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    • 5. 发明申请
    • Extended release formulations of poorly soluble antibiotics
    • 难溶性抗生素的延长释放制剂
    • US20060193908A1
    • 2006-08-31
    • US11267943
    • 2005-11-04
    • Beth BurnsideColin RowlingsSandra WassinkDonald TreacyJohn Koleng
    • Beth BurnsideColin RowlingsSandra WassinkDonald TreacyJohn Koleng
    • A61K31/7048A61K9/20
    • A61K9/2077A61K9/2009A61K9/2018A61K31/7048
    • An extended release pharmaceutical compressed composition and dosage form comprising poorly water soluble macrolide antibiotic, surfactant and non-lipophilic, non-polymeric excipient is disclosed. The composition releases the macrolide antibiotic over an extended period of time, generally at least over 12 hours, even in the absence of a release rate-retarding polymer, release rate-retarding coating or release rate-retarding lipophilic excipient. The composition is suitable for once daily or twice daily oral administration for the treatment of many different types of bacterial infections. One embodiment of the compressed composition includes a drug-containing granular composition and a binding composition, wherein the two are mixed together and then compressed into a tablet or pill. The surfactant is in admixture with or coated onto the macrolide antibiotic, and it can be included in the granular composition and/or the binding composition. The non-polymeric, non-lipophilic excipient is included in the granular composition and/or the binding composition.
    • 公开了包含难溶于水的大环内酯类抗生素,表面活性剂和非亲脂性非聚合物赋形剂的延长释放药物压缩组合物和剂型。 即使在没有释放速率阻滞性聚合物,释放速率阻滞涂层或释放速率延缓的亲脂性赋形剂的情况下,该组合物延长的时间段(通常至少超过12小时)释放大环内酯类抗生素。 该组合物适合于每天一次或每天两次口服给药以治疗许多不同类型的细菌感染。 压缩组合物的一个实施方案包括含药物的颗粒组合物和结合组合物,其中两者混合在一起,然后压制成片剂或药丸。 表面活性剂与大环内酯类抗生素混合或涂覆在其上,并且可以包含在颗粒组合物和/或粘合组合物中。 非聚合的非亲脂性赋形剂包括在颗粒组合物和/或粘合组合物中。
    • 6. 发明申请
    • Compressed composition comprising magnesium salt
    • 包含镁盐的压缩组合物
    • US20050220865A1
    • 2005-10-06
    • US10816771
    • 2004-04-02
    • John KolengMichael Crowley
    • John KolengMichael Crowley
    • A61K9/20A61K9/48A61K33/06A61K33/08A61K33/10
    • A61K9/2095A61K9/2054A61K9/2077A61K33/06A61K33/08A61K33/10
    • An oral solid compress composition comprising a magnesium salt is provided. The composition provides a rapid dissolution of the magnesium salt, wherein not less than 75% of the magnesium salt dissolves within 45 minutes after placement in hydrochloric acid (0.1 N, 900 mL) as per USP Method . In a particular embodiment, the magnesium salt is an inorganic salt such as MgO, Mg(OH)2, MgCl2, and others. The composition can be prepared by dry granulation, direct compression or another suitable process. The composition provides a substantially stable dissolution profile for the magnesium salt so that the dissolution profile changes only minimally even after an extended period of storage under pharmaceutically acceptable conditions when packaged in a sealed container-enclosure system. The solid composition may also exclude a cellulose-based composition. The compressed composition can be prepared and stored under anhydrous conditions.
    • 提供包含镁盐的口服固体压片组合物。 该组合物提供镁盐的快速溶解,其中不少于75%的镁盐在按照USP Method <711>放入盐酸(0.1N,900mL)后45分钟内溶解。 在一个具体实施方案中,镁盐是无机盐,例如MgO,Mg(OH)2,MgCl 2等。 组合物可以通过干法制粒,直接压片或其它合适的方法制备。 组合物为镁盐提供基本上稳定的溶出曲线,使得即使在包装在密封的容器 - 包封系统中的药学上可接受的条件下长时间的储存后,溶出曲线也仅最小化。 固体组合物还可以排除基于纤维素的组合物。 压缩的组合物可以在无水条件下制备并储存。