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    • 3. 发明授权
    • Pharmaceutically acceptable salts containing local anesthetic and anti-inflammatory activities and methods for preparing the same
    • 含有局部麻醉剂和抗炎活性的药学上可接受的盐及其制备方法
    • US07166641B2
    • 2007-01-23
    • US10262098
    • 2002-10-02
    • Fang-Yu LeeShan-Chiung ChenBin-Ken ChenChiung-Ju TsaiYen-Ling Yi
    • Fang-Yu LeeShan-Chiung ChenBin-Ken ChenChiung-Ju TsaiYen-Ling Yi
    • A61K31/195A61K31/19
    • C07D487/04A61K31/167A61K31/196A61K45/06C07C229/42C07C237/04Y10S514/97A61K2300/00
    • The present invention provides pharmaceutically acceptable salts having local anesthetic and anti-inflammatory activities. The preferred pharmaceutically acceptable salt is a diclofenac salt of lidocaine. Diclofenac is a non-steroidal anti-inflammatory drug (“NSAID”). Lidocaine is a local anesthetic. Other NSAID (except the salicylic acid derivatives of NSAID) can be used to replace diclofenac and/or other local anesthetics can be used to replace lidocaine. The pharmaceutically acceptable salts are crystalline compounds, which are distinctively different from either the NSAID alone or the local anesthetic alone, as indicated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), High Performance Liquid Chromatography (HPLC) and Fourier-Transformed Infrared Spectroscopy (FTIR) analyses. These pharmaceutically acceptable salts are suitable for use in topical treatment or parenteral injection to treat patients with localized pain, including muscle pain, joint pain, pain associated with herpes infection, and wound pain (such as surgical wound, burn wound etc.).
    • 本发明提供具有局部麻醉和抗炎活性的药学上可接受的盐。 优选的药学上可接受的盐是利多卡因的双氯芬酸盐。 双氯芬酸是非甾体抗炎药(“NSAID”)。 利多卡因是局麻药。 其他NSAID(NSAID的水杨酸衍生物除外)可用于替代双氯芬酸和/或其他局部麻醉剂,可用于替代利多卡因。 药学上可接受的盐是结晶化合物,它们与单独使用的NSAID或单独的局部麻醉剂明显不同,如差示扫描量热法(DSC),热重分析(TGA),高效液相色谱(HPLC)和傅里叶变换 红外光谱(FTIR)分析。 这些药学上可接受的盐适用于局部治疗或肠胃外注射以治疗局部疼痛的患者,包括肌肉疼痛,关节疼痛,与疱疹感染相关的疼痛和伤口疼痛(例如手术伤口,烧伤伤口等)。