Abstract

STUDIES ON ENTERIC COATED ATORVASTATIN CALCIUM LOADED MUCOADHESIVE SUSTAIN RELEASE MICROSPHERES

Dr. Shubhangi Aher* and Sandip Pavane

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Abstract

Atorvastatin calcium (ATC) is a water insoluble drug and is known to have antihyperlipidemic activity, which has low bioavailability and poor solubility. The present study aimed at developing and evaluating sustain release ATC-loaded mucoadhesive microsphere coated with poly methacrylate polymer. Atorvastatin calcium undergoes conversion to its lactate form under gastric acidic environment. To avoid release at gastric pH polymethacrylate (Eudragit- L100) coated mucoadhesive microsphere were developed. And also to enhance absorption at the duodenum and jejunum part of the small intestine. Ionotropic gelation technique was utilized used to formulate microspheres. Formulated microsphere were evaluated for percentage yield, drug content, drug entrapment efficiency, swelling index, invitro drug release. Beside this FTIR and DSC carried out for compatibility. Optimized formulation had percentage yield 98.14%, drug content > 94% w/w, entrapment efficiency > 94 %. Drug release at pH 1.2 which was observed to be successfully controlled in polymethacrylate coated microspheres. In vitro release data was fitted in mathematical model to confirm the release pattern of formulation. Ex-vivo permeation study was carried out by non- everted gut technique. Coated formulation F9B showed 49.67 ± 0.06 %. Microsphere of different size and drug content could be obtained by varying the formulation variables like polymer concentration. The multi-unit mucoadhesive microsphere of Atorvastatin calcium delivery system is accepted to provide clinician with new choice of an economical, safe and more bio- available formulation in the management of moderate to severe lipidemia. Therefore it may be concluded that enteric coated mucoadhesive microspheres are suitable delivery system for Atorvastatin calcium (ATC).

Keywords: (Atorvastatin Calcium, Anti-hypertensive, Poly-methacrylate, Non- everted).