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健康年轻巴西受试者口服环丙沙星的药代动力学

Pharmacokinetics of oral ciprofloxacin in healthy, young Brazilian subjects.

作者信息

Sudo R T, Melo P A, Suarez-Kurtz G

机构信息

Departamento de Farmacologia Básica e Clínica, Universidade Federal do Rio de Janeiro, Brasil.

出版信息

Braz J Med Biol Res. 1990;23(12):1315-21.

PMID:2136565
Abstract
  1. The pharmacokinetics of ciprofloxacin were determined in 8 healthy young volunteers (5 men and 3 women) after administration of single oral doses of 250 mg. 2. The peak plasma concentration of ciprofloxacin (Cmax = 1.26 +/- 0.21 mg/l), the time to reach Cmax (Tmax = 1.99 +/- 0.26 h), the area under the time-plasma concentration curve (AUC = 5.52 +/- 0.84 mg h l-1), the terminal phase half-life (T1/2 = 3.05 +/- 0.56 h), the volume of distribution (Vd/F = 195.4 +/- 14.0 l) and total body clearance (CL/F = 46.3 +/- 2.6 l/h), both expressed as functions of the oral bioavailability (F) of ciprofloxacin were within the corresponding values reported in the literature for other healthy population groups. 3. Multiple dose administration (250 mg, po, twice daily for 4 days) did not result in accumulation of ciprofloxacin in plasma. No adverse side effects occurred during the study. 4. The pharmacokinetic data are discussed in relation to the minimum inhibitory concentration (MIC) of ciprofloxacin for a number of common pathogens isolated from human infections in Rio de Janeiro.
摘要
  1. 在8名健康年轻志愿者(5名男性和3名女性)口服250毫克单剂量环丙沙星后,测定了其药代动力学。2. 环丙沙星的血浆峰浓度(Cmax = 1.26 +/- 0.21毫克/升)、达到Cmax的时间(Tmax = 1.99 +/- 0.26小时)、血浆浓度-时间曲线下面积(AUC = 5.52 +/- 0.84毫克·小时·升-1)、终末相半衰期(T1/2 = 3.05 +/- 0.56小时)、分布容积(Vd/F = 195.4 +/- 14.0升)和全身清除率(CL/F = 46.3 +/- 2.6升/小时),均表示为环丙沙星口服生物利用度(F)的函数,这些数值在文献报道的其他健康人群组的相应值范围内。3. 多次给药(250毫克,口服,每日两次,共4天)未导致环丙沙星在血浆中蓄积。研究期间未出现不良副作用。4. 结合从里约热内卢人类感染中分离出的多种常见病原体的环丙沙星最低抑菌浓度(MIC)对药代动力学数据进行了讨论。

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