Journal articles on the topic 'H-formulation'
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1
Tompson, Debra, Mark Whitaker, Rennan Pan, Geoffrey Johnson, Teresa Fuller, Vanessa Zann, Litza McKenzie, Kathy Abbott-Banner, Simon Hawkins, and Marcy Powell. "Development of a Once-Daily Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772 using DiffCORE Technology." Pharmaceutical Research 39, no. 1 (January 2022): 153–65. http://dx.doi.org/10.1007/s11095-021-03124-7.
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Abstract Purpose GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1 (RIPK1) with a short 2- to 3-h half-life. In a previous modified-release (MR) study, a matrix monolithic formulation (80% GSK2982772 released over 12 h) provided a once-daily (QD) pharmacokinetic (PK) profile in the fasted state; however, it was susceptible to food effects. The current study evaluated the safety and PK of MR formulations using GSK proprietary DiffCORE™ technology. Methods Part A evaluated PK following single-dose (240 mg) fasted and fed (high-fat meal) administration of three DiffCORE MR formulations within pre-defined in vitro extremes of 80% GSK2982772 released over 12 h (MR-12 h) to 80% GSK2982772 released over 18 h (MR-18 h) versus an immediate-release formulation. Part B evaluated MR-16 h (120–960 mg) in different prandial states. Results Pharmacokinetic profiles for all MR formulations and doses tested in the fasted and fed states were consistent with QD dosing. Conclusions The DiffCORE technology overcame the food effect vulnerability observed with the matrix monolithic formulation. The MR-16 h formulation was selected for further clinical development as a QD dosing regimen (NCT03649412 September 26, 2018).
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Somerton, B., D. Lindsay, J. Palmer, J. Brooks, and S. Flint. "Changes in Sodium, Calcium, and Magnesium Ion Concentrations That Inhibit Geobacillus Biofilms Have No Effect on Anoxybacillus flavithermus Biofilms." Applied and Environmental Microbiology 81, no. 15 (May 22, 2015): 5115–22. http://dx.doi.org/10.1128/aem.01037-15.
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ABSTRACTThis study investigated the effects of varied sodium, calcium, and magnesium concentrations in specialty milk formulations on biofilm formation byGeobacillusspp. andAnoxybacillus flavithermus. The numbers of attached viable cells (log CFU per square centimeter) after 6 to 18 h of biofilm formation by three dairy-derived strains ofGeobacillusand three dairy-derived strains ofA. flavithermuswere compared in two commercial milk formulations. Milk formulation B had relatively high sodium and low calcium and magnesium concentrations compared with those of milk formulation A, but the two formulations had comparable fat, protein, and lactose concentrations. Biofilm formation by the threeGeobacillusisolates was up to 4 log CFU cm−2lower in milk formulation B than in milk formulation A after 6 to 18 h, and the difference was often significant (P≤ 0.05). However, no significant differences (P≤ 0.05) were found when biofilm formations by the threeA. flavithermusisolates were compared in milk formulations A and B. Supplementation of milk formulation A with 100 mM NaCl significantly decreased (P≤ 0.05)Geobacillusbiofilm formation after 6 to 10 h. Furthermore, supplementation of milk formulation B with 2 mM CaCl2or 2 mM MgCl2significantly increased (P≤ 0.05)Geobacillusbiofilm formation after 10 to 18 h. It was concluded that relatively high free Na+and low free Ca2+and Mg2+concentrations in milk formulations are collectively required to inhibit biofilm formation byGeobacillusspp., whereas biofilm formation byA. flavithermusis not impacted by typical cation concentration differences of milk formulations.
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Ameen, A. O., J. R. Fuxa, and A. R. Richter. "Antagonism between Formulations of Different Bacillus thuringiensis Subspecies in Heliothis virescens and Helicoverpa zea (Lepidoptera: Noctuidae)." Journal of Entomological Science 33, no. 2 (April 1, 1998): 129–35. http://dx.doi.org/10.18474/0749-8004-33.2.129.
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Interactions between formulations of the aizawai and kurstaki subspecies of Bacillus thuringiensis Berliner were evaluated by bioassay in Heliothis virescens (F.) and Helicoverpa zea (Boddie). In preliminary experiments, a formulation of subspecies aizawai, Xentari AS®, had significantly (P < 0.05) higher median lethal concentrations (LC50s) in both insect species than formulations based on subspecies kurstaki. Helicoverpa zea was significantly (P < 0.05) more susceptible than H. virescens to one formulation of subspecies kurstaki (Dipel ES®), but the two insects did not differ in susceptibility to Xentari AS® or to a second formulation of subspecies kurstaki (Dipel 6AF®). In H. virescens, Xentari AS® was additive with Dipel 6AF® and significantly (P< 0.05) antagonistic with Dipel ES® and with a third formulation of subspecies kurstaki, Dipel 48A®. In H. zea, Xentari AS® was significantly antagonistic with all three formulations of subspecies kurstaki. This suggests that certain toxin combinations from B. thuringiensis subspecies might not be effective for managing H. virescens and H. zea populations.
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Najafi-Yazdi, Alireza, Guillaume A. Brès, and Luc Mongeau. "An acoustic analogy formulation for moving sources in uniformly moving media." Proceedings of the Royal Society A: Mathematical, Physical and Engineering Sciences 467, no. 2125 (June 30, 2010): 144–65. http://dx.doi.org/10.1098/rspa.2010.0172.
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Acoustic analogy methods are used as post-processing tools to predict aerodynamically generated sound from numerical solutions of unsteady flow. The Ffowcs Williams–Hawkings (FW–H) equation and related formulations, such as Farassat’s Formulations 1 and 1A, are among the commonly used analogies because of their relative low computation cost and their robustness. These formulations assume the propagation of sound waves in a medium at rest. The present paper describes a surface integral formulation based on the convective wave equation, which takes into account the presence of a mean flow. The formulation was derived to be easy to implement as a numerical post-processing tool for computational fluid dynamics codes. The new formulation constitutes one possible extension of Farassat’s Formulation 1 and 1A based on the convective form of the FW–H equation.
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Jha, Sajal Kumar, Roopa Karki, Venkatesh Dinnekere Puttegowda, and D. Harinarayana. "In Vitro Intestinal Permeability Studies and Pharmacokinetic Evaluation of Famotidine Microemulsion for Oral Delivery." International Scholarly Research Notices 2014 (December 7, 2014): 1–7. http://dx.doi.org/10.1155/2014/452051.
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The absolute bioavailability of famotidine after oral administration is about 40–45% and absorbance only in the initial part of small intestine may be due to low intestinal permeability. Hence, an olive oil based microemulsion formulation with Tween-80 as surfactant and PEG-400 as cosurfactant was developed by using water titration method with the aim of enhancing the intestinal permeability as well as oral bioavailability. In vitro drug permeation in intestine after 8 h for all formulations varied from 30.42% to 78.39% and most of the formulations showed enhanced permeation compared to pure drug (48.92%). Famotidine microemulsion exhibited the higher absorption and Cmax achieved from the optimized famotidine formulation (456.20 ng·h/ml) was higher than the standard (126.80 ng·h/mL). It was found that AUC0–24 h obtained from the optimized famotidine test formulation (3023.5 ng·h/mL) was significantly higher than the standard famotidine (1663.3 ng·h/mL). F-1 demonstrated a longer (6 h) Tmax compared with standard drug (2 h) and sustained the release of drug over 24 h. The bioavailability of F-1 formulation was about 1.8-fold higher than that of standard drug. This enhanced bioavailability of famotidine loaded in microemulsion system might be due to increased intestinal permeability.
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Wadhwa, Jyoti, Abhay Asthana, Sumeet Gupta, Gyati Shilkari Asthana, and Ranjit Singh. "Development and Optimization of Polymeric Self-Emulsifying Nanocapsules for Localized Drug Delivery: Design of Experiment Approach." Scientific World Journal 2014 (2014): 1–12. http://dx.doi.org/10.1155/2014/516069.
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The purpose of the present study was to formulate polymeric self-emulsifying curcumin nanocapsules with high encapsulation efficiency, good emulsification ability, and optimal globule size for localized targeting in the colon. Formulations were prepared using modified quasiemulsion solvent diffusion method. Concentration of formulation variables, namely,X1(oil),X2(polymeric emulsifier), andX3(adsorbent), was optimized by design of experiments using Box-Behnken design, for its impact on mean globule size (Y1) and encapsulation efficiency (Y2) of the formulation. Polymeric nanocapsules with an average diameter of 100–180 nm and an encapsulation efficiency of 64.85 ± 0.12% were obtained.In vitrostudies revealed that formulations released the drug after 5 h lag time corresponding to the time to reach the colonic region. Pronounced localized action was inferred from the plasma concentration profile (Cmax200 ng/mL) that depicts limited systemic absorption. Roentgenography study confirms the localized presence of carrier (0–2 h in upper GIT; 2–4 h in small intestine; and 4–24 h in the lower intestine). Optimized formulation showed significantly higher cytotoxicity (IC50value 20.32 μM) in HT 29 colonic cancer cell line. The present study demonstrates systematic development of polymeric self-emulsifying nanocapsule formulation of curcumin for localized targeting in colon.
