Title:Preparation and in vitro/in vivo Evaluation of Lacidipine by Adsorption onto Fumed Silica Using Supercritical Carbon Dioxide
VOLUME: 13 ISSUE: 7
Author(s):Yajie Geng, Qiang Fu, Bei Guo, Yun Li, Xiangrong Zhang, Xianglin Wang and Tianhong Zhang
Affiliation:Department of Pharmaceutical Analysis, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
Keywords:Fumed silica, lacidipine, oral bioavailability, supercritical carbon dioxide.
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.
