Preparation and in vitro/in vivo Evaluation of Lacidipine by Adsorption onto Fumed Silica Using Supercritical Carbon Dioxide

Author(s): Yajie Geng, Qiang Fu, Bei Guo, Yun Li, Xiangrong Zhang, Xianglin Wang, Tianhong Zhang

Journal Name: Current Drug Delivery

Volume 13 , Issue 7 , 2016

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Abstract:

The aim of this study was to design a silica-supported solid dispersion of lacidipine (LCDP) to enhance the dissolution rate and oral absorption using supercritical CO2 (scCO2) as a solvent. The formulation was characterized using differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy and fourier transformed infrared spectroscopy. In the dissolution test, LCDP-scCO2 formulation showed a significantly enhanced dissolution compared with LCDPsilica physical mixture and a faster dissolution rate than Lacipil® under different dissolution conditions. In an in vivo test, the area under concentration-time curve and Cmax of LCDP-scCO2 formulation was 9.23 and 23.78 fold greater than LCDP-silica physical mixture (1:15, w/w), respectively, whereas the corresponding values were 1.92 and 2.80 fold greater than Lacipil®, respectively. Our results showed that the solid dispersion prepared by supercritical fluids technology is a feasible method to enhance the oral bioavailability of LCDP.

Keywords: Fumed silica, lacidipine, oral bioavailability, supercritical carbon dioxide.

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Article Details

VOLUME: 13
ISSUE: 7
Year: 2016
Page: [1053 - 1064]
Pages: 12
DOI: 10.2174/1567201813666151203233232
Price: $65

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