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特布他林在哮喘儿童中的药代动力学。

Kinetics of terbutaline in asthmatic children.

作者信息

Hultquist C, Lindberg C, Nyberg L, Kjellman B, Wettrell G

出版信息

Eur J Respir Dis Suppl. 1984;134:195-203.

PMID:6586480
Abstract

Seven asthmatic children (8-12 years) were given terbutaline sulphate intravenously (5.5 micrograms/kg) and orally (50 micrograms/kg) one week apart. Unchanged terbutaline was measured in plasma and urine. In urine, conjugates were also assayed. The intravenous plasma concentration-time curve declined in a multiexponential manner. The terminal half-life ranged from 8.8 to 15.8 (mean 12.1) h. Body clearance (mean +/- SD) was 3.76 +/- 0.86, renal clearance 2.42 +/- 0.49 mL/min/kg. The volume of distribution at steady state was 1.57 +/- 0.19 L/kg. The extrapolated recovery of intact terbutaline in urine was 65.4 +/- 6.5% of the dose and the total recovery 80.8 +/- 8.4%. After oral administration, the recovery of intact terbutaline in urine was 6.2 +/- 1.1%. Absorption was on average 33%, but because of a mean first-pass elimination of 70%, bioavailability was 9.5 +/- 2.4%. It seems that children as a group have shorter terminal half-lives than adults and slightly higher weight-corrected clearances.

摘要

七名哮喘儿童(8至12岁)分别接受硫酸特布他林静脉注射(5.5微克/千克)和口服(50微克/千克),两次给药间隔一周。检测血浆和尿液中未变化的特布他林。同时也对尿液中的结合物进行了分析。静脉注射后的血浆浓度-时间曲线呈多指数下降。终末半衰期为8.8至15.8小时(平均12.1小时)。机体清除率(均值±标准差)为3.76±0.86,肾清除率为2.42±0.49毫升/分钟/千克。稳态分布容积为1.57±0.19升/千克。尿液中未变化特布他林的外推回收率为给药剂量的65.4±6.5%,总回收率为80.8±8.4%。口服给药后,尿液中未变化特布他林的回收率为6.2±1.1%。平均吸收率为33%,但由于平均首过消除率为70%,生物利用度为9.5±2.4%。儿童群体的终末半衰期似乎比成人短,且体重校正清除率略高。

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