摘要
目的研究多剂量静滴盐酸卡屈沙星葡萄糖注射液的药动学。方法选择10名中国健康成年志愿者，18-40岁，男女各半，静滴盐酸卡屈沙星葡萄糖注射液，每次400mg，每日1次，连续7d。用高效液相色谱法测定血及尿中药物浓度，利用血药浓度，以DAS软件拟合药动学参数；利用尿药浓度计算尿药累计排泄率。结果受试者静滴盐酸卡屈沙星葡萄糖注射液，体内过程符合二室模型。连续给药后，第1天与第7天的主要药动学参数分别是ρmax（7．33±1．67）和（7．91±1．85）mg·L^-1，AUC0-24（4124±8．11）和（44．07±10．72）mg·h·L^-1，AUC0-∞（43．04±8．39）和（44．39±10．85）mg·h·L^-1，t1/2β（5.3±1．34）和（4．95±0．98）h。经比较差异无统计学意义。平均稳态血药浓度ρav为（0．33±0．10）mg·L^-1，稳态血药浓度-时间曲线下面积AUCss为（39．23±12．63）mg·h·L^-1，波动度DF为（25．44±9．54）。单次及多次给药400mg后，0～24h内尿药累积排泄率分别为（68.90±5．31）％和（77．27±5．51）％，经t检验差异存在统计学意义。结论本品每天1次给药400mg，连续给药7d，在体内可达有效血浆浓度，体内未见蓄积。
OBJECTIVE To investigate the pharmacokinetics of caderofloxacin hydrochloride and glucose injections after intravenous multiple-dose in Chinese healthy volunteers. METHODS 10 Healthy volunteers （6 men and 6 women） were administrated 400 mg caderofloxacin hydrochloride and glucose injections once a day for 7 d by intravenous drip infusion. The plasma and urine concentrations were determined by HPLC method. The pharmacokinetic parameters were calculated by DAS software and the accumulate urinary excretion rates were acquired by urine concentrations. RESULTS The concentration-time curve was described by two compartment model. The main pharmacokinetic parameters of 1 st day and 7th day were as follows ,Omax ： （7.33±1.67） and （7.91±1.85） mg.L^-1, AUC0-24 （41.24±8.11） and （44.07±10.72） mg.h.L^-1, AUC0-∞ （43.04±8.39） and （44.39±10.85） mg.h.L^-1, t1/2β （5.3±1.34） and （4.95±0.98） h respectively . There were no remarkable differences of pharmacokinetic parameters between 1st day and 7th day. The parameters of ρav, AUCss and DF were （0.33±0.10） mg.L^-1, （39.23±12.63） mg.h.L^-1 and （25.44±9.54） respectively. The accumulate urinary excretion rates（0-24 h） of 1st day and 7th day were （68.90±5.31 ） % and （ 77.27±5.51 ） % respectively and there were statistic differences between them. CONCLUSION Effective concentrations in vivo could be achieved after intravenous infusion 400 mg eaderofloxacin hydroehloride and glucose injections once a day for 7 d and no accumulation in human body was observed after 7 d adminstrations.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2009年第3期217-221,共5页
Chinese Pharmaceutical Journal
