Pickup M E, Bird H A, Lowe J R, Lees L, Wright V
Br J Clin Pharmacol. 1981 Aug;12(2):111-5. doi: 10.1111/j.1365-2125.1981.tb01188.x.
1 Six healthy male volunteers received a total of 2500 mg of a new cephalosporin antibiotic Ro13-9904 by intramuscular injection in five divided doses at intervals of 12 h. 2 No significant systemic side-effects were observed and this was confirmed haematologically and biochemically. 3 The drug was distributed following intramuscular injection reaching a mean peak plasma concentration of 55 micrograms ml-1 (range 46-66) 1 to 2 h after the first injection. 4 Monoexponential elimination of drug was demonstrated. No significant difference was recorded in the plasma half-life after the initial dose (mean 6.7 h) and at steady state (mean 6.7 h). The half-life is long compared with other cephalosporin antibiotics. 5 On the basis of the observed half-life, steady state should be reached within 48 h. A mean peak plasma concentration of 74 micrograms ml-1 (range 65-87) was recorded at steady state. Steady state plasma concentrations of Ro13-9904 with a dose of 500 mg every 13 h may be predicted from the pharmacokinetics of a single dose.
六名健康男性志愿者分五次，每隔12小时肌肉注射新头孢菌素抗生素Ro13 - 9904，总量为2500毫克。
未观察到明显的全身副作用，血液学和生化检查证实了这一点。
肌肉注射后药物开始分布，首次注射后1至2小时达到平均血浆峰值浓度55微克/毫升（范围46 - 66）。
证明药物呈单指数消除。初始剂量后的血浆半衰期（平均6.7小时）与稳态时（平均6.7小时）无显著差异。与其他头孢菌素抗生素相比，半衰期较长。
根据观察到的半衰期，48小时内应达到稳态。稳态时记录的平均血浆峰值浓度为74微克/毫升（范围65 - 87）。每13小时500毫克剂量的Ro13 - 9904稳态血浆浓度可根据单剂量药代动力学预测。
