Microparticles comprising a biodegradable polymer controlling th

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert

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424423, 424426, 424486, 424489, A61F 1300

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active

048972673

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.

REFERENCES:
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patent: 4284627 (1981-08-01), Raether et al.
patent: 4416872 (1983-11-01), Alving et al.
Chemical Abstracts, vol. 85, No. 24, 12/76, p. 315, resume #182354d, D. L. Wise et al., "Sustained Release of an Antimalarial Drug Using a Copolymer of Glycolic/Lactic Acid", & Life Sci., 1976, 19(6), 867-73.
Chemical Abstracts, vol. 107, No. 2, 7/87, p. 349, resume #12756s, T. Laakso et al., "Biodegradable Microspheres Bound Antiparasitic Drugs from Starch Microparticles", & J. Pharm. Sci., 1987, 76(2), 134-40.
Journal of Pharmaceutical Sciences, vol. 73, No. 12, 12/84, pp. 1721-1724, American Pharmaceutical Association, S. Benita et al., "Characterization of Drug-Loaded Poly(d,1-Lactide) Microspheres".

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