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Treatment of pain with combinations of nalbuphine and Kappa opioid receptor agonists and antagosnistas opioid receptor

机译:纳布啡和κ阿片受体激动剂和拟南芥阿片受体组合治疗疼痛

摘要

Methods and compositions to treat, manage, or relieve pain in a subject (preferably a Mammal, preferably a human being and more) that comprise the Administration of an agonist Action (i.e., centralCrosses the blood Brain Barrier) of an opioid receptor antagonist and an action so that apioides central analgesia achieved by this administration is higher than that achieved with the Administration of the opioid receptor agonist or antagonist apioides alone.Preferably, the opioid receptor is nalbuphine or a Salt or prodrug of nalbuphine, and opioid antagonist is a Salt or prodrug of naloxone or nalbuphine, and opioid antagonist naloxone or is a Salt or prodrug of noloxona. Preferred methods include the Administration of Administration (For example intranasal mucosal or Lung) and intravenosoa.Other recipients include opioid pentazocine and butorphanol.Claim 1: a method to treat Pain comprising administering to a indiiduo mucosal way that need such treatment (0.1 mg) of 0.8 mg of an opioid antagonist clohidrato of Ao a cantidaad equivalent of a Free Base, prodrug, or a mixture of non hydrochloride, L Os, antagonist of Opioid and opioid antagonist, where this is Naltrexone, naloxoneMethylnaltrexone, nalmefene, nalorphine, levalorfan, or oxilorfan cyprenorphine, and (b) an amount of Free based clohidrato, prodrug, non -, hydrochloride, or a mixture of mimsos of nalbuphine, which results in a Greater analgesia to the Administration of the opioid antagonist clohidrato Or that nalbuphine alone.Claim 3: a method according to claim 1, wherein the opioid antagonist naloxone or is a Salt or prodrug of naloxone.Claim 40: a Pharmaceutical composition which comprises (a) 0.1 to 0.8 mg mg a hydrochloride opioid antagonist or an equivalent amount of Free Base, prodrug, non hydrochloride, or mixture thereof, the opioid antagonist, wherein Said opioid antagonist Methylnaltrexone is naloxone, naltrexone and nalmefene, nalorphine, levalorfan,Oxilorfan or cyprenorphine; (b) an amount of Free Base nalbifina nalbuphine, Salt, prodrug of nalbuphine, or mixture thereof, which results in a Greater analgesia that nalbuphine Administration Component or component opioid antagonist alone; and (c) a vehicle AC Eptable for pharmaceutical use, being This composition formulated for mucosal Administration.
机译:治疗,控制或减轻受试者(优选哺乳动物,优选人类等)的疼痛的方法和组合物,其包括给予阿片样物质受体拮抗剂和激动剂的激动剂作用(即,中枢穿越血脑屏障)。这样的作用,使这种给药所获得的阿片类药物中枢镇痛作用高于单独使用阿片类药物受体激动剂或拮抗剂阿片类药物所达到的镇痛作用。阿片类药物受体最好是纳布啡或纳布啡的盐或前药,而阿片拮抗剂是盐或纳洛酮或纳布啡的前药,以及阿片样物质拮抗剂纳洛酮或诺洛索纳的盐或前药。优选的方法包括给药(例如鼻内粘膜或肺)和静脉内给药。其他接受者包括阿片类喷他佐辛和布托啡诺。权利要求1:一种治疗疼痛的方法,包括以个别粘膜方式给药需要这种治疗(0.1mg)的0.8 mg Ao的阿片样物质拮抗剂clohidrato,相当于游离碱,前药或非盐酸盐,LOs,阿片样物质拮抗剂和阿片样物质拮抗剂的混合物,其中纳曲酮,纳洛酮,甲基纳曲酮,纳美芬,纳洛啡,levalorfan或oxilorfan cyprenorphine和(b)一定量的游离基clohidrato,前药,非盐酸盐酸盐或纳布啡的混合物,导致服用阿片类药物clohidrato或单独使用那布啡的镇痛效果更大。Claim3 2.根据权利要求1的方法,其中阿片样物质拮抗剂纳洛酮或纳洛酮的盐或前药。权利要求40:药物组合物,其包含(a)0.1至0.8 mg mg的盐酸盐类阿片拮抗剂或同等量的游离碱,前药,非盐酸盐或其混合物,阿片类拮抗剂,其中所述阿片类拮抗剂甲基纳曲酮是纳洛酮,纳曲酮和纳美芬,纳洛芬,勒伐洛芬,奥昔洛芬或cyprenorphine; (b)一定量的游离碱纳尔比芬纳布啡,盐,纳布啡的前药或它们的混合物,可导致单独使用纳布啡给药组分或阿片样物质拮抗剂的镇痛作用更大; (c)可药用的载剂AC,其为配制用于粘膜给药的组合物。

著录项

  • 公开/公告号AR042463A1

    专利类型

  • 公开/公告日2005-06-22

    原文格式PDF

  • 申请/专利权人 THE REGENTS OF THE UNIVERSITY OF CALIFORNIA;

    申请/专利号AR2003P104609

  • 发明设计人

    申请日2003-12-12

  • 分类号A61K31/485;A61K31/439;A61P25/04;

  • 国家 AR

  • 入库时间 2022-08-21 22:18:49

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