A thermal analysis method to predict the complete phase diagram of drug-polymer solid dispersions
A thermal analysis method to predict the complete phase diagram of drug-polymer solid dispersions
复制标题
预测药物-聚合物固体分散体完整相图的热分析方法
DOI：
10.1016/j.ijpharm.2010.08.013
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发表时间：
2010-10-31
影响因子：
5.8
通讯作者：
Huang, Yanbin
中科院分区：
文献类型：
--
作者：
Lin, Dexi;Huang, Yanbin
这项工作的目的是开发一种方法，使用实验获得的数据来预测药物-聚合物固体分散体系统的完整相图，在文献中的第一次。以非洛地平-聚丙烯酸（PAA）固体分散体为例说明了该方法的应用。制备具有不同载药量的样品，并使用差示扫描量热法（DSC）进行分析。根据药物晶体熔点降低数据计算药物-聚合物相互作用参数chi（T-m）的值。由于根据Flory-Huggins理论，chi是温度的函数（chi类似于1/T），因此获得的chi-T关系使得能够计算药物-聚合物固体分散体系统的完整温度-组成相图。在实验中，非洛地平被证明是不混溶与PM在几乎整个范围内的药物含量在室温下。观察到两个玻璃化转变温度，分别对应于几乎纯非洛地平和纯PM，与预测的相行为一致。(C)2010爱思唯尔有限公司版权所有。
The aim of this work was to develop a method which uses experimentally obtainable data to predict the complete phase diagram of drug-polymer solid dispersion systems, for the first time in literature. Felodipine-poly(acrylic acid) (PAA) solid dispersion was used as an example to illustrate the application of this method. Samples were prepared with different drug loading and analyzed using differential scanning calorimetry (DSC). Values of the drug-polymer interaction parameter chi(T-m) were calculated from the drug crystal melting point depression data. Since chi is a function of temperature (chi similar to 1/T) according to the Flory-Huggins theory, the obtained chi-T relationship thus enabled calculation of the complete temperature-composition phase diagram of a drug-polymer solid dispersion system. In experiments, felodipine was shown to be immiscible with PM in almost the whole range of drug content at room temperature. Two glass transition temperatures were observed, corresponding to almost pure felodipine and pure PM, respectively, in consistent with the predicted phase behavior. (C) 2010 Elsevier B.V. All rights reserved.