摘要
目的:评价中国健康男性受试者连续7 d静脉滴注头孢曲松钠/舒巴坦钠(4 1)的药代动力学特点。方法:12名受试者静脉滴注头孢曲松钠/舒巴坦钠(4 1)注射液2.50 g.d-1,连续7 d,采用高效液相色谱法测定给药后不同时间点头孢曲松和舒巴坦的血、尿浓度,计算主要药代动力学参数。结果:受试者静脉滴注头孢曲松钠/舒巴坦钠(4 1)注射液2.50 g.d-1连续7 d后耐受性良好,头孢曲松血药浓度约在d 4达到稳态,稳态后的平均峰浓度为202.60±26.31 mg.L-1,稳态血药浓度(Cav)为60.65±8.85 mg.L-1,AUCss为1455.68±212.41mg.h.L-1,经计算波动度为3.36%,波动百分数为96.77%;头孢曲松72 h后尿中的累积排泄百分率为43.61%±10.23%,舒巴坦12 h后尿中的累积排泄百分率为71.61%±10.06%。结论:连续应用头孢曲松钠/舒巴坦钠(4 1)7 d受试者耐受性良好,药代动力学参数结果显示,将头孢曲松钠和舒巴钠按4 1比例组成注射用复方制剂后,两种药物的药代动力学特征均未发生改变,两组分间无药物动力学的相互作用。
AIM： To evaluate the pharmacokinetics of multiple-dose Ceftriaxone/Sulbactam （4：1） injection in Chinese health volunteers. METHODS： The serum samples and urine samples of 12 healthy volunteers were collected after injecting 2.50 g Ceftriaxone/Sulbactam （4：1） injection for 7 days. RESULTS： All health volunteers were well tolerated. The pharmacokinetic parameters were calculated by DAS software. The average of Cmax was 202.60±26.31mg·L^-1, Cav was 60.65±8.85mg·L^-1, AUC, was 1455.68 ＋ 212.41mg·L^-1·h, DF was 3.36 %, FI was 96.77 %. The 72 h cumulative urinary excretion rate of Ceftriaxone was 43.61%± 10.23% and the 12 h cumulative urinary excretion rate of Sulbactam was 71.61%±10.06 %. CONCLUSION： 2.50 g multiple-dose Ceftriaxone/Sulbactam （4：1） injection is well tolerated in the health volunteers. According to the results of pharmacokinetic parameters, there is no pharmacokinetic change between the two drugs from the compound preparation, and there is no drug interaction between them.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2006年第4期458-463,共6页
Chinese Journal of Clinical Pharmacology and Therapeutics
