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甲基叔丁醚(MTBE)是在临床试验中的一种胆石溶解剂。体内研究表明它对溶解许多胆囊结石和一些胆道结石有效。为分析其效力和毒性,本文用气相色谱内标法测定了MTBE及主要代谢物甲醇在大鼠的血清浓度,并研究了MTBE的药物动力学。大鼠igMTBE0.379mg/kg后的MTBE血清浓度的变化符合一室开放模型。其药物动力学参数如下:k_a为3.7 h~(-1),k为0.57 h~(-1),T_(1/2ka)为0.32 h,T_(1/2k)为1.26 h,T_(max)为0.9h,C_(max)为5.9μg/ml,AUC_(0-6h)为16.4μg·h·ml~(m-1)。甲醇血清浓度在igMTBE后显示有积蓄。甲醇/MTBE的浓度比率有显著增加。结果提示在应用MTBE时,尽可能避免其吸收,且须预防甲醇毒性。
Methyl tert-butyl ether (MTBE) is a gallstone dissolving agent in clinical trials. In vivo studies have shown that it is effective in dissolving many gallstone and some biliary stones. In order to analyze its potency and toxicity, the serum concentration of MTBE and its major metabolite methanol in rats was determined by gas chromatography internal standard method, and the pharmacokinetics of MTBE was studied. The change of MTBE serum concentration after igMTBE0.379mg / kg accorded with the open-chamber model. The pharmacokinetic parameters were as follows: k_a was 3.7 h -1, k was 0.57 h -1, T 1 / 2ka was 0.32 h, T 1 / 2k was 1.26 h, T max ) Was 0.9h, C max was 5.9μg / ml, AUC_ (0-6h) was 16.4μg · h · ml ~ (m-1). Methanol serum concentrations showed accumulation after igMTBE. The methanol / MTBE concentration ratio increased significantly. The results suggest that in the application of MTBE, as far as possible to avoid its absorption, and the need to prevent methanol toxicity.