Preparation and in vitro/in vivo Evaluation of Lacidipine by Adsorption onto Fumed Silica Using 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.

journal_name

Curr Drug Deliv

journal_title

Current drug delivery

authors

Geng Y,Fu Q,Guo B,Li Y,Zhang X,Wang X,Zhang T

doi

10.2174/1567201813666151203233232

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

1053-1064

issue

7

eissn

1567-2018

issn

1875-5704

pii

CDD-EPUB-72248

journal_volume

13

pub_type

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