Pharmaceutical compositions of somatostatin-dopamine conjugates

Details Pharmaceutical compositions of somatostatin-dopamine conjugates Pharmaceutical compositions of somatostatin-dopamine conjugates

A - Human Necessities

61

K

A61K 38/31 (2006.01)

Patent

CA 2724534

The present invention is directed to improvements in compositions containing a somatostatin- dopamine conjugate which retains both somatostatin and dopamine activity in vivo, methods for preparing such compositions, and method of using such compositions to treat mammals. In particular, the present invention relates to a pharmaceutical composition comprising Dop2-DLys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 (SEQ ID NO: 1), in which the somatostatin-dopamine conjugate precipitates in vivo at physiological pH to form an in situ deposit that is slowly dissolved and released into the body fluid and bloodstream. The present invention may further comprise an organic component such as dimethylacetamide (DMA) or polyethylene glycol with an average molecular weight of 400 (PEG400).

La présente invention concerne des améliorations de compositions contenant un conjugué somatostatine-dopamine qui maintiennent lactivité de la somatostatine et de la dopamine in vivo, des procédés pour préparer de telles compositions, et un procédé dutilisation de telles compositions pour traiter des mammifères. En particulier, la présente invention concerne une composition pharmaceutique comprenant Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 (SEQ ID N° 1), où le conjugué somatostatine-dopamine précipite in vivo à pH physiologique pour former un dépôt in situ qui est lentement dissous et libéré dans le fluide corporel et la circulation sanguine. La présente invention peut comprendre en outre un composant organique tel que le diméthylacétamide (DMA) ou un polyéthylèneglycol ayant un poids moléculaire moyen de 400 (PEG400).

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