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1
Sharma, N., and T. Sinderpal. "Sterculia Gum: Chemical Structure, Composition and Physico-Chemical Properties." Asian Journal of Chemistry 32, no. 1 (November 18, 2019): 1–8. http://dx.doi.org/10.14233/ajchem.2020.22283.
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Physico-chemical properties are crucial characteristics of hydrocolloids as they decide the applicability of them. Rheology of system, flow behaviour and mechanical properties make hydrocolloids suitable for food industry. Modification of consistency or texture properties of functional polymers also controls their sensory characteristics, thereby they become significant essences such as thickener, gelling agents, foaming agent, texture modifier, viscosifier, emulsifier, stabilizer and binder. Industrial and pharmaceutical applications are also controlled by some suitable physico-chemical properties of hydrocolloids. The polysaccharide gum exudates constitute a architecturally distinct class of complex biomacromolecules having unique physico-chemical properties. Due to their good bio/tissue compatibility, non-toxicity, they are extensively used in the field of tissue engineering, drug delivery and wound healing. Chemical and molecular architecture of hydrocolloids in turn controls their physico-chemical and functional properties. Sterculia gum is a substituted rhamnogalacturonoglycan (pectic) type exudate gum used as suspending agent, gelling agents, emulsifier, bulk laxative, dental adhesive, drug delivery agent and wound healing agent. It exhibits high water retention capacity, high viscosity and least solubility. Solutions of sterculia gum are viscoelastic and thixotropic. Sterculia gum has been recommended as effective wound dressing material as it can form a intensely adhesive gel when dispersed in minimum ammount of water. Owing to wide applications and distinctive properties of sterculia gum, present work is an endeavor to summarize the molecular organization, chemical configuration and physico-chemical properties of sterculia gum and the factors affecting physico-chemical properties of sterculia gum.
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Sharma, Shyam Bihari, Suman Jain, and K. Ganesan. "Preformulation Studies of Pralidoxime Chloride for Formulation Development of Microspheres." Journal of Drug Delivery and Therapeutics 9, no. 4-s (August 15, 2019): 338–42. http://dx.doi.org/10.22270/jddt.v9i4-s.3336.
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Microspheres are one of the novel drug delivery system which possess several applications and are made up of assorted polymers. Microspheres can be defined as solid, approximately spherical particles ranging in size from 1 to 1000 μm range in diameter having a core of drug and entirely outer layers of polymers as coating material. They are made up of polymeric, waxy or other protective materials i.e. biodegradable synthetic polymer and modified natural products such as starches, gums, proteins, fats and waxes. Preformulation is a group of studies that focus on the physicochemical properties of a new drug candidate that could affect the drug performance and the development of a dosage form. This couldprovide important information for formulation design or support the need for molecular modification. Every drug has intrinsic chemical and physical properties which has been consider before development of pharmaceutical formulation. This property provides the framework for drugs combination with pharmaceutical ingredients in the fabrication of dosage form. Objective of preformulation study is to develop the elegant, stable, effective and safe dosage form by establishing kinetic rate profile, compatibility with the other ingredients and establish Physico-chemical parameter of new drug substances. The purpose of the present study was to systematically investigate some of the important physicochemical properties of pralidoxime chloride for preparation of microspheres. The physicochemical properties such as solubility, pKa, dissolution, melting point, assay development, excipient compatibility etc. of pralidoxime chloride was carried out. Before selection of excipients, the Preformulation study of drug pralidoxime is completed for successful formulation of microspheres. The result of Preformulation studies shows good flow properties, excipient compatibility, solubility efficiency and melting point. From this study we concluded that pralidoximewith HPMC and EC can be used to formulate pralidoxime microspheres for modified release.
Keywords: Microspheres, Preformulation, Pralidoxime chloride, Physico-chemical parameter.
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Tiwari, Sandip Prasad, and Gali Vidyasagar. "Identification, Characterization and Drug-Excipient Compatibility of Diltiazem Hydrochloride by Physico-Chemical Techniques." UK Journal of Pharmaceutical Biosciences 2, no. 5 (October 1, 2014): 49. http://dx.doi.org/10.20510/ukjpb/2/i5/91134.
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Bruni, Giovanna, Vittorio Berbenni, Chiara Milanese, Alessandro Girella, and Amedeo Marini. "Drug-excipient compatibility studies in binary and ternary mixtures by physico-chemical techniques." Journal of Thermal Analysis and Calorimetry 102, no. 1 (August 28, 2009): 193–201. http://dx.doi.org/10.1007/s10973-009-0382-z.
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Vivekanandan S, Raghunandan Reddy K, and Venkatesan P. "Preformulation characterization towards design and development of dexibuprofen loaded nanoparticles." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (December 21, 2020): 8138–45. http://dx.doi.org/10.26452/ijrps.v11i4.4892.
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The intention of the current study was to investigate the Physico-chemical characteristics of Dexibuprofen loaded nanoparticles. Dexibuprofen is an NSAID - non-steroidal anti-inflammatory drug intended for the treatment of rheumatoid arthritis related symptoms. In current market trends, the tablets and capsule dosage forms captures major market contribution. A systematic evaluation of physico chemical characteristics of the drug powder, it’s characteristics was performed as a basic step at the start of formulation development of the dosage form. The formulation development approach is decided based on the above data. Dexibuprofen nanoparticles was developed by an Ionotropic pre gelation technique comprising Chitosan, Calcium chloride and Sodium alginate as coating material. The preformulation evaluation of Dexibuprofen and it’s compatibility with selected excipients was performed to design an appropriate strategy for the development of Dexibuprofen modified release nanoparticles. The parameters like melting point, pKa, solubility, dissolution and assay method development, solid state stability, solution stability, flow properties, bulk density, microscopical assessment, entrapment efficiency, excipients compatibility, and nanoparticles release profile were evaluated. The results of this study, along with the experimental values, will be discussed in detail.
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Mohamed, Amir Ibrahim, Amal Abd-Elaal El-Khamery, Mohamed Ismail Herry, and Alaa Ibrahim Mohamed. "Compatibility Determination of Drug-Polymer, Drug-Excipient & Drug-Intravenous Admixtures Using Chemometric-assisted UVspectrophotometry." Current Pharmaceutical Analysis 16, no. 2 (January 23, 2020): 125–42. http://dx.doi.org/10.2174/1573412914666181011142351.
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Purpose: A new multivariate chemometric approach was developed for fast and economic compatibility determinations of ranitidine hydrochloride (as model drug) with certain pharmaceutical; polymers (Alginate & Chitosan), excipient (Lactose) and intravenous fluids (Dextrose, Ringer & Dextrose/ Ringer). Binary mixtures of the drug and each item were prepared and investigated by chemometric- assisted UV- spectrophotometry as well as by HPLC reference method. Methods: Five drug concentration levels (0.004-0.025mg/ml) of test-mixtures were used and the average drug recovery percent after two and seven days of storage from initial concentration was determined. Physico-chemical techniques including DSC, XRD, & FTIR were also performed to investigate the nature of the observed drug-additive interactions. Results: UV-chemometric and HPLC results showed that ranitidine stability in mixture aqueous solutions appears to be concentration dependent. The ranitidine content remained greater than 90% in alginate & chitosan test mixtures at all used drug concentrations (0.004-0.025mg/ml), while in lactose, dextrose, ringer & dextrose/ringer test mixtures fell below 90% at low drug concentrations (0.004- 0.009mg/ml), which suggests more ranitidine compatibility with alginate & chitosan rather than the other additives. Conclusion: The developed chemometric method, employing UV absorbance data successfully used as simple, rapid, and economic alternative tool in drug-additive compatibility determinations.
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Yadav, RK, Satyam Prakash, K. Yadav, NK Yadav, and M. Mostafa. "Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug." Janaki Medical College Journal of Medical Science 3, no. 2 (November 28, 2016): 4–12. http://dx.doi.org/10.3126/jmcjms.v3i2.16075.
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Background and Objectives: The prevention and treatment of peptic ulcers has become an important challenge in the current medicine world. Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time. Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated.Materials and Methods: Nine batches of the light liquid paraffin entrapped emulsion gel beads were prepared by a new emulsion gelation technique using sodium alginate and xanthan gum as polymers. The polymeric solution was extruded into Calcium chloride solution by the use of 21G needles. Morphology of beads, drug content, drug entrapment efficiency, floating lag time and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR.Results: Mean surface diameter were between 1.220 ± 2.259% (F1) to 1.230 ± 2.316% (F9) and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric fluid at 37ºC. The drug content and drug entrapment efficiency among the formulations were between 17.48%~19.68% and 71.06% ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile.Conclusion: The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug. Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12
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Kamin, Wolfgang, Astrid Schwabe, and Irene Krämer. "Inhalation solutions – which one are allowed to be mixed? Physico-chemical compatibility of drug solutions in nebulizers." Journal of Cystic Fibrosis 5, no. 4 (December 2006): 205–13. http://dx.doi.org/10.1016/j.jcf.2006.03.007.
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Kamin, Wolfgang, Frank Erdnüss, and Irene Krämer. "Inhalation solutions — Which ones may be mixed? Physico-chemical compatibility of drug solutions in nebulizers — Update 2013." Journal of Cystic Fibrosis 13, no. 3 (May 2014): 243–50. http://dx.doi.org/10.1016/j.jcf.2013.09.006.
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Ronowicz-Pilarczyk, Joanna. "Compatibility Study of Ketoprofen With Selected Excipients Used in Solid Dosage Forms: Experimental Design Approach." Acta Poloniae Pharmaceutica - Drug Research 80, no. 5 (November 21, 2023): 717–22. http://dx.doi.org/10.32383/appdr/172622.
