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氧氟沙星:禁食和非禁食状态下的血清及皮肤水疱液药代动力学

Ofloxacin: serum and skin blister fluid pharmacokinetics in the fasting and non-fasting state.

作者信息

Kalager T, Digranes A, Bergan T, Rolstad T

出版信息

J Antimicrob Chemother. 1986 Jun;17(6):795-800. doi: 10.1093/jac/17.6.795.

DOI:10.1093/jac/17.6.795
PMID:3460984
Abstract

Using an agar well diffusion assay, the concentrations of ofloxacin were measured in serum and skin blister fluid after an oral dose of 300 mg given with or without a standardized meal. The apparent lag time was longer when the drug was taken with food than in the fasting state and the serum peak concentrations occurred later; the rates of absorption being 1.72 +/- 1.12/h (S.D.) and 3.40 +/- 1.56/h respectively. The mean peak concentrations of each individual in serum and blister fluid were 3.8 +/- 1.6 mg/l and 1.7 +/- 0.5 mg/l, respectively, when the drug was taken with food, compared with 4.2 +/- 1.9 mg/l and 2.1 +/- 0.7 mg/l in the fasting state. The rate of penetration into blister fluid was not influenced by the intake of food. The elimination half-life was 9.0 +/- 6.2 h in serum and 13.5 +/- 7.8 h in blister fluid when the volunteers were fasting. The corresponding values in the non-fasting state were 6.3 +/- 5.5 h and 10.6 +/- 4.6 h. The ratio of the area under the concentration versus time curve (AUC0-infinity) for blister fluid and serum was 1.20 +/- 0.70 when ofloxacin was given without food and 1.03 +/- 0.34 when given with the meal.

摘要

采用琼脂孔扩散试验,测定了口服300mg氧氟沙星(无论是否搭配标准餐)后血清和皮肤水疱液中的药物浓度。与空腹状态相比,进食时服用该药物的表观滞后时间更长,血清峰浓度出现得更晚;吸收速率分别为1.72±1.12/h(标准差)和3.40±1.56/h。进食时服用该药物,血清和水疱液中各受试者的平均峰浓度分别为3.8±1.6mg/L和1.7±0.5mg/L,而空腹状态下分别为4.2±1.9mg/L和2.1±0.7mg/L。食物摄入对药物渗透入水疱液的速率没有影响。志愿者空腹时,血清中的消除半衰期为9.0±6.2小时,水疱液中为13.5±7.8小时。非空腹状态下的相应值分别为6.3±5.5小时和10.6±4.6小时。空腹服用氧氟沙星时,水疱液与血清的浓度-时间曲线下面积比(AUC0-∞)为1.20±0.70,进食时服用则为1.03±0.34。

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