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Piret, Jocelyne, Julie Lamontagne, André Désormeaux, and Michel G. Bergeron. "Efficacies of Gel Formulations Containing Foscarnet, Alone or Combined with Sodium Lauryl Sulfate, against Establishment and Reactivation of Latent Herpes Simplex Virus Type 1." Antimicrobial Agents and Chemotherapy 45, no. 4 (April 1, 2001): 1030–36. http://dx.doi.org/10.1128/aac.45.4.1030-1036.2001.
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ABSTRACT The influence of sodium lauryl sulfate (SLS) on the efficacies of gel formulations of foscarnet against herpes simplex virus type 1 (HSV-1) cutaneous lesions and on the establishment and reactivation of latent virus has been evaluated in a murine model of orofacial infection. Topical treatments were given twice daily for 3 days and were initiated at 6, 24, and 48 h after virus inoculation. The gel formulation that contained both 3% foscarnet and 5% SLS and that was administered within 48 h postinfection reduced the rate of development of herpetic skin lesions. This formulation also significantly decreased the viral content in skin tissues and in ipsilateral trigeminal ganglia when it was given within 24 and 6 h postinfection, respectively. A lower level of efficacy was observed for the gel formulation containing 3% foscarnet alone. Of prime interest, the gel formulation containing 5% SLS reduced significantly the mortality rate among mice in a zosteriform model of infection. Both formulations of foscarnet had no effect on the mean titers of reactivated virus in explant cultures of ipsilateral and contralateral trigeminal ganglia from latently infected mice. The use of a gel formulation containing combinations of foscarnet and SLS could represent an attractive approach for the treatment of herpetic mucocutaneous infections.
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Roopa, G., C. Jayanthi, R. Karki, H. Joshi, G. Divakar, and V. G. Rajalakshmi. "FABRICATION OF CURCUMIN LOADED GUAR GUM MICROPARTICLES FOR CONTROLLED RELEASE BY EMULSION GELATION TECHNIQUE." INDIAN DRUGS 54, no. 02 (February 25, 2017): 69–72. http://dx.doi.org/10.53879/id.54.02.10758.
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Cross-linked guar gum microparticles of curcumin were prepared for controlled release by emulsion gelation method using glutaraldehyde as cross-linking agent. Morphology and surface characteristics of the formulations were assessed by scanning electron microscopy. Particle size of the guar gum microparticles was determined by optical microscopy. The mean particle size ranged from 82 to 250 μ. The % drug loading was found to be in the range of 20 to 51% while the percentage encapsulation efficiency was ranging between 29 to 86%. FT-IR and DSC studies revealed the compatibility of the drug with the polymer. Formulation CGMP3 exhibited maximum % EE of 84%, In vitro drug-release studies were performed in simulated gastric fluid (without enzymes) for 2 h followed by simulated intestinal fluid (without enzymes) for 6 h and continued for 24 h. Formulation CGMP3 exhibited relatively more sustained release profile than the other formulations. All formulations of 1.5% guar gum (CGMP2, CGMP3 and CGMP4) have shown retarded release than 1.0 % guar gum formulations (CGMP6, CGMP7 and CGMP8). Optimal glutaraldehyde concentration was found to be 2%. The optimized formulation subjected to stability studies was found to be stable when observed for particle size and drug content.
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Adi-Dako, Ofosua, Kwabena Ofori-Kwakye, Seth Kwabena Amponsah, Isaac Boamah, Noble Kuntworbe, and Esther Eshun Oppong. "Potential of Cocoa Pod Husk Pectin-Based Modified Release Capsules as a Carrier for Chronodelivery of Hydrocortisone in Sprague-Dawley Rats." Journal of Drug Delivery 2018 (October 8, 2018): 1–8. http://dx.doi.org/10.1155/2018/9825363.
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The potential of cocoa pod husk (CPH) pectin-based modified release (MR) capsules as a carrier for chronodelivery of hydrocortisone in Sprague-Dawley rats was assessed. Extemporaneously formulated CPH pectin-based hydrocortisone (10 mg) capsules crosslinked with calcium chloride (Formulation A) or zinc (Formulation B) and a commercial immediate release hydrocortisone formulation were administered orally to Sprague-Dawley rats and the pharmacokinetic parameters were evaluated using noncompartmental analysis. Formulation A had a 2 h lag phase followed by an increase in serum drug concentration in the treated rats. Peak concentrations (Cmax) of 21.799 ± 1.993 ng/ml and 20.844 ± 2.661 ng/ml were achieved after 6 ± 0.23 h and 6 ± 0.35 h (Tmax), respectively, for capsules A and B. The immediate release formulation had a peak concentration of 15.322 ± 0.313 ng/ml within 1 ± 0.2 h. The relative bioavailability of the CPH pectin-based capsules A and B was 213% and 274%, respectively. Formulations A and B had half-lives more than three times that of the immediate release formulation. The MR capsules exhibited a higher exposure, greater bioavailability, and versatility in release of cortisol than the commercial immediate release formulation. Additionally, the MR capsules exhibited an extended drug release with overnight cortisol rise and early morning cortisol peak and hold promise in the management of adrenal insufficiency.
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Jin, Fengdan. "Liquid Chromatography-Tandem Mass Spectrometric Assay for Determination of Stavudine in Human Plasma." Journal of Spectroscopy 2014 (2014): 1–5. http://dx.doi.org/10.1155/2014/517089.
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A LC-MS/MS method for determination of stavudine in human plasma was established and validated, and it was applied to the pharmaceutical formulations bioequivalence study. 0.5 mL plasma sample was extracted by liquid-liquid extraction. Stavudine was detected by a LC-MS/MS system. The pharmacokinetic parameters of stavudine in different formulations were calculated by noncompartment model statistics. The method was linear over the concentration ranges 5.00–1000 ng/mL in plasma. The intra- and interassay relative standard deviation (RSD) was <10%. The average accuracies for the assay at three concentrations (5.00, 80.0, and 900 ng/mL) were from 100.2% to 102.5%. Pharmacokinetic parameters of stavudine reference formulation were obtained as follows:Tmaxwas0.6±0.2 h,Cmaxwas480.7±150.9 g/L,t1/2was1.7±0.4 h, andAUC0-twas872.8±227.8 g·h/L, and pharmacokinetic parameters of stavudine test formulation were obtained as follows:Tmaxwas0.5±0.2 h,Cmaxwas537.5±178.5 g/L,t1/2was1.7±0.3 h, andAUC0-twas (914.1±284.5) g·h/L. Calculated withAUC0-t, the bioavailability of two formulations was 105.0%.
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Kakuda, Thomas N., Monika Schöller-Gyμre, Cassy Workman, Keikawus Arasteh, Anton L. Pozniak, Goedele De Smedt, Greet Beets, et al. "Single- and multiple-dose pharmacokinetics of etravirine administered as two different formulations in HIV-1-infected patients." Antiviral Therapy 13, no. 5 (July 2008): 655–61. http://dx.doi.org/10.1177/135965350801300505.
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Background An open-label, randomized, crossover study to evaluate the pharmacokinetics of two different formulations of etravirine after single and multiple dosing. Methods Treatment-experienced HIV-1-infected patients with viral load <50 copies/ml continued their current antiretroviral regimen and added etravirine twice daily for 7 days with a morning intake on day 8. Etravirine was administered following food as either 800 mg twice daily of the Phase II formulation or 100 mg or 200 mg twice daily of the Phase III formulation. A 12 h pharmacokinetic assessment was performed on days 1 and 8. Results After single- and multiple-dose administration, the exposure to etravirine was lower with 100 mg twice daily and higher with 200 mg twice daily compared with 800 mg twice daily. On day 8, the mean (±sd) area under the plasma concentration-time curve over 12 h (AUC0–12 h) was 1,284 (±958) ng•h/ml when etravirine was administered as 100 mg twice daily ( n=33), 3,713 (±2,069) ng•h/ml when administered as 200 mg twice daily ( n=27) and 2,607 (±2,135) ng•h/ml when administered as 800 mg twice daily ( n=32). Both formulations and all doses of etravirine tested were generally safe and well tolerated. Conclusions The range of exposure to etravirine was comparable between 200 mg twice daily dose and 800 mg twice daily. The Phase III formulation of etravirine significantly improves the bioavailability of etravirine over the Phase II formulation with reduced interpatient variability in etravirine pharmacokinetics.
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D. Shivhare, Umesh, Vikrant P. Dorlikar, Kishore P. Bhusari, Vijay B. Mathur, and Bhiku N. Mirani. "Effect of Polymeric Compositions on Pharmacotechnical Properties of Carvedilol Transdermal Film." International Journal of Pharmaceutical Sciences and Nanotechnology 2, no. 1 (May 31, 2009): 457–64. http://dx.doi.org/10.37285/ijpsn.2009.2.1.10.
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Transdermal films of carvedilol were prepared by using Eudragit RL100 (ERL100) either alone or in combination with Eudragit RS100 (ERS100), hydroxypropyl methylcellulose K 15 LV (HPMC), and ethyl cellulose (EC). The drug release was extended over a period of 24 h from all formulations. The formulation A5 showed 98.33 cumulative % drug releases in 24 h and followed zero order kinetics. The drug transport mechanism was observed to be Fickian. The cumulative % drug diffused through artificial permeation membrane (cellophane A 393) from same formulation was 100.52 % over a 12 h. The mechanism of dug release was governed by Peppas model and the drug diffusion rate followed zero order kinetics. The formulation A5 comprising of polymers ERL 100, ERS 100, EC and HPMC in 7:1:1:1 ratio fulfills the requirement of good TDDS.