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A good understanding of the physico-chemical characteristics of a drug substance and excipients is necessary to obtain a safe and effective drug dosage form. Based on the current recommendations of the regulatory agencies (EMA, FDA) regarding the implementation of the Quality by Design concept at the drug product development stage, this article is focused on the application of the experimental design approach at the preformulation studies. The purpose of this work was the implementation of experimental design methodology in a compatibility study between ketoprofen (non-steroidal anti-inflammatory drug) and selected solid dosage forms excipients. The fractional factorial design was used to generate a matrix of multi-component mixtures of ketoprofen and selected excipients. In order to accelerate any chemical incompatibilities, the received mixtures were exposed to elevated temperature and humidity (60°C/75% RH) in a climate chamber for 3 weeks. The ketoprofen-excipients compatibility was studied by means of the RP-HPLC method. It was confirmed that the type of disintegrant had a strong impact on ketoprofen degradation. The incompatibility in mixtures of ketoprofen with sodium starch glycolate was indicated. According to literature data, it may be the result of a decrease in crystallinity and thus a decrease in the stability of ketoprofen in the presence of sodium starch glycolate. The effects of the other types of excipients were statistically insignificant (p > 0.05). The applied experimental design methodology allowed for a rational selection of optimal excipients and thus, this approach may support significantly decision-making in the pharmaceutical industry.
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Dr. P Perumal. "The Preparation and In-vitro Evaluation of Sustained Release Capsules of Rivastigmine Tartrate." Asian Journal of Medicine and Biomedicine 7, no. 2 (October 20, 2023): 139–65. http://dx.doi.org/10.37231/ajmb.2023.7.2.624.
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Rivastigmine tartrate is a cholinesterase inhibitor, used in the treatment of dementia associated with Parkinson’s disease and it is currently available in a capsule form. Hydroxy Propyl Methyl Cellulose (HPMC) is the most important hydrophilic carrier material used for the preparation of oral controlled drug delivery systems due to its high swellability and its significant effect on the release kinetics of an incorporated drug. The present study was designed to prepare sustained release granules of Rivastigmine tartrate by using HPMC as matrix former, Microcrystalline cellulose (MCC) as diluent and Magnesium Stearate as lubricant. Blend of Eudragit co-polymers on different ratio was used to coat the granules. The drug-excipient compatibility studies were carried out by using FT-IR, DSC and XRPD analysis. The results shown that there was no significant interaction between the drug and excipients. Granules were prepared by wet granulation method. The granules were subjected to physico-chemical, drug content and in-vitro drug release studies. The best fit release kinetics was achieved with Higuchi equations followed by first order kinetics from the above results it was concluded that extended release granules of Rivastigmine tartrate can be prepared by using HPMC and also found that coating of granules with Eudragit co-polymers also effective to extend the release of drug.
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Amin, Prakruti, and Manish Patel. "Preformulation Studies of Varenicline for Formulation and Development of a Novel Orally Disintegrating Film." Journal of Pharmaceutical Research International 35, no. 17 (July 7, 2023): 31–40. http://dx.doi.org/10.9734/jpri/2023/v35i177388.
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Objective: The major goal of pre-formulation research is to create a drug delivery system that is stable, elegant, safe, and effective by determining the drug's kinetic profile, the formulation's compatibility with various excipients, and the physico-chemical characteristics of new drug molecules. This could offer crucial support for executing formulation design or the need for the molecular change. Therefore, in the current study, studies on Varenicline (VAR)'s appropriateness for oral formulation were conducted. Similar to cytisine, VAR functions as a partial nicotine receptor agonist. It blocks alpha-4-beta-2 nicotinic acetylcholine receptor subtypes and is a partial agonist. Through partial agonism, VAR reduces the urge and withdrawal symptoms associated with quitting efforts by inhibiting the dopaminergic activation brought on by smoking. It stops nicotine from stimulating the mesolimbic dopamine pathway, which is linked to nicotine addiction.
Methods: The authenticity of VAR was established by DSC and FTIR spectra. A UV spectrophotometric method was employed for determination of VAR in bulk and active pharmaceutical ingredient (API).
Results: The authenticity of VAR was established by DSC and FTIR spectra. For the determination of VAR in bulk API (active pharmaceutical ingredient), a UV spectrophotometric approach was used. In the concentration range of 5–40 g/ml, the UV technique was linear. The lower% CV values of intraday and interday variability indicate the proposed methodology's robustness. The higher regression coefficient value(0.999) indicates the methodology is robust.
Conclusions: The outcome of the physico-chemical experiments of drug molecule indicates suitability of oral route. Additionally, at different conditions like solid as well as liquid state, the drugmoleculewasobservedstable.
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Qushawy, Mona. "Effect of the Surfactant and Liquid Lipid Type in the Physico-chemical Characteristics of Beeswax-based Nanostructured Lipid Carrier (NLC) of Metformin." Pharmaceutical Nanotechnology 9, no. 3 (August 13, 2021): 200–209. http://dx.doi.org/10.2174/2211738509666210222143716.
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Background: Metformin (MF) is an antidiabetic drug that belongs to class III of the biopharmaceutical classification system (BCS) characterized by high solubility and low permeability. Objective: The study aimed to prepare metformin as nanostructured lipid carriers (MF-NLCs) to control the drug release and enhance its permeability through the biological membrane. Methods: 22 full factorial design was used to make the design of MF-NLCs formulations. MFNLCs were prepared by hot-melt homogenization-ultra sonication technique using beeswax as solid lipid in the presence of liquid lipid (either capryol 90 or oleic acid) and surfactant (either poloxamer 188 or tween 80). Results: The entrapment efficiency (EE%) of MF-NLCs was ranged from 85.2±2.5 to 96.5±1.8%. The particle size was in the nanoscale (134.6±4.1 to 264.1±4.6 nm). The value of zeta potential has a negative value ranged from -25.6±1.1 to -39.4±0.9 mV. The PDI value was in the range of 0.253±0.01 to 0.496±0.02. The cumulative drug release was calculated for MF-NLCs and it was found that Q12h ranged from 90.5±1.7% for MF-NLC1 to 99.3±2.8 for MF-NLC4. Infra-red (IR) spectroscopy and differential scanning calorimetry (DSC) studies revealed the compatibility of the drug with other ingredients. MF-NLC4 was found to be the optimized formulation with the best responses. Conclusion: 22 full factorial design succeed to obtain an optimized formulation which controls the drug release and increases the drug penetration.
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Saleem, Anam, Naveed Akhtar, Muhammad Usman Minhas, Arshad Mahmood, Kifayat Ullah Khan, and Orva Abdullah. "Highly Responsive Chitosan-Co-Poly (MAA) Nanomatrices through Cross-Linking Polymerization for Solubility Improvement." Gels 8, no. 3 (March 21, 2022): 196. http://dx.doi.org/10.3390/gels8030196.
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In this study, we report the highly responsive chitosan-based chemically cross-linked nanomatrices, a nano-version of hydrogels developed through modified polymerization reaction for solubility improvement of poorly soluble drug simvastatin. The developed nanomatrices were characterized for solubilization efficiency, swelling studies, sol-gel analysis, in vitro drug release studies, DSC, FTIR, XRD, SEM, particle size analysis, and stability studies. An in vivo acute toxicity study was conducted on female Winstor rats, the result of which endorsed the safety and biocompatibility of the system. A porous and fluffy structure was observed under SEM analysis, which supports the great swelling tendency of the system that further governs the in vitro drug release. Zeta sizer analyzed the particle size in the range of 227.8 ± 17.8 nm. Nano sizing and grafting of hydrophilic excipients to the nanomatrices system explains this shift of trend towards the enhancement of solubilization efficiency, and, furthermore, the XRD results confirmed the amorphous nature of the system. FTIR and DSC analysis confirmed the successful grafting and stability to the system. The developed nanomatrices enhanced the release characteristics and solubility of simvastatin significantly and could be an effective technique for solubility and bioavailability enhancement of other BCS class-II drugs. Due to enhanced solubility, efficient method of preparation, excellent physico-chemical features, and rapid and high dissolution and bio-compatibility, the developed nanomatrices may be a promising approach for oral delivery of hydrophobic drugs.
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Khan, Hafeez Ullah, Fahmeed Nasir, Safirah Maheen, Syed Salman Shafqat, Shahid Shah, Ahmed Khames, Mohammed M. Ghoneim, et al. "Antibacterial and Wound-Healing Activities of Statistically Optimized Nitrofurazone- and Lidocaine-Loaded Silica Microspheres by the Box–Behnken Design." Molecules 27, no. 8 (April 14, 2022): 2532. http://dx.doi.org/10.3390/molecules27082532.
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In the current study, nitrofurazone- (NFZ) and lidocaine-loaded (LD) silica microspheres were fabricated to address pathological indications of skin infections. The microspheres were prepared by the sol–gel method applying the Box–Behnken design and evaluated for size distribution, morphology, zeta potential, physico-chemical compatibility, XRD, thermogravimetric analysis, antibacterial and cytotoxicity activities. The comparative in vitro drug release study of microspheres revealed a 30% release of NFZ and 33% of LD after 8 h. The microspheres showed 81% percentage yield (PY) and 71.9% entrapment efficiency. XRD patterns confirmed the entrapment of NFZ–LD in silica microspheres with a significant reduction in crystallinity of the drugs. Thermal and FTIR studies proved the absence of any profound interactions of the formulation ingredients. The smooth spherical microspheres had a −28 mV zeta potential and a 10–100 µm size distribution. In vitro antibacterial activities of the NFZ–LD microspheres showed an increased zone of inhibition compared to pure drug suspensions. The in vivo efficacy tested on rabbits showed a comparatively rapid wound healing with complete lack of skin irritation impact. The cytotoxicity studies revealed more acceptability of silica microspheres with negligible harm to cells. The study suggests that the NFZ- and LD-loaded silica microspheres would be an ideal system for accelerating and promoting rapid healing of various acute and chronic wounds.
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Eze, Fredrick Nwude, Chaweewan Jansakul, and Teerapol Srichana. "Insights into the formulation properties, biocompatibility, and permeability of poorly water-soluble methoxyflavones with PEG400 and propylene glycol." Acta Pharmaceutica 73, no. 3 (September 1, 2023): 385–404. http://dx.doi.org/10.2478/acph-2023-0030.
