finally, F3 showed faster dissolution rate (92.45%±1.66) after 30 min compared to other formulas.Conclusion: The net result of this study is the formulation of a stable oral NE containing MS which presents new easily swallowed dosage form that may enhance drug permeability as well as it may reduce drug metabolism leading to improving bioavailability for asthmatic patients.
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McManus, Jeffrey M., Hui Lu, Miranda J. Cullins, and Hillel J. Chiel. "Differential activation of an identified motor neuron and neuromodulation provide Aplysia's retractor muscle an additional function." Journal of Neurophysiology 112, no. 4 (August 15, 2014): 778–91. http://dx.doi.org/10.1152/jn.00148.2014.
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To survive, animals must use the same peripheral structures to perform a variety of tasks. How does a nervous system employ one muscle to perform multiple functions? We addressed this question through work on the I3 jaw muscle of the marine mollusk Aplysia californica's feeding system. This muscle mediates retraction of Aplysia's food grasper in multiple feeding responses and is innervated by a pool of identified neurons that activate different muscle regions. One I3 motor neuron, B38, is active in the protraction phase, rather than the retraction phase, suggesting the muscle has an additional function. We used intracellular, extracellular, and muscle force recordings in several in vitro preparations as well as recordings of nerve and muscle activity from intact, behaving animals to characterize B38's activation of the muscle and its activity in different behavior types. We show that B38 specifically activates the anterior region of I3 and is specifically recruited during one behavior, swallowing. The function of this protraction-phase jaw muscle contraction is to hold food; thus the I3 muscle has an additional function beyond mediating retraction. We additionally show that B38's typical activity during in vivo swallowing is insufficient to generate force in an unmodulated muscle and that intrinsic and extrinsic modulation shift the force-frequency relationship to allow contraction. Using methods that traverse levels from individual neuron to muscle to intact animal, we show how regional muscle activation, differential motor neuron recruitment, and neuromodulation are key components in Aplysia's generation of multifunctionality.
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Pecora, Tiziana Maria Grazia, Barbara Ragazzo, Walter Bertin, Alessia Ragonese, Marco Mascagni, Paola Maffei, and Rosario Pignatello. "Rheological Behavior of a New Mucoadhesive Oral Formulation Based on Sodium Chondroitin Sulfate, Xyloglucan and Glycerol." Journal of Functional Biomaterials 12, no. 2 (April 28, 2021): 28. http://dx.doi.org/10.3390/jfb12020028.
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Background: The study aimed at assessing the mucoadhesive properties and the barrier effect of a formulation, labelled as AL2106, containing sodium chondroitin sulfate (ChS), xyloglucan from tamarind seed extract, and glycerol, by evaluating the capacity to adhere to a layer of mucin, the rheological synergism and the barrier effect in comparison to the marketed Esoxx One medical device. AL2106 is a medical device distributed by Alfasigma SpA, Italy with REF FTP57 (Manufacturer: Labomar SpA); it is analogous to Esoxx One medical device: the two products are drinkable solutions that, after swallowing, adhere to the esophageal mucosa, protecting it from the corrosive effect of the gastric acid reflux. AL2106 has been conceived to be better performing in terms of duration of the barrier effect compared to Esoxx One. Methods: The mucoadhesive properties, rheological behavior, buffering capacity against acidity, and film-forming ability with the resultant protecting effect on esophagus mucosa (caffeine permeation test) was compared between the two products. Results: The mucoadhesivity of the formulations was shown in vitro: both remained adherent to a mucin layer, also when the support was rotated by 90°, and when the film layer was washed with water, intended to simulate the washout due to swallowing. AL2106 showed a good buffering efficacy, being able to absorb at least 50% of its weight of 0.03 M HCl while maintaining the pH above 4. The film-forming effect and barrier properties of AL2106 and Esoxx One were confirmed by an in vitro study on reconstructed human esophageal epithelium. A greater film-forming efficacy of AL2106, lasting for at least 5 h, than Esoxx One was observed. Noteworthy, the barrier function of esophageal tissues was shown to be preserved after the application of both formulations. Conclusions: The combination of ChS with the mucoadhesive glycerol−xyloglucan complex and other excipients, which contribute to the barrier effect and to mucoadhesion, contained in AL2106, allowed a longer-lasting protective effect than Esoxx One, proving its effectivity and safety for oral use.
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Pashikanti, Shailaja, and Jyothsna B. "FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF CIPROFLOXACIN." International Journal of Applied Pharmaceutics 11, no. 1 (January 9, 2019): 198. http://dx.doi.org/10.22159/ijap.2019v11i1.28603.
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Objective: The objective of the study was to develop floating in situ gel formulations of Ciprofloxacin that has a narrow absorption window and mainly absorbed in the proximal areas of GIT. These formulations increases the targeted action on bacteria for a longer time that can be used in the treatment of Helicobacter pylori (H. pylori) infections and urinary tract infections.Methods: In situ gel formulations were prepared by varying concentrations of sodium alginate as in situ gel forming bio-degradable polymer and calcium carbonate as a cross-linking agent. The formulations were evaluated for Physical appearance, pH, in vitro drug release, viscosity, in vitro floating behaviour, in vitro gelling capacity and drug content. FTIR was conducted for Ciprofloxacin, excipients used and optimized formulation.Results: All the formulations showed an optimum viscosity that will allow ease of administration and swallowing. Floating lag time of all formulations was between 32-70 seconds and floated for>12 h. The in vitro gelling capacity increased with increasing the polymer and gelling agent concentrations. Increase in polymer concentration decreased the rate and extent of the drug release. Among all the formulations, F4 containing 4% w/v of sodium alginate and 4% w/v of calcium carbonate showed sustained in vitro drug release (95.6%) over an extended period of 12 h. FTIR studies revealed no interaction between drug and excipients used. Drug release from the formulations followed First order kinetics with Fickian diffusion.Conclusion: Ciprofloxacin was successfully formulated as a pH-triggered floating in situ gelling system using sodium alginate.