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Mamood, S. N. H., O. Hidayatulfathi, S. B. Budin, G. Ahmad Rohi, and M. H. Zulfakar. "The formulation of the essential oil of Piper aduncum Linnaeus (Piperales: Piperaceae) increases its efficacy as an insect repellent." Bulletin of Entomological Research 107, no. 1 (November 7, 2016): 49–57. http://dx.doi.org/10.1017/s0007485316000614.
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AbstractThe essential oil (EO) of Piper aduncum Linnaeus, known as ‘sireh lada’ to locals Malaysian, has the potential to be used as an alternative to synthetic insect repellents such as N,N-diethyl-meta-toluamide. However, the EO's efficacy as a repellent decreases after application due to the high volatility of its active ingredients. A number of studies have showed that optimizing the formulation of plant-based EOs can improve their efficacy as repellents. The present study sought to evaluate the effectiveness of 10% P. aduncum EO in ethanol and in three different semisolid formulations: ointment, cream and gel. These formulations were tested on Aedes aegypti under laboratory conditions. Each formulation was applied to the subject's hands, which were then inserted into a cage containing 25 nulliparous A. aegypti. The number of mosquitoes landing on or biting each subject's hand was recorded, and the repellency percentage, landing/biting percentage and protection time for each of the formulations were compared. There were no statistically significant differences between the semisolid EO formulations with regards to the repellency percentage and the landing/biting percentage at 4 h post-application. All three semisolid EO formulations were able to repel >65% of the A. aegypti at 4 h post-application. The EO ointment formulation provided a protection time (182.5 ± 16.01 min) that was statistically significantly longer than that associated with the EO gel formulation (97.5 ± 14.93 min). Meanwhile, the EO cream formulation provided a protection time of 162.5 ± 6.29 min. As the EO cream and ointment formulations displayed better repellent properties than the EO gel formulation, they appear to be the most promising P. aduncum EO formulations to be developed and commercialized as alternatives to synthetic repellents.
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Rashid, Rizwana, Muhammad Zaman, Mahmood Ahmad, Mahtab Ahmad Khan, Muhammad Hammad Butt, Ahmad Salawi, Yosif Almoshari, Meshal Alshamrani, and Rai Muhammad Sarfraz. "Press-Coated Aceclofenac Tablets for Pulsatile Drug Delivery: Formulation and In Vitro Evaluations." Pharmaceuticals 15, no. 3 (March 8, 2022): 326. http://dx.doi.org/10.3390/ph15030326.
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The symptoms of some diseases show circadian rhythms, such as the morning stiffness associated with pain at the time of awakening in rheumatoid arthritis. Therapy for such diseases doesn’t require immediate release or sustained release of medicament. In such therapies, pulsatile drug release is more suitable with a programmed drug release. The purpose of this research was to formulate press-coated aceclofenac tablets for pulsatile drug delivery with a distinct delay time of no drug release and release of the drug when it is more likely desired (i.e., after 5 to 6 h). Immediate release core tablets having aceclofenac were formulated. Three formulations, F1, F2, and F3, were prepared with variable concentrations of sodium croscarmellose. Pre- and post-compression tests were performed on the core tablets. The selection criteria included the lowest disintegration time as a requirement of pulsatile drug delivery with an immediate release core and a delayed release coat. The disintegration times of F1, F2, and F3 were 120 s, 60 s, and 15 s, respectively. Therefore, the F3 formulation was selected as the core tablet formulation because it had the shortest disintegration time (15 s). The core tablets were press-coated using different polymers, such as HPMC K100M, Eudragit L100, HEC, and HPMC E5. The polymers were used in the coatings to hinder the release of the core for the desired time. 36 formulations of polymer were prepared: A1 to A10 had HPMC K100M and Avicel PH102; formulations B1 to B6 had HPMC K100M, Eudragit L100, and Avicel PH102; formulations C1 to C7 had HPMC K100M and hydroxyethyl cellulose; formulations D1 to D7 had HPMC K100M and HPMC E5; and formulations E1 to E6 had changed the coating weight of the formulation used for D6 (having HPMC K100M and HPMC E5 in the ratio of 12.5% to 87.5%). Evaluations of the press-coated tablets were carried out through thickness, hardness, weight variation, friability, and in vitro dissolution tests. These parameters concluded that the formulation of E6, having HPMC K100M and HPMC E5 in the ratio of 12.5% to 87.5% at 600 mg weight, was the most optimum formulation as it showed 3.5% drug release after 4 h, 21.4% drug release after 5 h, and 99.27% drug release after 6 h.
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Mehta, L. Sonali, D. V. Gowda, N. Vishal Gupta, and Manohar M. "FORMULATION AND DEVELOPMENT OF LENALIDOMIDE LOADED DELAYED RELEASE MINI TABLETS IN CAPSULES." International Journal of Applied Pharmaceutics 10, no. 5 (September 8, 2018): 239. http://dx.doi.org/10.22159/ijap.2018v10i5.26658.
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Objective: Formulation and development of delayed release mini tablets in the capsule of drug lenalidomidein terms of dissolution and stability was the objective of the present work.Methods: Tablets of less than or equal to 3 millimetres diameter are Mini-tablets, which were filled into a capsule. Direct compression method using multi-tip punch was used for compression and coated with eudragit L100 as a seal coating material and with eudragit L30D55 as an enteric coating material was done. Different formulations were prepared and subjected for evaluation like weight variation, hardness, friability, disintegration, and dissolution studies. The optimized formulation was compared to marketed product based on drug released profile and also subjected for stability studies.Results: The results revealed that the in vitro drug release of prepared formulations, F1, F2, F3, and F4 was subjected for acid resistance test for 2 h in 0.1N HCl and has a comparable dissolution profile in phosphate buffer of 6.8 pH. FormulationF4 was subjected for stability studies and no significant difference was observed in 3 mo 40 °C/75% RH accelerated stability condition.Conclusion: The dissolution profile of formulation F4 was found better than that of market product. Based on evaluation results, the study concluded that F4formulationwas considered as an optimized formulation.
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Flory, Sandra, Romina Männle, and Jan Frank. "The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation." Antioxidants 10, no. 11 (November 17, 2021): 1826. http://dx.doi.org/10.3390/antiox10111826.
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The biological activities of curcumin in humans, including its antioxidative and anti-inflammatory functions, are limited by its naturally low bioavailability. Different formulation strategies have been developed, but the uptake of curcumin from these galenic formulations into and efflux from intestinal cells, which may be critical processes limiting bioavailability, have not been directly compared. Furthermore, little is known about their effect on P-glycoprotein activity, an important determinant of the pharmacokinetics of potentially co-administered drugs. P-glycoprotein activity was determined in LS180 cells, incubated with 30 or 60 µmol/L of curcumin in the form of seven different formulations or native curcuma extract for 1 h. All formulations inhibited P-glycoprotein activity at both concentrations. Curcumin uptake, after 1 h incubation of LS180 cells with the formulations (60 µmol/L), showed significant variability but no consistent effects. After 1 h pre-treatment with the formulations and further 8 h with curcumin-free medium, curcumin in cell culture supernatants, reflecting the efflux, differed between individual formulations, again without a clear effect. In conclusion, curcumin inhibits P-glycoprotein activity independently of its formulation. Its uptake by and efflux from intestinal cells was not significantly different between formulations, indicating that these processes are not important regulatory points for its bioavailability.
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V., Rajalakshmi S., and Vinaya O. G. "FORMULATION DEVELOPMENT, EVALUATION AND OPTIMIZATION OF MEDICATED LIP ROUGE CONTAINING NIOSOMAL ACYCLOVIR FOR THE MANAGEMENT OF RECURRENT HERPES LABIALIS." International Journal of Applied Pharmaceutics 9, no. 6 (November 8, 2017): 21. http://dx.doi.org/10.22159/ijap.2017v9i6.19349.
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Objective: Aim of the study was to formulate, evaluate and optimize medicated Lip rouge containing acyclovir encapsulated inside a novel vesicular carrier, niosome so that the formulation can improve its membrane penetration. Formulating as a cosmetic Lip rouge formulation will also improve patient compliance in the treatment of herpes labialis.Methods: Acyclovir niosomes were prepared by thin film hydration method. Niosomes were evaluated and were optimized by considering the entrapment efficiency and in vitro release profile. The optimized niosomes were incorporated into lipstick, lip balm and lip rouge for selecting the best lip formulation. Based on the in vitro release profile, ease of application and properties of prepared formulations lip rouge was selected and further evaluations were carried out.Results: Among the six formulations of niosomes NF2 has showed 88.49 % entrapment efficiency and 86.97% cumulative drug release in 8 h. The formulation was optimized considering both entrapment efficiency and in vitro release. The optimized formulation of niosomes was incorporated into Lipstick, lip balm and lip rouge. The evaluation results of lipstick, lip balm and lip rouge for in vitro release suggested lip rouge as the best formulation. The percentage cumulative release of drug from optimized lip rouge at the end of 8 h was 84.77%. The percentage cumulative drug release in ex vivo studies for 8 h was 60.88 %.Conclusion: The results suggested that prepared lip rouge containing acyclovir niosomes can effectively deliver the drug than the marketed acyclovir cream and successful therapy of Recurrent Herpes labialis can be achieved.