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Abstract Herein, thermal and non-thermal techniques were used to elucidate the putative physical and chemical interactions between poorly water-soluble Kaempferia methoxyflavones and PEG400/propylene glycol. Additionally, the biocompatibility of methoxyflavone-glycol solutions was evaluated using Caco-2 cells whereas the absorptive transport was investigated by measuring the apparent permeability coefficient (P app) of the methoxyflavones and transepithelial electrical resistance (TEER) of the Caco-2 cell monolayer. Data from differential scanning calorimetry, Fourier-transform infrared (FTIR), and proton nuclear magnetic resonance (1H NMR) spectroscopic analysis revealed physico-chemical compatibility between the three methoxyflavones and PEG400/propylene glycol. Furthermore, PEG400 and propylene glycol solutions of the methoxyflavones were shown to be compatible with Caco-2 cells at pharmacologically effective concentrations. In vitro transport studies across the Caco-2 cell monolayer revealed high P app values of 24.07 × 10–6 to 19.63 × 10–6 cm s–1 for PEG400 solutions of the methoxyflavones. The TEER values of the Caco-2 cell monolayers indicated that the increased drug transport was partly due to increased tight junction openings, but without compromising the epithelial barrier integrity. The good pharmaceutical and biocompatibility profiles, as well as improved transport of the methoxyflavones in PEG400 and propylene glycol solutions, are suggestive of the worthiness of this approach for further consideration pertaining to the development of these drugs into oral liquid dosage forms.
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Kota, Ravi Kumar, and Suresh Gande. "Development and Evaluation of Olmesartan Medoxomil Controlled Release Floating Microspheres using Natural Gums." International Journal of Pharmaceutical Sciences and Nanotechnology 10, no. 4 (July 31, 2017): 3788–94. http://dx.doi.org/10.37285/ijpsn.2017.10.4.6.
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The present research was aimed to prepare Olmesartan medoxomil floating microspheres for controlled release using polymers such as sodium alginate, sodium bicarbonate, calcium chloride, Hydroxy propyl methyl cellulose (HPMC K4M, K15M), Olibanum gum and Xanthan gum by ionotropic gelation method. The prepared microspheres were evaluated for the percent drug content, entrapment efficiency, percentage buoyancy and in vitro dissolution studies. Among all the formulations F14 was selected as optimized formulation based on the micromeretic and physico-chemical parameters including drug release studies. Percentage buoyancy of optimized formulation was found to be 96.45%. In vitro release study of formulation F14 showed 98.11% drug release after 12 h in a controlled manner, which is desired for disease like Hypertension. The reference standard shows the drug release of 94.12% within 12 h. Drug and excipient compatibility studies were carried out by FT-IR and no interactions were observed. The SEM of microspheres show a hollow spherical structure with a rough surface morphology. Some of microspheres showed dented surface structure but they showed good floating ability on medium indicated intact surface. The shell of microspheres also showed some porous structure which might be due to release of carbon dioxide. F14 followed zero order, Higuchi and Korsmeyer Peppas kinetics indicating diffusion controlled with non-fickian (anomalous) transport, projecting that its active ingredient are delivered by coupled diffusion and erosion. From these results, it can be concluded that the polymer proportion controlled the drug release from the olmesartan floating microspheres.
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T.Ismail, Sara, Myasar M. Al-Kotaji, and Ahlam A. Khayrallah. "Formulation and Evaluation of Nystatin Microparticles as a Sustained Release System." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 24, no. 2 (March 26, 2017): 1–10. http://dx.doi.org/10.31351/vol24iss2pp1-10.
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Nystatin is the drug of choice for treatment of cutaneous fungal infections with main disadvantage that is the need for multiple applications to achieve complete eradication which may reduce patient compliance. Microparticles offer a solution for such issue as they are one of sustained release preparations that achieve slow release of drug over an extended period of time. The objectives of this study were to fabricate nystatin-loaded chitosan microparticles with the ultimate goal of prolonging drug release and to analyze the influence of polymer concentration on various properties of microparticles. Microparticles were prepared by chemical cross-linking method using glutaraldehyde as cross-linking agent. Five formulas, namely N1C1, N1C2, N1C3, N1C4 and N1C5, were prepared and the effect of drug to polymer ratio was studied with respect to drug loading, encapsulation efficiency, particle size and morphology. Furthermore the prepared microparticles were subjected to various physico-chemical studies, such as drug- polymer compatibility by Fourier Transform Infrared Spectroscopy (FTIR) and in-vitro drug release characteristics. Microparticles obtained from N1C1, N1C2 and N1C3 formulas were regular in shape with mean particle size ranging between 1µm and 10µm. N1C5 formula was resulted in particles with irregular shape while N1C4 showed a blend of microparticles and deformed particles. The effect of chitosan concentration on drug loading and entrapment efficiency was studied. The results showed increment in these parameters that was directly proportional to the increment in polymer concentration. Percentage yield showed a significant increment which was related to the increment in the ratio of chitosan used during the study. FTIR results showed no interactions between nystatin and chitosan. DSC studies proved the crystalline nature of nystatin and chitosan. On other hand, the thermogram of loaded microparticles showed the absence of endothermic peak corresponding to nystatin which may indicate the loss of the crystalline nature of the drug presented inside the microparticles. In- vitro release studies resulted in 95.6% release of nystatin for N1C1 after 15 hours. N1C1 appeared to be promising in formulating microparticles that provide nearly complete release of the drug within15 hours. This formula can be selected in future work to be formulated as topical gel that prolongs the release of nystatin.
Keywords: Nystatin, Chitosan, Glutaraldehyde, Chemical cross-linking.
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Alvi, Zunaira, Muhammad Akhtar, Nisar U. Rahman, Khaled M. Hosny, Amal M. Sindi, Barkat A. Khan, Imran Nazir, and Hadia Sadaquat. "Utilization of Gelling Polymer to Formulate Nanoparticles Loaded with Epalrestat-Cyclodextrin Inclusion Complex: Formulation, Characterization, In-Silico Modelling and In-Vivo Toxicity Evaluation." Polymers 13, no. 24 (December 12, 2021): 4350. http://dx.doi.org/10.3390/polym13244350.
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Epalrestat (EPL) is an aldose reductase inhibitor with poor aqueous solubility that affects its therapeutic efficacy. The research study was designed to prepare epalrestat-cyclodextrins (EPL-CDs) inclusion complexes to enhance the aqueous solubility by using beta-cyclodextrin (β-CD) and sulfobutyl ether₇ β-CD (SBE7 β-CD). Furthermore, polymeric nanoparticles (PNPs) of EPL-CDs were developed using chitosan (CS) and sodium tripolyphosphate (sTPP). The EPL-CDs complexed formulations were then loaded into chitosan nanoparticles (CS NPs) and further characterized for different physico-chemical properties, thermal stability, drug-excipient compatibility and acute oral toxicity studies. In-silico molecular docking of cross-linker with SBE7 β-CD was also carried out to determine the binding site of the CDs with the cross-linker. The sizes of the prepared NPs were laid in the range of 241.5–348.4 nm, with polydispersity index (PDI) ranging from 0.302–0.578. The surface morphology of the NPs was found to be non-porous, smooth, and spherical. The cumulative percentage of drug release from EPL-CDs loaded CS NPs was found to be higher (75–88%) than that of the pure drug (25%). Acute oral toxicity on animal models showed a biochemical, histological profile with no harmful impact at the cellular level. It is concluded that epalrestat-cyclodextrin chitosan nanoparticles (EPL-CDs-CS NPs) with improved solubility are safe for oral administration since no toxicity was reported on vital organs in rabbits.
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Vaishnavi, Bandari, G. Tarun Reddy, Akash Bansal, Deva Likitha, Deeksha Charagondla, and D. Prasanthi. "Solubility Enhancement of Efinaconazole using Neem Gum and Evaluation of Antifungal Activity." Indian Journal Of Science And Technology 17, no. 17 (April 14, 2024): 1735–44. http://dx.doi.org/10.17485/ijst/v17i17.311.
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Objectives: Efinaconazole is an anti-fungal drug of BCS class II used for treating Onchomycosis. Neem gum known for its antifungal properties was purified and used as hydrophilic carrier. Solid dispersions by physical mixture and solvent evaporation method were prepared using purified Neem gum. Methods: The prepared solid dispersions in ratios 1:1, 1:3 and 1:6 were characterized for percentage yield, assay, solubility, and dissolution studies. The optimized solid dispersion SD6 was formulated as gel for ease of application. Gels were characterized for physico-chemical properties and in-vitro diffusion studies. The optimized gel was evaluated for anti-fungal activity. Findings: FTIR, DSC and XRD studies of optimized SD6 showed compatibility and amorphous nature respectively. G2 gel formulation containing SD6 solid dispersion showed 80.4±0.14% when compared to G1 56.76±0.34% release in 8hrs. Both the gels followed zero order and Higuchi release. Antifungal studies indicated more efficiency of G2 gel by zone of inhibition when compared with G1 containing only drug. G2 gel was found to be stable for one month. Novelty : In the present research work purified neem gum, which is natural carrier and neem known for its antifungal activity was used to enhance the solubility of drug and evaluate the antifungal activity of drug with purified neem gum. Conclusion: Hence it can be concluded, purified Neem gum can be used as hydrophilic carrier and as solubility of Efinaconazole was enhanced its antifungal activity was also increased. Keywords: Onchomycosis, Efinaconazole, Neem gum, Solid dispersions, Antifungal
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Jumat, Mohamad Amin, Nor Syahiran Zahidin, Mohd Amirul Aizat Zaini, Nurul Afiqah Fadzil, Hadi Nur, and Syafiqah Saidin. "INCORPORATION OF ACALYPHA INDICA EXTRACT IN POLYVINYL ALCOHOL HYDROGELS: PHYSICO-CHEMICAL, ANTIBACTERIAL AND CELL COMPATIBILITY ANALYSES." Jurnal Teknologi 83, no. 2 (February 2, 2021): 57–65. http://dx.doi.org/10.11113/jurnalteknologi.v83.14763.
