A novel method for determination of drug solubility in polymeric matrices
A novel method for determination of drug solubility in polymeric matrices
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DOI：
10.1002/jps.20122
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发表时间：
2004-08-01
影响因子：
3.8
通讯作者：
Li, XL
中科院分区：
文献类型：
--
作者：
Jasti, BR;Berner, B;Li, XL
通过测定药物在粘性聚合物中的溶解度，可以避免药物在透皮药物递送装置中的亚稳、过饱和粘性聚合物基质中的结晶。描述了一种测定药物在聚合物基质中的溶解度的新方法。与现有的方法不同，该方法不需要长时间和不确定的实验时间，并且是准确的。本文根据药物的热力学活性与稳态流量之间的关系，提出了一种简便、准确的测定药物在聚合物中溶解度的方法。特别是，从参比饱和溶液穿过测试膜的稳态通量与实验确定的聚合物负载浓度和观察到的稳态通量之间的关系进行比较。该方法的有效性证明了通过比较结果的结晶的显微镜观察和老化的载药粘合剂的利多卡因作为模型药物和丙烯酸酯压敏粘合剂作为模型聚合物的研究。利多卡因在丙烯酸酯聚合物中的溶解度为20.8 +/- 0.5%（w/w）。(C)2004 Wiley-Liss，Inc.
Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing methods, this method does not require a long and uncertain experimental time, and is accurate. In this study, an easy and accurate method is presented for the determination of solubility of drugs in polymers based on the relationship between thermodynamic activity of drugs and steady-state flux. In particular, the steady-state flux from a reference saturated solution across a test membrane was compared to an experimentally determined relationship between the polymeric loading concentration and the observed steady-state fluxes. The validity of this method was demonstrated by comparing the results to microscopic observation of crystallization and the study of aged drug-loaded adhesives for lidocaine as a model drug and an acrylate pressure-sensitive adhesive as a model polymer. The solubility of lidocaine was 20.8 +/- 0.5% (w/w) in the acrylate polymer. (C) 2004 Wiley-Liss, Inc.