Zhou H H, Chan Y P, Arnold K, Sun M
Antimicrob Agents Chemother. 1985 Feb;27(2):192-6. doi: 10.1128/AAC.27.2.192.
The pharmacokinetics of ceftriaxone were investigated in six healthy mainland Chinese adults (four males and two females). A single 1.0-g dose was administered intravenously or intramuscularly in a two-way crossover design. Plasma and saliva samples were collected on 11 occasions between 0 and 36 h after dosing. Ceftriaxone was not detected in any saliva samples. The mean volume of distribution and mean elimination half-life of ceftriaxone in plasma were 8.5 liters and 8.1 h, respectively. The mean total body clearance after intravenous administration was 0.68 liter/h. The mean Tmax and Cmax after intramuscular injection were 1.4 h and 131 micrograms/ml, respectively. The area under the plasma concentration-time curves after intravenous and intramuscular administrations were 1,507 and 1,493 micrograms X h/ml, respectively. The bioavailability for a 1.0-g intramuscular dose of ceftriaxone was calculated to be 100%. These pharmacokinetic parameters for ceftriaxone in healthy Chinese adults were very similar to those previously reported in the literature. Thus, ceftriaxone may be administered to treat Chinese patients without any major modification in the standard dosing regimen.
在6名健康的中国大陆成年人(4名男性和2名女性)中研究了头孢曲松的药代动力学。采用双向交叉设计静脉注射或肌肉注射1.0 g单次剂量。给药后0至36小时内11次采集血浆和唾液样本。在任何唾液样本中均未检测到头孢曲松。血浆中头孢曲松的平均分布容积和平均消除半衰期分别为8.5升和8.1小时。静脉给药后的平均全身清除率为0.68升/小时。肌肉注射后的平均达峰时间和峰浓度分别为1.4小时和131微克/毫升。静脉注射和肌肉注射后血浆浓度-时间曲线下面积分别为1507和1493微克·小时/毫升。计算得出1.0 g肌肉注射剂量的头孢曲松生物利用度为100%。健康中国成年人中头孢曲松的这些药代动力学参数与文献中先前报道的参数非常相似。因此,治疗中国患者时,头孢曲松在标准给药方案中无需进行任何重大调整即可使用。