结肠靶向环丙沙星微球的研制与评价

Ch. Srilatha, T Giriraj kulkarni
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引用次数: 0

摘要

在本研究中,配制了结肠靶向盐酸环丙沙星微球,并评估了其体外特性,以确定抗生素是否可以给药到结肠。以span-80为乳化剂,采用乳剂-溶剂蒸发法制备结肠靶向用环丙沙星微球。根据初步试验结果,药物与聚合物的比例对微球的性能有影响。采用环丙沙星:尤德拉吉S-100+HPMC 6cps的比例分别为1:1、1:2、1:3、1:4、1:5、1:6制备结肠靶向微球,尤德拉吉S-100与HPMC的比例始终为1:1。Eudragit S-100与HPMC联用后释放滞后时间增加,释放速率调节,增强了对含药核心的保护作用。对于大多数被检查的配方,在药物开始从微球中流出之前,由于水凝胶的肿胀/延迟行为导致的时间延迟导致零级释放。在三种不同的pH环境(0.1 N HCL,磷酸缓冲液pH 6.8和磷酸缓冲液pH 7.4)下,对结肠靶向微球进行了12小时的显微测量、粒度和表面性质、药物含量百分比、包封效果和体外释药研究。进一步研究了微球的体外释药动力学和释药机制。最佳配方批粒径58.9 m,粒径近似球形,具有自由流动的特点,包封效率最高,为86.81%。其次为零级释放,具有非虚构扩散机制,释药率为82.77%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Evaluation of Colon Targeted Ciprofloxacin Microspheres
In the present study, Colon-targeted Ciprofloxacin hydrochloride microspheres were formulated and their in vitro properties were assessed to determine whether or not the antibiotic could be delivered to the colon. By utilizing span-80 as an emulsifying agent, ciprofloxacin hydrochloride microspheres for colon targeting were prepared using the emulsion-solvent evaporation method. According to the preliminary trial findings, the ratio of drug to polymer had an impact on the microspheres' properties. The Ciprofloxacin: Eudragit S-100+HPMC 6cps ratio of 1:1, 1:2, 1:3, 1:4, 1:5, and 1:6 were used to make the colon targeting microspheres, in which the ratio of Eudragit S-100 to HPMC was always 1:1. The combination of Eudragit S-100 and HPMC demonstrated increased release lag time and regulated release rate, which improved protection of the drug-containing core. For the majority of the formulations examined, zero-order release followed a time delay caused by the hydrogel's swelling/retarding behaviour before the medication started to come out of the microspheres. The colon-targeting microspheres were also tested for micrometrics, particle size and surface properties, percentage drug content, encapsulation effectiveness, and in vitro drug release study in the three different pH environments (0.1 N HCL, Phosphate buffer pH 6.8 and Phosphate buffer pH 7.4) for 12 hours. The kinetics of drug release in vitro and the drug release mechanism of the microspheres were further investigated. With a particle size of 58.9 m, an almost spherical shape, and free-flowing characteristics, the best formulation batch had the highest drug entrapment efficiency of 86.81%. It was followed by a zero-order rate release with a non-fiction-diffusion mechanism, which had an 82.77% drug release rate.
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