DESIGN AND EVALUATION OF LIQUISOLID COMPACTS OF NEBIVOLOL HYDROCHLORIDE

Objective: The aim of this study was to investigate the potential of a liquisolid system to improve the dissolution rate and the bioavailability of nebivolol hydrochloride. Methods: Solubility of nebivolol was determined in different nonvolatile solvents to finalize the best nonvolatile vehicle having maximum solubility. The liquisolid compacts were prepared using Fujicalin as a carrier material, Aerosil 200 as a coating material, Polyethylene glycol 400 as a liquid vehicle, and Croscarmellose sodium as a super disintegrating agent. 23 full factorial design was used to optimize the formulation in which the drug concentration, PVP K 30, Excipient ratio (R), and nebivolol containing nonvolatile solvent liquid level were selected as independent variables by using design expert software. The eight liquisolid compact formulations were prepared. Nebivolol liquisolid compacts were evaluated for drug content, tablet hardness, Friability, disintegration, and dissolution. An in vivo study was carried out in male Wistar rats. Results: The solubility of nebivolol hydrochloride in polyethylene glycol 400 was found to be greater than the other nonvolatile solvents. The liquisolid system of nebivolol was formulated successfully using Fujicalin, Aerosil 200, and polyethylene glycol 400. In vitro evaluation parameters for the liquisolid compact were within the prescribed limits. It was found that optimized liquisolid tablet formulation showed higher dissolution than the marketed tablet, with 88.33±0.94 % drug release within 120 min and the drug release was more than 75 % in 30 min for nebivolol LS-3N, which is optimized. LS-3N liquisolid compacts follow the Peppas model and exhibited first-order release. Conclusion: The liquisolid compacts can be a promising alternative for the formulation of water-insoluble drug nebivolol hydrochloride with improved dissolution and bioavailability

BIOANALYTICAL RP-HPLC METHOD DEVELOPMENT AND VALIDATION OF CLOPIDOGREL BISULFATE IN WISTAR RAT PLASMA AND ITS APPLICATION TO PHARMACOKINETIC STUDY

Objective: A novel, simple, precise, accurate, sensitive, and reproducible HPLC method for determining clopidogrel bisulfate in Wistar rat plasma was developed and validated. Methods: The chromatographic separation was performed using Xterra C18 (250 x 4.6 mm, 5μ) column. Mobile phase composed of Acetonitrile ACN: 0.05M potassium dihydrogen orthophosphate buffer pH 4.2 and in the ratio of 75:25% v/v at a flow rate of 1.2 ml/min. Detection was carried out using a PDA detector at 220 nm. The bioanalytical clopidogrel method was validated as per ICH guidelines. Results: The selected chromatographic condition was found to efficiently separate clopidogrel bisulfate (RT-2.838 min). The calibration curve was linear over the concentration range 40-200 ng/ml in Wistar rat plasma with a correlation coefficient of 0.999, respectively. The precision study revealed that the cumulative percentage variation was within the acceptable limit, and accuracy research showed the value of mean percent recovery between 99.72-99.83 %. Conclusion: A simple, rapid, specific, accurate, and precise analytical method was developed and validated using Wistar rat plasma. The technique was strictly validated according to the ICH guidelines. Acquired results demonstrate that the proposed strategy can be effortlessly and advantageously applied for routine analysis of clopidogrel in the Wistar rat plasma

Formulation and Evaluation of Floating and Mucoadhesive Tablets Containing Rosiglitazone

In this present study, floating mucoadhesive tablets of Rosiglitazone were formulated to improve the gastric retention time and overall bioavailability. Different mucoadhesive polymers like HPMC K200 M, Na CMC, Carbopol 974P, Karaya gum, Chitosan and Xanthan gum were selected to formulate the tablets. Various formulations were prepared by using these polymers in different concentration. The pre-compression blend of Rosiglitazone mucoadhesive tablets were characterized with respect to angle of repose, bulk density, tapped density, carr’s index and hausner’s ratio and all the results indicated that the blend was having good flow property and hence better compression properties. The swelling studies were performed for the formulations and the results depicted that all the formulations have a good swelling index. The drug release studies depicted that the formulations release the drug in first order. So based on the results, formulation RF13 was found to be an optimized formulation. Keywords: Mucoadhesive tablets, Rosiglitazone, Bioadhesive polymers