Gastro-retentive floating microspheres of carvedilol: formulation, characterisation and in-vitro evaluation

Yelugam, Mahathi and Koteshwara, KB and Reddy, Sreenivasa M (2013) Gastro-retentive floating microspheres of carvedilol: formulation, characterisation and in-vitro evaluation. International Journal of Pharmacy and Pharmaceutical Sciences, 5 (3). pp. 686-690. ISSN 0975-1491

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Abstract

The objective of the present study was to formulate and evaluate floating microspheres of carvedilol. Carvedilol has a terminal half-life of 7-10 hr, but most of the drug is eliminated with a half-life of about 2 hr. Besides being a beneficial drug compared to other drugs of the same class, it has narrow absorption window in upper part of the gastro intestinal tract, hence a floating drug delivery system is preferred, such that the formulation will be available for a longer duration than usual for absorption. Floating microspheres were prepared by emulsion solvent diffusion method using ethanol and dichloromethane as solvents. Ethyl cellulose andHydroxy propyl methyl cellulose K 4 M(HPMC K 4 M) were used to prolong the release of the drug from microspheres. The prepared microspheres were subjected to various evaluatory studies. All the microspheres were found to have a size in the range of 20-40 μ and were nearly spherical in shape. Optimised batch F11 exhibited good buoyancy (73 ± 1.00 %) and sustained release (45.41 ± 0.13 % Cumulative drug dissolved) ( % CDD) compared to other formulations. It was subjected to dissolution studies using USP type 1 apparatus and Rosette rice apparatus. Drug release data was compared with the release data obtained from marketed tablet Cardivas (Controlled Release) CR. The release kinetics obtained using Rosette Rice apparatus were good compared to USP type I apparatus. The release of the drug from microspheres and Cardivas CR followed non-fickiananamolous diffusion.

Item Type: Article
Uncontrolled Keywords: Buoyancy; Emulsion solvent diffusion method; Hypertension; Optimised batch; Rosette rice apparatus.
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Manipal
Date Deposited: 14 Jan 2014 04:14
Last Modified: 14 Jan 2014 04:14
URI: http://eprints.manipal.edu/id/eprint/138345

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