Scully B E, Fu K P, Neu H C
Am J Med. 1984 Oct 19;77(4C):112-6.
The pharmacokinetics of ceftriaxone were evaluated in eight adults after doses of 1 g administered by intravenous infusion and 1 and 0.5 g administered by intramuscular injection. Mean peak plasma concentrations were 168 micrograms/ml for 1 g given intravenously, 81 micrograms/ml for 1 g given intramuscularly, and 46 micrograms/ml for 0.5 g intramuscularly. Plasma concentrations were similar by both high pressure liquid chromatographic and microbiologic methods. The plasma half-lives were 7.6 and 8.3 hours, respectively, for the intravenous infusion and intramuscular injection. Plasma concentrations were equal for the 1 g intravenous and intramuscular routes by 2.5 hours. Plasma concentrations exceeded the minimal inhibitory concentrations (MICs) of most aerobic gram-positive and gram-negative organisms with the exception of Pseudomonas aeruginosa and Acinetobacter species for 24 hours. Urinary concentrations exceeded 100 micrograms/ml for 24 hours for the 1-g doses and for 12 hours for the 0.5-g dose. Urinary recovery of ceftriaxone within 24 hours was 40 percent for intravenous infusion and 33 and 34 percent for the intramuscular injection. A single 1-g dose daily will exceed the MICs of most staphylococcal and streptococcal species and Enterobacteriaceae for 12 to 24 hours.
对8名成年人进行了头孢曲松的药代动力学评估，静脉输注1g剂量以及肌内注射1g和0.5g剂量后，静脉注射1g的平均血浆峰浓度为168微克/毫升，肌内注射1g的为81微克/毫升，肌内注射0.5g的为46微克/毫升。通过高压液相色谱法和微生物学法测得的血浆浓度相似。静脉输注和肌内注射的血浆半衰期分别为7.6小时和8.3小时。静脉注射和肌内注射1g剂量时，2.5小时后血浆浓度相等。除铜绿假单胞菌和不动杆菌属外，血浆浓度超过大多数需氧革兰氏阳性和革兰氏阴性菌的最低抑菌浓度（MICs）达24小时。1g剂量时尿浓度超过100微克/毫升达24小时，0.5g剂量时达12小时。静脉输注24小时内头孢曲松的尿回收率为40%，肌内注射为33%和34%。每日单次1g剂量将超过大多数葡萄球菌、链球菌属和肠杆菌科细菌的MICs达12至24小时。
