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甲基丙烯酸和羟丙基甲基纤维素对氢溴酸右美沙芬片剂性质及体外释放的影响

Influence of methacrylic acid and hydroxypropylmethyl cellulose on the tablet properties and in vitro release of dextromethorphan hydrobromide.

作者信息

Takka S, Singh Bharaj S, Sakr A

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Gazi, Ankara, Turkey.

出版信息

Pharmazie. 2003 Dec;58(12):886-90.

Abstract

The release of dextromethorphan hydrobromide from matrices containing hydroxypropylmethyl cellulose (HPMC K100LV) and methacrylic acid copolymer (Eudragit L100-55) has been evaluated at different ratios of the polymers. The physicochemical properties (including weight, thickness, crushing strengh, friability and disintegration time) were also determined at 1000, 2000 and 4000 p compression forces. No significant differences in weight uniformity and thickness values were observed between the different formulations. The crushing strength of the tablets increased with increasing compression force and it reached a constant level at 4000 p. The formulations containing only HPMC K100LV resulted in an extended release pattern, however, Eudragit L100-55 alone could not effectively prolong the drug release. A combination of HPMC K100LV and Eudragit L100-55 in a 1:1 ratio at the 40% level provided an almost similar drug release profile than the marketed product.

摘要

已评估了含羟丙基甲基纤维素(HPMC K100LV)和甲基丙烯酸共聚物(Eudragit L100 - 55)的基质中氢溴酸右美沙芬在不同聚合物比例下的释放情况。还在1000、2000和4000磅的压缩力下测定了其物理化学性质(包括重量、厚度、抗压强度、脆碎度和崩解时间)。不同制剂之间在重量均匀度和厚度值方面未观察到显著差异。片剂的抗压强度随压缩力增加而提高,并在4000磅时达到恒定水平。仅含HPMC K100LV的制剂呈现缓释模式,然而,单独的Eudragit L100 - 55不能有效延长药物释放。在40%水平下,HPMC K100LV和Eudragit L100 - 55以1:1比例组合提供了与市售产品几乎相似的药物释放曲线。

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