甲磺酸帕珠沙星在健康受试者体内药动学研究

Pharmacokinetics of pazufloxacin mesilate in healthy volunteers

目的研究甲磺酸帕珠沙星在国人体内的药动学。方法10名健康受试者单次静脉滴注300,600mg后用HPLC测定体内帕珠沙星的血药浓度。采用3P97程序进行数据处理。结果两个剂量组的药动学参数ρmax分别为(10.799±1.773)和(22.729±4.686)mg·L-1,AUC0-t分别为(17.469±2.966)和(42.402±7.983)mg·h·L-1,t1/2β分别为(1.701±0.299)和(1.685±0.205)h,CLs分别为(17.806±3.261)和(14.678±2.947)L·h-1,Vc分别为(11.043±6.534)和(12.090±6.409)L。24 h尿药累积排泄率分别为(97.2±3.3)%和(96.6±4.3)%。结论两个剂量组在人体内的血药浓度变化符合二室模型,静脉滴注帕珠沙星后在体内迅速起效,且消除迅速。

ABSTRACT： OBJECTIVE To study the pharmaeokinetics of pazufloxaein mesilale in Chinese healthy volunteers. METHODS 300 or 600mg pazufloxaein mesilate was intravenously infused to 10 volunteers. The serum coneentration was determined by HPLC. The data were proeessed with 3P97 pharmaeokinetic program. RESULTS The pharmaeokinetic parameters of the two doses were a.s follows： ρmax were （ 10. 799±1.773） and （22.729 ± 4.686）mg· L^-1, AUC0～1 were （ 17.469± 2.966） and （42.402± 7.983）mg·h· L^-1, t1/2β were （ 1.701 ± 0.299） and （1.685±0.205）h, CLs were （17.806±3.261） and （14.678±2.947） L·h^-1,,were （11.043±6.534） and （12.090±6.409）L, the accumulate elimination rates of pazufloxacin in urine were ： （ 97.2 ± 3.3 ） % and （ 96.6 ± 4.3 ） % alter 24 h. CONCLUSION The coneentration-time curves of pazufloxaein at the dosage of 300,600 nag in volunteers can be diseribed with a two-compartment model. The distribution and elinfination are rapid.