Abstract

FORMULATION AND IN-VITRO EVALUATION OF BOSENTAN MONOHYDRATE GASTRORETENTIVE TABLETS FOR TREATMENT OF PULMONARY ARTERY HYPERTENSION

*Dr. Putta Rajesh Kumar, Shazina Maher, Syed Abdul Rehman, Dr. Avanapu Srinivasa Rao

Abstract

Aim: Bosentan monohydrate is an endothelin receptor antagonist which is used for the treatment of pulmonary artery hypertension. Bosentan monohydrate gastro retentive tablets were formulated in the present research by using various polymers, sodium bicarbonate as gas generating agent by wet granulation technique. Absorption maximum of Bosentan monohydrate was determined; analytical method was developed and calibration curve was constructed. Methods: The formulation blend was subjected to various flow properties, post compression and floating parameter studies. In vitro dissolution studies were conducted and release data was subjected to kinetic analysis. Results: Calibration curve showed high degree of linearity which represents the sensitivity and accuracy of developed UV analytical method. Pre compression parameters revealed that all results were within the ideal limits indicated the suitable flow properties of the powder blend. All Bosentan monohydrate gastro retentive tablets indicated uniform post compression parameters like weight uniformity, thickness, hardness, friability. Floating parameters indicated the floating ability and prolonged floating duration for gastro retentive delivery of Bosentan monohydrate. Drug content studies revealed all formulations showed uniform drug content. In vitro studies revealed that Bosentan monohydrate release is sustained and prolonged for 8 – 12 hr which ensures selective drug absorption from stomach and patience compliance. Conclusion: Formulation S6 was identified as optimised formulation with respect to its ideal pre and post compression properties, floating parameters and in vitro drug release sustained for prolonged period. Release kinetic analysis of optimized formulation revealed that the S6 formulation followed zero order kinetics of drug release.

Keywords: Floating matrix, Bosentan monohydrate, polymers, Effervescent agents, drug release studies.