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Mowlavi, S., J. Engmann, A. Burbidge, R. Lloyd, P. Hayoun, B. Le Reverend, and M. Ramaioli. "In vivo observations and in vitro experiments on the oral phase of swallowing of Newtonian and shear-thinning liquids." Journal of Biomechanics 49, no. 16 (December 2016): 3788–95. http://dx.doi.org/10.1016/j.jbiomech.2016.10.011.
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Bayoumi, Asmaa A. "FORMULATION, OPTIMIZATION, AND EVALUATION OF SITAGLIPTIN AND SIMVASTATIN RAPIDLY DISSOLVING TABLETS." International Journal of Applied Pharmaceutics 10, no. 5 (September 8, 2018): 270. http://dx.doi.org/10.22159/ijap.2018v10i5.28122.
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Objective: The scope of this work was to formulate sitagliptin and simvastatin rapidly dissolving tablets. However, simvastatin is practically insoluble in water. For improving its poor oral bioavailability and with the aim of facilitating administration to patients facing problems with swallowing rapidly dissolving tablets were preparedMethods: Tablets were prepared using superdisintegrant addition technique using croscarmellose sodium (Ac-di-sol), sodium starch glycolate (explotab) and crospovidone in different percentages. Evaluation tests such as weight variation, thickness, and content variation, and friability, disintegration, wetting time, in vitro dispersion and in vitro dissolution were carried out.Results: The results showed that the presence of crospovidone could enhance the dissolution rate of simvastatin greatly. The best-optimized formulae found were that F8, F9, and F10 which showed good disintegration and the dissolution rate of simvastatin and sitagliptin was more than 90% after 10 min while the dissolution rate for simvastatin and sitagliptin pure standards was 12% and 30%, respectively after 10 min.Conclusion: Some tablet formulae showed acceptable pharmacotechnical properties and complied with compendium requirements. Results of dissolution studies revealed that F8-F10 showed an increase in the dissolved sitagliptin and simvastatin to be more than 90% after 10 min.
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Bahnassi, Anas, and Diana Zidan. "Formulation & Evaluation of Aceclofenac Fast Dissolving Tablets Using Foam Granulation Technique." Indo Global Journal of Pharmaceutical Sciences 02, no. 04 (2012): 342–47. http://dx.doi.org/10.35652/igjps.2012.39.
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Orally dissolving tablets (ODT) provides a patient compliance solution for patients swallowing difficulties. Foam granulation is a newer technique that promises better distribution of the granulating system and better properties of the produced tablets. Aceclofenac (anti-inflammatory and analgesic) was selected as the model drug. The poor hydrophilicity of the drug results in variable dissolution rate and poor bioavailability. In this study, we tried to prepare aceclofenac ODT using the newer technique and various types of disintegrants, glidants, and lubricants. The resulted tablets were evaluated for hardness, friability, weight variation, in vitro disintegration time, and wetting time. All the formulation showed acceptable disintegration time. It was concluded that the prepared aceclofenac ODT by foam granulation technique using selective range of excipients can provide a dosage form with better patient compliance and effective therapy. © 2011 IGJPS. All rights reserved
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Cao, Weibiao, Ling Cheng, José Behar, Claudio Fiocchi, Piero Biancani, and Karen M. Harnett. "Proinflammatory cytokines alter/reduce esophageal circular muscle contraction in experimental cat esophagitis." American Journal of Physiology-Gastrointestinal and Liver Physiology 287, no. 6 (December 2004): G1131—G1139. http://dx.doi.org/10.1152/ajpgi.00216.2004.
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Cholinergic mechanisms are largely responsible for esophageal contraction in response to swallowing or to in vitro electrical field stimulation (EFS). After induction of experimental esophagitis by repeated acid perfusion, the responses to swallowing and to EFS were significantly reduced but contraction in response to ACh was not affected, suggesting that cholinergic mechanisms are damaged by acid perfusion but that myogenic mechanisms are not. Measurements of ACh release in response to EFS confirmed that release of ACh was reduced in esophagitis compared with normal controls. To examine factors contributing to this neuropathy, normal esophageal strips were incubated for 1–2 h with the proinflammatory cytokines IL-1β (100 U/ml), IL-6 (1 ng/ml), or TNF-α (1 ng/ml). IL-1β and IL-6 levels, measured by Western blot analysis, increased in esophagitis compared with normal circular muscle. IL-1β and IL-6 reduced contraction in response to EFS (2–10 Hz, 0.2 ms) but did not affect ACh-induced contraction, suggesting that these cytokines inhibit ACh release without affecting myogenic contractile mechanisms. EFS-induced ACh release was significantly reduced in normal esophageal strips by incubation in IL-1β or IL-6, suggesting that they may contribute to the contractility changes. TNF-α at 1 ng/ml, however, did not affect the response to ACh or to electrical stimulation but inhibited both at higher concentrations. TNF-α levels were low in normal muscle and did not increase with esophagitis. The data suggest that the proinflammatory cytokines IL-1β and IL-6 contribute to reduced esophageal contraction by inhibiting release of ACh from myenteric neurons.
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Jain, P., A. Mishra, and A. Pathak. "PREPARATION & EVALUATION OF ORODISPERSIBLE TABLET CONTAINING ASPIRIN BY SUBLIMATION METHOD." INDIAN DRUGS 52, no. 12 (December 28, 2015): 60–62. http://dx.doi.org/10.53879/id.52.12.10465.
