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    • 3. 发明申请
    • HIGH SURFACE-AREA LYOPHILIZED COMPOSITIONS COMPRISING ARSENIC FOR ORAL ADMINISTRATION IN PATIENTS
    • 包含ARSENIC的高表面积的LYOPHILED组合物用于患者口腔管理
    • WO2016123603A3
    • 2016-11-03
    • PCT/US2016015917
    • 2016-02-01
    • VADDI KRISHNAKURUMADDALI KUMAR
    • VADDI KRISHNAKURUMADDALI KUMAR
    • A61K33/36A61K9/16A61K9/48A61P35/00A61P35/02
    • A61K9/19A61K9/4858A61K33/36A61K45/06A61K2300/00
    • The present invention relates to treating malignancies such as tumors or cancers by orally administering lyophilized compositions comprising arsenic to a subject in such need. Malignancies include various hematological malignancies, such as acute myeloid leukemia (AML) including acute promyelocytic leukemia (APL), myelodysplasia syndrome (MDS), multiple myeloma (MM) and lymphomas and solid tumors including glioblastoma multiforme and breast cancer. Arsenic treatment has shown great promise in the treatment of several cancers but requires daily intravenous (IV) administration. This invention relates to a novel formulation comprising a lyophilized compositions comprising arsenic. As a result, the formulation facilitates a systemic bioavailability comparable to that of intravenous (IV) administration of arsenic trioxide currently practiced. The present invention also relates to a method for lyophilizing the arsenic trioxide, preparing the oral formulation comprising lyophilized compositions comprising arsenic, and a method for treating a subject with malignancies using the oral formulation.
    • 本发明涉及通过在需要时向受试者口服施用包含砷的冻干组合物来治疗诸如肿瘤或癌症的恶性肿瘤。 恶性肿瘤包括各种血液恶性肿瘤,如包括急性早幼粒细胞白血病(APL),骨髓增生异常综合征(MDS),多发性骨髓瘤(MM)和淋巴瘤的急性骨髓性白血病(AML)和包括多形性成胶质细胞瘤和乳腺癌的实体瘤。 砷治疗在治疗几种癌症方面表现出巨大的希望,但需要每日静脉内(IV)给药。 本发明涉及包含含砷的冻干组合物的新型制剂。 结果,该制剂促进了与目前实施的三氧化二砷的静脉内(IV)给药相当的全身生物利用度。 本发明还涉及一种用于冻干三氧化二砷的方法,制备包含砷的冻干组合物的口服制剂,以及使用口服制剂治疗恶性肿瘤患者的方法。