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    • 9. 发明申请
    • Pharmaceutically active lipid based formulation of SN-38
    • SN-38的药物活性脂质制剂
    • US20050238706A1
    • 2005-10-27
    • US11061044
    • 2005-02-18
    • Imran AhmadJia-Ai Zhang
    • Imran AhmadJia-Ai Zhang
    • A61K9/127A61K31/4745A61P31/12A61P35/00
    • A61K9/127A61K31/4745
    • SN38, camptothecin derivatives are poorly water soluble, highly lipophilic camptothecin derivatives and are very active against a variety of human cancers. Because of their very poor water solubility, SN38 has not been used to treat human patients with cancer due to the inability to administer sufficient quantities of dissolved in a pharmaceutical formulation. This invention overcomes these limitations by teaching novel pharmaceutically acceptable SN38 liposome complex formulation for the direct administration of the formulation to human patients with cancer. The claimed invention also describes the methods to prepare liposomal SN38 complexes and antitumor compositions of liposomal SN38 complexes to allow the administration in sufficient amounts to treat various types of cancer and as antiviral agents. This invention is also directed to injectable sterile solutions, antitumor compositions, liposomes. The present invention is for novel compositions and methods for treating diseases caused by cellular proliferation, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include SN38 lipid complexes in which the complexes can contain any of a variety of neutral or charged lipids and, desirably, cardiolipin. The compositions are capable of efficiently incorporating SN38 into complexes and are capable of solubilizing relatively high concentrations of SN38.
    • SN38,喜树碱衍生物水溶性差,高亲脂性喜树碱衍生物,对各种人类癌症非常活跃。 由于水溶性非常差,SN38不能用于治疗癌症患者,因为不能将足量的溶解在药物制剂中。 本发明通过教导用于直接给予人类癌症患者的制剂的新的药学上可接受的SN38脂质体复合物制剂来克服这些限制。 所要求保护的发明还描述了制备脂质体SN38复合物和脂质体SN38复合物的抗肿瘤组合物的方法,以允许给予足量的治疗各种类型的癌症和作为抗病毒剂。 本发明还涉及可注射的无菌溶液,抗肿瘤组合物,脂质体。 本发明是用于治疗由细胞增殖引起的疾病的新型组合物和方法,特别是用于治疗哺乳动物,特别是人类的癌症。 本发明的治疗组合物包括SN38脂质复合物,其中复合物可以含有各种中性或带电荷的脂质中的任何一种,并且理想的是含有心磷脂。 组合物能够有效地将SN38并入复合物中,并能够溶解相对高浓度的SN38。