Injectable buprenorphine microparticle compositions and...

A - Human Necessities – 61 – K

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Details

A61K 31/485 (2006.01) A61K 9/16 (2006.01) A61K 9/50 (2006.01) A61K 47/34 (2006.01) A61P 25/32 (2006.01) A61P 25/36 (2006.01)

Patent

CA 2382577

An injectable slow-release partial opioid agonist or opioid antagonist formulation is provided comprising a partial opioid agonist or opioid antagonist in a poly(D,L-lactide) excipient with a small amount of residual ethyl acetate. Upon intramuscular injection of the composition, a partial opioid agonist or opioid antagonist is released in a controlled manner over an extended period of time. The composition finds use in the treatment of heroin addicts and alcoholics to reduce consumption of the abused substances. Of particular interest are the drugs buprenorphine, methadone and naltrexone.

La présente invention concerne une formulation injectable et à libération retardée d'agoniste partiel opioïde, ou d'antagoniste opioïde, comprenant un agoniste partiel opioïde ou un antagoniste opioïde dans un poly(D,L-lactide) comme excipient et contenant une faible quantité d'acétate d'éthyle résiduelle. Lors de l'injection intramusculaire de la composition, un agoniste partiel opioïde ou un antagoniste opioïde est libéré de manière régulée sur une longue durée. La composition est utile dans le traitement des héroïnomanes et des alcooliques afin de réduire la consommation de ces substances faisant l'objet d'abus. La buprénorphine, la méthadone et le naltrexone sont des médicaments particulièrement intéressants.

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