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Orodispersible tablets are uncoated tablets which when taken into the mouth, get easily dispersed within 3 min before swallowing. they are also known as orally disintegrating tablets, mouth-dissolving tablets, rapid dissolving tablets fast-disintegrating tablets, fast-dissolving tablets. In this work, sublimation process was used to prepare orodispersible tablets of aspirin by formulating various batches using different concentration of sodium starch glycolate, camphor and cross povidone. An effort was made by using two modes, first, to increase water uptake for the fast dispersion by creating pores by sublimation methods in tablets and second, use of super disintegrantes like sodium starch glycolate to minimise disintegration time and promote fast dispersing ability. Prepared formulations were evaluated for weight variation, content uniformity, friability, hardness, wetting time, disintegration time, in vitro drug release and interaction study by differential scanning calorimetery. The best formulation was selected on the basis of evaluation results.
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Hornby, Hannah, Mar Collado-González, Xue Zhang, Nichola Abrehart, Meshari Alshammari, Serafim Bakalis, Alan Mackie, and Luca Marciani. "Size and Number of Food Boluses in the Stomach after Eating Different Meals: Magnetic Resonance Imaging Insights in Healthy Humans." Nutrients 13, no. 10 (October 16, 2021): 3626. http://dx.doi.org/10.3390/nu13103626.
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Oral processing of food results in the formation of food boluses, which are then swallowed and reach the stomach for further digestion. The number, size and surface properties of the boluses will affect their processing and emptying from the stomach. Knowledge of these parameters, however, is incomplete due to limitations of the techniques used. In this work, non-invasive magnetic resonance imaging (MRI) was used for the first time to measure boluses in the stomach a few minutes after swallowing. Three groups of nine healthy participants were fed three different meals: chicken and roasted vegetables (Meal 1), bread and jam (Meal 2) and cheese and yogurt (Meal 3), and then, their stomach content was imaged. The median number of boluses within the stomach was 282, 106 and 9 for Meal 1, Meal 2 and Meal 3 (p < 0.0001) with an average volume of 0.47 mL, 2.4 mL and 13.6 mL, respectively (p < 0.0001). The cohesiveness as well as the meal composition seem to play a key role in the resulting boluses. These new in vivo data from undisturbed organ imaging can improve knowledge of the digestion process, which will, in turn, inform in vitro and in silico modelling of digestion, thus improving their in vitro/in vivo relevance.
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Dubey, Abhay Kumar, and ,. Archana. "Development and In-Vitro Evaluation of Plantago ovata Based Rapid Disintegrating Tablets of Labetalol Hydrochloride." Journal of Drug Delivery and Therapeutics 12, no. 4 (July 15, 2022): 36–42. http://dx.doi.org/10.22270/jddt.v12i4.5430.
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Objectives: To avoid swallowing problems of conventional tablets and improved patient compliance Plantago Ovata based Labetalol HCl Rapid disintegrating tablets have been prepared. Methods: Six different (F1 to F6) batches of Labetalol HCl Rapid disintegrating tablets were developed by ‘direct compression method’ using Plantago ovata as a natural super-disintegrating agent. The formulated RDT were tested for angle of repose’, densities like tapped and bulk density, Hausner’s ratio, Carr’s index like pre-compression parameters and for thickness, weight variation or weight uniformity, tablet hardness, % drug content or content uniformity, water absorption ratio’, time require for wetting of tablets’ means wetting time, in-vitro drug disintegration time and in-vitro drug dissolution studies under post-compression parameters of evaluation. Results: It was found that the all the results of these pre-compression and post-compression parameters comply with official standards. The drug release was determined using dissolution media of pH 6.8 phosphate buffer through in-vitro dissolution of drug. This study showed that a rapid drug release by prepared tablets. The optimized formulation F6 showed higher water absorption ratio`, lower wetting time, minimum in-vitro disintegration time’ and higher drug release amongst all the formulations. The F6 formulation was considered the best among all formulations. Conclusion: The prepared rapid disintegrating tablets shows rapid onset of action by quick drug release, minimize side effects and enhanced patient compliance. These prepared tablets containing selective alpha-1 and non-selective beta adrenergic antagonist’ drug candidate Labetalol HCl, will be very useful in the treatment of high blood pressure with enhanced bioavailability.
Keywords: Rapid disintegrating tablets, Labetalol Hydrochloride, Bioavailability Enhancement, Natural Superdisintegrant, Plantago Ovata, High Blood Pressure, RDT, Patient Compliance
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Gaikwad, Bhavna B., Bhushan R. Rane, and Ashish S. Jain. "Formulation and Evaluation of Orodispersible Tablet of Sulindac." European Journal of Pharmaceutical Research 2, no. 3 (December 23, 2022): 11–19. http://dx.doi.org/10.24018/ejpharma.2022.2.3.41.
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Oral administration of dosage form is the most recommended mode of administration, because of its self-medication, accurate dose of the drug, and ease of administration. However, trouble swallowing in geriatric patients is one major negative of this route, which can mentally disrupt patients. The goal of this study was to use the direct compression method to make orodispersible tablets of sulindac utilizing various doses of super disintegrant agents such as Sodium starch glycolate Crospovidone and Croscarmellose sodium. Three distinct super disintegrants were used to create nine formulations with varying concentration levels. The preformulation, precompression, and post-compression properties of the powder combinations were assessed. In comparison to the other formulations, tablets from batch F3 containing crospovidone had superior organoleptic qualities, as well as outstanding drug release and in-vitro disintegration time. The super disntegrants addition technique was shown to be a viable method for manufacturing orodispersible tablets using the direct compression method.
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Caille, Coline, Mariem Boukraâ, Cécile Rannou, Angélique Villière, Clément Catanéo, Laurent Lethuaut, Araceli Lagadec-Marquez, Julia Bechaux, and Carole Prost. "Analysis of Volatile Compounds in Processed Cream Cheese Models for the Prediction of “Fresh Cream” Aroma Perception." Molecules 28, no. 20 (October 23, 2023): 7224. http://dx.doi.org/10.3390/molecules28207224.
