Preparation and study the 1:2 inclusion complex of carvedilol with beta-cyclodextrin

J Pharm Biomed Anal. 2004 Feb 18;34(3):517-23. doi: 10.1016/s0731-7085(03)00576-4.

Abstract

An inclusion complex of beta-cyclodextrin with carvedilol was prepared by using a convenient new method of microwave irradiation. Phase-solubility studies demonstrated the ability of beta-cyclodextrins to complex with carvedilol and increase drug solubility. The structure of inclusion complex was determined by fluorescence spectroscopy and 1H NMR, 13C NMR measurements in solution. The solid inclusion was characterised by infrared spectroscopy, differential scanning calorimetry (DSC) and element analysis. These experimental results confirmed the existence of 1:2 inclusion complex of carvedilol with beta-cyclodextrin, the formation constant of complex was determined by the fluorescence method. Molecular modeling predicted the energy-minimized structure of the complex.

MeSH terms

  • Carbazoles / analysis
  • Carbazoles / chemical synthesis*
  • Carbazoles / pharmacokinetics*
  • Carvedilol
  • Chemistry, Pharmaceutical
  • Cyclodextrins / analysis
  • Cyclodextrins / chemical synthesis*
  • Cyclodextrins / pharmacokinetics*
  • Propanolamines / analysis
  • Propanolamines / chemical synthesis*
  • Propanolamines / pharmacokinetics*
  • Solubility / drug effects
  • beta-Cyclodextrins*

Substances

  • Carbazoles
  • Cyclodextrins
  • Propanolamines
  • beta-Cyclodextrins
  • Carvedilol
  • betadex