title: Porous aerosil loading probucol using supercritical carbon dioxide: preparation, in vitro and in vivo characteristics.
abstract: 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 Cmax 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.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University , No. 103, Wenhua Road, Shenyang 110016 , PR China.
authors.forename: Chunxia
authors.initials: C
authors.lastname: Chu
authors.forename: Muhua
authors.initials: M
authors.lastname: Liu
authors.forename: Dongmei
authors.initials: D
authors.lastname: Wang
authors.forename: Jibin
authors.initials: J
authors.lastname: Guan
authors.forename: Cuifang
authors.initials: C
authors.lastname: Cai
authors.forename: Yuanpeng
authors.initials: Y
authors.lastname: Sun
authors.forename: Tianhong
authors.initials: T
authors.lastname: Zhang
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002245:Carbon Dioxide / Q000737:chemistry* / Q000378:metabolism*; D004285:Dogs; D016062:Porosity; D011208:Powders / Q000737:chemistry / Q000378:metabolism; D011341:Probucol / Q000737:chemistry* / Q000378:metabolism*; D012822:Silicon Dioxide / Q000737:chemistry* / Q000378:metabolism*; D012995:Solubility; D013607:Tablets / Q000737:chemistry / Q000378:metabolism
chemical_list: D011208:Powders; D013607:Tablets; D002245:Carbon Dioxide; D012822:Silicon Dioxide; D011341:Probucol