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非那西丁固体分散体的溶解热力学与红外光谱

Thermodynamics of dissolution and infrared-spectroscopy of solid dispersions of phenacetin.

作者信息

Gerasimov Alexander V, Varfolomeev Mikhail A, Ziganshin Marat A, Gorbatchuk Valery V, Rakipov Il'naz T, Klimovitskii Alexander E, Usmanova Liana S

机构信息

Department of Physical Chemistry, Butlerov Institute of Chemistry, Kazan Federal University, Kremlevskaya 18, Kazan 420008, Russia.

出版信息

J Adv Pharm Technol Res. 2016 Jan-Mar;7(1):6-12. doi: 10.4103/2231-4040.169874.

Abstract

In this work enthalpies of dissolution in water of polyethylene glycols (PEGs) having an average molecular weight of 1000 and 1400, Pluronic-F127, phenacetin as well as the composites prepared from them were measured using solution calorimetry at 298.15 K. Intermolecular interaction energies of polymer-phenacetin were calculated on the basis of an additive scheme. It was shown that for mixtures with high content of polymer (>90 wt%) Pluronic-F127 has the highest solubilizing effect, while for mixtures with (4-6):1 polymer: phenacetin ratio the best solubilizing agent is PEG-1400. Infrared-spectra showed a decrease of the number of self-associated molecules of phenacetin with increasing of polymer content in the composites. The obtained results enabled us to identify the features of intermolecular interactions of polymers with a model hydrophobic drug and may be used for optimizing the conditions for preparing solid dispersions based on hydrophilic polymers.

摘要

在这项工作中,使用溶液量热法在298.15 K下测量了平均分子量为1000和1400的聚乙二醇(PEG)、普朗尼克-F127、非那西丁以及由它们制备的复合材料在水中的溶解焓。基于加和方案计算了聚合物-非那西丁的分子间相互作用能。结果表明,对于聚合物含量高(>90 wt%)的混合物,普朗尼克-F127具有最高的增溶效果,而对于聚合物与非那西丁比例为(4-6):1的混合物,最佳增溶剂是PEG-1400。红外光谱显示,随着复合材料中聚合物含量的增加,非那西丁自缔合分子的数量减少。所得结果使我们能够确定聚合物与模型疏水药物分子间相互作用的特征,并可用于优化基于亲水性聚合物制备固体分散体的条件。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3702/4759984/acd172f884cc/JAPTR-7-6-g002.jpg

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