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呋塞米在健康男性中的处置与绝对生物利用度。

Disposition and absolute bioavailability of furosemide in healthy males.

作者信息

Waller E S, Hamilton S F, Massarella J W, Sharanevych M A, Smith R V, Yakatan G J, Doluisio J T

出版信息

J Pharm Sci. 1982 Oct;71(10):1105-8. doi: 10.1002/jps.2600711006.

Abstract

Furosemide (40 mg) was administered to 18 healthy adult males as an intravenous dose, an oral solution, and in tablet form. The pharmacokinetics of intravenous furosemide were studied, determining a total body clearance rate of 117.6 +/- 41.3 ml/min and a harmonic mean half-life of 78 min. The mean absolute bioavailability determined by ratio of areas under the plasma-time curves was 64 and 71% for the solution and tablet, respectively. The mean absolute bioavailability determined by the ratio of urinary cumulative excretion data was 61 and 66% for the solution and tablet, respectively. The absolute bioavailability of furosemide determined with plasma and urine data were not significantly different. Thus, urine data alone may be used to establish bioavailability of furosemide. Inspection of plasma-time curves revealed secondary maxima in several subjects, suggesting enterohepatic cycling.

摘要

将40毫克速尿以静脉注射剂量、口服溶液和片剂形式给予18名健康成年男性。研究了静脉注射速尿的药代动力学,确定总体清除率为117.6±41.3毫升/分钟,调和平均半衰期为78分钟。通过血浆-时间曲线下面积比确定的溶液和片剂的平均绝对生物利用度分别为64%和71%。通过尿累积排泄数据比确定的溶液和片剂的平均绝对生物利用度分别为61%和66%。用血浆和尿液数据确定的速尿绝对生物利用度没有显著差异。因此,仅尿液数据可用于确定速尿的生物利用度。血浆-时间曲线检查显示,部分受试者出现二次峰,提示存在肠肝循环。

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