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Controlling flavor perception by analyzing volatile and taste compounds is a key challenge for food industries, as flavor is the result of a complex mix of components. Machine-learning methodologies are already used to predict odor perception, but they are used to a lesser extent to predict aroma perception. The objectives of this work were, for the processed cream cheese models studied, to (1) analyze the impact of the composition and process on the sensory perception and VOC release and (2) predict “fresh cream” aroma perception from the VOC characteristics. Sixteen processed cream cheese models were produced according to a three-factor experimental design: the texturing agent type (κ-carrageenan, agar-agar) and level and the heating time. A R-A-T-A test on 59 consumers was carried out to describe the sensory perception of the cheese models. VOC release from the cheese model boli during swallowing was investigated with an in vitro masticator (Oniris device patent), followed by HS-SPME-GC-(ToF)MS analysis. Regression trees and random forests were used to predict “fresh cream” aroma perception, i.e., one of the main drivers of liking of processed cheeses, from the VOC release during swallowing. Agar-agar cheese models were perceived as having a “milk” odor and favored the release of a greater number of VOCs; κ-carrageenan samples were perceived as having a “granular” and “brittle” texture and a “salty” and “sour” taste and displayed a VOC retention capacity. Heating induced firmer cheese models and promoted Maillard VOCs responsible for “cooked” and “chemical” aroma perceptions. Octa-3,5-dien-2-one and octane-2,3-dione were the two main VOCs that contributed positively to the “fresh cream” aroma perception. Thus, regression trees and random forests are powerful statistical tools to provide a first insight into predicting the aroma of cheese models based on VOC characteristics.
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Baliga, S. B., B. P. Manjula, and M. Geetha. "FORMULATION AND EVALUATION OF MICROSPHERE BASED ORO DISPERSIBLE TABLETS OF SUMATRIPTAN SUCCINATE." INDIAN DRUGS 54, no. 03 (March 28, 2017): 28–38. http://dx.doi.org/10.53879/id.54.03.10794.
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Sumatriptan succinate (SS) is a drug used in the treatment of migraine headaches, but suffers from low patient compliance due to its unpalatable bitter taste. The purpose of the present work was to prepare taste-masked oro dispersible tablets (ODTs) of SS by incorporating drug loaded microspheres into tablets for use in patients experiencing difficulty in swallowing. Microspheres loaded with SS were prepared by solvent evaporation technique. Eudragit EPO, a pH-sensitive aminoalkylmethacrylate copolymer, was used for coating the drug particles, acetone as solvent for the polymer and light liquid paraffin as an encapsulating medium. Drug : polymer ratio of 1:1 was considered to be optimized formulation with a yield of 99.96%, entrapment efficiency of 61.55%, particle size ranging from 30.32 – 90.96μm and in vitro drug release of 85.06% within an hour. FTIR studies suggested absence of drug-excipient interaction. Tablets prepared by direct compression containing microspheres and effervescent agents were evaluated for pre-compression and post-compression parameters. The wetting time, in vitro dispersion time and in vitro disintegration time of the tablets were found to be 39 sec, 35 sec and 32 sec, respectively. The drug release from the tablet was about 85.44% within an hour. The SEM of final ODTs revealed that the microspheres remained intact even after compression. Stability studies indicated that the selected formulation was stable. The results obtained suggested that effective taste-masking was achieved for SS using the technique of microencapsulation and ODTs of acceptable characteristics were obtained by adding effervescent agents followed by direct compression.
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Varsha, Ahirwar, Khushwant S. Yadav, and Shailendra Bindaiya. "Formulation Development and Evaluation of Fast Dissolving Films of Oloptadine HCl." Asian Journal of Research in Pharmaceutical Sciences 11, no. 2 (May 10, 2021): 103–8. http://dx.doi.org/10.52711/2231-5659.2021-11-2-2.
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Our studies on the performance of formulation development and evaluation of fast dissolving films of Oloptadine HCL its anti-allergic drug. Prepare mouth dissolving film of Oloptadine HCl by solvent casting method. To characterize the prepared mouth dissolving film of Oloptadine HCL in terms of— Thickness, percent elongation, tack test, swelling index, in-vitro disintegration time and dissolution test. Oloptadine OLO), 11-[{z}-3-(Dimethlamino) propylidene]-6-11-dihydrobenz [b, e] oxepin-2-acetic acid hydrochloride, is widely used as an antihistaminic. Oloptadine HCL is a relatively selective histamine H1-receptor antagonist that inhibits the release of histamine from mast cells. Oloptadine does not affect alpha-adrenergic dopamine, muscarinic type 1 and 2 or serotonin receptor. They are hydrophobic in nature and non-polar, sparingly soluble in water and freely soluble methanol, ethanol. Olopatadine HCl is a mouth dissolving film. We is trying to sort out the problem of allergic. They are rapidly onset of action, when placed upon the tongue that it is disperse rapidly swallowing within 3-5 seconds without need of water or chewing.
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ÇOMOĞLU, Tansel. "FARKLI SÜPER DAĞITICILARIN KETOPROFEN İÇEREN AĞIZDA DAĞILAN TABLETLERİN İN VİTRO KARAKTERİZASYON PARAMETRELERİ ÜZERİNDEKİ ETKİSİNİN DEĞERLENDİRİLMESİ." Ankara Universitesi Eczacilik Fakultesi Dergisi 48, no. 2 (March 19, 2024): 10. http://dx.doi.org/10.33483/jfpau.1425266.
