Tham R, Norlander B, Hägermark O, Fransson L
Arzneimittelforschung. 1978;28(6):1017-20.
A method for estimation of clemastine in human plasma has been developed. By chronic acid oxidation the drug is degradated to chlorobenzophenone, which can then be analysed by gas-liquid-chromatography using electron-capture detection. The plasma levels of clemastine after oral and i.v. administration have been studied. Using different methods for extraction of the drug from plasma a metabolic degradation of the pyrrolidine part of clemastine is demonstrated. The metabolite proposed may be biologically active. The plasma level of the drug was found to be directly related to its biologic effect, measured as inhibition of the histamine-induced flare in human skin.
已开发出一种测定人血浆中氯马斯汀的方法。通过长期酸氧化，该药物降解为氯苯甲酮，然后可使用电子捕获检测通过气液色谱法进行分析。已研究了口服和静脉注射给药后氯马斯汀的血浆水平。使用不同方法从血浆中提取药物，结果表明氯马斯汀的吡咯烷部分存在代谢降解。所提出的代谢物可能具有生物活性。发现该药物的血浆水平与其生物效应直接相关，生物效应以对人皮肤中组胺诱导的风团的抑制作用来衡量。
