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Design developmetn and optimization of a sustained release tablet of bosentan monohydrate for pulmonary arterial hypertension

By: Dighe, P. P.
Contributor(s): Tank, H. M.
Publisher: Mumbai Indian Drug Manufacturers Association 2019Edition: Vol. 56(03), March.Description: 61-67p.Subject(s): DRUG STORE MANAGEMENTOnline resources: Click here In: Indian drugsSummary: Pulmonary arterial hypertension (PAH) means high blood pressure in the lungs caused by obstruction in the small arteries of the lungs.The current study involves the fabrication of oral matrix sustained release tablet of bosentan monohydrate, a dual endothelin receptor antagonist, the optimisation of its in vitro release and characterisation. Methocel K4M PremiumDC2, a directly compressible HPMC grade, has been used as the sustained release polymer. Pregelatinised starch is used as a diluent and release modifier and sodium lauryl sulphate as a solubiliser. The influence of the above variables on drug release is measured using a 23 factorial design using design expert software. Surface response plots show significant interaction among the formulation variables, thus aiding in optimization of bilayer tablet.
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Pulmonary arterial hypertension (PAH) means high blood pressure in the lungs caused by obstruction in the small arteries of the lungs.The current study involves the fabrication of oral matrix sustained release tablet of bosentan monohydrate, a dual endothelin receptor antagonist, the optimisation of its in vitro release and characterisation. Methocel K4M PremiumDC2, a directly compressible HPMC grade, has been used as the sustained release polymer. Pregelatinised starch is used as a diluent and release modifier and sodium lauryl sulphate as a solubiliser. The influence of the above variables on drug release is measured using a 23 factorial design using design expert software. Surface response plots show significant interaction among the formulation variables, thus aiding in optimization of bilayer tablet.

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