Dissolution mechanism of poorly water-soluble drug from extended release solid dispersion system with ethylcellulose and hydroxypropylmethylcellulose
Dissolution mechanism of poorly water-soluble drug from extended release solid dispersion system with ethylcellulose and hydroxypropylmethylcellulose
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DOI：
10.1016/j.ijpharm.2005.06.019
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发表时间：
2005-09-30
影响因子：
5.8
通讯作者：
Terada, K
中科院分区：
文献类型：
--
作者：
Ohara, T;Kitamura, S;Terada, K
本研究的目的是探究难溶性药物从含有水不溶性乙基纤维素（EC）和水溶性羟丙基甲基纤维素（HPMC）（1∶1）的缓释固体分散体系中的释放机制。吲哚美辛（IND）被用作难溶性药物的模型。通过溶剂蒸发法制备了两种固体分散体，它们配方相同但物理性能不同。结果表明，IND的溶出行为取决于EC - HPMC基质的结构，而该结构受制备方法的控制。此外，溶出行为呈现pH依赖性，即IND在酸性介质中的溶出速率比在中性介质中慢。实验结果显示，在较低pH值下，IND和EC之间发生疏水相互作用，极大地延缓了IND的溶出速率。还提出了这种疏水相互作用与IND溶出速率之间的关系。（c）2005爱思唯尔有限公司。保留所有权利。
The purpose of this Study is to investigate the release mechanism of poorly water-soluble drug from the extended release solid dispersion systems with water-insoluble ethylcellulose (EC) and water-soluble hydroxypropylmethylcellulose (HPMC) (1:1). Indomethacin (IND) was used as a model of poorly water-soluble drug. Two kinds of solid dispersions were prepared by the solvent evaporation methods, which consist of the same formulation but exhibit different physical performance. It appeared that the dissolution behavior of IND depended on the structures of EC-HPMC matrices, which were governed by the preparation method. In addition, the dissolution behavior showed pH dependency that the dissolution rate of IND was slower in acidic medium than that in neutral medium. The experimental results revealed that the hydrophobic interaction between IND and EC occurred under lower pH and strongly delayed the dissolution rate of IND. The relationship between this hydrophobic interaction and the dissolution rate of IND was also proposed. (c) 2005 Elsevier B.V. All rights reserved.