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Pharmacokinetics of the enantiomers of trans ‐tramadol and its active metabolite, trans ‐ O ‐demethyltramadol, in healthy male and female chinese volunteers
Author(s) -
Huichen Liu,
Yang Yu,
Na Wang,
Ming Deng,
Jianfang Liu,
Hongyuan Xue
Publication year - 2003
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/chir.10316
Subject(s) - pharmacokinetics , enantiomer , metabolite , chemistry , stereoselectivity , active metabolite , pharmacology , stereochemistry , chirality (physics) , medicine , biochemistry , nambu–jona lasinio model , chiral symmetry breaking , physics , quantum mechanics , quark , catalysis
By using a high‐performance capillary electrophoresis method, the pharmacokinetics of the enantiomers of trans ‐tramadol ( trans ‐T) and its active metabolite, trans ‐ O ‐demethyltramadol (M1), was studied in healthy male and female Chinese volunteers after oral administration of 100 mg trans ‐T hydrochloride. The values of C max for the enantiomers of trans ‐T and M1, and AUC 0 –∞ for (–)‐ trans T, (+)‐M1, and (–)‐M1 were higher in females than in males. The values of V d /F for the enantiomers of trans ‐T and CL r for (+)‐M1 were lower in females than in males. The value of t 1/2 for (–)‐M1 was longer in females than in males. There were significant differences in pharmacokinetic parameters of the two enantiomers of trans ‐T or M1 both in males and in females. The (+)/(–)‐enantiomeric ratios of t max , V d /F for trans ‐T in males were significantly different from those in females and the (+)/(–)‐enantiomeric ratios of pharmacokinetic parameters for M1 in males were similar to those in females. There are gender‐related differences in the pharmacokinetics of the enantiomers of trans ‐T and M1 which may be due to the greater body weights for men and/or the higher CYP2D6 activity in women. The pharmacokinetics of trans ‐T and M1 is stereoselective in men and women. There is a gender‐related difference in the stereoselectivity in pharmacokinetics of trans ‐T in human and the stereoselectivity in pharmacokinetics of M1 in men is similar to that in women. Chirality 16:112–118, 2004 . © 2004 Wiley‐Liss, Inc.