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Acalypha indica (A. indica) possesses antibacterial properties and has capability to accelerate wound healing due to its active therapeutic compounds of flavonoid and alkaloid. The incorporation of A. indica extracts in polymer hydrogels is useful for wound treatment, despite the advancement in synthetic medicines and drugs. In this study, polyvinyl alcohol (PVA) hydrogels with different concentrations of A. indica extract (0.5, 1.0, 1.5 and 2.0 mg) were fabricated. The ATR-FTIR spectra testified the presence of A. indica in the hydrogels. More enormous spotted agglomerations were visualized on the higher concentrations of A. indica hydrogels. The A. indica hydrogels became less moisture, more hydrophobic and has low water uptake ability compared to the control hydrogel (without A. indica). The antibacterial activities of the hydrogels against Escherichia coli and Staphylococcus aureus were acted in a dose-dependent manner where higher inhibition zones and higher bacterial retardations were recorded on the hydrogels with higher concentrations of A. indica. The incorporation of A. indica (1.0 - 1.5 mg/mL) has also induced cell viability, cell migration, and proliferation of the human skin fibroblasts. Therefore, optimization of the A. indica hydrogels is crucial in accommodating the bi-functional properties of antibacterial and biocompatibility for wound treatment.
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Semberova, Jana, Karel Holada, Olga Simakova, Monique P. Gelderman-Fuhrmann, and Jan Simak. "Carbon Nanotubes Activate Platelets by Facilitating Extracellular Ca2+ Influx." Blood 112, no. 11 (November 16, 2008): 992. http://dx.doi.org/10.1182/blood.v112.11.992.992.
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Abstract Due to a unique combination of their physico-chemical properties, carbon nanotubes (CNTs) are among the principal materials used in biomedical nanotechnologies. Superior mechanical characteristics like elasticity (CNTs 1012Pa vs. steel 108Pa) and tensile strength (CNTs 100 GPa vs. steel 2 GPa) make CNTs very attractive candidates as materials for plastic composites for various biomedical applications including devices for collection, processing, and storage of blood transfusion products. Moreover, CNTs have a profound impact on the development of diagnostic biosensors, drug delivery nanosystems, or imaging nanoprobes for intravascular use. Thus the investigation of CNT activities on platelets is a critical safety issue. We studied the effects of PBS suspensions of structurally different purified CNT materials from different manufacturers (Nanolab, NanoAmor, SES, MER) on human platelets (PLTs) and compared their effects to amorphous carbon black nanoparticles (ACB; > 99%, mean size 30 nm, Aldrich), C60 fullerene (nC60; 99.9%), fullerenol C60(OH)24 (both from MER Corp.), and NIST standard polystyrene nanobeads (PNBs; 20nm and 200nm; Duke Scientific Corp.). Using aggregometry of human platelet rich plasma (PRP), we found that CNT materials induced PLT aggregation in a concentration dependent manner. Single wall CNTs (SWCNTs) at 100 μg/mL showed PLT-aggregation 34 ± 10%, similarly to most tested multiwall CNTs (MWCNTs), which was significantly higher compared to ACB 15 ± 4%; p = 0.03. In contrast, fullerene nC60, fullerenol C60OH24, PNBs, or vehicle (PBS) did not cause any significant PLT aggregation (4 ± 0.5%; positive control collagen 100%). Interestingly, the thicker MWCNTs of d = 60nm (MWCNT60) exhibited significantly higher aggregating activity (27 ± 6%) compared to MWCNTs of d = 15nm (13 ± 3%; p = 0.007). Moreover, the bamboo structured MWCNTs showed only very low aggregating activity (7 ± 6%) compared to the corresponding hollow MWCNTs (33 ± 15%; p = 0.001). The PLT aggregation response (MA, AUC) induced by CNTs was proportional to the extracellular Ca2+concentration and was completely inhibited by 100 μM EDTA. The activation-dependent Ca2+ channel blocker SKF 96365 at 100 μM caused a significant inhibition (64 ± 16%) of MWCNT60-induced PLT-aggregation response. In contrast, no inhibitory effect on CNT-induced PLT-aggregation response was observed with 2-APB (20 μM; IP3 receptor inhibitor), NF 449 (1 μM; P2X1 blocker), MRS 2500 (5 nM; P2Y1 blocker), or TBHQ (20 μM; SERCA3 blocker). The effect of CNTs on intracellular free Ca2+ concentration [Ca2+]i was studied using a ratio fluorometry in platelets loaded with a Ca2+-sensitive probe FURA-2AM. Changes in fluorescence in individual platelets (n=100) were monitored using an epifluorescence/contrast phase microscope with a low light-level CCD camera/microphotometer assembly. We demonstrated that in contrast to ACB or PNBs, MWCNTs induced in platelets a rapid concentration dependent elevation of [Ca2+]i. For example, MWCNT60 at 100 μg/mL caused a 107 ± 4 nM increase in [Ca2+]i in platelets. No response was observed in Ca2+ free buffer. In addition, the flow cytometric analysis demonstrated that CNT-induced PLT activation led to surface exposure of CD62P and CD63 and a release of CD62P+ and CD63+ platelet membrane microparticles (MPs). In conclusion, we demonstrated that CNTs activate platelets and cause a platelet release reaction, aggregation, and release of MPs. The PLT-activating effect of CNTs is structure dependent: the hollow and thicker (60 nm) MWCNTs were most potent. A likely mechanism is that CNTs induce extracellular Ca2+ influx with involvement of activation-dependent Ca2+ channels. Our results warrant further studies on blood compatibility of CNT materials for biomedical applications. Caution needs to be applied when considering CNT materials as additives for plastics for transfusion devices and other devices that come in contact with blood. The findings and conclusions in this study have not been formally disseminated by the Food and Drug Administration and should not be construed to represent any Agency determination or policy.
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Babu, Gorantla Naresh, Menaka Muthukarupan, Hindustan Abdul Ahad, and Veerabomma Sreedhar. "Fabrication and Preliminary Assessment of Neem Fruit Mucilage as Mucoadhesive Abetting Assets with Methpol-934P for Acyclovir Delivery from Mucoadhesive Microcapsules." Biomedical and Pharmacology Journal 15, no. 4 (December 20, 2022): 2179–84. http://dx.doi.org/10.13005/bpj/2554.
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In this study, we investigated the mucoadhesive properties of neem fruit mucilage by incorporating it into mucoadhesive microcapsules with Acyclovir (ACR). Methpol-934P and Neem fruit mucilage (NFM) was used to construct 12 different mucoadhesive microcapsules. We assessed FTIR and DSC capabilities for compatibility with ACR and NFM. ACR mucoadhesive microcapsules (ANMM) were characterized for mucoadhesion and ACR release Physico-chemical characteristics. CR was found to be compatible with NFM in the research. The entrapment increased as the levels of NFM in the formulations increased, and mucoadhesion time was longer in formulations with higher levels of NFM. As levels of NFM increase in formulations, the release of drugs is slightly reduced. NFM may be responsible for this due to its release retarding properties. An additive of neem fruit mucilage allowed for the retention of ACR after ingestion when a mucoadhesive polymer (methpol 934P) was used.
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Ashwin, Kancham, Tummuluru R. Reddy, and Puttaswamy Nirmala. "Preparation and Evaluation of Extended Release Trilayered Matrix Tablets of Ramipril Using Design of Experiment." International Journal of Pharmaceutical Sciences and Drug Research 13, no. 06 (November 30, 2020): 629–37. http://dx.doi.org/10.25004/ijpsdr.2021.130605.
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The current work is aimed to design, prepare, and evaluate the trilayer matrix tablets incorporated with ramipril for extended drug release. Twenty-seven formulations (RF1-RF27) for active layer (middle layer) were prepared by direct compression method using 33 Response surface method of polymers of different HPMC K4M, HPMC K15M and xanthan gum (low, middle, and high concentrations) by using Design of experiment software. Based on physico-chemical properties and drug release one formulation was chosen and formulated into extended release trilayered matrix tablets were by varying proportions of polymers by direct compression method and they were evaluated. The best optimized formulation was characterized for FTIR studies. Out of 27 active layer formulations, RF23 was chosen as best based with maximum drug release of 98.11% and was formulated into extended release trilayered matrix tablets (ARF23-HRF23) by varying proportions of polymers. The range of swelling index for all batches (ARF23-HRF23) was 82.34 to 97.46%, similarly the range of drug content was 95.49 to 99.11% and drug released in 24 hours sustainably over an extended period was 84.98 to 98.26% with all highest values exhibited by GRF23. The release order kinetics data indicate the zero-order release with highest (R2) = 0.983 for GRF23 better when compared to marketed product which followed first order showed R2 value 0.962. Further the formulation (GRF23) showed best fit to Korsmeyer-Peppas plots i.e., 0.957 indicating non Fickian (anomalous) transport coupled diffusion and erosion. The FT-IR data assure the compatibilityof drug and excipients. GRF23 was found to be stable for 180 days at accelerated conditions.
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D’Huart, Elise, Pauline Lider, Jean Vigneron, and Béatrice Demoré. "Evolution of the Stabilis® Database: Creation of a Level of Evidence for Stability Studies." Pharmaceutical Technology in Hospital Pharmacy 3, no. 1 (March 26, 2018): 3–12. http://dx.doi.org/10.1515/pthp-2018-0002.