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Venkateswarlu, Kambham. "Formulation and Evaluation of Sustained Release Matrix Tablets of Repaglinide." Bangladesh Pharmaceutical Journal 19, no. 1 (August 10, 2016): 92–99. http://dx.doi.org/10.3329/bpj.v19i1.29244.
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The aim of present investigation was to formulate and evaluate the sustained release matrix tablets of Repaglinide (RPGN). These matrix tablets were prepared by wet granulation method using synthetic and natural polymers like HPMC K4M, HPMC 100M and Guar gum (GG), Carrageenan (CG), respectively. Invitro drug release studies were performed by USP dissolution apparatus type-II (paddle method) using 0.1 N HCl buffer and pH 6.8 phosphate buffer for 12 h. Amongst all the 12 formulations, formulation F12 showed maximum drug release of 97.9% for 12 h study. It was observed from the kinetic studies that all the formulations followed first order kinetics and particularly the drug release from its dosage form was fickian diffusion (F9, F12), non-fickian diffusion (F1-F8, F10-F11). Formulation F12 was subjected to stability studies and confirmed that formulation F12 was stable upto the period of 1 month.Bangladesh Pharmaceutical Journal 19(1): 92-99, 2016
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Zhao, Yongdong, and Suhada Jayasuriya. "An H∞ Formulation of Quantitative Feedback Theory." Journal of Dynamic Systems, Measurement, and Control 120, no. 3 (September 1, 1998): 305–13. http://dx.doi.org/10.1115/1.2805401.
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The QFT robust performance problem in its entirety may be reduced to an H∞ problem by casting each specification as a frequency domain constraint either on the nominal sensitivity function or the complementary sensitivity function. In order to alleviate the conservative nature of a standard H∞ solution that is obtainable for a plant with parametric uncertainty we develop a new stability criterion to replace the small gain condition. With this new stability criterion it is shown that the existence of a solution to the standard H∞ problem guarantees a solution to the QFT problem. Specifically, we provide an explicit characterization of necessary frequency weighting functions for an H∞ embedding of the QFT specifications. Due to the transparency in selecting the weighting functions, the robust performance constraints can be easily relaxed, if needed, for the purpose of assuring a solution to the H∞ problem. Since this formulation provides only a sufficient condition for the existence of a QFT controller one can then use the resulting H∞ compensator to initiate the QFT loop shaping step.
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Feng, Paul C. C., Jan S. Ryerse, and R. Douglas Sammons. "Correlation of Leaf Damage with Uptake and Translocation of Glyphosate in Velvetleaf (Abutilon theophrasti)." Weed Technology 12, no. 2 (June 1998): 300–307. http://dx.doi.org/10.1017/s0890037x00043852.
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Uptake and translocation of glyphosate in three commercial formulations were examined in velvetleaf, a dicotyledonous weed that is commonly treated with glyphosate. The formulations included Roundup®(MON 35085), Roundup Ultra, and Touchdown®as sold in Canada. A minimal amount of14C-glyphosate was spiked into a lethal rate of each formulation, and the short-term (3 to 72 h) uptake into the treated leaf and subsequent translocation into the plant were measured. Time-course studies showed very rapid uptake and translocation of glyphosate in the Ultra formulation. In comparison, the uptake and translocation of glyphosate in Touchdown was much slower but continued throughout the 72-h period. Glyphosate in the Roundup formulation showed intermediate uptake and translocation. Tissue necrosis at the application sites of Ultra and Roundup was visible within 24 h after treatment. Examinations using stereo and fluorescence microscopy revealed extensive cell death and tissue disruption. Tissue necrosis from Ultra and Roundup was also observed in blank formulations containing no glyphosate and therefore was likely caused by the surfactants. In contrast, the application sites of Touchdown produced little to no leaf damage. Our results demonstrated a direct correlation between tissue necrosis and rapid rates of glyphosate uptake and translocation.
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Saengklub, Nakkawee, Tussapon Boonyarattanasoonthorn, Anusak Kijtawornrat, and Doungdaw Chantasart. "Preliminary Bioequivalence of an Oral Pimobendan Solution Formulation with Reference Solution Formulation in Beagle Dogs." Veterinary Sciences 9, no. 3 (March 17, 2022): 141. http://dx.doi.org/10.3390/vetsci9030141.
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Oral capsule and tablet formulations of pimobendan are widely used but may present difficulties for accurately dosing small patients. This study aimed to compare the pharmacokinetic (PK) characteristics, bioequivalence, and cardiovascular effects of a custom-made oral pimobendan solution (PS) formulation compared to a reference solution (RS) formulation in conscious, healthy dogs. A randomized crossover design was performed on dogs that received RS and PS formulations at a dose of 0.3 mg/kg. Blood samples were collected at 0, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, and 24 h after oral administration for PK analysis; bioequivalence was also calculated. Echocardiography was also performed to assess the cardiovascular effects. The results revealed that the plasma concentrations of pimobendan and o-desmethyl-pimobendan (active metabolite) in the case of both formulations were comparable. The relative ratios of geometric mean concentrations for all significant parameters of PK were within a range of 80–125%, indicating bioequivalence. In addition, both formulations increased cardiac contraction significantly when compared with the baseline, and no differences in cardiac contractility were detected between the formulations. The PS formulation can be used as alternative to the RS formulation for the management of congestive heart disease because of the bioequivalence between the two formulations.
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Kılıç, Nihal. "Efficacy of Dust and Wettable Powder Formulation of Diatomaceous Earth (Detech®) in the Control of Tyrophagus putrescentiae (Schrank) (Acari: Acaridae)." Insects 13, no. 10 (September 20, 2022): 857. http://dx.doi.org/10.3390/insects13100857.
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Tyrophagus putrescentiae (Schrank) (Acari: Acaridae) is a cosmopolite mite species commonly in found food and stored products. In this study, the acaricidal activity of two Turkish diatomaceous earth (DE) formulations (Detech® WP95 and Detech® Dust) were applied on a concrete surface at five different concentrations (1, 2.5, 5, 7.5, and 10 g/m2) and dead individuals were counted at 11 different time intervals (1, 3, 6, 9, 12, 15, 18, 21, 24, 27, and 30 h) at a temperature of 25 ± 1 °C and 75 ± 5% relative humidity (RH). Mite mortalities were observed after 6- and 18-hour exposure periods at all concentrations of dust and wettable powder (WP) formulations, respectively. Specifically, 100% mortality for the WP formulation was achieved at the highest concentration of 10 g/m2 after 15 h of exposure and after 27 h and 30 h for the lowest concentration. In the case of dust formulation, mortalities were observed after 3 h of exposure at all concentrations except at 1 g/m2, while a 100% mortality rate was achieved after 21 h of exposure to all concentrations and after 18 h of exposure for 7.5 g/m2 and 10 g/m2. This study indicates that both WP and dust formulations of local diatomaceous earth can cause 100% mortality in 24 h on average and can be a promising alternative to conventional chemical acaricides.
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El-Masry, Soha Mahmoud, and Noha Mahmoud El-Khodary. "Pharmacokinetic and Tolerability Comparison of Sustained and Immediate Release Oral Formulations of Nifedipine Tablet Formulations: A Single-Dose, Randomized, Open-Label, Two-Period, Two-Way Crossover Study in Healthy, Fasting Egyptian Male Volunteers." Drug Research 70, no. 02/03 (November 19, 2019): 91–96. http://dx.doi.org/10.1055/a-1035-9212.
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AbstractNifedipine is one of calcium channel blockers that commonly used clinically to treat hypertension and angina in Egyptian patients. A sustained-release (SR) formulation of nifedipine is available in the Egyptian community and administered twice daily. This study aimed to to compare the pharmacokinetics and safety profiles of a 20 mg SR and IR (immediate release) formulation of nifedipine after single-dose administration in healthy Egyptian subjects. Randomized, crossed open-label two- way clinical trial, in 16 healthy adult volunteers, of 24.75±5.20 years, with BMI 23.26±1.756 were assessed. Blood samples were collected at predefined times for 48 h and analyzed for Nifedipine plasma concentrations using validated reversed phase liquid chromatography method with ultraviolet detection. Pharmacokinetics was determined using non- compartmental model pharmacokinetics and analyzed using one-way ANOVA (P≤0.05). Following a single oral administration, SR formulation had a lower Cmax, compared to IR formulation (54.46±17.75 , 107.45±29.85 ng/mL, respectively), and Tmax was significantly longer (2.97 vs. 1.13 h) for the SR and IR formulation, respectively. There was no significant difference between the SR and the IR formulations for AUC0–last and AUC0-∞ (326.7±98.28 vs. 309.27±105.53 ng·h·mL−1 and 380.9 ± 105.24 vs. 334.36±108.1 ng·h·mL−1, respectively). SR formulation of nifedipine showed similar pharmacokinetics to the IR Formulation (F%=1.049), but it additionally allows a less frequent administration. Therefore, The nifedipine SR and IR formulations were well tolerated and displayed comparable safety profiles.
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Guo, Wenxiu, Xun Yan, and Richou Han. "Adapted formulations for entomopathogenic nematodes, Steinernema and Heterorhabditis spp." Nematology 19, no. 5 (2017): 587–96. http://dx.doi.org/10.1163/15685411-00003072.
