European Journal of Biomedical and Pharmaceutical Sciences

PREPARATION AND EVALUATION OF SUSTAINED RELEASE FORMULATION OF BOSENTAN

Alireza Gholami* and Dr. Rama Bukka

ABSTRACT

The main objective of the present study was to prepare sustained release capsules of Bosentan which constitute an innovative dosage form that overcome the problems of large frequency of dosing. In the view of enhancing bioavailability, an attempt has been made to prepare sustained release capsules and to know the effect of different types of polymers. Polyelectrolyte complex was prepared by using cationic polymer like PVP and anionic polymer like Carbopol. Different PVP grades such as PVP k30 and k90 were used. The capsules were subjected to pre compression and evaluation parameters. The selected formulation was subjected to stability studies as per ICH guidelines. The effect of polymers loading in In- Vitro drug release and the mechanism of release was studied by different mathematical models. This can be adjusted by maintaining the concentration of the suitable polymers. Capsules showed no appreciable changes with respect to appearance, drug content and dissolution profiles on storage for 45 days at accelerated stability conditions. It was found that the Bosentan drug release depends on combination of two polymers (Carbopol and PVP k90 or k30) which modifies the release profile by controlling water penetration and leads to drug release. The objective was to achieve drug release at 24 hours. It was concluded that sustained release capsules of Bosentan can be successfully formulated by polyelectrolyte complex method with improved patient compliance. And also it can be concluded that among all the formulations Carbopol and PVP k90 or k30 combinations was considered as the optimised formulations in the present research work.

Keywords: Bosentan, Hypertension, Sustained release, PVP, Carbopol, Polyelectrolyte Complex.