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Objective: Orally Disintegrating Tablets (ODTs) have revolutionized pharmaceutical drug delivery, offering a patient-friendly alternative for those struggling with conventional tablet swallowing. This study delves into the impact of superdisintegrants (crospovidone, sodium starch glycolate, and croscarmellose sodium) on the in vitro characterization of Ketoprofen-containing ODTs. ODTs are designed to rapidly disintegrate in the oral cavity without water, enhancing patient compliance, ensuring faster therapeutic onset, and providing convenience. Material and Method: The micromeritic properties of pre-compression Ketoprofen ODT blends were assessed for bulk density, tapped density, Hausner ratio, and compressibility index. ODTs were formulated using a direct compression method to maintain component uniformity. Comprehensive characterization included weight variation, tablet hardness, friability, wetting time, and in vitro disintegration time assessments. The drug content was determined through UV spectrophotometry of dissolved ODTs, and dissolution studies were conducted in pH 6.8 phosphate buffer using USP apparatus XXIV. Result and Discussion: Results showed uniform tablet mass and favorable powder mixture flowability, ensuring ODT physical properties. Tablets exhibited excellent mechanical resistance with consistent hardness and low friability loss. All formulations demonstrated high and uniform drug content. Different superdisintegrants influenced wetting, disintegration, and dissolution times. Crospovidone exhibited the fastest wetting time but longer disintegration times, attributed to increased tablet hardness. Dissolution studies revealed that crospovidone-containing ODTs had faster drug release compared to croscarmellose sodium and sodium starch glycolate, aligning with literature findings. The study emphasized the importance of considering both wetting and disintegration times for a comprehensive evaluation of ODT performance. Croscarmellose sodium and sodium starch glycolate hindered drug release, forming gel-like masses impeding dissolution, while crospovidone enhanced drug release in formulated ODTs. In conclusion, the study provides valuable insights for pharmaceutical development and patient-centric drug delivery solutions, showcasing the influence of superdisintegrants on ODT performance and emphasizing the importance of considering various parameters for comprehensive evaluation.
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Chinnala, Krishna Mohan, and Sirish Vodithala. "FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISINTEGRATING TABLETS OF CINITAPRIDE HYDROGEN TARTARATE BY USING DIRECT COMPRESSION TECHNIQUE." International Journal of Current Pharmaceutical Research 9, no. 6 (November 14, 2017): 98. http://dx.doi.org/10.22159/ijcpr.2017v9i6.23659.
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Objective: In the present study, efforts were taken to develop fast disintegrating tablets of Cinitapride hydrogen tartrate, is a gastro-prokinetic agent and antiulcer agent with an objective to achieve rapid disintegration, and further improving the bioavailability of the drug. Also, to resolve the swallowing problems (Dysphasia) in pediatric, geriatric patients by rapid disintegration in saliva and improve the patient compliance.Methods: Fast disintegrating tablets were prepared by direct compression method using superdisintegrants like crospovidone (CP), croscarmellose sodium (CCS), sodium starch glycolate (SSG) and combination of super-disintegrants in different concentrations. The prepared formulations were evaluated for the pre-compression parameters like bulk density, tapped density, Carr’s compressibility, Hausner’s ratio and angle of repose. The prepared batches of fast disintegrating tablets of Cinitapride hydrogen tartarate were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time, water absorption ratio, and in vitro dissolution profile.Results: Bulk density and tapped density were found in the range of 0.412–0.432 g/cc and 0.507–0.528 g/cc respectively. In all formulations, tablet weight and thickness were within mean±9.5% and mean±5% respectively. Wetting time values lie between 19.76 to 39.53 sec. Water absorption ratio ranged from 57.30 to 78.82 %. The in vitro disintegration time for all the 12 formulations varied from 17.43 to 38.61 seconds. Formulation F8 which contained crosspovidone have recorded drug release 96.94±0.47% at the end of 30 min.Conclusion: The formulation containing crospovidone (F8) showed better performance in terms of disintegration time and drug release when compared to other formulations.
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Pamlényi, Krisztián, Géza Regdon, Dániel Nemes, Ferenc Fenyvesi, Ildikó Bácskay, and Katalin Kristó. "Stability, Permeability and Cytotoxicity of Buccal Films in Allergy Treatment." Pharmaceutics 14, no. 8 (August 5, 2022): 1633. http://dx.doi.org/10.3390/pharmaceutics14081633.
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Oral mucoadhesive systems, such as polymer films, are among innovative pharmaceutical products. These systems can be applied in swallowing problems and can also be used in geriatrics and paediatrics. In our earlier work, we successfully formulated buccal mucoadhesive polymer films, which contained cetirizine-hydrochloride (CTZ) as the API. The present study focused on investigating the stability and permeability of the prepared films. The stability of the films was studied with an accelerated stability test. During the stability test, thickness, breaking hardness and in vitro mucoadhesivity were analysed. Furthermore, the interactions were studied with FT-IR spectroscopy, and the changes in the amount of the API were also monitored. Cytotoxicity and cell line permeability studies were carried out on TR 146 buccal cells. Compositions that can preserve more than 85% of the API after 6 months were found. Most of the compositions had a high cell viability of more than 50%. Citric acid (CA) decreased the stability and reduced every physical parameter of the films. However, cell line studies showed that the permeability of the films was enhanced. In our work, we successfully formulated CTZ-containing buccal films with adequate stability, high cell viability and appropriate absorption properties.
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Ahmed, Mohd Salman, Nikita Upadhyay, and P. K. Dubey. "A REVIEW ON FAST DISSOLVING TABLET." International Journal of Pharmaceutical Sciences and Medicine 7, no. 5 (May 30, 2022): 37–47. http://dx.doi.org/10.47760/ijpsm.2022.v07i05.004.
