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Dose proportionality of reboxetine enantiomers in healthy male volunteers

✍ Scribed by E. Rey; P. Dostert; Ph. d'Athis; M.G. Jannuzzo; I. Poggesi; G. Olive

Publisher: John Wiley and Sons
Year: 1999
Tongue: English
Weight: 125 KB
Volume: 20
Category: Article
ISSN: 0142-2782
DOI: 10.1002/(sici)1099-081x(199905)20:4<177::aid-bdd172>3.0.co;2-i

No coin nor oath required. For personal study only.

✦ Synopsis

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 9 13.5, 76.6 9 26.3, 99.8 924.1 ng/mL and AUC : 605.8 9 233.2, 1288.3 9796.4, 1780.7 9 669.3 ng•h/mL for 1.5, 3, 4.5 mg, respectively) than for FCE 21684 (C max : 15.2 95.3, 34.69 14.0, 43.19 12.3 ng/mL and AUC : 247.09103.9, 529.19 278.4, 773.09 355.3 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.

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