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Dose proportionality of reboxetine enantiomers in healthy male volunteers.

作者信息

Rey E, Dostert P, d'Athis P, Jannuzzo M G, Poggesi I, Olive G

机构信息

Clinical Pharmacology, Hôpital Saint-Vincent de Paul, Paris, France.

出版信息

Biopharm Drug Dispos. 1999 May;20(4):177-81. doi: 10.1002/(sici)1099-081x(199905)20:4<177::aid-bdd172>3.0.co;2-i.

DOI:10.1002/(sici)1099-081x(199905)20:4<177::aid-bdd172>3.0.co;2-i
PMID:10440792
Abstract

Reboxetine is a racemic mixture of FCE 22071 and FCE 21684 enantiomers. The pharmacokinetics of the enantiomers of reboxetine were observed to be linear in male healthy subjects (n = 6) after the administration of 1.5, 3, 4.5 mg dose of reboxetine as solutions. Kinetic analysis was based on chiral HPLC assay of the enantiomers in plasma collected up to 72 h after each administration. C(max) and AUC were more than double for FCE 22071 (C(max): 38.3+/-13.5, 76. 6+/-26.3, 99.8+/-24.1 ng/mL and AUC(infinity): 605.8+/-233.2, 1288. 3+/-796.4, 1780.7+/-669.3 ng. h/mL for 1.5, 3, 4.5 mg, respectively) than for FCE 21684 (C(max): 15.2+/-5.3, 34.6+/-14.0, 43.1+/-12.3 ng/mL and AUC(infinity): 247.0+/-103.9, 529.1+/-278.4, 773.0+/-355.3 ng. h/mL), whatever the administered dose. The half-lives of the enantiomers were similar (FCE 22071: 13.1, 11.0, 12.6 h and FCE 21684: 12.8, 11.2, 12.2 h after 1.5, 3, 4.5 mg, respectively) and not substantially affected by the dose level.

摘要

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