Sustained release microsphere preparation containing...

A - Human Necessities – 61 – K

Patent

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A61K 9/16 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 31/4515 (2006.01) A61K 31/505 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) A61K 45/00 (2006.01)

Patent

CA 2148823

A sustained release microsphere preparation which is produced by including a hydrophobic antipsychotic drug such as bromperidol, haloperidol or the like into a base composed of a high molecular weight polymer having in vivo histocompatibility such as polylactic acid, poly(lactic-co- glycolic)acid or the like, and a process for the production thereof. When a long-term administration is required, desired pharmacological effects can be obtained by one injection per 1 to 8 weeks, in stead of daily administration. As the result, considerable improvement in compliance at the time of maintenance therapy can be expected. Also, since a high molecular weight polymer having in vivo histocompatibility is used, surgical operations such as embedding and the like are not required at all, and subcutaneous and intramuscular administrations can be made easily absolutely in the same manner as the case of conventional suspension injections so that recovery of the material is not required. In addition, resistance and pain at the time of administration are small.

On produit une microsphère à libération prolongée en enfermant un antipsychotique hydrophobe tel que brompéridol ou halopéridol dans une base qui comprend un polymère biocompatible tel que l'acide polylactique ou un copolymère acide lactique/acide glycolique. Lorsque s'impose une administation à long terme, elle peut offrir un effet pharmacologique désiré grâce à une injection toutes les 1 à 8 semaines et non chaque jour. On peut donc escompter une amélioration remarquable du respect des posologies pendant une thérapie de maintien. De plus, l'utilisation du polymère biocompatible permet d'éviter entièrement des opérations chirurgicales telles que des implantations, facilite les injections hypodermiques et intramusculaires comme dans le cas des injections suspendues, et évite le retrait de la microsphère. On peut en outre administrer cette microsphère moyennant peu d'appréhension et de douleur.

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