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氨甲环酸常用于溶纤维蛋白过多引起的出血症。其在人体内的代谢率不到10％,口服2g时的生物利用度仅34％。为了改善其体内吸收,合成了氨甲环酸前药Cyklokapron[化学名为1-(乙氧基羰基)羟乙基氨甲环酸盐]以减低分子的两性和提高其亲脂性。本文报道本品在人体内的吸收。健康男性志愿受试者口服单剂本品1、2、3或3.5mmol,对照组口服单剂氨甲环酸9.6mmol,定期抽取血样和尿样,用电子俘获GC法测定氨甲环酸浓度。结果表明,本品3mmol(930mg)组和氨甲环酸9.6mmol
Tranexamic acid is commonly used for bleeding disorders caused by excessive fibrinolytic. Its metabolic rate in the human body is less than 10% and the bioavailability at oral 2g is only 34%. In order to improve its absorption in vivo, Cyklokapron (a chemical name of 1- (ethoxycarbonyl) hydroxyethyl tranexamic acid] was synthesized to reduce the amphiphilicity and lipophilicity of the molecule. This article reports the absorption of this product in the human body. Healthy male volunteers oral single-dose of this product 1, 2, 3 or 3.5mmol, the control group oral single-dose of tranexamic acid 9.6mmol, blood samples and urine samples were taken regularly by electron capture GC method for the determination of tranexamic acid concentration . The results show that the product 3mmol (930mg) group and tranexamic acid 9.6mmol