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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.

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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