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尤特奇凝胶的制备与评价。II:水杨酸、水杨酸钠和酮洛芬从尤特奇L和S有机凝胶中的体外释放

Preparation and evaluation of Eudragit gels. II: In vitro release of salicylic acid, sodium salicylate, and ketoprofen from Eudragit L and S organogels.

作者信息

Kawata M, Suzuki T, Kim N S, Ito T, Kurita A, Miyagoe Y, Goto S

机构信息

Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.

出版信息

J Pharm Sci. 1991 Nov;80(11):1072-4. doi: 10.1002/jps.2600801115.

Abstract

The in vitro dissolution characteristic of salicylic acid, sodium salicylate, and ketoprofen from Eudragit L and S organogels was investigated by the rotation disk method. The dissolution pattern of salicylic acid and erosion of Eudragit L polymer from the organogels followed apparent zero-order kinetics, providing strong evidence for a surface erosion mechanism and negligible diffusional release of salicylic acid. On the other hand, the dissolution of salicylic acid from Eudragit S organogels was a linear function of the square root of time. The apparent dissolution rate of salicylic acid from Eudragit S organogels increased with increasing temperature from 32 to 42 degrees C and agitation rate from 50 to 200 rpm. A linear relationship was obtained between the logarithm of apparent dissolution rate constants and the reciprocal of absolute temperatures. The activation energy for release of salicylic acid from Eudragit S organogels was in the range of 2.99 to 5.57 kcal/mol. From various experimental results, it was concluded that the release process of salicylic acid from Eudragit S organogels was diffusion controlled through the organogels matrix.

摘要

采用旋转圆盘法研究了水杨酸、水杨酸钠和酮洛芬在Eudragit L和S有机凝胶中的体外溶出特性。水杨酸的溶出模式以及Eudragit L聚合物从有机凝胶中的侵蚀遵循明显的零级动力学,这为表面侵蚀机制以及水杨酸可忽略不计的扩散释放提供了有力证据。另一方面,水杨酸从Eudragit S有机凝胶中的溶出是时间平方根的线性函数。水杨酸从Eudragit S有机凝胶中的表观溶出速率随温度从32℃升高到42℃以及搅拌速率从50 rpm增加到200 rpm而增加。表观溶出速率常数的对数与绝对温度的倒数之间呈线性关系。水杨酸从Eudragit S有机凝胶中释放的活化能在2.99至5.57 kcal/mol范围内。从各种实验结果得出结论,水杨酸从Eudragit S有机凝胶中的释放过程是通过有机凝胶基质的扩散控制过程。

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