Physical trapping type polymeric micelle drug preparation
    4.
    发明授权
    Physical trapping type polymeric micelle drug preparation 失效
    物理捕获型聚合胶束药物制剂

    公开(公告)号:US5449513A

    公开(公告)日:1995-09-12

    申请号:US105535

    申请日:1993-08-11

    摘要: The present invention relates to drug carriers composed of a block copolymer having hydrophilic and hydrophobic segments, a polymeric micelle type drug comprising hydrophobic drugs trapped by physical treatments in said drug carrier and methods for trapping hydrophobic drugs in the drug carrier. The drugs carrier composed of the block copolymer according to the invention forms a stable polymeric micelle structure with which hydrophobic drugs can be incorporated very efficiently via physical trapping. It was found that the incorporated drug is stably maintained in micelles even in the presence of serum. In addition, a drug difficult to administer into the living body owing to sparing water-solubility for its high hydrophobicity can be administered in the form of polymeric micelle drug.

    摘要翻译: 本发明涉及由具有亲水和疏水性片段的嵌段共聚物组成的药物载体,包含通过所述药物载体中的物理治疗而被捕获的疏水性药物的聚合物胶束型药物和用于在药物载体中捕获疏水性药物的方法。 由根据本发明的嵌段共聚物组成的药物载体形成稳定的聚合胶束结构,通过物理捕获可以非常有效地引入疏水性药物。 发现即使在血清存在下,掺入的药物稳定地保持在胶束中。 此外,由于疏水性高的水溶性而难以施用于生物体的药物可以以聚合物胶束药物的形式施用。

    Anthracycline compound derivative and pharmaceutical preparation
containing the same
    9.
    发明授权
    Anthracycline compound derivative and pharmaceutical preparation containing the same 失效
    蒽环类化合物衍生物和含有它们的药物制剂

    公开(公告)号:US6080396A

    公开(公告)日:2000-06-27

    申请号:US836965

    申请日:1997-08-18

    CPC分类号: A61K9/1075

    摘要: A dimer, trimer or tetramer of an anthracycline compound which can be obtained by directly, chemically bonding anthracycline compounds having anticancer activities to each other by an alkali treatment. A high molecular block copolymer-drug complex pharmaceutical preparation in which the high molecular block copolymer having a hydrophilic polymer segment and a hydrophobic polymer segment forms a micelle having the hydrophilic segment as its outer shell and contains in its hydrophobic inner core a dimer, trimer or tetramer of anthracycline compound alone or together with other drugs. A high molecular block copolymer-drug complex pharmaceutical preparation in which the high molecular block copolymer having a hydrophilic polymer segment and a hydrophobic polymer segment forms a micelle having the hydrophilic segment as its outer shell and contains in its hydrophobic inner core an anthracycline anticancer agent, wherein, when the pharmaceutical preparation is intravenously administered to a CDF1 mouse, the amount of the anthracycline anticancer agent in 1 ml of the mouse blood plasma after 1 hour of its administration becomes 10 (% of dose/ml) or more, provided that the amount of anthracycline anticancer agent in the administered preparation is defined as 100. The aforementioned pharmaceutical preparations have high drug effects and low toxicities.

    摘要翻译: PCT No.PCT / JP96 / 02789第 371日期:1997年8月18日 102(e)日期1997年8月18日PCT提交1996年9月26日PCT公布。 公开号WO97 / 12895 日期1997年04月10日可以通过碱处理直接化学键合具有抗癌活性的蒽环类化合物而获得的蒽环类化合物的二聚体,三聚体或四聚体。 一种高分子嵌段共聚物 - 药物复合药物制剂,其中具有亲水性聚合物链段和疏水性聚合物链段的高分子嵌段共聚物形成具有亲水链段作为其外壳的胶束,并且在其疏水内核中含有二聚体,三聚体或 蒽环类化合物的四聚体单独或与其他药物一起。 一种高分子嵌段共聚物 - 药物复合药物制剂,其中具有亲水性聚合物链段和疏水性聚合物链段的高分子嵌段共聚物形成具有亲水链段作为其外壳并在其疏水内核中含有蒽环类抗癌剂的胶束, 其中,当向CDF1小鼠静脉内施用药物制剂时,在施用1小时后1ml小鼠血浆中的蒽环类抗癌剂的量为10(%/剂量)以上,条件是 给药制剂中蒽环类抗癌剂的量定义为100.上述药物制剂具有高药物作用和低毒性。