Solubility, Dissolution Rate and Bioavailability Enhancement of Irbesartan by Solid Dispersion Technique

被引:40
作者
Boghra, Rikisha Jaysukhbhai [1 ]
Kothawade, Pranita Chandrakant [1 ]
Belgamwar, Veena Shailendra [1 ]
Nerkar, Pankaj Padmakar [1 ]
Tekade, Avinash Ramrao [1 ]
Surana, Sanjay Javerilal [1 ]
机构
[1] RC Patel Inst Pharmaceut Educ & Res, Dept Pharmaceut & Qual Assurance, Shirpur 425405, Maharashtra, India
关键词
Irbesartan; solubility enhancement; solid dispersion; bioavailability; devitrification; SOLUBLE DRUG;
D O I
10.1248/cpb.59.438
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The objective of present work was to enhance the solubility and bioavailability of poorly aqueous soluble drug Irbesartan (IBS). The solid dispersions were prepared by spray drying method using low viscosity grade HPMC E5LV. Prepared solid dispersions were characterized by dissolution study, fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray diffraction studies (XRD). Results of the SEM, DSC and XRD study showed the conversion of crystalline form of IBS to amorphous form. The dissolution rate was remarkably increased in case of solid dispersion compared to pure IBS. Solubility and stability of solid dispersion was increased due to surfactant and wetting property, slowing devitrification and having anti-plasticization effect of HPMC E5LV. In vivo studies were performed in healthy rabbits (New Zealand grey) and compared with plain IBS. Solid dispersions showed increase in relative bioavailability than the plain IBS suspension. In conclusion, the prepared solid dispersions showed remarkable increase in solubility, dissolution rate and hence bioavailabilty of poorly water soluble drug Irbesartan.
引用
收藏
页码:438 / 441
页数:4
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