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使用增塑剂从乙烯-醋酸乙烯酯基质中控制释放普拉洛芬。

Controlled release of pranoprofen from the ethylene-vinyl acetate matrix using plasticizer.

作者信息

Cho Cheong-Weon, Choi Jun-Shik, Shin Sang-Chul

机构信息

College of Pharmacy, Chungnam National University, Daejeon, South Korea.

出版信息

Drug Dev Ind Pharm. 2007 Jul;33(7):747-53. doi: 10.1080/03639040601012965.

Abstract

An ethylene-vinyl acetate (EVA) matrix containing pranoprofen was prepared using the casting method and the release patterns of pranoprofen were observed. The solubility of pranoprofen was determined to be a function of the volume fraction of polyethylene glycol 400. The release of the drug from the matrix was examined as a function of temperature and drug concentration. Plasticizers such as the citrates and the phthalates were added to prepare the membrane in order to increase the flexibility of the EVA matrix. The solubility of pranoprofen was the highest when the PEG 400 concentration was 20% (v/v). The rate of drug release from the EVA matrix increased with increasing temperature and drug loading dose. There was a linear relationship between the flux of pranoprofen and the square root of the loading dose. The activation energy of release (Ea), which was measured from the slope of the log P versus 1000/T plots, was estimated to be 17.44, 16.14, 14.88, and 14.78 kcal/mol for loading doses of 0.5, 1, 1.5, and 2%, respectively. Among the plasticizers used such as the citrate and the phthalate groups, diethyl phthalate had the best enhancing effects on drug release. In conclusion, the application of an EVA matrix containing a plasticizer might be useful in the development of a controlled drug delivery system.

摘要

采用流延法制备了含普拉洛芬的乙烯 - 醋酸乙烯酯(EVA)基质,并观察了普拉洛芬的释放模式。测定了普拉洛芬的溶解度是聚乙二醇400体积分数的函数。研究了药物从基质中的释放与温度和药物浓度的关系。添加柠檬酸盐和邻苯二甲酸盐等增塑剂来制备膜,以提高EVA基质的柔韧性。当聚乙二醇400浓度为20%(v/v)时,普拉洛芬的溶解度最高。药物从EVA基质中的释放速率随温度和载药量的增加而增加。普拉洛芬的通量与载药量的平方根之间存在线性关系。从log P对1000/T图的斜率测得的释放活化能(Ea),对于载药量分别为0.5%、1%、1.5%和2%时,估计为17.44、16.14、14.88和14.78 kcal/mol。在所使用的柠檬酸盐和邻苯二甲酸盐类增塑剂中,邻苯二甲酸二乙酯对药物释放的增强效果最佳。总之,含增塑剂的EVA基质在控释给药系统的开发中可能具有应用价值。

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