左氧氟沙星基质缓释片治疗微生物感染的设计与评价

B. Wilson, Patel Hardikkumar Sitarambhai, M. S. Sajeev, G. Vinothapooshan
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引用次数: 12

摘要

目的:制备左氧氟沙星基质缓释片,并对其治疗微生物感染的效果进行评价。左氧氟沙星是氧氟沙星外消旋体的有效成分,用于治疗多种临床病症,如下呼吸道感染、急性鼻窦炎、无并发症的皮肤软组织感染、并发症的尿路感染等。采用不同的控制释放速率的亲水聚合物,采用湿造粒法制备了不同的配方。对配方进行硬度、重量变化、脆性和药物含量均匀性评价。在pH为1.2的酸性缓冲液和pH为6.8的磷酸盐缓冲液中对制剂的体外释放进行了研究,发现所制片剂具有缓释作用。左氧氟沙星片的释放为扩散控制,释放机制为非菲克式。综上所述,所开发的制剂可以缩短给药间隔,减少剂量相关副作用,提高药物治疗感染的疗效。关键词:基质片,左氧氟沙星,HPMC,瓜尔胶,黄原胶,刺槐豆胶,魔芋淀粉
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design and evaluation of sustained release matrix tablets of levofloxacin for effective treatment of microbial infections
The objective of present work was to formulate and evaluate sustained release matrix tablets of levofloxacin for treating microbial infections effectively. Levofloxacin is the active component of the racemate ofloxacin, and used for treating a variety of clinical conditions such as lower respiratory tract infections, acute sinusitis, uncomplicated skin and soft-tissue infections and complicated urinary tract infections. Different formulations were prepared by wet granulation method using various release rate controlling hydrophilic polymers. The formulations were evaluated for hardness, weight variation, friability and drug content uniformity. The in vitro release of drug from the formulations was studied in pH 1.2 acidic buffer and pH 6.8 phosphate buffer, and it was found that the prepared tablets were able to sustain the release of the drug. The release of levofloxacin from the tablets was diffusion controlled and the release mechanism was non-Fickian. For conclusion, the developed formulations may reduce the dosing intervals, reduce the dose related side effects and increase the drug’s efficacy for treating infections. Keywords: Matrix tablets, levofloxacin, HPMC, guar gum, xantham gum, locust bean gum, Amorphophallus starch.
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