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新型组胺H2受体拮抗剂奥美替丁单次口服和静脉给药后的药代动力学

Pharmacokinetics of oxmetidine, a new histamine H2-receptor antagonist, after single oral and intravenous doses.

作者信息

Jönsson K A, Bodemar G, Gotthard R, Norlander B, Walan A

出版信息

Eur J Clin Pharmacol. 1983;24(3):353-6. doi: 10.1007/BF00610054.

Abstract

The plasma concentration curves and urinary excretion of oxmetidine after administration of single i.v. (100 mg) and oral (200 mg) doses have been studied in 11 patients with peptic ulcer disease. The mean bioavailability of the drug was 70% (range 53-91%). After intravenous administration, the mean plasma t 1/2 beta was 3.0 h, the mean apparent volume of distribution 0.7 l/kg, the mean total plasma clearance 12.3 l/h and the mean plasma renal clearance was 0.7 l/h. Following intravenous and oral administration an average of 6% and 3%, respectively, of unchanged drug was found in the urine. The plasma concentration curve after oral administration in most patients exhibited two maxima, with peak concentrations appearing between 45 and 210 min after dosing.

摘要

在11例消化性溃疡病患者中研究了单次静脉注射(100mg)和口服(200mg)剂量奥美替丁后的血药浓度曲线和尿排泄情况。该药的平均生物利用度为70%(范围53 - 91%)。静脉给药后,平均血浆β半衰期为3.0小时,平均表观分布容积为0.7升/千克,平均总血浆清除率为12.3升/小时,平均血浆肾清除率为0.7升/小时。静脉注射和口服给药后,尿中分别平均发现6%和3%的原形药物。大多数患者口服给药后的血药浓度曲线呈现两个峰值,给药后45至210分钟出现峰浓度。

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