Full textAbstract:
Fast dissolving tablets (FDTs) emerged as one of the popular and widely accepted dosage forms. Few solid dosage forms like capsules and tablets are present days facing the problems like difficulty in swallowing (dysphagia) resulting many incidences of non-compliance and making the therapy ineffective. Specifically for paediatric patients because of incomplete development of the muscular and nervous system and case of geriatric patients suffering from Parkinson’s disorder. Oral dosage form and oral route are the most preferred administration route for various drugs with limitations like first-pass metabolism, bedridden, psychiatric patients and uncooperative patients. There is no need of excess water to dissolve and disintegrate FDT tablets. Fast dissolving tablets are designed to dissolve in within 60 seconds in saliva remarkably faster. FDTs formulations contain super disintegrants to enhance the disintegration rate of tablet in the buccal cavity. FDTs have disintegrated quickly, absorb faster so, in vitro drug release time improve and this property of drugs (dosage form) enhanced bioavailability. FDTs have advantages such as easy portability and manufacturing, accurate dosing, good chemical and physical stability and an ideal alternative for geriatric and paediatric patients. FDT formulations have advantage over both conventional tablets and liquid dosage form.
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Stie, Mai Bay, Johan Ring Gätke, Ioannis S. Chronakis, Jette Jacobsen, and Hanne Mørck Nielsen. "Mucoadhesive Electrospun Nanofiber-Based Hybrid System with Controlled and Unidirectional Release of Desmopressin." International Journal of Molecular Sciences 23, no. 3 (January 27, 2022): 1458. http://dx.doi.org/10.3390/ijms23031458.
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The sublingual mucosa is an attractive route for drug delivery, although challenged by a continuous flow of saliva that leads to a loss of drug by swallowing. It is of great benefit that drugs absorbed across the sublingual mucosa avoid exposure to the harsh environment of the gastro-intestinal lumen; this is especially beneficial for drugs of low physicochemical stability such as therapeutic peptides. In this study, a two-layered hybrid drug delivery system was developed for the sublingual delivery of the therapeutic peptide desmopressin. It consisted of peptide-loaded mucoadhesive electrospun chitosan/polyethylene oxide-based nanofibers (mean diameter of 183 ± 20 nm) and a saliva-repelling backing film to promote unidirectional release towards the mucosa. Desmopressin was released from the nanofiber-based hybrid system (approximately 80% of the loaded peptide was released within 45 min) in a unidirectional manner in vitro. Importantly, the nanofiber–film hybrid system protected the peptide from wash-out, as demonstrated in an ex vivo flow retention model with porcine sublingual mucosal tissue. Approximately 90% of the loaded desmopressin was retained at the surface of the ex vivo porcine sublingual mucosa after 15 min of exposure to flow rates representing salivary flow.
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Yadav, Nitesh, Pushpendra Soni, and Lavakesh Kumar Omray. "Formulation, Development and Evaluation of Fast Dissolving Oral Film of a Selective Serotonin-Reuptake Inhibitor (SSRIS) Escitalopram Oxalate." Journal of Drug Delivery and Therapeutics 10, no. 2 (March 15, 2020): 175–79. http://dx.doi.org/10.22270/jddt.v10i2.3938.
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The purpose of this research was to develop fast dissolving oral film of Escitalopram oxalate. Fast dissolving oral film offers a solution for paediatrics, geriatrics; psychiatric or mentally ill people and those have difficulty in swallowing tablets/capsules resulting in improved patient compliance. Selective serotonin reuptake inhibitors (SSRIs), which are broad spectrum antidepressants that are effective for major depressive disorder and several anxiety disorders. Escitalopram Oxalate is highly selective, more effective and better than other SSRIs. The prepared formulations were evaluated for Thickness, Weight uniformity, Folding Endurance, Percentage of Moisture Content, Drug Content Analysis, Disintegrating time and In vitro dissolution study. Stability studies were carried out with optimized formulation F5 which was stored for a period of one, two and three months at 40±2oC temperature and 75±5% relative humidity for a period 3 months. Thus it can be concluded that Escitalopram oxalate fast dissolving films could be commercially exploited for the treatment of panic disorder using Escitalopram oxalate with merits of faster onset of action, avoidance of extensive first pass metabolism, low dosage regimen, enhanced bioavailability and improved patient compliance.
Keywords: Escitalopram oxalate, Fast dissolving oral film, Evaluation
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Koizumi, H., K. Nomura, K. Ishihama, T. Yamanishi, A. Enomoto, and M. Kogo. "Inhibition of Trigeminal Respiratory Activity by Suckling." Journal of Dental Research 86, no. 11 (November 2007): 1073–77. http://dx.doi.org/10.1177/154405910708601110.
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The trigeminal motor system is involved in many rhythmic oral-motor behaviors, such as suckling, mastication, swallowing, and breathing. Despite the obvious importance of functional coordination among these rhythmic activities, the system is not well-understood. In the present study, we examined the hypothesis that an interaction between suckling and breathing exists in the brainstem, by studying the respiratory activity in trigeminal motoneurons (TMNs) during fictive suckling using a neonatal rat in vitro brainstem preparation. The results showed that fictive suckling, which was neurochemically induced by bath application of N-methyl-D,L-aspartate and bicuculline-methiodide, or by local micro-injection of the same drugs to the trigeminal motor nucleus, inhibited the inspiratory activities in both respiration TMNs and respiratory rhythm-generating neurons. Under patch-clamp recording, fictive suckling caused membrane potential hyperpolarization of respiration TMNs. We conclude that the brainstem preparation contains an inhibitory circuit for respiratory activity in the trigeminal motor system via the rhythm-generating network for suckling. Abbreviations: BIC, bicuculline methiodide; GABA, gamma aminobutyric acid; NMA, N-methyl-D,L-aspartate; NMDA, N-methyl-D-aspartate; and TMN, trigeminal motoneuron.
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Manrique-Torres, Yady Juliana, Danielle J. Lee, Faiza Islam, Lisa M. Nissen, Julie A. Y. Cichero, Jason R. Stokes, and Kathryn J. Steadman. "Crushed Tablets: Does the Administration of Food Vehicles and Thickened Fluids to Aid Medication Swallowing Alter Drug Release?" Journal of Pharmacy & Pharmaceutical Sciences 17, no. 2 (May 5, 2014): 207. http://dx.doi.org/10.18433/j39w3v.
