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熊去氧胆酸乙氧基化产物类新型表面活性剂对选定非甾体治疗药物的胶束增溶作用

Micellar solubilization of selected non-steroidal therapeutic agents by new surface-active agents of the class of the products of oxyethylation of ursodeoxycholic acid.

作者信息

Zgoda Marian Mikołaj, Lukosek Marek, Nachajski Michał Jakub

机构信息

Drug Form Technology Unit, Department of Applied Pharmacy, Medical University in łódź.

出版信息

Polim Med. 2006;36(4):13-30.

Abstract

A new class of non-ionic surface-active agents were synthesized by means of oxyethylation of ursodeoxycholic acid (UDOCh acid) with the application of modified generation of catalysts in the form of a model prodrug. Basic viscosity values ([eta], Meta, Ro, Robs., Omga) as well as the analytic level of hyrohilic-lipophilic balance HLB in the notation of Griffin, Davies and 'HNMR method were determined. In the state of equilibrium the solubilizing properties of aqueous solutions of the products of oxyetyenation of UDOCh acid x nTE were estimated with respect to non-steroidal therapeutic agents such as diclofenac, ibuprofen, ketoprofen, and naproxen. The surface activity of solubilizers of UDOCh acid > or = nTE = 30 type and the thermodynamic stability deltaGm of an adduct emerging in the state of equilibrium were determined.

摘要

通过对熊去氧胆酸(UDOCh酸)进行氧乙基化反应,应用模型前药形式的改性催化剂,合成了一类新型非离子表面活性剂。测定了基本粘度值([η]、Meta、Ro、Robs.、Omga)以及采用格里芬、戴维斯表示法和'HNMR方法的亲水亲油平衡HLB的分析水平。在平衡状态下,针对双氯芬酸、布洛芬、酮洛芬和萘普生等非甾体治疗剂,评估了UDOCh酸x nTE氧乙基化产物水溶液的增溶性能。测定了UDOCh酸≥nTE = 30型增溶剂的表面活性以及平衡状态下形成的加合物的热力学稳定性ΔGm。

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