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    • 31. 发明申请
    • PHARMACEUTICAL COMPOSITIONS OF SOMATOSTATIN-DOPAMINE CONJUGATES
    • 磺酰胺多巴胺结合物的药物组合物
    • WO2009139855A3
    • 2009-12-30
    • PCT/US2009002943
    • 2009-05-12
    • IPSEN PHARMA SASDONG ZHENG XINZHANG JUNDONG
    • DONG ZHENG XINZHANG JUNDONG
    • A61K38/31
    • A61K38/31
    • 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).
    • 本发明涉及在体内含有生长抑素和多巴胺活性的生长抑素 - 多巴胺缀合物的组合物的改进,以及制备这种组合物的方法以及使用这些组合物治疗哺乳动物的方法。 特别地,本发明涉及包含多巴二肽(Dop2) - 环[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH2(SEQ ID NO:1)的药物组合物,其中生长抑素 - 多巴胺结合物在生理pH下体内沉淀,形成缓慢溶解并释放到体液和血液中的原位沉积物。 本发明还可以包含平均分子量为400(PEG400)的有机组分如二甲基乙酰胺(DMA)或聚乙二醇。