【摘要】 目的研究中国健康成年志愿者多次静滴甲磺酸帕珠沙星注射液的药动学。方法按GCP指导原则设计试验方案,选择10名18~40岁健康男性志愿者,多次静滴500 mg甲磺酸帕珠沙星注射液后,应用高效液相色谱法测定血药浓度,采用3P97软件进行数据处理,求出药动学参数。结果受试者分别给药后,药-时曲线符合二房室模型,首次与第7日给药后主要药动学参数分别为ρmax(13.07±5.27),(11.08±1.42)mg.L-1;tmax分别为(0.91±0.17),(1.0±0)h;t1/2β分别为(1.504±0.242),(1.551±0.235)h;Vd分别为(10.151±3.232),(11.155±2.272)L;CL分别为(22.863±3.703),(23.095±2.633)L.h-1。首次给药AUC0-∞为(23.141±3.824)mg.h.L-1,第7日给药AUC0-τ为(22.203±2.511)mg.h.L-1。受试者多剂静滴甲磺酸帕珠沙星注射液,平均稳态血药浓度ρav为(1.85±0.21)mg.L-1,稳态药-时曲线下面积AUCss为(22.698±2.625)mg.h.L-1,累积比为(1.090±0.357),波动系数(1.922±0.023)。结论静脉滴注甲磺酸帕珠沙星,每日2次,每次500 mg,在人体内可达到有效血浆浓度,且连续给药7 d体内未见蓄积。该方案适宜在临床推广应用。更多还原

【Abstract】 OBJECTIVE To investigate the pharmacokinetics of pazufloxacin mesilate after multiple doses in Chinese healthy volunteers.METHODS The protocol was designed according to GCP principle.10 Volunteers were given multiple doses of pazufloxacin mesilate and the plasma concentrations were determined by HPLC method.The pharmacokinetic parameters were calculated by 3P97 software.RESULTS The concentration-time curve was diseribed by two-compartment model.The main pharmacokinetic parameters of ρ_max in the 1st day and 7th day were（13.07±5.27） and（11.08±1.42）mg·L^-1,respectively,t_1/2β were（1.504±0.242） and（1.551±0.235）h,respectively,AUC_0-∞ in the 1st day is（23.141±3.824）mg·h·L^-1 and AUC_0～τ of the 7th day was（22.203±2.511）mg·h·L^-1;ρ_av was（1.85±0.21）mg·L^-1,AUCss was（22.698±2.625）mg·h·L^-1.The accumulation ratio is（1.090±0.357）,fluctuation coefficient was（1.922±0.023）.CONCLUSION Effective concentration in vivo is achieved after intravenous infusions of 500 mg pazufloxacin mesilate twice a day for 7 days and no accumulation in human body is observed after 7 day administration.The dosing schedule is recommended.更多还原