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Purpose. To evaluate the influence of co-administered vehicles on in vitro dissolution in simulated gastric fluid of crushed immediate release tablets as an indicator for potential drug bioavailability compromise. Methods. Release and dissolution of crushed amlodipine, atenolol, carbamazepine and warfarin tablets were tested with six foods and drinks that are frequently used in the clinical setting as mixers for crushed medications (water, orange juice, honey, yoghurt, strawberry jam and water thickened with Easythick powder) in comparison to whole tablets. Five commercial thickening agents (Easythick Advanced, Janbak F, Karicare, Nutilis, Viscaid) at three thickness levels were tested for their effect on the dissolution of crushed atenolol tablets. Results. Atenolol dissolution was unaffected by mixing crushed tablets with thin fluids or food mixers in comparison to whole tablets or crushed tablets in water, but amlodipine was delayed by mixing with jam. Mixing crushed warfarin and carbamazepine tablets with honey, jam or yoghurt caused them to resemble the slow dissolution of whole tablets rather than the faster dissolution of crushed tablets in water or orange juice. Crushing and mixing any of the four medications with thickened water caused a significant delay in dissolution. When tested with atenolol, all types of thickening agents at the greatest thickness significantly restricted dissolution, and products that are primarily based on xanthan gum also delayed dissolution at the intermediate thickness level. Conclusions. Dissolution testing, while simplistic, is a widely used and accepted method for comparing drug release from different formulations as an indicator for in vivo bioavailability. Thickened fluids have the potential to retard drug dissolution when used at the thickest levels. These findings highlight potential clinical implications of the addition of these agents to medications for the purpose of dose delivery and indicate that further investigation of thickened fluids and their potential to influence therapeutic outcomes is warranted. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.
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Levy, Miryam, Jian Jing, and Abraham J. Susswein. "An in vitro analog of learning that food is inedible inAplysia: decreased responses to a transmitter signaling food after pairing with transmitters signaling failed swallowing." Learning & Memory 30, no. 11 (October 18, 2023): 278–81. http://dx.doi.org/10.1101/lm.053867.123.
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An in vitro analog of learning that a food is inedible provided insight into mechanisms underlying the learning.Aplysialearn to stop responding to a food when they attempt but fail to swallow it. Pairing a cholinergic agonist with an NO donor or histamine in theAplysiacerebral ganglion produced significant decreases in fictive feeding in response to the cholinergic agonist alone. Acetylcholine (ACh) is the transmitter of chemoreceptors sensing food touching the lips. Nitric oxide (NO) and histamine (HA) signal failed attempts to swallow food. Reduced responses to the cholinergic agonist after pairing with NO or HA indicate that learning partially arises via a decreased response to ACh in the cerebral ganglion.
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Drushel, R. F., D. M. Neustadter, I. Hurwitz, P. E. Crago, and H. J. Chiel. "Kinematic models of the buccal mass of Aplysia californica." Journal of Experimental Biology 201, no. 10 (May 15, 1998): 1563–83. http://dx.doi.org/10.1242/jeb.201.10.1563.
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The feeding behavior of the marine mollusc Aplysia californica is an intensively studied model system for understanding the neural control of behavior. Feeding movements are generated by contractions of the muscles of the buccal mass. These muscles are internal and cannot be visualized during behavior. In order to infer the movements of the muscles of the buccal mass, two kinematic models were constructed. The first kinematic model assumed that the complex consisting of the pincer-like radula and the underlying odontophore was spherical in shape. In this model, the radula/odontophore was moved anteriorly or posteriorly and the more superficial buccal muscles (I1/I3 and I2) were fitted around it. Although the overall buccal mass shapes predicted by this model were similar to those observed in vivo during protraction, the shapes predicted during retraction were very different. We therefore constructed a second kinematic model in which the shape of the radula/odontophore was based on the shapes assumed by those structures in vitro when they were passively forced into protraction, rest or retraction positions. As each of these shapes was rotated, the second kinematic model generated overall shapes of the buccal mass that were similar to those observed in vivo during swallowing and tearing, and made predictions about the antero-posterior length of the buccal mass and the relative location of the lateral groove. These predictions were consistent with observations made in vivo and in vitro. The kinematic patterns of intrinsic buccal muscles I1 and I2 in vivo were estimated using the second model. Both models make testable predictions with regard to the functions and neural control of intrinsic buccal muscles I2 and I3.
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Reiprich, A., L. Skalden, A. Raab, N. Bolotina, and C. Lang. "Lactobacillus crispatus DSM25988 as novel bioactive agent to co-aggregate Streptococcus pyogenes and to exclude it by binding to human cells." Beneficial Microbes 13, no. 1 (February 28, 2022): 83–94. http://dx.doi.org/10.3920/bm2021.0103.
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Streptococcus pyogenes, a group A streptococcus, is the major bacterial pathogen responsible for acute bacterial infection of the human oropharynx and the causative agent of scarlet fever. Estimates of the global burden of S. pyogenes related diseases revealed 616 million cases of pharyngitis, and at least 517,000 deaths due to severe invasive diseases and sequelae. Here we describe Lactobacillus crispatus DSM25988 that was identified among hundreds of Lactobacillus strains (referring to all organisms that were classified as Lactobacillaceae until 2020) showing ability to prevent adhesion of S. pyogenes to Detroit 562 cells, and to exhibit a masking and co-aggregating effect on S. pyogenes in vitro. L. crispatus DSM25988 also inhibits invasion of cultured human epithelial pharyngeal cells by S. pyogenes. Competitive binding to fibronectin might be involved in the inhibition process. Antiviral activity of the L. crispatus DSM25988 cells were identified in an in vitro cell model demonstrating that L. crispatus effectively excludes viruses from epithelial cells using SARS-CoV2 proteins as a model. This finding points to the potential of DSM25988 to protect cells from virus infection. Biological activity is retained in heat treated cells. The heat-treated Lactobacillus strain was further developed into functional throat lozenges, wherein its biological activity is stably maintained in the formulation. Lozenges containing L. crispatus DSM25988 underwent testing in an uncontrolled, prospective user study in 44 subjects with symptoms of sore throat for a period of up to 14 days. The study data shows promising safety and efficacy of the medical device when used against symptoms of sore throat like scratchy feeling, hoarse voice and swallowing pain.
