title: 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.
authors.forename: Yajie
authors.initials: Y
authors.lastname: Geng
authors.forename: Qiang
authors.initials: Q
authors.lastname: Fu
authors.forename: Bei
authors.initials: B
authors.lastname: Guo
authors.forename: Yun
authors.initials: Y
authors.lastname: Li
authors.forename: Xiangrong
authors.initials: X
authors.lastname: Zhang
authors.forename: Xianglin
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutical Analysis, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
authors.forename: Tianhong
authors.initials: T
authors.lastname: Zhang
mesh_terms: D000327:Adsorption; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002245:Carbon Dioxide / Q000737:chemistry*; D004095:Dihydropyridines / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D004285:Dogs; D004339:Drug Compounding; D004355:Drug Stability; D008855:Microscopy, Electron, Scanning; D033362:Powder Diffraction; D012822:Silicon Dioxide / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility; D014961:X-Ray Diffraction
chemical_list: D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D002245:Carbon Dioxide; C060285:lacidipine; D012822:Silicon Dioxide