摘要
目的研究比较静脉滴注哌拉西林/舒巴坦(4∶1)复方制剂在健康志愿者中的药动学。方法10名健康志愿者分别随机交叉静脉滴注哌拉西林/舒巴坦(2000m g/500m g)复方制剂、哌拉西林(2000m g)、舒巴坦(500m g),用反相高效液相法分别测定血清和尿样中哌拉西林和舒巴坦的药物浓度。结果哌拉西林和舒巴坦在体内的血药浓度-时间曲线可以用二室模型进行最佳拟合。所得到的药动学参数为:对单独的哌拉西林和哌拉西林/舒巴坦中哌拉西林cm ax分别为(124.40±20.19)和(138.70±25.53)m g/L;消除半衰期t1/2分别为(0.80±0.16)h和(0.88±0.39)h;药-时曲线下面积AUC0-∞分别为(129.23±32.91)和(155.81±58.52)m g.h/L;12h尿药回收率分别为(55.4±22.0)%和(43.6±12.3)%。舒巴坦和哌拉西林/舒巴坦中舒巴坦的峰浓度cm ax分别为(27.50±3.22)和(35.10±4.68)m g/L,药-时曲线下面积AUC0-∞分别为(29.25±4.99)和(44.37±6.48)m g.h/L;消除半衰期t1/2分别为(1.03±0.24)h和(1.02±0.15)h;12h尿药回收率分别为(51.8±25.6)%和(41.5±19.4)%。结论受试者对三种制剂在30m in静脉滴入均耐受性良好,舒巴坦对哌拉西林的体内处置影响不明显,但哌拉西林对舒巴坦的体内处置有明显影响。复方制剂中哌拉西林和舒巴坦的尿排泄率均小于单独给药时的排泄率,提示哌拉西林和舒巴坦可能竞争结合同样的尿路消除位点。
Objective To study the pharmacokinetics of a single dose of piperacillin/sulbactam （4 ： 1） injection in healthy volunteers. Methads Ten healthy volunteers were selected to receive a single dose of piperacillin/sulbactam （2000mg/500mg） injection or piperacillin （2000mg） alone or sulbactam （500mg） alone in an open randomized cross-over study. The concentrations of piperacillin and sulbactam in serum and urine were determined respectively by two different highrperformance liquid chromatography （HPLC） methods. Results The concentration-time curves of piperacillin and sulbactam were best fitted by an open two-compartment model. The pharmacokinetic parameters were as follows ： cmax of piperacillin alone and in compound at the end of infusion were （124.40±20. 19） mg/L and （138.70±25.53） mg/l. respectively, AUC0-∞ were （129. 23 ±32.91） mg - h/L and （155.81±58.52） mg · h/L respectively, t1/2 were （0.80±0. 16）h and （0. 88±0.39）h respectively. The cmax of sulbaetam alone and in compound preparation at the end of infusion were （29.25± 4.99 ） mg/L and （44.37± 6.48） mg/L respectively, AUC0-∞ were （27.98 ± 4.83） mg · h/L and （42. 63±5.65） mg · h/L respectively, t1/2 were （1.03± 0.24）h and （1.02± 0. 15）h respectively. Urinary recovery rates of piperacillin alone and in compound between 0 to 12h were （55. 4± 22. 0）% and （43. 6± 12.3）% respectively. Urinary recovery rates of sulbactam alone and in compound preparation between 0 to 12 h were （51.8± 25.6）% and （41.5± 19.4）% respectively. Conclusions All volunteers were well tolerated with the three preparations by iv infusion in 30 rain. Sulbactam had no interaction on the disposition of piperacillin, but piperacillin had significant influence on the disposition of sulbactam. The urinary recovery rates of piperacillin and sulbactam were significantly lower in compound preparation than in single one, which means piperacillin and sulbactam may compete the same urinary elimination sites.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2007年第2期95-99,共5页
Chinese Journal of Antibiotics