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Brózman, Ondřej, Barbara Kubickova, Pavel Babica, and Petra Laboha. "Microcystin-LR Does Not Alter Cell Survival and Intracellular Signaling in Human Bronchial Epithelial Cells." Toxins 12, no. 3 (March 7, 2020): 165. http://dx.doi.org/10.3390/toxins12030165.
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Changes in ecological and environmental factors lead to an increased occurrence of cyanobacterial water blooms, while secondary metabolites-producing cyanobacteria pose a threat to both environmental and human health. Apart from oral and dermal exposure, humans may be exposed via inhalation and/or swallowing of contaminated water and aerosols. Although many studies deal with liver toxicity, less information about the effects in the respiratory system is available. We investigated the effects of a prevalent cyanotoxin, microcystin-LR (MC-LR), using respiratory system-relevant human bronchial epithelial (HBE) cells. The expression of specific organic-anion-transporting polypeptides was evaluated, and the western blot analysis revealed the formation and accumulation of MC-LR protein adducts in exposed cells. However, MC-LR up to 20 μM neither caused significant cytotoxic effects according to multiple viability endpoints after 48-h exposure, nor reduced impedance (cell layer integrity) over 96 h. Time-dependent increase of putative MC-LR adducts with protein phosphatases was not associated with activation of mitogen-activated protein kinases ERK1/2 and p38 during 48-h exposure in HBE cells. Future studies addressing human health risks associated with inhalation of toxic cyanobacteria and cyanotoxins should focus on complex environmental samples of cyanobacterial blooms and alterations of additional non-cytotoxic endpoints while adopting more advanced in vitro models.
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Drumond, Nélio, and Sven Stegemann. "An Investigation into the Relationship between Xanthan Gum Film Coating Materials and Predicted Oro-Esophageal Gliding Performance for Solid Oral Dosage Forms." Pharmaceutics 12, no. 12 (December 20, 2020): 1241. http://dx.doi.org/10.3390/pharmaceutics12121241.
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Oral drug therapy is generally provided in the form of solid oral dosage forms (SODF) that have to be swallowed and move throughout the oro-esophageal system. Previous studies have provided evidence that the oro-esophageal transit of SODF depends on their shape, size, density, and surface characteristics. To estimate the impact of SODF surface coatings during esophageal transit, an in vitro system was implemented to investigate the gliding performance across an artificial mucous layer. In this work, formulations comprised of different slippery-inducing agents combined with a common film forming agent were evaluated using the artificial mucous layer system. Xanthan gum (XG) and polyethylene glycol 1500 (PEG) were applied as film-forming agents, while carnauba wax (CW), lecithin (LE), carrageenan (CA), gellan gum (GG) and sodium alginate (SA), and their combination with sodium lauryl sulfate (SLS), were applied as slippery-inducing components. All tested formulations presented lower static friction (SF) as compared to the negative control (uncoated disc, C, F0), whereas only CW/SLS-based formulations showed similar performance to F0 regarding dynamic friction (DF). The applied multivariate analysis approach allowed a higher level of detail to the evaluation and supported a better identification of excipients and respective concentrations that are predicted to improve in vivo swallowing safety.
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Khan, MD Abdul Aali, M. S. Sudheesh, and Rajesh Singh Pawar. "Formulation Development and Evaluation of Oro-Dispersible Tablets Based On Solid Dispersion of Cimetidine." Journal of Drug Delivery and Therapeutics 12, no. 6-S (December 15, 2022): 42–46. http://dx.doi.org/10.22270/jddt.v12i6-s.5696.
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The most common problem about conventional dosage form is dysphagia (difficulty in swallowing). So, we design a new approach in a conventional dosage form which is oral dispersible tablet. Oral dispersible tablet is also called as mouth dissolving tablet, fast dissolving tablet, or oral disintegrating tablet. Oral dispersible tablet has advantage as it quickly disintegrates into saliva when it is put on the tongue. The faster the drug disintegrates or is dissolved, the faster the absorption and the quicker the therapeutic effect of drug will be attained. The objective of present study was to formulate directly compressible orodispersible tablets of cimetidine with improved solubility and bioavailability by using solid dispersion technique. Cimetidine is a histamine H2-receptor antagonist. It is widely prescribed in active duodenal ulcers, gastric ulcers, Zollinger-Ellison syndrome, gastroesophageal reflux disease and erosive esophagitis. Solid dispersion of cimetidine was prepared by anti-solvent addition method and physical mixture using novel polymer eudragit E 100. Saturation solubility of drug was determined in physical mixture and solid dispersion formulation. The prepared solid dispersion formulations were further characterized by drug contents, HPLC, and encapsulation efficiency. Orodispersible tablets of cimetidine were prepared by direct compression method and blend was evaluated for the pre-compression parameters such as bulk density, compressibility, angle of repose etc. The tablets were prepared by using selected solid dispersion formulation and excipients with sodium starch glycolate as a superdisintegrant and evaluated for hardness, friability, weight variation, content uniformity, wetting time, dispersion time and in-vitro drug release. Orodispersible tablet shows wetting time 27±1 seconds and in-vitro drug release 93.20±3.181%, which is better as compare to tablet containing pure drug (82.36±1.986) within 20min. Thus formulation of orodispersible tablet of cimetidine solid dispersion showed increased solubility and bioavailability with patient complies and convenience.
Keywords: Cimetidine, Orodispersible tablets, Solid dispersion, Anti solvent addition method, Superdisintegrant