Porous aerosil loading probucol using supercritical carbon dioxide: preparation, in vitro and in vivo characteristics

被引：7

作者：

Chu, Chunxia ^{[1
]}

Liu, Muhua ^{[1
]}

Wang, Dongmei ^{[1
]}

Guan, Jibin ^{[1
]}

Cai, Cuifang ^{[1
]}

Sun, Yuanpeng ^{[1
]}

Zhang, Tianhong ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Sch Pharm, Dept Pharmaceut, Shenyang 110016, Liaoning Provin, Peoples R China

来源：

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY | 2014年 / 19卷 / 04期

关键词：

Aerosil; bioavailability; dissolution; physicochemistry property; probucol; supercritical carbon dioxide; DRUG-POLYMER MISCIBILITY; SOLID DISPERSIONS; DISSOLUTION-RATE; FLUID TECHNOLOGY; BIOAVAILABILITY; MICROPARTICLES; IMPROVEMENT; SOLUBILITY; SYSTEMS;

D O I：

10.3109/10837450.2013.800109

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The aim of this study was to enhance the dissolution rate and oral bioavailability of probucol. Probucol was adsorbed onto aerosils via supercritical carbon dioxide (ScCO2) and the physicochemistry properties of probucol-aerosil powder were evaluated by differential scanning calorimetry, X-ray diffraction, infrared spectroscopy and scanning electron microscopy. Tablets of the probucol-aerosil powder were prepared by direct compression method. In the dissolution test, the probucol-aerosil tablets showed a significant enhanced dissolution rate compared with commercial tablets. Bioavailability study was carried out in beagle dogs. Probucol-aerosil tablets exhibited higher AUC and C-max than commercial tablets. The improved dissolution and bioavailability of probucol-aerosil tablets were attributed to the amorphous state and good dispersion of probucol. It is a feasible method to enhance the oral bioavailability by adsorbing probucol onto aerosils via ScCO2.

引用

页码：501 / 506

页数：6

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