Influence of beta-cyclodextrin complexation on carbamazepine release from hydroxypropyl methylcellulose matrix tablets

Eur J Pharm Biopharm. 2003 Jan;55(1):85-91. doi: 10.1016/s0939-6411(02)00127-3.

Abstract

The in vitro release profiles of carbamazepine and beta-cyclodextrin either complexed or simply mixed and subsequently incorporated in hydrophilic matrix tablets containing 15 or 30% hydroxypropyl methylcellulose were evaluated. Solubility studies revealed a linear relationship between the increase in carbamazepine solubility and the increase in beta-cyclodextrin concentration. Drying methods (spray-drying and freeze-drying) were used to obtain carbamazepine/beta-cyclodextrin solid complexes in order to prepare tablets. The results demonstrated that matrix tablets containing carbamazepine/beta-cyclodextrin solid complexes displayed faster carbamazepine and beta-cyclodextrin release compared to that containing simple physical mixture. Gelling and matrix formation was impaired in formulation containing 15% hydroxypropyl methylcellulose and spray-dried complex. The comparison of spray-drying and freeze-drying revealed no significant influence of both drying methods on carbamazepine and beta-cyclodextrin dissolution rate when carbamazepine/beta-cyclodextrin complexes were incorporated in 30% hydroxypropyl methylcellulose matrix tablets. The results point to the possibility of modulating carbamazepine release using a hydroxypropyl methylcellulose matrix associated to the drug complexed with beta-cyclodextrin.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticonvulsants / chemistry*
  • Calorimetry, Differential Scanning
  • Carbamazepine / chemistry*
  • Chemistry, Pharmaceutical
  • Chromatography, High Pressure Liquid
  • Cyclodextrins / chemistry*
  • Excipients / chemistry*
  • Hypromellose Derivatives
  • Methylcellulose / analogs & derivatives*
  • Methylcellulose / chemistry*
  • Microscopy, Electron, Scanning
  • Solubility
  • Spectrophotometry, Infrared
  • Tablets
  • beta-Cyclodextrins*

Substances

  • Anticonvulsants
  • Cyclodextrins
  • Excipients
  • Tablets
  • beta-Cyclodextrins
  • Carbamazepine
  • Hypromellose Derivatives
  • Methylcellulose
  • betadex