吸收、分配和排泄
克立马丁（2-(2-(1-(4-氯苯基)-1-苯乙氧基乙基))-1-甲基吡咯烷）的代谢在三个成年男性志愿者单次口服20毫克琥珀酸盐剂量后进行了研究。经过酶促水解，尿液的溶剂提取物用N-甲基-N-三甲基硅基三氟乙酰胺-碘化铵进行衍生化，并通过气相色谱-质谱分析。代谢产物的结构是基于电子冲击和化学电离质谱确定的，一些代谢产物的身份（例如甲醇、4-氯二苯甲酮和4-氯苯基苯乙烯）通过使用真实标准得到确认。克立马丁在人體内的主要代谢途径包括直接氧化、O-脱烷基化（醚键断裂）、芳香族羟基化、脂肪族氧化、醇脱水，然后是酶促水解。在尿液中排出的总代谢物中，35%是甲醇（代谢物M3，主要代谢物），15%是M1，17%是M2，11%是M4，9%是M5，8%是M6，5%是M7。
The metabolism of clemastine, 2-(2-(1-(4-chlorophenyl)-1-phenylethoxylethyl])-1-methylpyrrolidine, has been studied in three adult male volunteers after a single oral dose of 20 mg as the fumarate. After enzymatic hydrolysis solvent extracts of urine were derivatized with N-methyl-N-trimethylsilyltrifluoroacetamide-ammonium iodide and analysed by gas chromatography-mass spectrometry. The structures of metabolites were determined on the basis of electron impact and chemical ionization mass spectra and the identities of some (e.g. carbinol, 4-chlorobenzophenone and 4-chlorophenylstyrene) were confirmed by use of authentic standards. The principal route of metabolism of clemastine in man involves direct oxidation, O-dealkylation (fission of the ether bond), aromatic hydroxylation, aliphatic oxidation, alcoholic dehydration, and then enzymatic hydrolysis. Of the total amount of metabolites excreted in the urine 35% was carbinol (metabolite M3, major metabolite), 15% was M1, 17% was M2, 11% was M4, 9% was M5, 8% was M6 and 5% was M7.
来源:Hazardous Substances Data Bank (HSDB)
