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1. 发明申请

WO2017053936A8 COCRYSTALS OF NALOXONE AND NALTREXONE 审中-公开
标题翻译：纳洛酮和NALTREXONE的共晶体
公开(公告)号：WO2017053936A8
公开(公告)日：2017-04-27
申请号：PCT/US2016053695
申请日：2016-09-26
申请人： PAIN THERAPEUTICS INC , ZAMLOOT MICHAEL
发明人： ZAMLOOT MICHAEL , BARBIER REMI , FRIEDMANN NADAV , SRIRANBHATLA VIJAY , WATT SEPHEN
IPC分类号： A61M11/00 , A61J1/00 , A61K9/00 , A61K31/485
CPC分类号： A61K9/7084 , A61K9/14 , A61K9/7038 , A61K31/485
摘要： This invention relates to cocrystals of naloxone and of naltrexone and thier use as opioid antagonists. The cocrystais of the invention include naloxone isonicotinamide cocrystal, naloxone hydrochloride piperazine cocrystal, naltrexone menthol cocrystal, naltrexone thymine cocrystal, naltrexone 2,5-dihydroxybenzoic acid cocrystal, naltrexone salicylic acid cocrystal, naltrexone hydrochloride piperazine cocrystal and naltrexone hydrochloride sulfathiazole cocrystal. A drug-in¬ adhesive transdermal patch con taining the opioid analgesic fentanyl or an analog thereof and a cocrystal of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof. Also disclosed is an improved transdermal patch for administering fentanyl or an analog thereof, or for administering a mu opioid agonist, the improvement wherein the transdermal patch contains a cocrystal of the invention in an abuse limiting amount. The improved transdermal patch may be a drug-in-adhesive transdermal patch or a reservoir transdermal patch.
摘要翻译：本发明涉及纳洛酮和纳曲酮的共结晶以及它们作为阿片样物质拮抗剂的用途。本发明的共晶体包括纳洛酮异烟酰胺共晶体，盐酸纳洛酮哌嗪共晶体，纳曲酮薄荷醇共晶体，纳曲酮胸腺嘧啶共晶体，纳曲酮2,5-二羟基苯甲酸共晶体，纳曲酮水杨酸共晶体，纳曲酮盐酸盐哌嗪共晶体和纳曲酮盐酸盐磺胺噻唑共晶体。公开了包含阿片样镇痛芬太尼或其类似物和纳络酮或纳曲酮共晶体的药物粘附透皮贴剂。还公开了通过将本发明的药物粘附型透皮贴剂应用于有需要的患者的皮肤来治疗疼痛（例如急性，慢性或间歇性疼痛）的方法。还公开了用于施用芬太尼或其类似物或用于施用mu阿片样物质激动剂的改进的透皮贴剂，其中透皮贴剂含有滥用限制量的本发明共结晶。改进的透皮贴剂可以是药物粘附透皮贴剂或储库透皮贴剂。

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