title: Increased dissolution rate and oral bioavailability of hydrophobic drug glyburide tablets produced using supercritical CO₂ silica dispersion technology.
abstract: The aim of this study was to design a silica-supported solid dispersion of a water-insoluble drug, glyburide, to increase its dissolution rate and oral absorption using supercritical fluid (SCF) technology. DSC and PXRD results indicated that the encapsulated drug in the optimal solid dispersion was in an amorphous state and the product was stable for 6 months. Glyburide was adsorbed onto the porous silica, as confirmed by the SEM images and BET analysis. Furthermore, FT-IR spectroscopy confirmed that there was no change in the chemical structure of glyburide after the application of SCF. The glyburide silica-based dispersion could also be compressed into tablet form. In vitro drug release analysis of the silica solid dispersion tablets demonstrated faster release of glyburide compared with the commercial micronized tablet. In an in vivo test, the AUC of the tablets composed of the new glyburide silica-based solid dispersion was 2.01 times greater than that of the commercial micronized glyburide tablets. In conclusion, SCF technology presents a promising approach to prepare silica-based solid dispersions of hydrophobic drugs because of its ability to increase their release and oral bioavailability.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Jibin
authors.initials: J
authors.lastname: Guan
authors.affiliation: School of Pharmacy, Institute for Science and Technology in Medicine, Keele University, Staffordshire, UK.
authors.forename: Jihong
authors.initials: J
authors.lastname: Han
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Dong
authors.initials: D
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Chunxia
authors.initials: C
authors.lastname: Chu
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Hongzhuo
authors.initials: H
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Jin
authors.initials: J
authors.lastname: Sun
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Zhonggui
authors.initials: Z
authors.lastname: He
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China. Electronic address: zhangth_student@aliyun.com.
authors.forename: Tianhong
authors.initials: T
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002245:Carbon Dioxide / Q000737:chemistry*; D025924:Chromatography, Supercritical Fluid / Q000379:methods*; D004285:Dogs; D005905:Glyburide / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D012822:Silicon Dioxide / Q000737:chemistry / Q000378:metabolism*; D012995:Solubility; D013607:Tablets; D013997:Time Factors
chemical_list: D013607:Tablets; D002245:Carbon Dioxide; D012822:Silicon Dioxide; D005905:Glyburide
keywords: Dissolution; Glyburide; Oral bioavailability; Silica; Supercritical fluid; Tablet