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AbstractBackgroundStabilis®is an international database on stability and compatibility of drugs. The stability data comes mainly from publications of pharmaceutical journals. As the quality of the published stability studies is not equivalent, the objective of this work was to propose a level of evidence for the physico-chemical stability studies selected for the database.MethodsAt first, we evaluated the main pharmacological class consulted by the users. This work was then divided into 5 steps: (1) updating of the criteria to validate a stability study, (2) creating a grid rating articles, (3) rating of the articles of stability studies for anticancer, antifungal and antiviral drugs by 2 evaluators, (4) creation of new screens in the database to enter rating, to visualize the pictograms and commentaries by the users, (5) creation of a guideline to explain the different levels of evidence.ResultsThe main pharmacological class consulted by Stabilis®users is the anticancer drugs and then antiinfectives. We have selected anticancer, antifungal and antiviral drugs for our study. Two hundred and forty publications were evaluated. The highest level attributed was A for anticancer and antifungal drugs and C for antiviral drugs. This difference can be explained by the fact that the majority of publications about antiviral drugs were older.The most frequent anomalies in the rating of articles were an incomplete or imperfect validation of the analytical method (high value of the coefficient of variation) and a defect in the evaluation of the stability indicating capacity.It must be noted that the level of evidence is not the quality level of the analytical method but the mixture of the quality of the method validation and of the results. This aspect was a choice of the Stabilis®team and seems important because the security of the patient is impacted by both aspects.ConclusionsThis new function contributes to help the Stabilis®users to evaluate the stability data published and to take a decision for their use in daily practice. This function will be progressively extended to other pharmacological classes of injectable drugs and then for non-injectable preparations.
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Nadendla, Rama Rao, Prachet Pinnamaneni, Siva Prasad Morla, and Patchala Abhinandana. "Physico-Chemical Characterization of Paliperidone Palmitate and Compatibility Studies with its Pharmaceutical Excipients." Journal of Pharmaceutical Research International, March 1, 2021, 85–91. http://dx.doi.org/10.9734/jpri/2021/v33i531183.
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Aim: The main aim of the present study was to characterize and perform the compatibility studies of paliperidone with its excipients.
Study Design: Physico-chemical characterization and compatibility studies.
Place and Duration of the Study: Chalapathi Drug Testing Laboratory, Chalapathi Institute of Pharmaceutical Sciences, Chalapathi Nagar, Lam, Guntur-522034 between December 2020 and January 2021.
Methodology: Physico-chemical characterization and compatibility studies of paliperidone palmitate with its excipients like HPMC, lactose, magnesium stearate, talc, microcrystalline cellulose was done using the FTIR spectrophotometer, Scanning electron microscopy, X-ray diffraction, Differential scanning calorimeter.
Results: Interaction of the paliperidone palmitate with its excipients were studied by this technique. Paliperidone palmitate showed the transition at 117.920C with the specific heat of 101.9J/g. The IR spectrum of paliperidone palmitate and excipients mixture has shown a characteristic stronger band of the N-H at 3412.75cm-1, C-H at 2921.98 cm-1, stretching vibrations of C=O at 1737.47 cm-1, C=C at 1651.94 cm-1, N-O at 1541.16 cm-1 followed by C-F at 1160.46 cm-1. XRD showed good crystalline properties with relative crystallinity index of 60.01%. The photomicrographs obtained by SEM did not evidence any interaction between paliperidone palmitate and the excipients, providing visual support for the results.
Conclusion: There were no interactions of drug with selected excipients and found to be compatible. Therefore, it is a mandatory clause for the compound compatibility with various excipients in the formulation which affect the stability and efficacy of the formulation.
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Nadendla, Rama rao, Satyanarayana Juluri, Sai shanmukh srinivas Doppalapudi, Venkata harshavardhan Pyda, Avinash Tadiboina, Vishnuvarddhaan Addanki, and Sriharshavardhan Kalluri. "Physico-Chemical Characterization of Rivaroxaban and Compatibility Studies with Its Pharmaceutical Excipients." International Journal of Life Science and Pharma Research, May 1, 2021, P25—P32. http://dx.doi.org/10.22376/ijpbs/lpr.2021.11.3.p25-p32.
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Physico-chemical compatibility studies were performed to check the effect of different excipients on API and it is the prerequisite in the preformulation studies. The main aim of this research is to study the behavior of the API individually and with the selected pharmaceutical excipients which mainly contribute in the selection of suitable excipients for developing an ideal dosage form. Rivaroxaban is an oral anticoagulant that mainly acts by blocking coagulant factor Xa. Incompatibility studies were performed for rivaroxaban with selected pharmaceutical excipients like HPMC, lactose, magnesium stearate, sodium lauryl sulfate, microcrystalline cellulose, croscarmellose sodium, HPC using the Scanning electron microscopy, X-ray powder diffraction and differential scanning calorimeter. A 1:1 physical mixture of rivaroxaban and selected excipient was analysed using differential scanning calorimeter. Rivaroxaban showed the transition at 231.79 0C with 114.2J/g specific heat of fusion. The transition temperature of rivaroxaban has not changed much when compared with the combination of rivaroxaban with excipients. The 2θ values of the standard drug were compared with the spectrum obtained from the XRD study. This comparison showed that there was no evidence regarding the incompatibility of the drug with excipients. The photomicrographs obtained by SEM did not showed any interaction between rivaroxaban and the excipients, providing visual support for the results.
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Patel, Dhaval J., Saurav M. Patel, Sanjesh G. Rathi, and Shrenik K. Shah. "Formulation and Evaluation of Transdermal Patch of Blonanserin." International Journal of Pharmaceutical Sciences Review and Research 69, no. 2 (August 15, 2021). http://dx.doi.org/10.47583/ijpsrr.2021.v69i02.011.
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The objective of the present study was to formulate and evaluate transdermal patch of Blonanserin. Blonanserin transdermal patches were prepared by solvent casting method using natural and synthetic polymer. Various plastisizer were screened along with polymers. Drug excipient compatibility studies concluded that the drug and excipient are compatible with each other. The prepared patches were evaluated for physico-chemical parameters to justify their suitability for transdermal use. Formulations containing Xanthan Gum with plasticizer propylene glycol gives best drug release in 8 hours. More than 90% drug release found after 8 hours in formulation F5. Hence F5 formulation is considered as optimized batch. F5 batch was found stable during stability study. Blonanserin transdermal patches were successfully prepared by solvent casting method using Xanthan Gum natural polymer.
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Thi, Phuong Le, Thi Yen Nhi Tran, Hung Cuong Luu, Dieu Linh Tran, Thai Thanh Hoang Thi, and Dai Hai Nguyen. "In situ forming gelatin: Cyclodextrin hydrogels prepared by “click chemistry” to improve the sustained release of hydrophobic drugs." Journal of Bioactive and Compatible Polymers, June 7, 2022, 088391152210980. http://dx.doi.org/10.1177/08839115221098058.
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Injectable hydrogels offer a wide range of attractive benefits in drug delivery applications, such as non-invasive administration, easy drug incorporation and locally controlled release at the target sites. Herein, we designed a simple and efficient method to prepare injectable hydrogels composed of gelatin and cyclodextrin (CD) for high loading capacity of hydrophobic drugs. The hydrogels were formed by thiol-functionalized gelatin (GSH) and βCD-vinyl sulfone (βCD-VS) as cross-linker, via thiol-ene “click” chemistry. Hydrogels comprising of different cross-linker feed amount were investigated in terms of their physico-chemical properties, such as gelation time, mechanical strength, swelling ratio, porosity and degradation rates. For the use as a drug delivery vehicle, dexamethasone (DEX), a commonly anti-inflammatory, immunosuppressive but poorly water soluble drug was chosen to show the high drug loading capacity and prolonged drug release of hydrogels. The drug release was found to be depended on the concentration of βCD-VS due to the drug-CD interaction. In vitro cytotoxicity experiment also showed the cell compatibility of these hydrogels against human dermal fibroblasts. In summary, we expect this gelatin-CD “click” hydrogel will be a promising candidate for localized and long-term delivery of hydrophobic drugs.
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D, Prasanthi, PRASHANTI S, and MEGHANA G. "FORMULATION AND EVALUATION OF PRESS COATED TABLETS OF LANSOPRAZOLE." International Journal of Applied Pharmaceutics, April 11, 2019, 49–56. http://dx.doi.org/10.22159/ijap.2019v11i4.32617.
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Objective: Lansoprazole an proton pump inhibitor, degrades in acidic environment, hence protection of drug is done by coating the drug with enteric coating polymers. The aim and objective of the present study was to prepare enteric coated delayed release tablets of lansoprazole by using press coating technique.
Methods: Core tablets were prepared by direct compression and evaluated for their physico-chemical properties. Press coated tablets were formulated by using different combinations of ethyl cellulose, HPMC E15 and HPMC K4M as a coating layer. Core and coated tablets were optimized by dissolution studies. Fourier transform infra-red spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies were performed to know the compatibility of drug with various excipients. Surface morphology and uniformity of coat was evaluated by Scanning electron microscopy (SEM). Stability of optimized formulation was evaluated according to ICH guidelines.
Results: Among the various formulations F5 containing ethyl cellulose: HPMC E15 (10:90) and F9 containing ethyl cellulose: HPMC K4M (25:75) were optimized based on the better drug release within 8 h. DSC studies and FTIR studies revealed compatibility of drug with excipients. Obtained SEM photographs of tablets showed that the surface of core tablet is uniformly coated with coat by press coating. Stability studies showed that the formulations were stable.
Conclusion: As a result, delayed release press coated tablets developed in this study delivered lansoprazole in the intestine and protected the drug from degradation.
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Hecq, Jean-Daniel, Benoit Bihin, Jacques Jamart, and Laurence Galanti. "Criteria for Judging the Quality of a Publication on Physicochemical Stability of Ready to Use Injectable Drugs." Pharmaceutical Technology in Hospital Pharmacy 2, no. 2 (August 28, 2017). http://dx.doi.org/10.1515/pthp-2017-0012.