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The effects of carriers, temperatures, concentrations of the infective juveniles (IJ) and a fungicide on the survival and infectivity of five nematode species, Steinernema carpocapsae, S. feltiae, S. longicaudum, Heterorhabditis bacteriophora and H. indica, were evaluated to establish the adapted formulations for these nematodes. Vermiculite and humus were good carriers for the storage of the three Steinernema species, with more than 90% IJ survival after 120 days at 5°C, 80 days at 15°C and at least 20 days at 25°C, and 90% survival for the storage of H. bacteriophora after 10 days at 5°C and 15°C. After 10 days at 25°C, ca 80% IJ survival was recorded for H. bacteriophora and H. indica. Although ca 90% IJ survival was found after 10 days at 15°C for H. indica, this species did not tolerate low temperature, with survival less than 40% after 10 days at 5°C. The ratios of the IJ and the carriers in the ranges of 1:0.8-1:1.2 (w/w) did not significantly influence the survival of all nematode species. The vermiculite formulation containing a fungicide Proxel GXL at concentrations of 0.1% and 0.2% increased the survival of two Heterorhabditis species. Heterorhabditis bacteriophora and H. indica could be stored for 60 and 40 days, respectively, at 15°C in aerated water with 90% IJ survival, compared with the vermiculite formulation. The tested formulations did not significantly influence the infectivity of the IJ from the formulations with IJ survival more than 80%. The results provide alternative formulation methods for the commercial storage of these beneficial nematodes.
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Aslam, Mohammed, Syed Sarim Imam, Mohammed Aqil, Yasmin Sultana, and Asgar Ali. "Levofloxacin loaded gelrite-cellulose polymer based sustained ocular drug delivery: formulation, optimization and biological study." Journal of Polymer Engineering 36, no. 8 (October 1, 2016): 761–69. http://dx.doi.org/10.1515/polyeng-2015-0218.
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Abstract In the present work, levofloxacin in situ gel formulation was developed using gelrite as a gelling agent in combination with hydroxy propyl methyl cellulose. The developed formulations were evaluated for physicochemical parameters, in vitro release, ex vivo transcorneal study, sterility testing, antimicrobial efficacy, ocular irritation study, histopathological and stability evaluation. The in vitro drug release study showed the extended drug release up to 12 h, and the best fit kinetic model was found to be Peppas model (R2=0.9654), suggesting a Fickian diffusion process. The developed formulations showed optimized physicochemical results for all parameters. The optimized formulation showed therapeutically efficacious antimicrobial activity. Hens egg test-chorioallantoin membrane assay (HET-CAM) showed a mean score of 0.33 up to 24 h, which indicated the non-irritant property of the developed formulation. This non-irritant and stable in situ gel formulation of levofloxacin was found to be promising and safe for use as ocular delivery. The degradation rate constant and shelf life of developed optimized formulation (F14) were found to be low (1.213×10-4 at 25°C) and 2.14 years, respectively. This renders them favorable for ocular use as they would gel once in contact with the tear fluid, thus reducing nasolacrimal drainage, but would thin upon shearing, preventing ocular irritation and therefore induced lacrimation.
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Ernst, W. R., and K. G. Doe. "A Comparison of the Aquatic Toxicity of Fenitrothion Flowable and Fenitrothion Liquid Technical Formulations." Water Quality Research Journal 24, no. 4 (November 1, 1989): 553–68. http://dx.doi.org/10.2166/wqrj.1989.034.
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Abstract Fenitrothion, a popular spruce budworm (Choristoneura fumiferarna) insecticide, has recently been produced as a “flowable” formulation which consists of finely milled particles of the active ingredient in suspension. In order to determine if such a formulation change could alter the chemical’s toxicity and bioconcentration potential to non-target aquatic fauna, a series of bioassays was undertaken. In acute (48- and 96-h LC50s) tests using rainbow trout (Oncorhynchus mykiss), threespine stickleback (Gasterosteus aculeatus), freshwater clams (Anodonta spp.), blue mussels (Mytilus edulis) and the water flea (Daphnia magna), the toxicity of conventional fenitrothion (liquid technical) formulations was not substantially different from that of the “flowable” (particulate) formulation. The exception was that the flowable formulation was less toxic than the liquid technical formulation to the freshwater clam by a factor of 1/3 to 1/5. Bioconcentration factors to blue mussels for the flowable formulation (15 to 36) were approximately 1/8 to 1/2 the blue mussel bioconcentration factors previously reported for the liquid technical formulations. The results indicate that the flowable formulation does not represent an increased hazard to the aquatic organisms tested, compared with the conventional liquid technical formulations.
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Tompson, Debra J., Mark Whitaker, Rennan Pan, Geoffrey Johnson, Teresa Fuller, Litza McKenzie, Vanessa Zann, Marcy Powell, Kathy Abbott-Banner, and Simon Hawkins. "Development of a Prototype, Once-Daily, Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772." Pharmaceutical Research 38, no. 7 (June 16, 2021): 1235–45. http://dx.doi.org/10.1007/s11095-021-03059-z.
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Abstract Purpose GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1, with a 2–3 h half-life. This study evaluated if a once-daily modified-release formulation of GSK2982772 could be developed with no significant food effect. Methods Part A evaluated the pharmacokinetics of GSK2982772 following fasted single-dose (120 mg) administration of two matrix minitab formulations (MT-8 h and MT-12 h) vs 120 mg immediate release (IR) and MT-12 h with a high-fat meal. Part B evaluated once-daily MT-12 h for 3 days at three dose levels. Part C evaluated a matrix monolithic (MM-12 h) formulation at two dose levels in different prandial states. Results All modified-release formulations dosed in the fasted state reduced maximum plasma concentration (Cmax), delayed time to Cmax, and decreased area under the curve (AUC) vs IR. When MT-12 h or MM-12 h were co-administered with a meal (standard or high-fat) Cmax and AUC increased. Dosing MM-12 h 1 h before a standard or high-fat meal had minimal impact on exposure vs fasted. Conclusions MT-12 h and MM-12 h provided a QD pharmacokinetic profile in the fasted state, however when MT-12 h was dosed with a high-fat meal a QD profile was not maintained. (ClinicalTrials.gov Identifier: NCT03266172).
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Gadad, A., A. Patil, V. K. Sariki, P. Dandagi, and V. Masthiholimath. "DESIGN AND CHARACTERIZATION OF BIODEGRADABLE TIZANIDINE NANOPARTICLES FOR IMPROVED ORAL BIOAVAILABILITY." INDIAN DRUGS 53, no. 03 (March 28, 2016): 57–59. http://dx.doi.org/10.53879/id.53.03.10438.
Full textAbstract:
Tizanidine HCl is a drug with poor water solubility, oral bioavailability and high first pass metabolism. The present study aims at developing a nano formulation by nanoprecipitation method to improve the oral bioavailability. Five formulations (F1-F5) with different polymer ratios were prepare and optimized on the basis of entrapment efficiency. In vitro release kinetics of formulations shows extended release of drug over a period of 128 h. Optimized formulation F3 shows better stability and oral bioavailability 3.6 times more than pure drug.
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Hempel, Judith, Anja Fischer, Monique Fischer, Josef Högel, Anja Bosy-Westphal, Reinhold Carle, and Ralf M. Schweiggert. "Effect of aggregation form on bioavailability of zeaxanthin in humans: a randomised cross-over study." British Journal of Nutrition 118, no. 9 (November 14, 2017): 698–706. http://dx.doi.org/10.1017/s0007114517002653.
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AbstractCarotenoid bioavailability from plant and animal food is highly variable depending on numerous factors such as the physical deposition form of carotenoids. As the carotenoid zeaxanthin is believed to play an important role in eye and brain health, we sought to compare the human bioavailability of an H-aggregated with that of a J-aggregated deposition form of zeaxanthin encapsulated into identical formulation matrices. A randomised two-way cross-over study with sixteen participants was designed to compare the post-prandial bioavailability of an H-aggregated zeaxanthin and a J-aggregated zeaxanthin dipalmitate formulation, both delivering 10 mg of free zeaxanthin. Carotenoid levels in TAG-rich lipoprotein fractions were analysed over 9·5 h after test meal consumption. Bioavailability from the J-aggregated formulation (AUC=55·9 nmol h/l) was 23 % higher than from the H-aggregated one (AUC=45·5 nmol h/l), although being only marginally significant (P=0·064). Furthermore, the same formulations were subjected to an internationally recognisedin vitrodigestion protocol to reveal potential strengths and weaknesses of simulated digestions. In agreement with our human study, liberation of zeaxanthin from the J-aggregated formulation into the simulated duodenal fluids was superior to that from the H-aggregated form. However, micellization rate (bioaccessibility) of the J-aggregated zeaxanthin dipalmitate was lower than that of the H-aggregated zeaxanthin, being contradictory to ourin vivoresults. An insufficient ester cleavage during simulated digestion was suggested to be the root cause for these observations. In brief, combining ourin vitroandin vivoobservations, the effect of the different aggregation forms on human bioavailability was lower than expected.
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Sharma, Rakesh Kumar, and Anil Kumar Middha. "Investigations on noval method for the formulation of solid dispersions part- I Formulation, characterization and selection." International Journal of Drug Delivery 9, no. 3 (October 31, 2017): 71. http://dx.doi.org/10.5138/09750215.2173.
