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天然胶和纤维素衍生物在缓释美托洛尔片生产中的应用。

Use of natural gums and cellulose derivatives in production of sustained release metoprolol tablets.

作者信息

Varshosaz Jaleh, Tavakoli Nasser, Eram S Ali

机构信息

Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Drug Deliv. 2006 Mar-Apr;13(2):113-9. doi: 10.1080/10717540500313356.

Abstract

Metoprolol tartrate sustained-release tablets (100 mg) were prepared using xanthan/guar gums and also hydroxypropyl methyl cellulose (HPMC) carboxymethyl-Cellulose (CMC) polymers by direct compression method. Physical characteristics of the tablets and water uptake in addition to their dissolution profiles were compared with standard (Lopressor SR) tablets. Dissolution test was performed in the phosphate buffer solution (pH 6.8) and the samples were analyzed spectrophotometerically in 275.7 nm. Dissolution studies showed that formulations containing 100 and 80% of HPMC, 100% of guar, and 20% of xanthan followed the Higuchi model, while those containing 60 and 40% HPMC and 100 and 80% xanthan followed a zero-order model. The tablets with 40% xanthen followed a Hixon-Crowell model. In cellulose derivatives the highest MDT and dissolution efficiency until 8 hr (DE8%) belonged to tablets with 40% HPMC, increasing the amount of CMC decreased the drug release rate, and formulations containing 60 and 40% of HPMC had the USP dissolution standards. While, in the gum formulations, the highest mean dissolution time and the lowest DE(8)% belonged to tablets with 100% xanthan, increasing the xanthan decreased the release rate of metoprolol, and formulations containing 80 and 100% xanthan had the USP dissolution standards. Results showed that natural gums are suitable for production of sustained-release tablets of metoprolol.

摘要

采用直接压片法,使用黄原胶/瓜尔胶以及羟丙基甲基纤维素(HPMC)、羧甲基纤维素(CMC)聚合物制备了酒石酸美托洛尔缓释片(100毫克)。将这些片剂的物理特性、吸水性及其溶出曲线与标准(倍他乐克缓释片)片剂进行了比较。在磷酸盐缓冲溶液(pH 6.8)中进行溶出试验,并在275.7纳米处用分光光度计对样品进行分析。溶出度研究表明,含有100%和80% HPMC、100%瓜尔胶和20%黄原胶的制剂符合Higuchi模型,而含有60%和40% HPMC以及100%和80%黄原胶的制剂符合零级模型。含有40%黄原胶的片剂符合Hixon - Crowell模型。在纤维素衍生物中,直到8小时最高的平均溶出时间(MDT)和溶出效率(DE8%)属于含有40% HPMC的片剂,增加CMC的量会降低药物释放速率,含有60%和40% HPMC的制剂符合美国药典溶出标准。而在胶体制剂中,最高的平均溶出时间和最低的DE(8)%属于含有100%黄原胶的片剂,增加黄原胶会降低美托洛尔的释放速率,含有80%和100%黄原胶的制剂符合美国药典溶出标准。结果表明,天然胶适合用于生产美托洛尔缓释片。

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