交联海藻酸钠制备利福昔明缓释片及评价

Wajid Ahmad, Rihan Sheikh, Razia Ahmad, Suhana Khan
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引用次数: 0

摘要

利福昔明通过阻止引起腹泻的细菌的生长来治疗旅行者腹泻和肠易激综合征。利福昔明治疗肝性脑病的方法是阻止产生毒素并可能使肝病恶化的细菌的生长。药物的半衰期短,给药频率高,是设计持续给药系统的合适人选。以海藻酸钠和交联海藻酸钠为原料制备利福昔明缓释基质片,并对其释放动力学进行评价。为了达到所需的缓释特性,采用湿造粒法制备了该片剂。对制剂的压缩前后参数进行了表征,均在可接受范围内。通过体外溶出试验获得药物释放数据,拟合各种释放动力学模型,以评价其释放机制和动力学。选择最佳拟合模型的标准是线性(相关系数)。发现药物释放机制遵循扩散,肿胀和侵蚀的复杂混合。该剂型具有控制药物释放速度和延长药物作用时间的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and Evaluation of Sustained Release Tablet of Rifaximin by using Cross linked Sodium Alginate
Rifaximin treats traveler's diarrhea and irritable bowel syndrome by stopping the growth of the bacteria that cause diarrhea. Rifaximin treats hepatic encephalopathy by stopping the growth of bacteria that produce toxins and that may worsen liver disease. The short half life and high frequency of administration of drug makes it a suitable candidate for designing sustained drug delivery system. The aim of the present investigation was to develop a sustained release matrix tablet of Rifaximin using sodium alginate and cross linked sodium alginate and to evaluate the drug release kinetics. In order to achieve the required sustained release profile, the tablets were prepared by a wet granulation method. The formulated tablets were characterized for pre-compression and post-compression parameters and they were in the acceptable limits. The drug release data obtained after an in vitro dissolution study was fitted to various release kinetic models in order to evaluate the release mechanism and kinetics. The criterion for selecting the best fit model was linearity (coefficient of correlation). Drug release mechanism was found to follow a complex mixture of diffusion, swelling and erosion. The dosage form holds the potential to control the release rate of drug and extend the duration of action of a drug.
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