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Abstract

FORMULATION DEVELOPMENT, OPTIMIZATION AND CHARACTERIZATION OF GASTRORETENTIVE HOLLOW MICROSPHERES OF CAPTOPRIL

*Kapoor D., Vyas RB, Lad C, Patel M, Sharma S.

ABSTRACT

The objective of the present study was to develop floating microballoons of captopril in order to achieve an extended retention in the upper GIT which may enhance the absorption and improve the bioavailability. Hollow microspheres (Microballoons) floatable in USP XXI (SGFpH1.2) solution were developed as a dosage form characterized by excellent buoyant properties in the stomach. Microballons were prepared by the novel emulsion solvent diffusion method utilizing enteric acrylic polymers codissolved with drug in a mixture of dichloromethane and ethanol. The drug polymer compatibility was determined by FTIR studies. For optimization of prepared microspheres effects of varying polymer ratio concentration, drug concentration, surfactant concentration, and stirring speed on particle size and drug loading were studied. Optimized formulation was then characterized for particle size, scanning electron microscopy (SEM), drug entrapment and buoyancy percentage. The results obtained were found in desired ranges where the drug entrapment efficiency of microspheres was found to be 92.83.1%, size of microspheres found 175.62.7 μm. The shape of the microspheres was found to be spherical by SEM. The microspheres on floatation along with surfactant, floated continuously for more than 9 hrs. in SGF (pH-1.2). The percentage cumulative amount of drug release was found to 91.23.5% in SGF (PH 1.2) after 24 hrs. The results evidently advocate that prepared hollow microsphere formulation of captopril may prove to be a potential candidate for prolonged drug release in stomach, thereby improving the bioavailability and patient compliance.

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