Improving the Bioavailability of Diltiazem Hydrochloride by Forming Complexes with β-Cyclodextrin

2014 
The enhancement of oral bioavailability of poorly water soluble drugs remains one of the most challenging aspects. Utilization of cyclodextrins attracted the attention of many researchers for the enhancement of the dissolution rate. The complexation of diltiazem hydrochloride with βcyclodextrin (CD) was investigated by phase solubility. Phase solubility study was performed to determine stiochiometric proportion of Diltiazem HCl and complexing agent -cyclodextrin. Solid inclusion complexes of diltiazem hydrochloride-βCD in 1:1 and 1:2 ratios were prepared by different methods, and the results were satisfactorily and complied with compendia. Mouth dissolving tablets were formulated employing Diltiazem hydrochloride alone and their βCD complexes with an objective of evaluating the feasibility of employing drug-βCD complexes in the design of immediate release tablet formulations for obtaining flow and complete drug release in 01 h. All the tablets prepared by optimizing the formula and were evaluated for pre compression, post compression, drug content, and drug release. The overall results indicate that formulation M3 was better and that it satisfies all the criteria as a fast mouth dissolving tablet.
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