Abstract
<p><strong>Objective: </strong>The aim of the present study was to carry out characterization and intrinsic dissolution rate study of microwave assisted inclusion complex of poorly water soluble, lipid lowering agent gemfibrozil [5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid]<strong> </strong>with naturally occurring β-cyclodextrins (CDs) or cycloheptaamylase.</p><p><strong>Methods: </strong>In this work, the phase solubility study was performed to find the ratio of drug and cyclodextrin complexes. Inclusion complexes were prepared by kneading and the prepared complex was subjected to microwave drying and conventional drying techniques. The prepared complexes were evaluated by intrinsic dissolution rate studies and equilibrium solubility study. Further characterization was done by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray powder diffractometry (DSC).</p><p><strong>Results: </strong>The phase solubility studies showed a linear A<sub>L</sub>-type diagram indicating the formation of inclusion complexes in 1:1 molar ratio β-CD-gemfibrozil complex with maximum stability constant of 148.88 M<sup>-1</sup>was selected for preparation of inclusion complex. The microwave dried product was identified as the inclusion complex with maximum IDR when compared to the conventional dried product.</p><p><strong>Conclusion: </strong>This study was concluded that the microwave drying is the most suitable of the previously occurring drying techniques. Since it showed the highest solubility and IDR value.</p>
Highlights
The bioavailability of drugs depends on the rate of dissolution in case of poorly water soluble drug where the dissolution is rate limiting step for absorption
Gemfibrozil was obtained as a gift sample from Teva Pharmaceuticals Limited, India and β-cyclodextrin were supplied as gift sample from Albert David Pvt Ltd, Ghaziabad
The slope values of 0.0610 for β-gemfibrozil complex indicated the formation of inclusion complexes in the molar ratio of 1:1
Summary
The bioavailability of drugs depends on the rate of dissolution in case of poorly water soluble drug where the dissolution is rate limiting step for absorption. The poor solubility and low dissolution rate of poorly water-soluble drugs especially those belonging to Class II of the Biopharmaceutical Classification System (BCS), can be enhanced by complexation with cyclodextrin (hydrophilic carrier) because dissolution into the gastrointestinal fluids and intestinal membrane permeation are essential steps in the absorption of orally administered drugs [3]. Among the several carriers used to improve the solubility of poorly soluble drugs, cyclodextrins have been extensively studied and reported to improve solubility and dissolution [4]. They are cyclic oligosaccharides containing at least 6D-(+) glucopyranose units attached by α-(1, 4) glucosidic bonds. It has generally been assumed that the mechanism wherein, CDs exert their effects especially enhancement of solubility due to non-covalent, dynamic inclusion complexes [5]
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