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AbstractIn hospitals, a major part of the drugs is administered via the intravenous route. When one wants to evaluate or know the stability of a drug in solution, it is necessary to know several physico-chemical parameters. Several reference works are available to help the hospital pharmacist with this research. However, reading these different sources can make you discover conflicting data. It is therefore necessary at this time to obtain the publications with contradictory results and to read them again. Seven criteria have been identified for judging the quality of a publication on physicochemical stability: full description of equipment, methods and analytical conditions of molecules studied; complete description of the procedures used to validate the analytical method; full indication of time testing and measurement bases or control; documentation on the analytical reproducibility; adequate statistical analysis; appropriate conclusions; appropriate references. In conclusion, everything in a compatibility study is important.
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Chawla, Ruchi, Venkatanaidu Karri, Varsha Rani, Mohini Mishra, and Krishan Kumar. "Factorial Design-Based Nanocarrier Mediated Formulation of Efavirenz and Its Characterization." Nano LIFE, February 25, 2022. http://dx.doi.org/10.1142/s1793984422500027.
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Efavirenz (EFV) suffers from poor aqueous solubility which results in low bioavailability of the drug. Nanocarrier-based drug delivery systems offer a suitable alternative for improving the physico-chemical properties of the drug and hence its efficacy. Nanosuspension (NS) of EFV was formulated by solvent-anti solvent precipitation method using PVP K-30 as stabilizer and sodium lauryl sulphate (SLS) as the wetting agent. Multi-level factorial design was applied to select the optimal formulation which was further characterized. The optimal batch exhibited mean particle size of 305[Formula: see text]nm and polydispersity index (PDI) of 0.345. Solid-state characterization studies of the NS conducted using scanning electron microscopy, Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction, and differential scanning calorimetry (DSC) revealed compatibility between the drug and the excipients and modest alteration in the crystallinity of the drug. There was progressive increase in the solubility of the drug when incorporated in NS from 17.39[Formula: see text][Formula: see text]g/ml to 256[Formula: see text][Formula: see text]g/ml. Further, drug release studies showed significantly better and controlled drug release pattern in comparison to the free drug due to the presence of nanosized particles in the formulation.
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Patel, Chirag Karshanbhai, Disha Suthar, Hetal Patel, Vinit Movaliya, and Punit Parejiya. "Assessment of suitability of saxagliptin hydrochloride for development of controlled release parenteral formulation by preformulation studies." International journal of health sciences, April 21, 2022, 3223–36. http://dx.doi.org/10.53730/ijhs.v6ns3.6336.
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The main objective of pre-formulation study is to develop the stable, elegant, safe and effective drug delivery system by establishing drug kinetic profile, formulation compatibility with different excipients and physico-chemical parameters of new drug molecules. This could provide key evidence for implementing formulation design or requirement of the molecular alteration. So, in the present study preformulation studies were performed on Saxagliptin Hydrochloride (SXG) to assess its suitability for parenteral formulation. SXG is a potent and selective reversible inhibitor of dipeptidyl peptidase-4 used to treat type –II diabetes mellitus. The authenticity of SXG was established by differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy(FTIR) spectra. An ultraviolet–visible (UV) spectrophotometric and high performance liquid chromatography (HPLC) methods were employed for determination of SXG in bulk API (active pharmaceutical ingredient). The UV method was linear within the range of 1-40 μg/ml. The proposed methodology is robust which can be concluded from the lower percentage standard deviation percentage co efficient of variance (% CV) values of intraday and inter day variability. The retention time was observed 1.3 min of SXG in HPLC method. The higher regression coefficient value (0.999) indicates the methodology is robust.
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Sinézia, Celimar, Tháyna Sisnande, Luis Peña Icart, and Luís Maurício T. R. Lima. "Oral delivery of the amylin receptor agonist pramlintide." Peptide Science, January 31, 2024. http://dx.doi.org/10.1002/pep2.24346.
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AbstractAmylin receptor agonism safely benefit diabetic patients, reducing the insulin requirements and glycemic excursions. Pramlintide is the triple proline human amylin analogue first used as injectable drug, but lacking physico‐chemical compatibility when co‐formulated with insulin. Here, we report the design and characterization of polymeric microparticles for oral delivery of pramlintide. Eudragit S100, a gastric‐resistant polymer, was used in preparation of pramlintide‐loaded spherical microcapsules by double emulsion and solvent evaporation technique, with approximately 66 μm ± 11 particle size, with 83.2% ± 2.7 efficiency for pramlintide entrapment and 67.6% ± 2.1 yield. Intra‐venous pramlintide free in solution showed a plasmatic half‐life of 6.8 min in mice. In contrast, oral delivery of acid‐resistant pramlintide‐loaded microparticles in mice showed a protracted release for 120 min compared to 30 min obtained for pramlintide in solution. Our data provide evidences for the potential use of the oral route in the therapeutic development of pramlintide formulations.
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Wadaskar, Pallavi, Pallavi Kharkar, and Pallavi Ispade. "Preparation and Evaluation of Yohimbine Hydrochloride Agglomerates by Crystallo Co-Agglomeration technique." Research Journal of Pharmaceutical Dosage Forms and Technology, April 30, 2022, 105–10. http://dx.doi.org/10.52711/0975-4377.2022.00016.
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Crystallo-co-agglomeration (CCA) is an innovative technique developed with the intention to produce the drugs with good micromeritic and mechanical characteristics. Yohimbine Hydrochlorideis an anti-retroviral drug with poor dissolution and poor flow properties. Hence the aim of the study is to prepare the crystallo co-agglomerates of Yohimbine Hydrochloridewhich may improve the properties of Yohimbine Hydrochloride.The present study was carried out in order to develop pharmaceutically equivalent, stable, and quality improved agglomerates of Yohimbine Hydrochloridewith enhanced solubility wettability, dissolution rate, flow properties and mechanical properties using hydrophilic polymers and to characterize the physico-chemical properties of prepared crystallo-co-agglomeration.The present work was carried out using PVA and PEG 6000 as the polymers in different ratios by crystallo-co agglomeration method. The various evaluations of prepared agglomerates like micromeritics of the agglomerates such as flowability, packability and compatibility were dramatically improved. The dissolution and disintegration rate of agglomerate was increased in presence of PEG 6000 than compared with PVA.TheYohimbine Hydrochloridepolymer agglomerates were successfully prepared by crystallo-co-agglomeration technique and it was concluded that crystallo-co-agglomeration technique can be successfully employed as an alternative to conventional wet agglomeration.
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Namdev, Nidhi, Mousumi Kar Pillai, Sujit Pillai Pillai, Ruchita Raghuvanshi, Ujjawal Ahirwal, and R. Yadav. "POLYSACCHARIDE BASED CONTROLLED RELEASE MUCOADHESIVE DRUG DELIVERY SYSTEM FOR PAIN MANAGEMENT." International Journal of Pharmaceutical Sciences and Drug Research, March 30, 2024, 206–12. http://dx.doi.org/10.25004/ijpsdr.2024.160210.
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Mucoadhesion is one of the most extensively studied methods for the administration of medication for faster onset of action with enhanced bioavailability. Present investigation was concerned with the development and characterization of controlled release muco-adhesive drug delivery system for the drug Tramadol Hydrochloride (TRD) to extend the duration of analgesia for patients suffering from acute to chronic pain. Formulations were made using the solvent casting technique, incorporating natural polymers like Guar Gum, Xanthum Gum and Chitosan in conjunction with HPMC (hydroxy propyl methyl cellulose) to modify the drug release. The compatibility of film components were validated by Fourier Transform Infra- Red (FTIR) spectroscopy and subjected to physico-chemical evaluation parameters and ex-vivo drug diffusion study. Optimized formulation was tested for analgesic efficacy in vivo to determine extent of their suitability in therapeutic use. All the prepared formulations exhibited superior pharmaceutical qualities with respect to drug content, folding endurance, swelling index and mucoadhesion time. In ex-vivo drug diffusion study, all the films displayed a controlled release lasting longer than eight hours. Formulations containing Chitosan in combination with HPMC (F6) showed better controlled drug release over other combinations. The formulation F6 bring out remarkable in vivo analgesic efficacy with 58.10 % analgesia in contrast to the standard (61.16%). It was deduced that Tramadol hydrochloride mucoadhesive films were found to be an effective treatment for moderate to severe pain with a quick onset and a lengthy half-life.
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Patel, Chirag, Disha Suthar, Hetal Patel, Vinit Movaliya, and Punit Parejiya. "Preformulation Study of Glimepiride: An Insight for Formulation and Development of Parenteral Formulation." Journal of Pharmaceutical Research International, February 25, 2022, 38–49. http://dx.doi.org/10.9734/jpri/2022/v34i15b35718.
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Aim: The objective of preformulation study is to develop the elegant, stable, effective and safe dosage form by establishing kinetic profile, compatibility with other formulation excipients and physico-chemical parameters of new drug substance. This could provide important information for formulation design or support the need for molecular modification. So, in the present study preformulation studies were performed on Glimepiride (GMP) to assess its suitability for parenteral formulation. Glimepiride is the first IIIrd generation sulphonyl urea used to treat type –II diabetes mellitus.
Methods: The authenticity of GMP was established by DSC and FTIR spectra. A UV spectrophotometric method and HPLC method were employed for determination of GMP in bulk active pharmaceutical ingredient (API).
Results: The UV method was linear in the range of 3-10 μg/ml. The low % CV values of intra-day and inter-day variations revealed that the proposed method is robust. The retention time of GMP in HPLC method was found to be 1.9 min. The method was proven robust by obtaining very high regression coefficient value (0.999).
Conclusions: The results of the physicochemical study of drug revealed suitability of GMP for parenteral route. Moreover, the drug was found stable in both solid as well as liquid state at different conditions.
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Rajesh Pavan, Ampapuram, R. V. D. Praveen, Gorantla Naresh Babu, P. Ramakrishna Reddy, and G. Thirumala Roopesh. "Formulation Development and Evaluation of Desloratadine Sugar Free Oral Liquid Dosage Form." Research Journal of Pharmacy and Technology, December 24, 2022, 5425–30. http://dx.doi.org/10.52711/0974-360x.2022.00914.
