Carlsson S M, Denneberg T, Emanuelsson B M, Kågedal B, Lindgren S
Department of Nephrology, University Hospital, Linköping, Sweden.
Eur J Clin Pharmacol. 1990;38(5):499-503. doi: 10.1007/BF02336691.
The pharmacokinetics of 2-mercaptopropionylglycine (2-MPG) was studied in ten healthy volunteers after a single i.v. injection of 250 mg (1532 mumol). The total and non-protein-bound concentrations versus time curves were best described by a three-exponential function with terminal half-lives of 55 and 59 h respectively. Body clearance based upon the total concentration was estimated to be 105 and 231 ml/min based on the non-protein-bound 2-MPG. The corresponding values for Vss were 99 l and Vss,n 173 l, and for V gamma 485 l and V gamma,n 1121 l respectively. 75% of the dose was excreted in the urine, mainly during the first 6 h after injection. The proportion of non-protein-bound 2-MPG diminished exponentially during the first 15 h and then levelled off at about 30%. There was a nonlinear increase in the non-protein-bound fraction of 2-MPG as the total plasma concentration of the drug increased.
在10名健康志愿者单次静脉注射250mg（1532μmol）2-巯基丙酰甘氨酸（2-MPG）后，对其药代动力学进行了研究。总浓度和非蛋白结合浓度随时间的曲线最适合用三指数函数描述，终末半衰期分别为55小时和59小时。基于总浓度的机体清除率，以非蛋白结合的2-MPG计算，估计为105和231ml/min。相应的稳态分布容积（Vss）值分别为99L和Vss,n 173L，Vγ值分别为485L和Vγ,n 1121L。75%的剂量经尿液排泄，主要在注射后的最初6小时内。非蛋白结合的2-MPG比例在最初15小时内呈指数下降，然后在约30%的水平趋于平稳。随着药物血浆总浓度的增加，2-MPG的非蛋白结合分数呈非线性增加。
