Office of Research Support,Venus Medicine Research Centre, Hill Top Industrial Estate, Bhatoli Kalan, Baddi, HP, India.
J Toxicol Sci. 2010 Aug;35(4):459-64. doi: 10.2131/jts.35.459.
We have evaluated pharmacokinetics of a fixed dose combination (FDC) of ceftriaxone and sulbactam (2:1) or sulbactomax in eight healthy volunteers. A 1.5 g dose of sulbactomax, 1 g dose of ceftriaxone and 0.5 g sulbactam were given intravenously in a balanced two-ways cross-over study. Serially collected plasma sample was analyzed for ceftriaxone and sulbactam by high performance liquid chromatography (HPLC). The mean peaks of ceftriaxone and sulbactam concentrations in plasma were 152.06+/-6.65 microg/ml and 21.32+/-1.80 microg/ml, respectively and plasma half-lives for ceftriaxone and sulbactam were 5.2+/-0.35 hr and 0.94+/-0.038 hr, respectively. The AUC0-24 for ceftriaxone and sulbactam was 760.16+/-27.68 microg.hr/ml and 20.74+/-2.34 microg.hr/ml, respectively, with elimination rate constant of 0.133+/-0.009 hr(-1) and 0.732+/-0.029 hr(-1), respectively. The kinetics of ceftriaxone and sulbactum did not change in combination as compared to the alone treatment. Also, concentration of the ceftriaxone after 24 hr is higher than the minimum inhibitory concentration (MIC) of the most of the gram positive and gram negative bacteria indicating that one dose in a day is sufficient to treat the disease caused by these organisms.
我们评估了头孢曲松和舒巴坦（2：1）或舒巴坦钠固定剂量组合（FDC）在 8 名健康志愿者中的药代动力学。在一项平衡的两交叉研究中，静脉内给予 1.5g 舒巴坦钠、1g 头孢曲松和 0.5g 舒巴坦。通过高效液相色谱法（HPLC）对连续采集的血浆样本进行头孢曲松和舒巴坦分析。头孢曲松和舒巴坦在血浆中的平均峰浓度分别为 152.06+/-6.65μg/ml 和 21.32+/-1.80μg/ml，头孢曲松和舒巴坦的血浆半衰期分别为 5.2+/-0.35 小时和 0.94+/-0.038 小时。头孢曲松和舒巴坦的 AUC0-24 分别为 760.16+/-27.68μg.hr/ml 和 20.74+/-2.34μg.hr/ml，消除率常数分别为 0.133+/-0.009hr(-1) 和 0.732+/-0.029hr(-1)。与单独治疗相比，头孢曲松和舒巴坦的组合动力学没有变化。此外，24 小时后头孢曲松的浓度高于大多数革兰氏阳性和革兰氏阴性细菌的最低抑菌浓度（MIC），表明每天一剂足以治疗这些生物体引起的疾病。
