PHARMACOKINETICS OF ELTOPRAZINE IN HEALTHY MALE-SUBJECTS AFTER SINGLE DOSE ORAL AND INTRAVENOUS ADMINISTRATION

被引：6
|
作者：
RAGHOEBAR, M [1 ]
MAK, M [1 ]
COURNOT, A [1 ]
PISTORIUS, MCM [1 ]
VANHARTEN, J [1 ]
ROSEBOOM, H [1 ]
机构：
[1] THERAPHARM,RECH,F-92100 BOULOGNE BILLANCO,FRANCE
来源：
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY | 1990年 / 30卷 / 06期
关键词：
D O I：
10.1111/j.1365-2125.1990.tb05454.x
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The kinetics, safety and tolerability of eltoprazine hydrochloride were studied in an open, cross‐over, partially randomised design after single oral (8 mg) and intravenous (3 and 8 mg) doses to 12 healthy male subjects. After intravenous administration, the mean t1/2 ranged from 7 to 9 h, the MRT was 11 h, CL was 487 +/‐ 148 (3 mg dose) and 471 +/‐ 56 (8 mg dose) ml kg‐1 h‐1, while CLR was 226 +/‐ 124 (3 mg dose) and 189 +/‐ 38 (8 mg dose) ml kg‐1 h‐1. The Vss was 3.3 +/‐ 0.7 (3 mg dose) and 3.8 +/‐ 0.5 (8 mg dose) 1 kg‐1. Cumulative renal excretion was 40%. The AUC and the cumulative urinary excretion were directly proportional to dose within the range of 3‐8 mg. Values of tmax varied from 1 to 4 h after oral administration. The mean Cmax value was 24 ng ml‐1 after an oral dose of 8 mg. The plasma elimination half‐life after oral administration was 9.8 +/‐ 3.9 h. Absolute oral bioavailability was 110 +/‐ 32%. Dose‐dependent somnolence was observed. 1990 The British Pharmacological Society
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收藏
页码：879 / 883
页数：5
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