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The aim of the present work is to formulate and evaluate Desloratadine Sugar free oral liquid dosage form. Desloratadine is an anti-histamine drug which is used to treat allergic reactions such as chronic utricaria, watery eyes and runny nose. In this Present work Desloratadine sugar free oral liquid dosage form was formulated by using artificial sweeteners with the help of simple mixing technique and subjected to various evaluation tests. The Pre-formulation studies like identification of pure drug by melting point method, solubility, Drug-Excipients compatibility studies by FTIR studies were evaluated. Post formulation studies like oranganoleptic properties, Physico-chemical properties, Assay, Related substances and Microbial examination were evaluated. Organoleptic property has shown that the all formulations was found to be clear orange and complies with innovator. Assay of Desloratadine and sodium benzoate of all six formulations F1, F2, F3, F4, F5, and F6 were determined and found to be 99.1%, 99.8%, 100.1%, 100.2%, 100.1% and 99.9% respectively. Related substances of all the formulations were determined and the impurities A and B were found to be within the limits and there is no any unspecified impurity. Microbial examinations of all the formulations are determined and the total bacterial count and fungal count are within the limits and E.coli is absent. The formulation of Desloratadine sugar free oral liquid dosage form by using artificial sweeteners was Developed and evaluated.
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Firdous, Zohra, Pankaj Dhapake, Nitin Padole, Nilakshi Dhoble, and Jagdish Baheti. "Different Approaches for Transdermal Nano-Carrier Delivery System." Research Journal of Topical and Cosmetic Sciences, November 28, 2023, 94–104. http://dx.doi.org/10.52711/2321-5844.2023.00015.
Full textAbstract:
Transdermal drug delivery is a validated technology that makes a significant contribution to global pharmaceutical care. Since 1980, the sector has seen impressive growth with several commercial successes. The term transdermal drug delivery refers to the delivery of a drug across the layers of skin with the intention of allowing the drug to be absorbed through the skin in a predetermined and controlled rate manner. Skin is one of the largest organs that act as an efficient barrier for drug delivery. The present study focuses on the different approaches of nano-carrier system that delivers the nano-carrier drug across the skin barrier with the help of transdermal delivery system. Nano-carrier drug delivery systems are one of the biggest challenges to deliver drug into systemic circulation by crossing the skin barrier providing a passive drug delivery strategy that is known to be safer and faster than the conventional method. In this review, we describe the diverse types of nano-carriers approaches that have been synthesized for transdermal delivery system includes liposomes, niosomes, ethosomes, solid lipid nanoparticles (SLN), nanostructured lipid carrier (NLC), polymeric nanoparticles, nanocrystals, nanofibers and nanosuspension/nanoemulsion. Several characterization methods of transdermal delivery system have been proposed to control the behavior of nano-carriers, along with in-vitro and in-vivo and other evaluation parameters. It was concluded that the compatibility of nano-carriers with the skin structure should be considered for transdermal nanocarrier delivery systems, which will be the most preferred route for drug delivery in the future as it offers high patient compliance, controlled dosing, low frequency of dosing, high physico-chemical stability and better dermal bioavailability, etc.
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Lalan, Manisha, Divya Patel, Maanika Menon, Pranav Shah, and Meenakshi Patel. "Application Of D-Optimal Mixture Design In The Development Of Nanocarrier-Based Darifenacin Hydrobromide Gel." Recent Advances in Drug Delivery and Formulation 17 (February 21, 2023). http://dx.doi.org/10.2174/2667387817666230221141501.
Full textAbstract:
Background: Darifenacin hydrobromide, a BCS Class II drug, is poorly bioavailable due to extensive first-pass metabolism. The present study is an attempt to investigate an alternative route of drug delivery by developing a nanometric microemulsion-based transdermal gel for the management of an overactive bladder. Method: Oil, surfactant, and cosurfactant were selected based on the solubility of the drug, and surfactant: cosurfactant in surfactant mixture (Smix) was selected at a 1:1 ratio as inferred from the pseudo ternary phase diagram. The D-optimal mixture design was used to optimize the o/w microemulsion wherein the globule size and zeta potential were selected as dependable variables. The prepared microemulsions were also characterized for various physico-chemical properties like transmittance, conductivity, and TEM. The optimized microemulsion was gelled using Carbopol 934 P and assessed for drug release in-vitro and ex-vivo, viscosity, spreadability, pH, etc. Results: Drug excipient compatibility studies showed that the drug was compatible with formulation components. The optimized microemulsion showed a globule size of less than 50 nm and a high zeta potential of -20.56 mV. The ME gel could sustain the drug release for 8 hours as reflected in in-vitro and ex-vivo skin permeation and retention studies. The accelerated stability study showed no significant change in applied storage conditions. Conclusion: An effective, stable, non-invasive microemulsion gel containing darifenacin hydrobromide was developed. The achieved merits could translate into increased bioavailability and dose reduction. Further confirmatory in-vivo studies on this novel formulation, which is a cost-effective & industrially scalable option, can improve the pharmacoeconomics of overactive bladder management.
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Prasanthi, D., Shreya Ajay Rajguru, C. Aishwarya, and Aisha Rahman. "Pulsatile Delivery of Fexofenadine Hydrochloride Pulsincap by Box-Behnken Design." Journal of Pharmaceutical Research International, December 16, 2021, 649–63. http://dx.doi.org/10.9734/jpri/2021/v33i59a34316.
Full textAbstract:
Objective: Fexofenadine hydrochloride is a selective peripheral H1-blocker, used for allergy symptoms, such as hay fever and urticaria. Allergic symptoms are aggressive during early morning hours, so a pulsatile delivery system with a lag time of 4-5 hours was formulated and optimized by Box-Behnken design.
Materials and Methods: Pulsincap system using formaldehyde-treated capsules and hydrogel plug. Box-Behnken design was applied for optimization in which three independent variables, X1= Drug: polymer ratio, X2 = Polymer: polymer ratio (Ethylcellulose: HPMC E15) and X3 = Plug weight were selected. Three dependent variables R1 = Percent release of drug after 4 hours, R2 = percent release after 10 hours and R3 = Lag time were selected.
Results: FTIR and DSC studies confirmed compatibility of drug and excipients. The empty formaldehyde-treated capsules were evaluated for physical appearance, solubility, capsule dimensions and formaldehyde content. Hydrogel plugs, powder blend and pulsincap formulations were evaluated for Physico-chemical parameters and all the parameters were within acceptable limits. Contour plots and Response surface plots indicated that as Drug: Polymer ratio (X1) and Plug weight (X3) increased, Lag time increased but% drug release decreased. As Polymer: Polymer ratio (X2) increased, the lag time was at a moderate level. Predicted vs actual responses showed the correlation of 0.786 for% release in 4hrs, 0.9744 for% release in 10hrs and 0.6281 for lag time. Optimized formulation G1 was suggested by design (with criteria 4.5-6hrs lag time, 10-20% release in 4hrs & 60-70% drug release within 10hrs). The optimised formulation was stable.
Conclusion: Pulsincap system of Fexofenadine hydrochloride can be obtained by using retarding polymers like ethyl cellulose, HPMC E15 and formaldehyde cross-linked capsules.
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Sharma, Shushank. "An overview of Natural Superdisintegrants." Research Journal of Topical and Cosmetic Sciences, December 22, 2021, 113–24. http://dx.doi.org/10.52711/2321-5844.2021.00016.
Full textAbstract:
The oral route is the most convenient route of administration for various drugs. It is viewed as the most convenient, most secure, and economical route for patients. Fast disintegrating tablets are popular these days as they disintegrate in the mouth within a few seconds without the use of water. The burdens of regularly used medications in pediatric and geriatric patients have been overwhelmed by quick-dissolving tablets. Natural superdisintegrants have been used for fast-dissolving tablets because they are biodegradable, chemically inert, non-harmful, more affordable, and generally accessible. Natural polymer improves the properties of the tablet as it is commonly used as diluents and binders. Natural super disintegrants decrease the release time and give healthful results to the patients. Most polymers are obtained from nature, they are cost-effective, non-toxic, and non-irritants. Disintegration is the most important step for releasing the drug from the tablet matrix to decrease the disintegration time. In this, drug and polymers come in contact with water, it swells, hydrate, and react chemically to release the drug in the mouth and gastrointestinal tract. Superdisintegrants are those substances that encourage the quick breaking down with a lesser amount contrasted with disintegrants. The quick disintegrants tablets are set up by utilizing suitable polymers which rely on the Physico-chemical properties of drugs and excipients, for example, drug and polymer compatibility, hardness and thickness of tablet, nature of drug and excipients, PH of drug and release parameters of drug formulation. Superdisintegrants are the vehicles added to tablet formulation to advance the breaking of tablets and capsules into small microparticles in aqueous media resulting in to increase in the surface area and promote quick drug release. The disintegrants have a significant capacity to oppose the efficacy of tablet binders and compression forces to form the tablet. Commonly there are three methods to incorporate disintegrants into the tablet: A. Inner addition, B. External expansion, C. Internal, and external addition. Most of the regularly based tablets are those expected to be swallow, disintegrate and release medicaments in the gastrointestinal tract but over a while tablets are manufactured to deliver medicaments in the mouth and gastrointestinal tract within few seconds of swallowing. It has been demonstrated that characteristic polymers are more effective than synthetic polymers. Some research is going to develop safe and effective medication with super disintegrating agents that can be dissolved rapidly to treat the disease.
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Sharma, Shushank, and Sikha Chauhan. "A review: An overview of Natural Superdisintegrants." Research Journal of Topical and Cosmetic Sciences, May 17, 2021, 13–24. http://dx.doi.org/10.52711/2321-5844.2021.00003.
