Abstract

STUDY OF COMPOSITIONS FOR PROLONGED DRUG RELEASE GRANULES

Nguyen Pham Quynh Anh, Doan Thi Thanh Vinh, Nguyen Hoang Khue Tu*

ABSTRACT

Prolonged release is one of the drug delivery systems that gains concern in drug development due to its ability to increase bioavailability and to prolong activity of a drug. The prolonged release matrices are mainly made of matrix forming polymers combined with appropriate excipients and bound together by the binder. In this project, we optimized the excipients that could facilitate the prolonged release. Particularly, we studied the release profile of gallic acid from several combinations of components including carboxymethyl cellulose (CMC), hydroxyethylcellulose (HEC), polyvinylpyrrolidone K30 (PVP K30) and lactose in order to obtain the longest prolonged release. After screening for the ratio of CMC and HEC in the polymer mixture, optimizing the percentage of polymers and PVP K30, the longest release was observed from the formulation containing 50% of polymer content (including 60% of CMC and 40% of HEC), 10% of PVP, and 40% of lactose in the total weight of the granules. The time for 95% of gallic acid to be released in that formulation was around 10 hours while other formulations showed release duration varying from 3 hours to 8 hours. This is the first report on drug release on prolonged release granules containing gallic acid.

Keywords: carboxymethyl cellulose, hydroxyethylcellulose, polymers, PVP K30, prolonged release, optimization.