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酮洛芬单次静脉推注或输注后的临床药代动力学。

Clinical pharmacokinetics of ketoprofen after single intravenous administration as a bolus or infusion.

作者信息

Debruyne D, Hurault de Ligny B, Ryckelynck J P, Albessard F, Moulin M

出版信息

Clin Pharmacokinet. 1987 Mar;12(3):214-21. doi: 10.2165/00003088-198712030-00003.

Abstract

The pharmacokinetics of ketoprofen were evaluated in 29 patients suffering from acute renal colic following a single intravenous administration as a bolus or short infusion (1.5 and 2 hours), and after a loading dose and a 24-hour infusion. Serum concentrations of ketoprofen were measured by high pressure liquid chromatography. The mean (+/- SD) values of clinical parameters were as follows: distribution half-life = 0.34 +/- 0.19 h; elimination half-life = 2.05 +/- 0.58 h; kel = 0.968 +/- 0.282 h-1; k21 = 0.943 +/- 0.425 h-1; k12 = 1.004 +/- 0.708 h-1; volume of central compartment = 5.58 +/- 1.67L; volume of tissue compartment = 5.14 +/- 2.12L; plasma clearance = 5.10 +/- 1.14L/h. These results concur with previously published data obtained after oral or intramuscular administration. According to clinical observations, administration of a ketoprofen bolus suppressed pain within 5 to 30 minutes; the administration of a loading dose and a 24-hour infusion is almost never followed by a recurrence of pain, and this regimen was proposed as the dosage schedule of ketoprofen to treat renal colic.

摘要

对29例急性肾绞痛患者单次静脉推注或短时间输注(1.5小时和2小时)酮洛芬后,以及给予负荷剂量和24小时输注后,评估了酮洛芬的药代动力学。采用高压液相色谱法测定血清中酮洛芬的浓度。临床参数的平均值(±标准差)如下:分布半衰期=0.34±0.19小时;消除半衰期=2.05±0.58小时;kel=0.968±0.282小时-1;k21=0.943±0.425小时-1;k12=1.004±0.708小时-1;中央室容积=5.58±1.67升;组织室容积=5.14±2.12升;血浆清除率=5.10±1.14升/小时。这些结果与先前发表的口服或肌肉注射给药后获得的数据一致。根据临床观察,静脉推注酮洛芬可在5至30分钟内缓解疼痛;给予负荷剂量和24小时输注后几乎不会出现疼痛复发,因此该方案被提议作为酮洛芬治疗肾绞痛的给药方案。

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