Acceptance of Oclacitinib Maleate (Apoquel®) Chewable Tablets In Client-Owned Dogs With Allergic And Atopic Dermatitis.

Background: The oral acceptance of oclacitinib maleate (Apoquel®) chewable tablets administered twice daily for 7 days at the labeled dose range of 0.4-0.6 mg/kg was evaluated in 121 dogs treated at ten general practice veterinary clinics in the United States. Results: Dogs that were enrolled in the study ranged were client-owned, from 1 to 14 years of age, weighed 3.7 to 60.7 kg, and required twice daily treatment with oclacitinib for allergic or atopic dermatitis. One hundred and twenty-one (121) dogs with 1,673 total dose administrations successfully completed the study and were included in the data summary. Out of a total number of 1673 administrations, 1533 (91.6%) were accepted voluntarily within 5 minutes, 134 (8%) were consumed with assistance (with food treats or by pilling) outside of the 5 minutes offering time and 6 (0.4%) doses were not consumed. The per dose percent acceptance rate for the 14 offered doses showed minimal variation ranging from 89.9% to 93.3%. Conclusions: Client-owned dogs from the general veterinary patient population that required treatment with oclacitinib found the Chewable tablets to be very palatable and no aversion occurred with repeated dosing. Oclacitinib chewable tablets were well tolerated and is a palatable alternative to the film-coated tablet.

FORMULATION AND IN VITRO–IN VIVO PHARMACOKINETIC EVALUATION OF CARDIOVASCULAR DRUG-LOADED PULSATILE DRUG DELIVERY SYSTEMS

Objective: This study is to formulate Nebivolol into a Pulsatile liquid, solid composite compression coated tablet, which will delay the release of the drug in early morning hypertension conditions. Methods: The liquid, solid composite tablet was formulated and compressed with the ethylcellulose coating polymer. The percent in vitro drug release of the liquid solid composite compressed tablet was tested. Based on disintegration time and wetting time, the LCS2, LCS3, LSC6, LCS7 and LCS12 formulations were found to be the optimized solid-liquid compacts fast-dissolving core tablet formulations, which may be excellent candidates for further coating with polymer to transfer into press coated pulsatile tablet formulations. Coating the core tablet with varying ethyl cellulose concentrations resulted in five different formulations of the pulsatile press-coated tablet (CT1, CT2, CT3, CT4, CT5). In vitro drug release, in vitro release, kinetic studies, in vivo pharmacokinetic and stability tests were all performed for the prepared pulsatile press coated tablet. Results: CT3 tablets are coated with ethyl cellulose polymer, which shows maximum controlled drug release from the core tablet i.e. 96.34±1.2% at 8th h. It shows there was an efficient delay in drug release form core tablet i.e. up to 3 h, followed by the maximum amount of drug release of 96.34±2.4 at 8h. Which shows the core drug will be more efficiently protected from the gastric acid environment 1.2 pH, duodenal environment 4.0 pH and release drug only in the small intestine. Conclusion: According to the findings, CT3 Pulsatile press-coated tablet increased the bioavailability of Nebivolol by 3.11 percent.

A Novel Pulsatile Release Film Coated Tablet of Zaltoprofen Loaded SNEDDS

The aim of the present study was to formulate pulsatile release film coated tablet of zaltoprofen for the treatment of rheumatoid arthritis. Initially solubility of zaltoprofen was enhanced by formulating self emulsifying fast disintegrating tablet of zaltoprofen. Core fast disintegrating tablet of zaltoprofen was coated with ethyl cellulose and eudragit L100 in various proportions as coating polymer. Ethanol was used as coating solvent and dibutyl phthalate as plasticizer. Film coated tablet with different coating levels were formulated and were evaluated for parameters like lag time, rupture time, in vitro dissolution etc. Amongst the nine different formulations P-4 formulation containing 3:1 ratio of ethyl cellulose and eudragit L100 with 5% coating level gives desired lag time with best drug dissolution profile. Formulated film coated tablet of zaltoprofen can be useful for chronotherapeutic treatment of rheumatoid arthritis.

COMPARATIVE STUDY OF SEVEN BRANDS OF LEVOFLOXACIN 500 MG FILM-COATED TABLET MARKETED IN YEMEN

Objective: The objective of the current study was to evaluate the quality control parameters of seven brands of levofloxacin 500 mg film-coated tablet available in the Yemeni market. Methods: Physicochemical parameters assay was performed for seven brands of levofloxacin 500 mg film-coated tablet. Each brand was subjected to official and unofficial in vitro quality control tests, including weight variation, thickness, hardness, friability, disintegration, dissolution, and content uniformity assay by High-Performance Liquid Chromatography (HPLC). Results: Out of seven, six brands of levofloxacin 500 mg film-coated tablet passed official specified assay tests according to the United States Pharmacopeia (USP) specifications. They showed a similar profile of thickness ranged between±0.01 and 0.10%, friability ranged between 0.01% and 0.34%, disintegration time ranged between 3.00 and 15.00 min, dissolution percentage ranged between 90.650 and 103.05 and content uniformity ranged between 93.62 and 107.12%. Regarding weight variation and hardness, six brands passed the weight variation test and only three brands showed optimum range (10-20 kg) of hardness test. Only one brand failed to pass the weight variation test, and four brands failed to pass the optimum range (10-20 kg) of hardness. Conclusion: There are no remarkable differences between the seven brands regarding in vitro quality control tests of content uniformity, thickness, friability, disintegration, and dissolution. Even though four brands were above the optimum range of hardiness, they showed complete disintegration and dissolution within the acceptable limit. Regular assessment of marketed drugs is required to ensure bioequivalent to their innovators.

Quality by Design Applied Development of Immediate-Release Rabeprazole Sodium Dry-Coated Tablet

The aim of this study was to develop immediate-release oral rabeprazole sodium tablets with rapid efficacy and gastric stability for the treatment of gastroesophageal reflux disease. Rabeprazole sodium is a commonly prescribed proton pump inhibitor; however, it is extremely unstable and degrades in acidic environments. Hence, it has been manufactured and supplied only in enteric-coated tablet form, while immediate-release (IR) formulations for this drug are very limited. In this study, we applied the quality by design (QbD) approach to formulate and optimize an IR dry-coated tablet containing rabeprazole sodium as an inner core with an outer sodium bicarbonate layer to stabilize the active pharmaceutical ingredient at gastric pH. We also investigated the stability of the pharmaceutical dosage form and its pharmacokinetic profile. The results show that the developed tablets are stable for approximately 12 months and have a high dissolution rate, greater than or equal to 90% at 30 min. Further, in vivo beagle pharmacokinetics confirmed that the newly developed IR tablet had an AUCt which is bioequivalent to the existing delayed-release rabeprazole tablet; however, its Tmax was 0.5 h, which is up to seven times faster than that of the existing tablet. Moreover, the IR tablet was found to immediately absorb in the stomach. Hence, the development of IR tablets can be used as a platform to overcome the technical and commercial limitations currently associated with various proton pump inhibitors used to treat patients with gastroesophageal reflux disease that require immediate therapeutic relief.