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The concentration of trans-4-aminomethylcyclohexanecarboxylic acid (tranexamic acid) in human serum was determined by peak matching operation. N-Heptafluorobutyryl amide derivative of tranexamic acid n-butyl ester was found to be the most suitable derivative for this purpose. The present operation enabled to confirm that peak due to tranexamic acid had no contaminants at all. Deuterium labeled tranexamic acid was used as an internal standard for quantiation of tranexamic acid in human serum. It was also found that proteins in human serum were precipitated completely with heptafluorobutyric acid which was readily removed by evaporation. On the oral administration of 250 mg of tranexamic acid, the serum level concentration reached maximum at 3-4 hour post-dose period.
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Miyazaki et al. (1975) studied this question.
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