Increased dissolution rate and oral bioavailability of hydrophobic drug glyburide tablets produced using supercritical CO2 silica dispersion technology

Guan, Jibin; Han, Jihong; Zhang, Dong; Chu, Chunxia; Liu, Hongzhuo; Sun, Jin; He, Zhonggui; Zhang, Tianhong

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.

• Journal Article Type: Article
• Acceptance Date: Oct 21, 2013
• Online Publication Date: Oct 30, 2013
• Publication Date: 2014-04
• Deposit Date: Jun 12, 2023
• Journal: European Journal of Pharmaceutics and Biopharmaceutics
• Print ISSN: 0939-6411
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 86
• Issue: 3
• Pages: 376-382
• DOI: https://doi.org/10.1016/j.ejpb.2013.10.008
• Keywords: Pharmaceutical Science; General Medicine; Biotechnology
• Additional Information: This article is maintained by: Elsevier; Article Title: Increased dissolution rate and oral bioavailability of hydrophobic drug glyburide tablets produced using supercritical CO2 silica dispersion technology; Journal Title: European Journal of Pharmaceutics and Biopharmaceutics; CrossRef DOI link to publisher maintained version: https://doi.org/10.1016/j.ejpb.2013.10.008; Content Type: article; Copyright: Copyright © 2013 Elsevier B.V. All rights reserved.