Research Article DESIGN OF BUCCAL DRUG DELIVERY SYSTEM FOR A POORLY SOLUBLE DRUG (original) (raw)

2009

Abstract

Carvedilol is an antihypertensive drug used in the treatment of congestive heart failure, cardiac arrhythmias and angina pectoris. It exhibits poor bioavailability of 25-30% which is attributed to its poor solubility and high first pass metabolism. The present work was aimed at overcoming these two limitations. Drug-Methyl-β-cyclodextrin complex was prepared by kneading method and characterized by Fourier Transformation Infrared spectroscopy, Differential Scanning Calorimetry and powder X-Ray Diffractometry studies. Dissolution rate of complex was compared with plain drug and physical mixture. The complex was incorporated into buccal tablet. The buccal tablets were evaluated for drug release, mucoadhesive strength and ex-vivo permeability. Characterization of binary system revealed the formation of inclusion complex of drug with Methyl-β-cyclodextrin. The complex showed complete release as compared to 32.8% and 42.7% from plain drug and physical mixture respectively in 60min. Tablets containing complex showed complete release at the end of 180min compared to 40.23% from tablets containing plain drug. The buccal tablets containing complex had good mucoadhesive strength. The amount of drug permeated from these tablets across the porcine buccal mucosa at the end of 5h was 6.2mg as compared to 2.51mg from tablets containing plain drug. Thus it can be concluded that buccal tablet containing complexed CAR would have improvement in bioavailability.

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