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<p>The solid dispersions of indomethacin with hydrophilic polymers were prepared by lyophilization. The polymers used in the investigation were HPMC, PVP K30, CBR and PLF 127. The solubility and dissolution of indomethacin from prepared lyophilized solid dispersions were investigated in 0.1 N HCl, purified water and USP-NF dissolution media. Out of fifteen lyophilized formulations from F1 to F15, five formulations F2, F5, F8, F12 and F14 showed highest solubility in purified water. Formulation F2, F8 failed to comply with the USP-NF dissolution test for indomethacin capsules. Formulation F14 showed maximum dissolution in the respective dissolution media within 60 min. Sustained drug release was observed for 6 h with formulations F2 and F8 in USP-NF media. The formulations F2, F5, F8, F12 and F14 were characterized by modulated DSC and FT-IR spectroscopy. Some Formulations on stability testing were found physico-chemically stable at accelerated temperature conditions.</p>
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M, Sindhoor S., Sneh Priya, and Amala Maxwell. "FORMULATION AND EVALUATION OF NOVEL IN SITU GEL OF LAFUTIDINE FOR GASTRO RETENTIVE DRUG DELIVERY." Asian Journal of Pharmaceutical and Clinical Research 11, no. 8 (August 7, 2018): 88. http://dx.doi.org/10.22159/ajpcr.2018.v11i8.25582.
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Objective: The aim of the present study was to formulate and evaluate the novel in situ gel of lafutidine for gastroretentive drug deliveryMethods: A gastroretentive in situ gel of lafutidine was formulated by pH-triggered ionic gelation method using different concentrations of gelling polymer such as sodium alginate, gellan gum, and xanthum gum. Prepared formulations were evaluated for viscosity, density, buoyancy lag time and buoyancy duration, and drug content. In vitro drug release studies of all formulations were also performed. In vivo fluorescence imaging study was conducted for optimized formulation and compared with control.Results: The concentration of gelling agents and release retardant polymers significantly affected viscosity, floating behavior, and in vitro drug release of the formulations. The pH and drug content were found in the range of 6.72–7.20 and 88.74–95.33%, respectively. Floating lag time was <2 min; duration of floating was more than 12 h. Minimum and maximum in vitro drug release were found to be for formulation F9 (51.74%) and F1 (82.76%), respectively, at the end of 12 h. The drug was released from the all the formulations in a sustained manner. In vivo studies confirmed the gastroretention of the formulation in mice stomach for 8 h. Stability studies indicated that the there was no significant change in the visual appearance, floating behavior, and drug content.Conclusion: The gastroretentive in situ gel system, prolonged the gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract.
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Lee, Jaehyeok, Chul Haeng Lee, Jong-Geon Lee, So Yeon Jeon, Min-Koo Choi, and Im-Sook Song. "Enhancing Dissolution and Oral Bioavailability of Ursodeoxycholic Acid with a Spray-Dried pH-Modified Extended Release Formulation." Pharmaceutics 14, no. 5 (May 11, 2022): 1037. http://dx.doi.org/10.3390/pharmaceutics14051037.
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Ursodeoxycholate (UDCA) has low oral bioavailability and pH-dependent solubility and permeability. Thus, we developed a pH-modified extended-release formulation of UDCA using Na2CO3 as the alkalizing agent and hydroxypropyl methylcellulose (HPMC) as the release-modifying agent. The optimized pH-modified controlled-release UDCA formulation, with the UDCA:HPMC:Na2CO3 ratio of 200:600:150 (w/w/w), was prepared using a spray-drying method. Then, the formulation’s solubility, dissolution, and pharmacokinetic properties were characterized. In a pH-modified extended-release formulation of UDCA, the solubility of UDCA was increased to 8 mg/mL with a sustained dissolution for 12 h. Additionally, the spray-dried formulation exhibited amorphous states without molecular interaction among UDCA, Na2CO3, and HPMC. Moreover, the plasma UDCA concentration of the formulation maintained a higher UDCA concentration for up to 48 h than that of UDCA itself or the non-extended-release UDCA formulation. Consequently, the formulation significantly increased the AUC compared to UDCA or the non-extended-release UDCA formulation in rats. In conclusion, we have improved UDCA’s solubility and dissolution profile by preparing a pH-modified extended-release formulation with the UDCA:HPMC:Na2CO3 ratio of 200:600:150 (w/w/w), which effectively increased the oral bioavailability of UDCA by 251% in rats.
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Elkomy, Mohammed H. "Changing the Drug Delivery System: Does it Add to Non-Compliance Ramifications Control? A Simulation Study on the Pharmacokinetics and Pharmacodynamics of Atypical Antipsychotic Drug." Pharmaceutics 12, no. 4 (March 25, 2020): 297. http://dx.doi.org/10.3390/pharmaceutics12040297.
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This study investigates the pharmacokinetic (PK) and pharmacodynamic (PD) consequences of shifting from Quetiapine fumarate immediate-release (IR) to extended-release (XR) formulation in non-adherent schizophrenia patients. Monte-Carlo simulations using population PK and PD models were implemented to predict the time course of plasma concentration and Brief Psychiatric Rating Scale (BPRS) scores following the oral administration of 200 mg Seroquel® every 12 h and 400 mg Seroquel XR® every 24 h in patients experiencing dose delay, omission or doubling. Parameters were computed and their distributions were compared using the Kolmogorov–Smirnov test. Dose irregularities with both formulations had different effects on plasma concentration and %reduction in BPRS scores from baseline. However, the odds ratio of getting a %reduction in BPRS below 14%, or plasma concentration exceeding 500 µg/L, were comparable for adherent and non-adherent patients. Plasma therapeutic concentration after treatment cessation was maintained for <24 h in 48% and 29.6% of patients, and a steady state recovery time of <48 h was achieved in 51% and 13.4% of patients on the IR and XR formulations, respectively. Monte-Carlo simulations predict that the risks associated with the IR dose irregularities are not worsened when the XR formulation is used instead. Non-adherence events involving a single dose of either formulation do not require rescue doses.
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Mahalingam, Alamelu, Adam P. Simmons, Shweta R. Ugaonkar, Karen M. Watson, Charlene S. Dezzutti, Lisa C. Rohan, Robert W. Buckheit, and Patrick F. Kiser. "Vaginal Microbicide Gel for Delivery of IQP-0528, a Pyrimidinedione Analog with a Dual Mechanism of Action against HIV-1." Antimicrobial Agents and Chemotherapy 55, no. 4 (January 18, 2011): 1650–60. http://dx.doi.org/10.1128/aac.01368-10.
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ABSTRACTPyrimidinediones, a novel class of compounds, have previously been shown to possess antiviral activity at nanomolar concentrations. One member of this class of compounds, IQP-0528, was selected as the lead molecule for formulation development owing to its stability at physiologically relevant conditions, wide therapeutic window, and antiviral activity in the nanomolar range. Here, we report the development of two vaginal gels—3.0% hydroxyethyl cellulose (HEC) formulation and a 0.65% Carbopol formulation—for the sustained delivery of IQP-0528. Stability studies under accelerated conditions confirmed the chemical stability of IQP-0528 and mechanical stability of the gel formulation for 3 months.In vitrorelease studies revealed that diffusion-controlled release of IQP-0528 occurred over 6 h, with an initial lag time of approximately 1 h. Based on the drug release profile, the 3.0% HEC gel was selected as the lead formulation for safety and activity evaluations. Thein vitroandex vivosafety evaluations showed no significant loss in cell viability or significant inflammatory response after treatment with a 3.0% HEC gel containing 0.25% IQP-0528. In anin vitroHIV-1 entry inhibition assay, the lead formulation showed an 50% effective concentration of 0.14 μg/ml for gel in culture media, which corresponds to ∼0.001 μM IQP-0528. The antiviral activity was further confirmed by using polarized cervical explants, in which the formulation showed complete protection against HIV infection. In summary, these results are encouraging and warrant further evaluation of IQP-0528 gel formulations inin vivomodels, as well as the development of alternative formulations for the delivery of IQP-0528 as a microbicide.
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Naseem, Faiza, Shefaat Ullah Shah, Sheikh Abdur Rashid, Arshad Farid, Mazen Almehmadi, and Saad Alghamdi. "Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of H. pylori: Preparation and In Vitro Characterization." Polymers 14, no. 3 (January 27, 2022): 519. http://dx.doi.org/10.3390/polym14030519.
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Metronidazole has the potential to produce local stomach specific action in order to treat Helicobacter pylori induced peptic ulcer disease. The current project executes the development of osmotically controlled bioadhesive metronidazole loaded effervescent floating tablets with optimized floating and swelling behavior. Direct compression technique was used to prepare the tablets. The designed formulations exhibited physico-chemical properties within acceptable optimum limits as per pharmacopeial requirements. The results of tablet floating studies revealed that all formulations, except F1 and F5, had good buoyancy characteristics (TFT > 12 h except F2 and F8 with TFT of 6 h). Formulation F2 containing guar gum in higher concentration with carbopol and formulation F8 containing guar gum in 50% decreased concentration in combination with HPMC and carbopol had enhanced FLT appreciably, with least TFT as compared to formulations F3, F4, and F6 (ANOVA; p ≤ 0.05). Formulation batches of F3, F4, and F6 exhibited appreciable FLT as well as TFT and were optimized formulations. Out of the above mentioned optimized batches, F4 and F6 formulations showed low FLT (4 and 5 s respectively). The results of the swelling study indicated a proportionate increase in the swelling index with increase in time. A significantly higher swelling ratio was found with formulation F6 and F4 compared with that of F7 and F8 (ANOVA; p ≤ 0.05). Additionally, the impact of pH change, agitational intensity, as well as increasing concentration of NaCl was investigated on drug release. It was observed that agitational intensity had no effect on drug release rate while increasing concentration of NaCl produced an increased drug release from the dosage form as compared to the drug release exhibited by the formulations in the absence of NaCl. Overall, this project could have valuable contribution in the fabrication of metronidazole loaded effervescent floating tablets. Gastro-retentive systems are expected to enhance local stomach specific action of anti H. pylori agents based on their buoyancy and swelling behavior.
