The effects of surfactants on the solubility and dissolution profiles of a poorly water-soluble basic drug, carvedilol


İNCEÇAYIR T.

PHARMAZIE, vol.70, no.12, pp.784-790, 2015 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 70 Issue: 12
  • Publication Date: 2015
  • Doi Number: 10.1691/ph.2015.5081
  • Journal Name: PHARMAZIE
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.784-790
  • Gazi University Affiliated: Yes

Abstract

This study investigated the most suitable surfactant medium for the dissolution testing of a poorly soluble basic drug, namely, carvedilol reflecting the in vivo behavior. Sodium lauryl sulfate (SLS), hexadecyltrimethylannmonium bromide (CTAB) and polysorbate 80 were used as anionic, cationic and nonionic surfactants, respectively. Saturation solubilities of carvedilol were determined in the presence of SLS, CTAB and polysorbate 80 (0.5, 1 and 2% (w/v)) at pH 1.2 and 6.8. Dissolution behaviors of the commercial tablets were studied using USP apparatus II in pH 1.2, 4.5 and 6.8 buffers and pH 6.8 dissolution media with 0.5% (w/v) SLS, polysorbate 80 and CTAB. Polysorbate 80 enhanced the solubility of carvedilol irrespective of pH, while SLS and CTAB exhibited larger solubilization effect than polysorbate 80 depending on pH and the ionic nature of the surfactant. Based on in vitro dissolution profile similarity, pH 6.8 dissolution medium with 0.5% (w/v) polysorbate 80 was found to be the most biorelevant medium, which probably reflects the bioequivalence of test products to the reference product of carvedilol.