Formulation and in vitro evaluation of bosentan osmatic controlled release tablets

Abstract

In the present work, an industrially important project entitled “Formulation and In vitro Evaluation of Bosentan Osmotic
Controlled Release Tablets” was undertaken. The study was undertaken with an aim to formulate Bosentan as osmotic
controlled release tablets. During this phase of investigation various factors that likely to affect the performance of the
osmotic controlled release was studied. The release kinetics, dissolution rate, process variables such as hardness, weight
variation are some of the factors found critical during the development based on the experimental findings. Preformulation
studies were done initially and results directed the further course of formulation. With the literature review data,
Preformulation and prototype formulation trails were started. Direct compression method was used for formulation.
Granules were evaluated for tests such as bulk density, Tapped density, Compressibility Index and Hausner ratio before
being punched as tablets. Tablets were tested for weight variation, thickness and friability, in-vitro dissolution tests were
performed and percentage drug release was calculated. Dissolution profile of formulation – F7 was optimized based on
evaluation parameters. In the dissolution modeling all the developed formulations followed Korsemeyer-peppas drug
release. The optimized formulation F7 followed Korsemeyer-peppas drug release kinetics model i.e super case 2 transports
and non-Fickian model. In the present study, polymethacrylates were found to play a great role in controlling release of
drug Bosentan from the osmotic system. Accordingly, it can be concluded that the formulation is robust in the
performance and it is less likely to be affected by various factors studied.