佐米曲坦控释给药系统的配方开发及体外表征

Shambhavi Pandala, V. Bakshi, R. Jadi
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引用次数: 3

摘要

背景:佐米曲坦是一种人工色胺,用于急性治疗伴有或不伴有先兆和丛集性头痛的偏头痛发作。目的:研制安全有效治疗偏头痛的佐米曲坦基质缓释片(ZMT)。方法:采用天然聚合物或瓜尔胶、黄原胶、卡拉亚胶等胶,采用6mm冲孔直接加压法制备。结果:采用不同比例(5%、10%、15%和20%)的配方(F1 - F12)的粉末共混物进行了预压缩参数(休歇角、容重、攻丝密度、压缩指数、豪斯纳比、相容性研究)和压缩后参数(重量变化、厚度、脆度、硬度、含量、体外溶出度研究)的表征。用卡拉亚胶制备F1 - F4配方,并与剩余胶进行比较;Gum karaya表现出更强的迟滞能力。加瓜尔胶的F9 ~ F12不能达到理想的缓释效果,而加黄原胶的F5 ~ F8随着聚合物浓度的增加表现出较好的缓释效果。结论:对制备的配方(F1 - F12)进行了表征,并对F3配方进行了优化(8 h释药97.3%)。所有制备的配方(F1 - F12)均表现出良好的流动性能和释放模式。因此,ZMT基质片的制剂具有很好的给药系统,可以提高生物利用度,获得更大的治疗效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation Development and In Vitro Characterization of Zolmitriptan Controlled Release Drug Delivery Systems
Background: Zolmitriptan is an artificial tryptamine, employed for the acute cure of migraine attack with or exclusive of aura and cluster headaches. Objective: It is an attempt to develop the extended release (ER) of Zolmitriptan matrix (ZMT) tablets to treat migraine safely and effectively. Methods: All formulations were prepared with natural polymers or gums like guar gum, xanthan gum, karaya gum through direct compression method using 6mm punch. Results: Powder blend of all formulations (F1 - F12) using different ratios of the above mentioned gums (5%, 10%, 15% and 20%) were characterized with pre-compression parameters (angle of repose, bulk density, tapped density, compressibility index, hausner ratio, compatibility studies) and post-compression parameters (weight variation, thickness, friability, hardness, assay, in vitro dissolution studies). F1 - F4 formulations were prepared with gum karaya and compared with remaining gums; gum karaya shows more retardance capacity. F9 - F12 (with guar gum) formulations were unable to produce the desired release, whereas F5 - F8 formulations containing with xanthan gum exhibited more retarding effect with increasing concentration of polymer. Conclusion: All prepared formulations (F1 - F12) were characterized and F3 formulation was optimized (97.3% drug released in 8 hours). All prepared formulations (F1 - F12) showed good flow properties and release patterns. Hence, formulations of ZMT matrix tablets have a promising delivery system which will enhance bio-availability and achieve greater therapeutic efficacy.
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