Preformulation Study of the Inclusion Complex Irbesartan-β-Cyclodextrin

被引：46

作者：

Hirlekar, Rajashree ^{[1
]}

Kadam, Vilasrao ^{[1
]}

机构：

[1] Bharati Vidyapeeths Coll Pharm, Dept Pharmaceut, Navi Mumbai 400614, Maharashtra, India

来源：

AAPS PHARMSCITECH | 2009年 / 10卷 / 01期

关键词：

beta-cyclodextrin; dissolution; inclusion complex; Irbesartan; solubility;

D O I：

10.1208/s12249-009-9206-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The aim of the present work was to improve the solubility and dissolution profile of Irbesartan (IRB), a poorly water-soluble drug by formation of inclusion complex with beta-cyclodextrin (beta CD). Phase solubility studies revealed increase in solubility of the drug upon cyclodextrin addition, showing A(L)-type of graph with slope less than one indicating formation of 1:1 stoichiometry inclusion complex. The stability constant (K (s)) was found to be 104.39 M(-1). IRB-beta CD binary systems were prepared by cogrinding, kneading using alcohol, kneading using aqueous alcohol, and coevaporation methods. Characterization of the binary systems were carried out by differential scanning calorimetry, Fourier transform infrared spectroscopy, scanning electron microscopy, X-ray diffraction, and proton nuclear magnetic resonance. The dissolution profiles of inclusion complexes were determined and compared with those of IRB alone and physical mixture. Among the various methods, coevaporation was the best in which the solubility was increased and dissolution rate of the drug was the highest. The study indicated the usefulness of cyclodextrin technology to overcome the solubility problem of IRB.

引用

页码：276 / 281

页数：6

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