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MD, Rawoof, Rajnarayana K, and Ajitha M. "Development and In Vivo Evaluation of Mesalazine Colon Targeted Tablets." International Journal of Pharmaceutical Sciences and Nanotechnology 12, no. 3 (May 31, 2019): 4552–58. http://dx.doi.org/10.37285/ijpsn.2019.12.3.6.
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The main objective of the present study was to develop colon-targeted tablets of mesalazine by wet granulation method using 33 Response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16 % of mesalazine after 24 h, whereas marketed product drug release was 92.02 ± 2.15 after 24 h. From in vivo bioavailability studies, after oral administration of colon targeted tablet containing 400 mg mesalazine, the Cmax, Tmax, and AUC0–∞ of optimized formulation and marketed product was found to be 683.21 ± 0.03 ng/mL, 6.01 ± 0.04 h, 4150.12 ± 5.12 ng*h/mL and 445.34 ± 3.22 ng/mL, 4.00 ± 0.01 h, 3457.18 ± 5.32 ng*h/mL respectively. Cmax, Tmax and AUC values of optimized formulation were found to be significantly higher than of marketed product. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of mesalazine for the treatment of disease at colon region.
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Badawy, Abdulla A. B., Donald M. Dougherty, and Dawn M. Richard. "Specificity of the Acute Tryptophan and Tyrosine plus Phenylalanine Depletion and Loading Tests Part II: Normalisation of the Tryptophan and the Tyrosine Plus Phenylalanine to Competing Amino Acid Ratios in a New Control Formulation." International Journal of Tryptophan Research 3 (January 2010): IJTR.S5169. http://dx.doi.org/10.4137/ijtr.s5169.
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Current formulations for acute tryptophan (Trp) or tyrosine (Tyr) plus phenylalanine (Phe) depletion and loading cause undesirable decreases in ratios of Trp or Tyr + Phe to competing amino acids (CAA), thus undermining the specificities of these tests. Branched-chain amino acids (BCAA) cause these unintended decreases, and lowering their content in a new balanced control formulation in the present study led to normalization of all ratios. Four groups (n = 12 each) of adults each received one of four 50 g control formulations, with 0% (traditional), 20%, 30%, or 40% less of the BCAA. The free and total [Trp]/[CAA] and [Phe + Tyr]/[BCAA+ Trp] ratios all decreased significantly during the first 5 h following the traditional formulation, but were fully normalized by the formulation containing 40% less of the BCAA. We recommend the latter as a balanced control formulation and propose adjustments in the depletion and loading formulations to enhance their specificities for 5-HT and the catecholamines.
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Petersen, Phil J., Lloyd C. Haderlie, Raymond H. Hoefer, and Ray S. McAllister. "Dicamba Absorption and Translocation as Influenced by Formulation and Surfactant." Weed Science 33, no. 5 (September 1985): 717–20. http://dx.doi.org/10.1017/s0043174500083156.
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Absorption and translocation of14C-dicamba (3,6-dichloro-o-anisic acid) in seven salt formulations were determined 60 h after application to leaves of soybean [Glycine max(L.) Merr. ‘Williams’] grown in nutrient solution. The dimethylamine (DMA) formulation was consistently absorbed and retained in the plant in amounts equal to or greater (46% of recovered14C) than other formulations (which averaged 19% of recovered14C) when applied without surfactant. Absorption and subsequent retention of the DMA formulation in the plant was least affected of all formulations by the addition of a surfactant. With a surfactant, absorption of the DMA, monoethanolamine (MEA), and inorganic salt formulations was similar (>75% of recovered14C). Addition of seven surfactants to the K-salt of dicamba increased both the amount of14C absorbed by 35 to 56% and the amount recovered in the plant. All surfactants except one enhanced absorption of the K-salt of dicamba to a similar degree. Dicamba exhibited predominantly symplastic translocation with the majority of14C being recovered in the new second trifoliolate leaves and nutrient solution. As much as 66% of the radioactivity absorbed through the leaves was exuded by roots into the nutrient solution 60 h after leaf treatment.
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Kreil, Verónica, Luis Ambros, Ana Paula Prados, Lisa Tarragona, Agustina Monfrinotti, Guillermo Bramuglia, and Marcela Rebuelto. "Pharmacokinetics of Immediate and Sustained Release Cephalexin Administered by Different Routes to Llamas (Lama glama)." Advances in Pharmacological Sciences 2016 (2016): 1–6. http://dx.doi.org/10.1155/2016/4621039.
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We investigate the pharmacokinetics of two different cephalexin formulations administered to llamas by the intravenous (IV), intramuscular (IM), and subcutaneous (SC) routes, the minimum inhibitory concentration (MIC) of cephalexin against someEscherichia coliand staphylococci isolated from llamas, and we apply the PK/PD modelling approach, so that effective dosage recommendations for this species could be made. Six llamas received immediate (10 mg/kg, IV, IM, and SC) and sustained (8 mg/kg IM, SC) release cephalexin. Pharmacokinetic parameters were calculated by noncompartmental approach. Immediate release SC administration produced a significantly longer elimination half-life as compared with the IV and IM administration (1.3±0.2versus0.6±0.1and0.6±0.1 h, resp.) and higher mean absorption time as compared with the IM administration (1.7±0.5versus0.6±0.4 h). Absolute bioavailability was in the range of 72–89% for both formulations and routes of administration. Cephalexin MIC90values against staphylococci andE. coliwere 1.0 and 8.0 μg/mL, respectively. Our results show that the immediate release formulation (10 mg/kg) would be effective for treating staphylococcal infections administered every 8 h (IM) or 12 h (SC), whereas the sustained release formulation (8 mg/kg) would require the IM or SC administration every 12 or 24 h, respectively.
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Anderson, Lars W. J., Nathan Dechoretz, David Bayer, and Gary L. Darmstadt. "Effect of Three Formulations on Uptake and Efficacy of Copper inHydrilla verticillata." Weed Science 35, no. 2 (March 1987): 263–69. http://dx.doi.org/10.1017/s0043174500079170.
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Copper content and growth of excised hydrilla [DioeciousHydrilla verticillata(L.f.) Royle # HYLLI] apical shoot segments were determined following exposure to copper sulfate (CuSO4), copper-triethanolamine (Cu-TEA), and copper-ethylenediamine (Cu-EDA). For all copper formulations, inhibition of growth was related to the amount of copper associated with the excised shoots. At equal copper exposure, the Cu-EDA formulation produced the greatest inhibition of growth and generally the highest copper levels in the plants. The Cu-EDA formulation inhibited dry weight gain by more than 80% 3 weeks after a 2-h exposure to 2.0 or 4.0 ppmw copper. Under similar conditions, CuSO4or Cu-TEA produced 60% inhibition. The presence or absence of light during a 2-h exposure had no effect on the efficacy of uptake of copper from any of the formulations. Formulation-dependent differences in the mechanism of copper uptake is suggested because rinsing of exposed shoots with dilute acid (0.01N HNO3) removed copper from shoots treated with CuSO4or Cu-TEA but not from those treated with Cu-EDA.
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Brandon, Roslyn A., J. A. G. Emmett, M. J. Eadie, A. C. W. Curran, and I. H. Bunce. "Peripheral Venous Plasma Aspirin Concentrations and Platelet Aggregation Inhibition Produced by Enteric-Coated Aspirin Formulations." Thrombosis and Haemostasis 55, no. 02 (1986): 222–27. http://dx.doi.org/10.1055/s-0038-1661526.
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SummaryIn a random cross-over design, six healthy consenting adult volunteers were given on separate occasions single doses of 300-650 mg of 3 different formulations of enteric-coated aspirin. Over various intervals for 48-54 h following dosage, plasma aspirin and salicylate concentrations were measured together with percentage inhibition of platelet aggregation activated by threshold concentrations of sodium arachidonate alone and combined with ADP and collagen. In all subjects each formulation delivered measurable quantities of aspirin to the peripheral circulation, the unchanged drug being detected at various times up to and including 28 h after dosage. Moreover, low aspirin concentrations were found to co-exist with unimpaired platelet aggregation. All 3 formulations yielded statistically significant (P <0.01) inhibition of platelet aggregation activated both by arachidonate and by the combination of aggregants when tested 24-29 and 48-54 h after dosage; there were no significant differences (P >0.05) between the 3 formulations in this regard. Two different patterns of delivery of unchanged aspirin to the systemic circulation from these enteric-coated formulations were apparent. These patterns may be important when considering which aspirin formulation might be most appropriate in chronic use for an antiplatelet effect. None of the enteric-coated formulations used in this study may be optimal in this regard.
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Kumar, K. Sathish, C. Kumaresan, and R. Anantharaj. "DEVELOPMENT AND COMPARISON OF ORALLY INHALABLE SUSTAINED RELEASE FORMULATIONS FOR THREE RESPIRATORY DRUGS FOR ASTHMA." JOURNAL OF ADVANCES IN CHEMISTRY 12, no. 25 (December 26, 2016): 5679–99. http://dx.doi.org/10.24297/jac.v12i25.4658.
