Microparticles comprising a biodegradable polymer controlling the release of an antimalaria active principle, pharmaceutical compositions comprising it and process for its preparation

US4897267A · kind A · utility

Assignee

• Ire-Celltarg S.A. · BE

Inventors

• Jose Bontemps · Xhendremael, BE
• Philippe Pirson · Wezembeek-Oppem, BE
• Jean-Bernard Falmagne · Wavre, BE
• Robert Jerome · Tilff, BE
• Philippe Teyssie · Flémalle, BE
• Luc Delattre · Oupeye, BE
• Brigitte Evrard · Embourg, BE

Key dates

• Filing date: Jul 28, 1988
• Grant date: Jan 30, 1990
• Expiry date: Jul 28, 2008

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to microparticles containing an active principle against malaria, such as primaquine, one of its amino acid derivatives, or their conjugates with a hepatotropic vector or their pharmaceutically acceptable salts, and a biocompatible and biodegradable polymer controlling the kinetics of release of the active principle, like (DL)polylactide. The invention also relates to pharmaceutical compositions comprising microcapsules according to the invention. Lastly, the invention relates to processes for the preparation of microparticles as mentioned above, the processes comprising: dissolving the polymer in a volatile solvent, adding to this solution the active principle and possibly a substance regulating the size of the microparticles, and at the end of evaporation, recovering the microparticles by centrifugation and filtration.