靛蓝、偶氮玉红和胭脂红作为马尼地平的光保护剂。

Indigotine, azorubine, and cochineal red as photoprotectors of manidipine.

机构信息

Department of Inorganic and Analytical Chemistry, Poznań University of Medical Sciences, Grunwaldzka, Poznań, Poland.

出版信息

Drug Dev Ind Pharm. 2010 Mar;36(3):302-6. doi: 10.1080/03639040903140597.

DOI:10.1080/03639040903140597

PMID:19663559

Abstract

BACKGROUND

The calcium antagonists from the group of 1,4-dihydropyridine (DHP) derivatives are photolabile, and the products of their photochemical decomposition have no pharmacological activity. Like the other DHP derivatives, after exposure to light, manidipine undergoes decomposition leading to a weakening of the pharmacological activity.

METHOD

The protective influence of selected dyes on manidipine has been tested. The photodegradation of manidipine was performed according to the first version of the ICH Guideline for photostability testing. The solutions were illuminated by a high-pressure lamp HBO-200, and the methods used for evaluation of manidipine photodegradation were HPLC, HPLC-MS, and UV-vis spectrophotometry. Quantitative evaluation of photodegradation was made on the basis of the quantum yields of the processes with the use of Reinecke salt as a chemical actinometer.

RESULTS

Results have shown that all the dyes studied, indigotine, azorubine, and cochineal red, slow down the process of manidipine photodegradation, and the most effective is azorubine. The role of the dyes has been determined on the basis of the Stern-Volmer dependence.

CONCLUSION

The dyes studied, indigotine, azorubine, and cochineal red, can be potential photoprotectors of manidipine as they quench the excited states of the compound.

摘要

背景

钙拮抗剂属于 1,4-二氢吡啶（DHP）衍生物类，对光不稳定，光化学反应分解产物无药理活性。与其他 DHP 衍生物一样，在光照条件下，马尼地平会发生分解，导致药理活性减弱。

方法

测试了几种染料对马尼地平的保护作用。根据 ICH 光稳定性测试指南的第一版进行了马尼地平的光降解实验。使用高压灯 HBO-200 对溶液进行照射，采用 HPLC、HPLC-MS 和紫外分光光度法等方法评估马尼地平的光降解情况。使用 Reinecke 盐作为化学光量计，基于过程的量子产率对光降解进行定量评估。