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聚丙烯酸树脂RS 30D和滑石粉对药物层状基质包衣微丸中盐酸维拉帕米释放的影响。

Effect of Eudragit RS 30D and talc powder on verapamil hydrochloride release from beads coated with drug layered matrices.

作者信息

El-Malah Yasser, Nazzal Sami

机构信息

Department of Basic Pharmaceutical Sciences, College of Pharmacy, University of Louisiana at Monroe, Monroe, Louisiana 71209-0497, USA.

出版信息

AAPS PharmSciTech. 2008;9(1):75-83. doi: 10.1208/s12249-007-9008-6. Epub 2008 Jan 9.

Abstract

The aim of this study was to investigate the effect of Eudragit RS 30D, talc, and verapamil hydrochloride on dissolution and mechanical properties of beads coated with "drug-layered matrices". This was accomplished with the aid of a three-factor multiple-level factorial design using percent drug release in 1 and 2 h, T(50), tensile strength, brittleness, stiffness and toughness as the responses. Beads were coated in a fluidized-bed coating unit. Surface morphology and mechanical properties were evaluated by surface profilometry and texture analysis, respectively. No cracks, flaws and fissures were observed on the surfaces. The mechanical properties were dependent on the talc/polymer ratio. The release of verapamil from the beads was influenced by matrix components. Increasing the level of both talc and Eudragit decreased the percent drug released from 67% to 4.8% and from 80.7% to 6.7% in 1 and 2 h, respectively, and increased T(50) from 0.8 to 25.7 h. It was concluded that beads could be efficiently coated with "drug-layered matrices". The release of drug, however, depends on a balance between the levels of drug, talc, and polymer, whereby desired dissolution and mechanical properties could be controlled by the talc/polymer ratio and the level of drug loading.

摘要

本研究的目的是考察丙烯酸树脂RS 30D、滑石粉和盐酸维拉帕米对“药物层状基质”包衣微丸的溶出度和机械性能的影响。这是借助三因素多水平析因设计完成的,以1小时和2小时的药物释放百分比、T(50)、拉伸强度、脆性、硬度和韧性作为响应指标。微丸在流化床包衣装置中进行包衣。分别通过表面轮廓仪和纹理分析对表面形态和机械性能进行评估。在表面未观察到裂缝、瑕疵和裂隙。机械性能取决于滑石粉/聚合物比例。微丸中维拉帕米的释放受基质成分的影响。滑石粉和丙烯酸树脂水平的增加分别使1小时和2小时药物释放百分比从67%降至4.8%,从80.7%降至6.7%,并使T(50)从0.8小时增加至25.7小时。得出的结论是,微丸可以有效地用“药物层状基质”进行包衣。然而,药物的释放取决于药物、滑石粉和聚合物水平之间的平衡,由此可以通过滑石粉/聚合物比例和载药量来控制所需的溶出度和机械性能。

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