Formulations and methods of use 2,2'-dithio-bis-esthane sulfonate
    3.
    发明授权
    Formulations and methods of use 2,2'-dithio-bis-esthane sulfonate 失效
    2,2'-二硫代 - 双 - 甲磺酸盐的配方和方法

    公开(公告)号:US5866617A

    公开(公告)日:1999-02-02

    申请号:US844544

    申请日:1997-04-18

    摘要: This invention describes novel formulations containing a water soluble disulfide, 2,2'-dithio-bis-ethane sulfonate, with or without cis-diammine dichloro platinum present in the same formulation, wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate is used to reduce the risk or prevent or retard the development of cisplatin induced nephrotoxicity, myelosuppression, and neurotoxicity, and wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate potentiates the antitumor activity of cisplatin when treating human patients with cancer. This invention also teaches novel formulations containing 2,2'-dithio-bis-ethane sulfonate alone or in combination with cisplatin in lyophilized or dissolved in an aqueous formulations which can be administered to patients with cancer who are being treated with cisplatin. The invention also teaches methods of preparing said formulations and their use in preventing cisplatin related toxicities and potentiation of cisplatin antitumor activity.

    摘要翻译: 本发明描述了含有水溶性二硫化物,2,2'-二硫代双乙磺酸盐的新型制剂,其具有或不存在于同一制剂中的顺式二氨基二氯铂,其中经口或口服给予2,2'-二硫代 双乙磺酸盐用于降低风险,或预防或阻止顺铂诱导的肾毒性,骨髓抑制和神经毒性的发展,并且其中肠外或口服给予2,2'-二硫代双乙磺酸盐增强抗肿瘤活性 的顺铂在治疗癌症患者时。 本发明还教导了含有2,2'-二硫代双 - 乙烷磺酸盐的单独或与顺铂联合使用的冻干或溶解在水性制剂中的新型制剂,其可以施用于正在用顺铂治疗的癌症患者。 本发明还教导了制备所述制剂的方法及其在预防顺铂相关毒性和增强顺铂抗肿瘤活性方面的用途。

    Formulations and methods of use of 2,2'-dithio-bis-ethane sulfonate
    4.
    发明授权
    Formulations and methods of use of 2,2'-dithio-bis-ethane sulfonate 失效
    2,2'-二硫代双乙磺酸盐的配方和使用方法

    公开(公告)号:US5866169A

    公开(公告)日:1999-02-02

    申请号:US878244

    申请日:1997-06-18

    摘要: This invention describes novel formulations containing a water soluble disulfide, 2,2'-dithio-bis-ethane sulfonate, with or without cis-diammine dichloro platinum present in the same formulation, wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate is used to reduce the risk or prevent or retard the development of cisplatin induced nephrotoxicity, myelosuppression, and neurotoxicity, and wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate potentiates the antitumor activity of cisplatin when treating human patients with cancer. This invention also teaches novel formulations containing 2,2'-dithio-bis-ethane sulfonate alone or in combination with cisplatin in lyophilized or dissolved in an aqueous formulations which can be administered to patients with cancer who are being treated with cisplatin. The invention also teaches methods of preparing said formulations and their use in preventing cisplatin related toxicities and potentiation of cisplatin antitumor activity.

    摘要翻译: 本发明描述了含有水溶性二硫化物,2,2'-二硫代双乙磺酸盐的新型制剂,其具有或不存在于同一制剂中的顺式二氨基二氯铂,其中经口或口服给予2,2'-二硫代 双乙磺酸盐用于降低风险,或预防或阻止顺铂诱导的肾毒性,骨髓抑制和神经毒性的发展,并且其中肠外或口服给予2,2'-二硫代双乙烷磺酸盐增强抗肿瘤活性 的顺铂在治疗癌症患者时。 本发明还教导了含有2,2'-二硫代双 - 乙烷磺酸盐的单独或与顺铂联合使用的冻干或溶解在水性制剂中的新型制剂,其可以施用于正在用顺铂治疗的癌症患者。 本发明还教导了制备所述制剂的方法及其在预防顺铂相关毒性和增强顺铂抗肿瘤活性方面的用途。

    Pharmaceutical formulations of poorly water soluble camptothecin
analogues and NMP
    9.
    发明授权
    Pharmaceutical formulations of poorly water soluble camptothecin analogues and NMP 失效
    药用配方水溶性差的喜树碱类似物和NMP

    公开(公告)号:US5955467A

    公开(公告)日:1999-09-21

    申请号:US955956

    申请日:1997-10-22

    摘要: A- and/or B-ring substituted camptothecin derivatives, which are poorly water soluble (less than 5 micrograms per milliliter of water), are highly lipophilic camptothecin derivatives (HLCD) and are very active against a variety of human cancers. Because of their very poor water solubility, HLCD have not been used to treat human patients with cancer due to the inability to administer sufficient quantities of the HLCD dissolved in a pharmaceutical formulation. This invention overcomes these limitations by teaching novel pharmaceutically acceptable HLCD formulations for the direct administration of HLCD to human patients with cancer. The claimed invention also describes the methods to create solutions of HLCD and antitumor compositions of HLCD to allow the administration of HLCD in sufficient amounts to treat human patients with various types of cancer. This invention is also directed to injectable sterile solutions, antitumor compositions, solutions and suspensions comprising N-methyl-2-pyrrolidinone and a highly lipophilic camptothecin derivative.

    摘要翻译: A-和/或B-环取代的喜树碱衍生物,其水溶性差(小于5微克/毫升水)是高度亲脂性的喜树碱衍生物(HLCD),并且对多种人类癌症非常有活性。 由于水溶性非常差,由于不能施用足够量的溶解在药物制剂中的HLCD,HLCD不能用于治疗癌症患者。 本发明克服了这些限制,通过教导用于将HLCD直接给予癌症患者的HLCD的药学上可接受的HLCD制剂。 所要求保护的发明还描述了创建HLCD和HLCD抗肿瘤组合物的溶液的方法,以允许以足够的量施用HLCD来治疗患有各种类型的癌症的患者。 本发明还涉及可注射的无菌溶液,抗肿瘤组合物,包含N-甲基-2-吡咯烷酮和高亲脂性喜树碱衍生物的溶液和悬浮液。