Schäfer-Korting M, Korting H C, Maass L, Klesel N, Grigoleit H G, Mutschler E
Eur J Clin Pharmacol. 1986;30(3):295-8. doi: 10.1007/BF00541531.
Cefodizime pharmacokinetics was investigated, evaluating drug concentrations in serum, skin suction blister fluid (SBF), saliva and urine in six healthy male subjects who were administered a 1-g dose intravenously. Serum levels in five subjects can be described according to a two-compartment open model; terminal half-life is 181 +/- 14 min. Volume of distribution (Vd beta) amounts to 15.3 +/- 1.61, serum clearance to 59 +/- 6 ml/min, renal clearance to 33 +/- 3 ml/min. Of the administered dose, 54% is renally excreted unchanged within 27 h. Unbound drug fraction in serum is 19.0% and in SBF 38.4%. Thus renal clearance of free cefodizime amounts to 172 ml/min, Vdss to 68.9 l (free drug). Whereas cefodizime has not been detected in saliva samples, SBF concentration 3-9 h post administration parallel serum levels, amounting to 40% of the respective serum concentration. At 9 h, unbound cefodizime concentrations in SBF amount to 1.4 +/- 0.4 micrograms/ml, this value being well above the MIC90% values of many clinically relevant bacteria.
对头孢地嗪的药代动力学进行了研究,评估了6名健康男性受试者静脉注射1g剂量后血清、皮肤吸引水疱液(SBF)、唾液和尿液中的药物浓度。5名受试者的血清水平可根据二室开放模型进行描述;终末半衰期为181±14分钟。分布容积(Vdβ)为15.3±1.61,血清清除率为59±6ml/分钟,肾清除率为33±3ml/分钟。给药剂量的54%在27小时内以原形经肾脏排泄。血清中游离药物分数为19.0%,SBF中为38.4%。因此,游离头孢地嗪的肾清除率为172ml/分钟,稳态分布容积为68.9L(游离药物)。虽然在唾液样本中未检测到头孢地嗪,但给药后3-9小时SBF浓度与血清水平平行,相当于各自血清浓度的40%。在9小时时,SBF中游离头孢地嗪浓度为1.4±0.4μg/ml,该值远高于许多临床相关细菌的MIC90%值。