Formulation and evaluation of novel tableted chitosan microparticles for the controlled release of clozapine

J Microencapsul. 2004 Nov;21(7):709-18. doi: 10.1080/02652040400008473.

Abstract

Controlled release formulations of clozapine microparticulated tablets were prepared by using chitosan. Microparticles were characterized for particle size and size distribution. Microparticles were compressed into tablets using the directly compressible excipients. SEM photographs of the fractured part of the tablet revealed the presence of discrete particles in the tablets, suggesting that the system chosen is ideal for tableting. Drug release from the tableted microparticles exhibited an initial burst effect, but the release decreased with increasing extent of cross-linking. Tablets were coated with chitosan or cellulose acetate, which significantly lowered the initial burst effect when compared to uncoated tablets. Drug release from chitosan-coated tablets was slightly higher than the tablets coated with cellulose acetate. Tablets prepared were effective in delivering clozapine over a period of 12 h.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cellulose / analogs & derivatives*
  • Chitosan
  • Clozapine / pharmacokinetics*
  • Delayed-Action Preparations
  • Drug Compounding / methods
  • Humans
  • Microscopy, Electron, Scanning
  • Microspheres
  • Serotonin Antagonists / pharmacokinetics*
  • Tablets, Enteric-Coated

Substances

  • Delayed-Action Preparations
  • Serotonin Antagonists
  • Tablets, Enteric-Coated
  • acetylcellulose
  • Cellulose
  • Chitosan
  • Clozapine