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    • 2. 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)。
    • 7. 发明授权
    • Orally administrable nifedipine pellet and process for the preparation thereof
    • 口服给药的硝苯地平丸剂及其制备方法
    • US06168806A
    • 2001-01-02
    • US09263693
    • 1999-03-05
    • Fang-Yu LeeShan-Chiung ChenHan-Chiang Kuo
    • Fang-Yu LeeShan-Chiung ChenHan-Chiang Kuo
    • A61K916
    • A61K31/4422A61K9/1676A61K9/5078Y10S514/962
    • The present invention relates to a fast-release as well as a prolonged release type of nifedipine pellets and the process for the preparation thereof. The fast-release type of nifedipine pellets comprises a particulate core which is covered by a nifedipine coating layer. The particulate core comprises water-soluble or water-insoluble excipient(s) and a pharmacologically acceptable carrier. The nifedipine coating layer comprises an effective amount of nifedipine dissolved in organic solvent(s). This nifedipine coating layer can further be mixed with a suspension which comprises an adhesive, an emulsifier, and a dispersant. The preferred composition of the fast-release type of nifedipine includes 20-70% of the particulate core, 3-15% of nifedipine, 1-20% of emulsifier, 1-20% of adhesive, and 1-30% of dispersant. The prolonged-release type of nifedipine pellets comprises, in addition to the particulate core and the nifedipine coating layer, a surface coating layer which is made of at lease one consisting of hydroxypropylcellulose, hydroxypropylmethylcellulose and ethylcellulose. This surface coating layer further comprises a plasticizer which is selected from the group consisting of triethylcitrate, triacetin, and diethyl phthalate.
    • 本发明涉及快速释放和延缓释放型硝苯地平丸剂及其制备方法。 硝苯地平丸剂的快速释放类型包括被硝苯地平涂层覆盖的颗粒芯。 颗粒核心包括水溶性或水不溶性赋形剂和药理学上可接受的载体。 硝苯地平涂层包含溶解在有机溶剂中的有效量的硝苯地平。 该硝苯地平涂层可以进一步与包含粘合剂,乳化剂和分散剂的悬浮液混合。 快速释放型硝苯地平的优选组成包括20-70%的颗粒核,3-15%的硝苯地平,1-20%的乳化剂,1-20%的粘合剂和1-30%的分散剂。 硝苯地平丸剂的延长释放型除了颗粒状核心和硝苯地平涂层外还包含由至少由羟丙基纤维素,羟丙基甲基纤维素和乙基纤维素组成的表面涂层。 该表面涂层还包含选自柠檬酸三乙酯,三醋精和邻苯二甲酸二乙酯的增塑剂。