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The present work was designed to develop and compare orally inhalable sustained release formulation for salbutamol sulphate (SS), ambroxol hydrochloride (AH) and montelukast sodium (MS).The emulsion solvent evaporation method was used to prepare microparticles with the polymers. The prepared polymer encapsulated microparticles were blended with carrier inhalable lactose and filled in size 3 hard empty gelatin capsule. Formulations T1-T9 were prepared with 1:1 ratio of PLGA (50:50), PLGA (75:25) and Eudragit RS100. The formulation T1 prepared with SS:PLGA (50:50) produces best result when compared with other formulations T2-T9. Formulation T1 gives in vitro release 91.23% at 12 h and having particle size of microparticles (D0.5 µm) 1.94±0.6 and respiratory fraction 34.9± 2.59 %.
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Chourasia, Ayushi, and Shikha Agrawal. "DEVELOPMENT AND EVALUATION OF CIPROFLOXACIN HYDROCHLORIDE LOADED OCULAR INSERT BY USING “PLANTAGO OVATA” AS NATURAL POLYMER." International Journal of Current Pharmaceutical Research 10, no. 4 (July 16, 2018): 79. http://dx.doi.org/10.22159/ijcpr.2018v10i4.28474.
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Objective: The present work focus in the direction of “Development and evaluation of Ciprofloxacin Hydrochloride loaded ocular insert by using “plantago ovata” as natural polymer”. The current work was carried out to evaluate the control release profile of ocular insert. Natural polymer in ocular insert was used for studying the long acting property. Natural polymer is also used to enhance the bioavailability of drug and reduce toxicity. It is also used to increase the duration of action of drug for prolongs action and gives better in vitro performance as compare than to the conventional ocular formulation.Methods: Solvent casting method was used in the formulation of Ciprofloxacin Hydrochloride loaded ocular inserts. Different ocular insert formulations of varying polymer concentration were prepared. Ocular insert formulation H-1 to H-3 was prepared by using different concentration of HPMC and formulation P-1 to P-4 was prepared by using different concentration of Plantago Ovata.Results: The ocular inserts formulation was within the acceptable limits. All the pre formulation parameters of polymers such as derived properties, compressibility index, Hausner’s ratio, viscosity, melting point, swelling ratio, loss on drying, PH of mucilage solution and pre formulation of active pharmaceutical ingredient such as estimation of drug by using UV spectroscopy, determination of melting point, solubility, partition coefficient and FTIR for compatibility study of drug and excipient were evaluation. FTIR analysis also confirmed no drug-excipient interaction.Conclusion: Prepared inserts in the present study were semitransparent. The mixing of the drug in to the polymer is uniform, due to this; the drug content of all formulation is good. Formulation P4 was selected because it showed better release profile, drug content and other physicochemical properties than other formulated batch when compare. All the prepared inserts showed in vitro drug release for the period of 4 h as compare to the marketed formulation. An in vitro drug release study revealed that ocular formulation gives a prolong action. The formulation was found to be long acting.
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Chen, Jie, and J. Ron Patton. "Standard H ∞ Filtering Formulation of Robust Fault Detection." IFAC Proceedings Volumes 33, no. 11 (June 2000): 261–66. http://dx.doi.org/10.1016/s1474-6670(17)37370-6.
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Chen, J., and R. J. Patton. "H ∞ Formulation and Solution for Robust Fault Diagnosis." IFAC Proceedings Volumes 32, no. 2 (July 1999): 7808–13. http://dx.doi.org/10.1016/s1474-6670(17)57332-2.
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Hwang, Stephen, and Henric Rhedin. "The BRST formulation of G/H WZNW models." Nuclear Physics B 406, no. 1-2 (September 1993): 165–84. http://dx.doi.org/10.1016/0550-3213(93)90165-l.
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Bonet, Javier, and Miguel X. Rodríguez-Paz. "Hamiltonian formulation of the variable-h SPH equations." Journal of Computational Physics 209, no. 2 (November 2005): 541–58. http://dx.doi.org/10.1016/j.jcp.2005.03.030.
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Shilakari Asthana, Gyati, Parveen Kumar Sharma, and Abhay Asthana. "In VitroandIn VivoEvaluation of Niosomal Formulation for Controlled Delivery of Clarithromycin." Scientifica 2016 (2016): 1–10. http://dx.doi.org/10.1155/2016/6492953.
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The present study was focused on formulating and evaluating clarithromycin (CLR) containing niosomal formulation forin vitroandin vivopharmacokinetic behavior. Niosomal formulations (empty and drug loaded) were prepared by using different ratio of surfactant (various Span grades 20, 40, 60, and 80) and cholesterol by thin film hydration method and were evaluated forin vitrocharacteristics, stability studies, andin vivostudy. Dicetyl phosphate (DCP) was added to the niosomal formulation. Various pharmacokinetic parameters were determined from plasma of male SD rats. Span 60 containing niosomal formulation NC2(cholesterol to surfactant ratio 1 : 1) displayed highest entrapment efficiency with desired particle size of 4.67 μm. TEM analyses showed that niosomal formulation was spherical in shape. Niosomes containing Span 60 displayed higher percentage of drug release after 24 h as compared to other formulations. NC2formulation was found to be stable at the end of the study on storage condition. Various pharmacokinetic parameters, namely, AUC, AUMC, and MRT of niosomal formulation, were found to be 1.5-fold, 4-fold, and 3-fold plain drug, respectively. The present study suggested that niosomal formulations provide sustained and prolonged delivery of drug with enhance bioavailability.
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Hernawan, Hernawan, Septi Nurhayati, Khoirun Nisa, A. W. Indrianingsih, Cici Darsih, and Muhammad Kismurtono. "FORMULATION AND IN VITRO STUDY OF PROPRANOLOL HYDROCHLORIDE CONTROLLED RELEASE FROM CARBOXYMETHYL CHITOSAN-BASED MATRIX TABLETS." Indonesian Journal of Chemistry 13, no. 3 (December 18, 2013): 242–47. http://dx.doi.org/10.22146/ijc.21283.
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Formulation and in vitro study of propranolol hydrochloride controlled release from carboxymethyl chitosan-based matrix tablets have been conducted. Formulations with various concentrations of carboxymethyl chitosan 2% (F1), 4% (F2), 6% (F3) were done by wet granulation method. Compatibility test was conducted by XRD and FTIR spectroscopy to determine interaction between propranolol hydrochloride and polymer excipients. Dissolution profiles was obtained through in vitro tests release using simulated gastric fluid (without enzymes, pH 1.2) for the first 2 h and followed by simulated intestinal fluid (phosphate buffer solution without enzyme, pH 7.2) for 2 h remaining. The dissolution profile of each formulation was fitted with five kinetics modeling of drug release (zero order, first order, Higuchi, Peppas-Korsmeyer, and Hixson-Crowell). The compatibility test results showed that formulation caused physical interactions between propranolol hydrochloride and polymer excipient but doesn't make crystallinity nature of propranolol hydrochloride disturbed even after formulation. Dissolution profiles of each formulation showed that controlled release of propranolol hydrochloride from the tablet followed Peppas-Korsmeyer model. It is concluded that carboxymethyl chitosan in appropriate proportions is suitable for formulating propranolol hydrochloride controlled release tablets which exhibit Peppas-Korsmeyer release kinetics.
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Gulledge, Brett M., Kristen M. Messenger, Karen K. Cornell, Heather Lindell, and Chad W. Schmiedt. "Pharmacokinetic comparison of two buprenorphine formulations after buccal administration in healthy male cats." Journal of Feline Medicine and Surgery 20, no. 4 (June 1, 2017): 312–18. http://dx.doi.org/10.1177/1098612x17710843.
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Objectives The objective of this study was to compare the pharmacokinetics of compounded and commercially available aqueous formulations of buprenorphine after a single buccal dose to healthy cats and to evaluate the concentrations of a compounded buprenorphine solution over 21 days when stored at room temperature (RT; 22–24°C) with exposure to light or when refrigerated at 4°C while protected from light. Methods Six young healthy male cats were administered single buccal doses of compounded and commercially available formulations of buprenorphine (0.03 mg/kg) using a randomized, blinded, two-period crossover design. Blood samples were obtained over a 24 h period and plasma buprenorphine concentrations were determined using ultra-high-pressure liquid chromatography with mass spectrometry detection. Three batches of the compounded formulation were stored at RT or 4°C and aliquots were evaluated over 21 days for buprenorphine concentration using high-performance liquid chromatography with fluorescence detection. Results Plasma concentrations of buprenorphine were above the limit of quantification up to 6 h in some cats and up to 3 h in all cats. The area under the curve was significantly less for the compounded formulation ( P = 0.004). A significant difference was not detected between formulations for time to maximum concentration ( P = 0.11), maximum concentration ( P = 0.06), half-life ( P = 0.88) and mean residence time ( P = 0.57). Buprenorphine concentration in the compounded formulation was not affected by storage condition or time and remained between 90% and 110% of the target concentration at all time points. Conclusions and relevance A buprenorphine solution prepared from sublingual tablets is absorbed after buccal administration in healthy cats. The extent of absorption is significantly less than that of the commercially available formulation. The compounded solution maintains an acceptable buprenorphine concentration for at least 21 days when stored at RT or refrigerated.