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呋塞米静脉注射和口服给药后在人体内的药代动力学。矩量法的应用。

Pharmacokinetics of furosemide in man after intravenous and oral administration. Application of moment analysis.

作者信息

Hammarlund M M, Paalzow L K, Odlind B

出版信息

Eur J Clin Pharmacol. 1984;26(2):197-207. doi: 10.1007/BF00630286.

Abstract

Furosemide 40 mg was administered to 8 healthy subjects as an i.v. bolus dose, as 1 tablet in the fasting state, and as 1 tablet and a solution after food intake. The i.v. data gave a total body clearance of 162 +/- 10.8 ml/min and a renal clearance of 117 +/- 11.3 ml/min; the volume of distribution at steady state was 8.3 +/- 0.61. Oral administration gave a bio-availability of the tablet (fasting) of 51%. Food intake slightly reduced the bioavailability, but not to a significant extent. There was no significant difference in availability between the tablet and the solution. Moment analysis gave a mean residence time after the i.v. dose, MRTi .v., of 51 +/- 1.5 min. The mean absorption times (MAT) for all oral doses were significantly longer than the MRTi .v., indicating absorption rate-limited kinetics of furosemide. On average, food delayed the absorption by 60 min. The MAT for the tablet in the postprandial state was significantly longer than for the solution, indicating dissolution rate-limited absorption of the tablet.

摘要

将40毫克呋塞米以静脉推注剂量给予8名健康受试者,在禁食状态下给予1片,进食后给予1片及一种溶液。静脉注射数据得出总体清除率为162±10.8毫升/分钟,肾清除率为117±11.3毫升/分钟;稳态分布容积为8.3±0.61。口服给药时,片剂(禁食)的生物利用度为51%。进食略微降低了生物利用度,但降幅不显著。片剂与溶液之间的生物利用度无显著差异。矩量法得出静脉注射剂量后的平均驻留时间MRTiv为51±1.5分钟。所有口服剂量的平均吸收时间(MAT)均显著长于MRTiv,表明呋塞米的吸收速率受限动力学。平均而言,食物使吸收延迟60分钟。餐后状态下片剂的MAT显著长于溶液的MAT,表明片剂的溶出速率受限吸收。

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