Full textAbstract:
The oral route is the most convenient route of administration for various drugs. It is viewed as the most convenient, most secure, and economical route for patients. Fast disintegrating tablets are popular these days as they disintegrate in the mouth within a few seconds without the use of water. The burdens of regularly used medications in pediatric and geriatric patients have been overwhelmed by quick-dissolving tablets. Natural superdisintegrants have been used for fast-dissolving tablets because they are biodegradable, chemically inert, non-harmful, more affordable, and generally accessible. Natural polymer improves the properties of the tablet as it is commonly used as diluents and binders. Natural super disintegrants decrease the release time and give healthful results to the patients. Most polymers are obtained from nature, they are cost-effective, non-toxic, and non-irritants. Disintegration is the most important step for releasing the drug from the tablet matrix to decrease the disintegration time. In this, drug and polymers come in contact with water, it swells, hydrate, and react chemically to release the drug in the mouth and gastrointestinal tract. Superdisintegrants are those substances that encourage the quick breaking down with a lesser amount contrasted with disintegrants. The quick disintegrants tablets are set up by utilizing suitable polymers which rely on the Physico-Chemical properties of drugs and excipients, for example, drug and polymer compatibility, hardness and thickness of tablet, nature of drug and excipients, PH of drug and release parameters of drug formulation. Superdisintegrants are the vehicles added to tablet formulation to advance the breaking of tablets and capsules into small microparticles in aqueous media resulting in to increase in the surface area and promote quick drug release. The disintegrants have a significant capacity to oppose the efficacy of tablet binders and compression forces to form the tablet. Commonly there are three methods to incorporate disintegrants into the tablet: A. Inner addition, B. External expansion, C. Internal, and external addition. Most of the regularly based tablets are those expected to be swallow, disintegrate and release medicaments in the gastrointestinal tract but over a while tablets are manufactured to deliver medicaments in the mouth and gastrointestinal tract within few seconds of swallowing. It has been demonstrated that characteristic polymers are more effective than synthetic polymers. Some research is going to develop safe and effective medication with super disintegrating agents that can be dissolved rapidly to treat the disease.
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Rajyam, R. Lakshmi, M. Keerthana, D. V. Sowmya, and M. Vidyavathi. "Extraction and Evaluation of Musa paradisiaca Stem Mucilage as a Pharmaceutical Excipient." Journal of Pharmaceutical Research International, December 30, 2021, 566–80. http://dx.doi.org/10.9734/jpri/2021/v33i64a36133.
Full textAbstract:
Aim: In present Pharmaceutical trend, natural excipients are gaining more importance because of their availability, safety, performance, and cost. The present work aimed at extraction of the mucilage from the stem of Musa paradisiaca (banana) and evaluation of extracted mucilage for its binding and disintegrating properties with Paracetamol as a model drug.
Methodology: The mucilage was extracted by aqueous extraction method followed by precipitation and evaluated for various physico-chemical properties. Drug-mucilage compatibility studies were conducted by FT-IR spectrometer. The extracted mucilage in three different concentrations was used to prepare 2 different sets of tablets for evaluation of its binding as well as disintegrating properties. Binding properties and disintegrating properties of the mucilage were compared with starch as standard binder and microcrystalline cellulose as standard disintegrant for the first and second set of tablets respectively. Wet granulation method was used to prepare total eight batches of 1 gm tablets of Paracetamol. Pre compression and post compression parameters of tablets were evaluated. Then the similarity factor for both (binding and disintegration test) were calculated by comparing test and standard tablets in each set.
Results and Discussion: The results of the work shown that the mucilage extracted from the Musa paradisiaca stem (MPS) has similar binding properties as of starch and release retarding effect at increased concentration as disintegrating time was increased when compared to microcrystalline cellulose.
Conclusion: Thus, the mucilage can be used as a better binding agent in the tablet formulation and its high disintegrating time can be explored for its slow release or extended release effect.
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Rajyam, R. Lakshmi, M. Keerthana, D. V. Sowmya, and M. Vidyavathi. "Extraction and Evaluation of Musa paradisiaca Stem Mucilage as a Pharmaceutical Excipient." Journal of Pharmaceutical Research International, December 30, 2021, 566–80. http://dx.doi.org/10.9734/jpri/2021/v33i64a36133.
Full textAbstract:
Aim: In present Pharmaceutical trend, natural excipients are gaining more importance because of their availability, safety, performance, and cost. The present work aimed at extraction of the mucilage from the stem of Musa paradisiaca (banana) and evaluation of extracted mucilage for its binding and disintegrating properties with Paracetamol as a model drug.
Methodology: The mucilage was extracted by aqueous extraction method followed by precipitation and evaluated for various physico-chemical properties. Drug-mucilage compatibility studies were conducted by FT-IR spectrometer. The extracted mucilage in three different concentrations was used to prepare 2 different sets of tablets for evaluation of its binding as well as disintegrating properties. Binding properties and disintegrating properties of the mucilage were compared with starch as standard binder and microcrystalline cellulose as standard disintegrant for the first and second set of tablets respectively. Wet granulation method was used to prepare total eight batches of 1 gm tablets of Paracetamol. Pre compression and post compression parameters of tablets were evaluated. Then the similarity factor for both (binding and disintegration test) were calculated by comparing test and standard tablets in each set.
Results and Discussion: The results of the work shown that the mucilage extracted from the Musa paradisiaca stem (MPS) has similar binding properties as of starch and release retarding effect at increased concentration as disintegrating time was increased when compared to microcrystalline cellulose.
Conclusion: Thus, the mucilage can be used as a better binding agent in the tablet formulation and its high disintegrating time can be explored for its slow release or extended release effect.
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Khan, Hafeez Ullah, Samar Aziz, Safirah Maheen, Ikramullah Khan, Mehwish Andleeb, Hina Younis, Sajjad Haider, Adnan Haider, Muhammad Saeed Akhtar, and Syed Salman Shafqat. "Superporous acrylic acid and HPMC hydrogels of mefenamic acid: Formulation, characterization and optimization by central composite design." Frontiers in Bioengineering and Biotechnology 10 (December 15, 2022). http://dx.doi.org/10.3389/fbioe.2022.1057627.
Full textAbstract:
The purpose of the study was to devise the superporous hydrogels (SPHs) of mefenamic acid (MA) to acquire the sustained action of the MA in the body. The superporous hydrogels of mefenamic acid were formulated by employing the gas blowing method. The central composite rotatable design (CCRD) was applied to optimize the effect of independent formulation factors like acrylic acid (AC), HPMC and glycerol (GLY) over dependent variables like porosity, viscosity, drug content and swelling ratio of superporous hydrogels in water, phosphate buffer (pH 6.8) and in 0.1N HCl (pH 1.2). A number of characteristics such as void fraction, surface morphology by Scanning electron microscopy (SEM) and in vitro drug release study were governed along with physico-chemical analysis by Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and appraised statistically by employing the ANOVA. The comparative analgesic activity of optimized superporous hydrogel formulation SPH17 was also analyzed by using tail flick method. The Fourier transform infrared spectroscopy and Differential scanning calorimetry studies approved the physical compatibility between the polymers and the drug. The Scanning electron microscopy study specified micrographic insight about the structure of formed formulations comprising presence of pores, fibers and drug-hole aggregates. The superporous hydrogels were detected to be low dense as they expressed density lower than 0.75 g/cc. The decrease in concentration of the polymers and cross linker contributed towards the increase in the void fraction of the superporous hydrogel formulations. The optimized formulation SPH 17 exhibited a highly sustained release of MA for up to 10 h in the both 0.1 N HCl and phosphate buffer (66.6%) media. The non-fickian release of drug revealed the coupling of the diffusion and polymer relaxation mechanism of the drug release from the formulations. The obtained outcomes suggested that analgesic effect of SPH 17 was significantly (p < 0.05) higher than that of simple suspension of mefenamic acid and total analgesic effect duration for superporous hydrogel was also doubled as compared to the duration of analgesic effect produced by drug suspension. The successfully formulated SPH with HPMC K100M as a gelling agent had sustained the action of the mefenamic acid (MF) by improving its poor solubility and permeability. The introduction of inter-penetrating polymeric network (acrylic acid) using glycerol as a cross linker impart increased residence time to superporous hydrogels which ultimately enhanced the feasibility of using superporous hydrogel as oral sustained release devices particularly for gastric retention.
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Damato, Anna, Fabio Vianello, Enrico Novelli, Stefania Balzan, Matteo Gianesella, Elisa Giaretta, and Gianfranco Gabai. "Comprehensive Review on the Interactions of Clay Minerals With Animal Physiology and Production." Frontiers in Veterinary Science 9 (May 10, 2022). http://dx.doi.org/10.3389/fvets.2022.889612.
Full textAbstract:
Clay minerals are naturally occurring rock and soil materials primarily composed of fine-grained aluminosilicate minerals, characterized by high hygroscopicity. In animal production, clays are often mixed with feed and, due to their high binding capacity towards organic molecules, used to limit animal absorption of feed contaminants, such as mycotoxins and other toxicants. Binding capacity of clays is not specific and these minerals can form complexes with different compounds, such as nutrients and pharmaceuticals, thus possibly affecting the intestinal absorption of important substances. Indeed, clays cannot be considered a completely inert feed additive, as they can interfere with gastro-intestinal (GI) metabolism, with possible consequences on animal physiology. Moreover, clays may contain impurities, constituted of inorganic micronutrients and/or toxic trace elements, and their ingestion can affect animal health. Furthermore, clays may also have effects on the GI mucosa, possibly modifying nutrient digestibility and animal microbiome. Finally, clays may directly interact with GI cells and, depending on their mineral grain size, shape, superficial charge and hydrophilicity, can elicit an inflammatory response. As in the near future due to climate change the presence of mycotoxins in feedstuffs will probably become a major problem, the use of clays in feedstuff, given their physico-chemical properties, low cost, apparent low toxicity and eco-compatibility, is expected to increase. The present review focuses on the characteristics and properties of clays as feed additives, evidencing pros and cons. Aims of future studies are suggested, evidencing that, in particular, possible interferences of these minerals with animal microbiome, nutrient absorption and drug delivery should be assessed. Finally, the fate of clay particles during their transit within the GI system and their long-term administration/accumulation should be clarified.