Patel I H, Weinfeld R E, Konikoff J, Parsonnet M
Antimicrob Agents Chemother. 1982 Jun;21(6):957-62. doi: 10.1128/AAC.21.6.957.
The effects of 1% lidocaine as a diluent on the pharmacokinetics and tolerance of ceftriaxone administered intramuscularly were investigated in 12 adult volunteers. Each subject received two 0.5-g doses of ceftriaxone (one in water and the other in 1% lidocaine) at least 1 week apart in a randomized crossover fashion. Plasma and urine samples were collected serially and assayed for ceftriaxone content by high-performance liquid chromatography. The mean peak plasma concentration, time to attain the peak, area under the plasma curve from time zero to infinity, and elimination half-life were 45 micrograms/ml, 2.5 h, 578 micrograms . h/ml, and 7.1 h, respectively, after intramuscular administration of ceftriaxone in water diluent. The corresponding mean values in 1% lidocaine diluent were 42 micrograms/ml, 3 h, 577 micrograms . h/ml, and 7.0 h. The pharmacokinetic data suggested that 1% lidocaine does not alter either the elimination parameters or the bioavailability of intramuscularly administered ceftriaxone. The intensity and frequency of pain at the injection site were reduced considerably by the coadministered lidocaine.
在12名成年志愿者中研究了1%利多卡因作为稀释剂对肌内注射头孢曲松的药代动力学和耐受性的影响。每位受试者以随机交叉方式，至少间隔1周接受两剂0.5克头孢曲松（一剂用注射用水稀释，另一剂用1%利多卡因稀释）。连续采集血浆和尿液样本，并用高效液相色谱法测定头孢曲松含量。肌内注射用注射用水稀释的头孢曲松后，平均血浆峰浓度、达峰时间、从零至无穷大的血浆曲线下面积和消除半衰期分别为45微克/毫升、2.5小时、578微克·小时/毫升和7.1小时。在1%利多卡因稀释剂中的相应平均值分别为42微克/毫升、3小时、577微克·小时/毫升和7.0小时。药代动力学数据表明，1%利多卡因既不改变肌内注射头孢曲松的消除参数，也不改变其生物利用度。同时给予利多卡因可显著降低注射部位疼痛的强度和频率。
