Formulation and In-vitro Evaluation Of Sustained Release Tablets Of Bosentan

Bosentan is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer®. Bosentan is used to treat pulmonary hypertension by blocking the action of endothelin molecules that would otherwise promote narrowing of the blood vessels and lead to high blood pressure. The aim of the present study was to develop sustained release formulation of Bosentan to maintain constant therapeutic levels of the drug for over 12 hrs. Various synthetic polymers were employed as polymers. Bosentan dose was fixed as 62.5 mg. Total weight of the tablet was considered as 200 mg. the tablets are prepared by employing direct compression method using 8mm punch. And the Polymers were used in the concentration of 31.5, 41.25, 62.5 mg concentration. All the formulations were passed various physicochemical evaluation parameters and they were found to be within limits. And the drug and excipient compatibility studies showed that there is no interaction between the drug and polymers employed in the formulation. Whereas from the dissolution studies it was evident that the formulation F3, F16 showed better and desired drug release pattern i.e., 98.15±0.06, 96.64±0.02 % respectively in 12 hours. the project work is successful in developing sustained release formulations of Bosentan.

Keywords: Bosentan, anti hypertension, sustained release, etc.