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亲水性天然胶在盐酸曲马多缓释骨架片制剂中的应用。

Use of hydrophilic natural gums in formulation of sustained-release matrix tablets of tramadol hydrochloride.

作者信息

Varshosaz Jaleh, Tavakoli Naser, Kheirolahi Fatemeh

机构信息

Department of Pharmaceutics, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

AAPS PharmSciTech. 2006 Mar;7(1):E168-E174. doi: 10.1208/pt070124. Epub 2017 Mar 8.

Abstract

The objective of this work was to develop matrix sustained-release tablets of highly water-soluble tramadol HCl using natural gums (xanthan [X gum] and guar [G gum]) as cost-effective, nontoxic, easily available, and suitable hydrophilic matrix systems compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose [HPMC]/carboxymethyl cellulose [CMC] with respect to in vitro drug release rate) and hydration rate of the polymers. Matrix tablets of tramadol (dose 100 mg) were produced by direct compression method. Different ratios, of 100∶0, 80∶20, 60∶40, 20∶80, 0∶100 of G gum (or X):HPMC, X gum:G gum, and triple mixture of these polymers (G gum, X gum, HPMC) were applied. After evaluation of physical characteristics of tablets, the dissolution test was, performed in the phosphate buffer media (pH 7.4) up to 8 hours. Tablets with only X had the highest mean dissolution time (MDT), the least dissolution efficiency (DE%), and released the drug following a zero-order model via swelling, diffusion, and erosion mechanisms. Guar gum alone could not efficiently control the drug release, while X and all combinations of natural gums with HPMC could retard tramadol HCl release. However, according to the similarity factor (f ), pure HPMC and HG were the most similar formulations to Topalgic-LP as the reference standard.

摘要

本研究的目的是使用天然胶(黄原胶[X胶]和瓜尔胶[G胶])开发高水溶性盐酸曲马多的基质缓释片,与广泛研究的亲水性基质(即羟丙基甲基纤维素[HPMC]/羧甲基纤维素[CMC],就体外药物释放速率而言)相比,天然胶具有成本效益高、无毒、易于获得且合适的亲水性基质系统,同时还研究了聚合物的水化速率。通过直接压片法制备了曲马多(剂量100mg)的基质片。应用了不同比例的G胶(或X胶):HPMC、X胶:G胶以及这些聚合物的三元混合物(G胶、X胶、HPMC),比例分别为100∶0、80∶20、60∶40、20∶80、0∶100。在评估片剂的物理特性后,在磷酸盐缓冲介质(pH 7.4)中进行了长达8小时的溶出试验。仅含X胶的片剂平均溶出时间(MDT)最长,溶出效率(DE%)最低,并且通过溶胀、扩散和侵蚀机制遵循零级模型释放药物。单独的瓜尔胶不能有效地控制药物释放,而X胶以及天然胶与HPMC的所有组合都可以延缓盐酸曲马多的释放。然而,根据相似因子(f),纯HPMC和HG是与作为参比标准的Topalgic-LP最相似的制剂。

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