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在给予单一对映体后,氟比洛芬在健康受试者中的立体选择性分布。

Stereoselective disposition of flurbiprofen in healthy subjects following administration of the single enantiomers.

作者信息

Geisslinger G, Lötsch J, Menzel S, Kobal G, Brune K

机构信息

Department of Experimental and Clinical Pharmacology and Toxicology, University of Erlangen-Nürnberg, Germany.

出版信息

Br J Clin Pharmacol. 1994 Apr;37(4):392-4. doi: 10.1111/j.1365-2125.1994.tb04295.x.

Abstract

Plasma concentrations of the enantiomers of flurbiprofen were measured following oral administration of (S)-flurbiprofen 50 mg and (R)-flurbiprofen 50 mg and 100 mg to sixteen healthy subjects. Chiral inversion did not occur to a measurable extent. Significantly higher values of AUC (55.2 +/- 17.0 vs 44.6 +/- 11.2 micrograms ml-1h) elimination half-life (5.6 +/- 1.4 vs 4.0 +/- 1.0 h) and mean residence time (7.5 +/- 1.6 vs 5.7 +/- 1.2 h) were observed after 50 mg (S)-flurbiprofen as compared with 50 mg (R)-flurbiprofen. With the exception of Cmax and AUC values pharmacokinetic data for the 50 mg and the 100 mg dose of (R)-flurbiprofen did not differ significantly. The data are of clinical relevance if (R)-flurbiprofen also has analgesic activity in humans and is to be developed as an analgesic.

摘要

对16名健康受试者口服50毫克(S)-氟比洛芬、50毫克和100毫克(R)-氟比洛芬后,测定了血浆中氟比洛芬对映体的浓度。未观察到可测量程度的手性转化。与50毫克(R)-氟比洛芬相比,口服50毫克(S)-氟比洛芬后,AUC(55.2±17.0对44.6±11.2微克·毫升⁻¹·小时)、消除半衰期(5.6±1.4对4.0±1.0小时)和平均驻留时间(7.5±1.6对5.7±1.2小时)的值显著更高。除Cmax和AUC值外,50毫克和100毫克剂量的(R)-氟比洛芬的药代动力学数据无显著差异。如果(R)-氟比洛芬在人体中也具有镇痛活性并将被开发为镇痛药,这些数据具有临床相关性。

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