Abstract

FORMULATION DEVELOPMENT AND INVITRO EVALUATION OF AZATHIOPRINE TABLETS FOR COLON DRUG DELIVERY SYSTEM”

Eswar Kumar A.*, Sharada Nalla and Bhogini Thirupathaiah

ABSTRACT

Azathioprine is an immunosuppressive antimetabolite pro-drug. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound. Azathioprine is converted into 6-mercaptopurine in the body where it blocks purine metabolism and DNA synthesis. In this present research work sustained release matrix formulation of Azathioprine targeted to colon by using various polymers developed. Colon targeted tablets were prepared in two steps. Initially core tablets were prepared and then the tablets were coated by using different pH dependent polymers. Ethyl cellulose, Eudragit L100 and S100 were used as enteric coating polymers. The precompression blend of all formulations was subjected to various flow property tests and all the formulations were passed the tests. The tablets were coated by using polymers and the coated tablets were subjected to various evaluation techniques. The tablets were passed all the tests. Among all the formulations F3 formulation was found to be optimized as it was retarded the drug release up to 12 hours and showed maximum of 97.66% drug release. It followed zero order kinetics mechanism.

Keywords: azathioprine, Colon targeted, Sodium starch glycollate, direct compression.