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

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

Research output: Contribution to journalArticlepeer-review

24 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)376-382
Number of pages7
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume86
Issue number3
DOIs
StatePublished - Apr 2014
Externally publishedYes

Bibliographical note

Funding Information:
This work was financially supported by the National Nature Science Foundation of China (No. 81173008 ).

Keywords

  • Dissolution
  • Glyburide
  • Oral bioavailability
  • Silica
  • Supercritical fluid
  • Tablet

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