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    • 3. 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。