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Solubility enhancement and formulation of buccal patches of Ramipril cyclodextrin complex
Published in
2013
Volume: 6
   
Issue: 2
Pages: 83 - 90
Abstract
Ramipril is an ACE inhibitor used for management of hypertension and myocardial infarction. It exhibits poor bioavailability of 28% which is due to its poor solubility and high first pass metabolism. The present work was aimed at overcoming these two limitations. Drug-$\beta$-cyclodextrin and Hydroxy propyl $\beta$-cyclodextrin complexes were prepared and characterized by Fourier Transformation Infrared spectroscopy, Differential Scanning Calorimetry and powder X-Ray Diffractometry studies. In vitro studies showed that the solubility and dissolution rate of Ramipril were significantly improved by complexation with $\beta$-cyclodextrin and Hydroxy propyl $\beta$-cyclodextrin with respect to drug alone. The kneaded complex showed higher dissolution rate than other complex and it was incorporated into buccal Patches. The patches were prepared by solvent casting method using hydroxyl propyl methyl cellulose (HPMC K15) and Poloxomer WSR205NF. The patches were found to be smooth in appearance, uniform in thickness, weight uniformity, drug content, swelling index, folding endurance, surface pH and in vitro diffusion study using Keshery chien diffusion cell. The Patch of 0.5% HPMC K15 exhibit in vitro release of 81.16% through cellophane membrane and 75.72% release through egg membrane and the Patch of 0.5% Poloxomer WSR205 NF exhibit in vitro release of 77.24% through cellophane membrane and 71.08% release through egg membrane in 8 hrs showing good mucoadhesive strength and mucoadhesive time. The Optimized patch was subjected to ex vivo studies through goat buccal mucosa showed 63.49% release in 8 hrs.
About the journal
JournalAsian Journal of Pharmaceutical and Clinical Research
ISSN09742441
Open AccessNo