High concentration formulations of opioids and opioid...

A - Human Necessities – 61 – K

Patent

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A61K 31/44 (2006.01) A61K 9/08 (2006.01) A61K 31/19 (2006.01) A61K 31/445 (2006.01) A61K 47/12 (2006.01)

Patent

CA 2507356

The present invention provides opioid formulations suitable for long-term delivery to a subject. The formulation of the invention comprises an opioid or opioid derivative (e.g., morphine, hydromorphone, fentanyl or a fentanyl congener), and an aqueous solvent comprising a low molecular weight carboxylic acid (e.g., C2-4, C2-7). The invention thus provides for formulations comprising morphine, hydromorphone, fentanyl or fentanyl congeners in concentrations significantly in excess of conventional aqueous formulations, e.g., on the order about 2-fold to about 10,000-fold greater than conventional formulations, e.g., currently commercially available formulations.

L'invention concerne des formulations d'opioïdes convenant pour une administration à long terme à un sujet. La formulation de l'invention comprend un opioïde ou un dérivé d'opioïde (par exemple, morphine, hydromorphone, fentanyl ou substance organoleptique de fentanyl) et un solvant aqueux renfermant un acide carboxylique (par exemple, C¿2-4?, C¿2-7?) de faible poids moléculaire. L'invention permet donc de produire des formulations contenant morphine, hydromorphone, fentanyl ou substances organoleptiques de fentanyl en concentrations significativement plus élevées que dans les formulations aqueuses classiques, par exemple, de l'ordre d'environ 2 fois à 10 000 fois supérieures aux formulations classiques, par exemple, des formulations actuellement commercialement disponibles.

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