DEVELOPMENT AND CHARACTERIZATION OF PIOGLITAZONE- β CYCLODEXTRIN INCLUSION COMPLEX CONTAINING CONTROLLED RELEASE TABLETS.

摘要

The objective of the present investigation was to developed Pioglitazone- β cyclodextrin inclusion complex containing controlled release tablets for enhancement of solubility and controlled delivery of pioglitazone. For this Pioglitazone, β- cyclodextrin inclusion complex (1:1, 1:2, 1:3, 1:5) ratios were prepared by Kneading method and evaluate for their phase solubility study, derived properties, drug content and in vitro drug release study. The 1:1 inclusion complex was optimized in relation to % cumulative drug released after 200 minutes employed for controlled release matrix tablets. Matrix tablets were prepared by direct compression technology 8-station tablet punch machine (Rimek Minipress-I, India) using various polymers such as HPMC K4M, Ethyl cellulose ect. Total of 9 formulations were prepared by varying concentrations of polymer blends. Formulation F9 containing 116 mg (HPMC K4M) and 80 mg Ethyl cellulose was found to be released the drug in controlled mannior upto 10 and 11 hrs respectively might be due to a more rigid complex formed by hydrophilic polymers when used in much concentrations along with the presence of EC which helped in retaining the drug in the matrix and did not allowed rapid diffusion of soluble drug from the matrix. The in vitro release pattern of the optimized formulation was also analysed by fitting the dissolution data into various kinetic models. It was seen that R2 value was higher when fitted to zero order equation followed by Higuchi model as compared to first order equation indicated a zero order release from the optimized matrix tablets. Furthermore 'n' value was greater than 1 which indicates the predominant matrix swelling and erosion