Population pharmacokinetic and pharmacodynamic evaluation of Xuesaitong injection,a typical multiple constituent tradition Chinese medicine in patients with cerebral ischemia

作     者：LI Xiao-yu~(1,2) WANG Guang-ji~2 XIONG Yu-qing~3 SUN Jian-guo~2 HAO Hai-ping~2 ZOU Lang~4 ZHENG Yuan-ting~2 YAN Bei~2 XIA Chun-hua~(2,3) LIU Gao-lin~1 1 Department of Clinical Pharmacy,Affiliated First People Hospital of Shanghai Jiaotong University,Shanghai 200080,China 2 Key Laboratory of Drug Metabolism and Pharmacokinetics,China Pharmaceutical University,Nanjing 210009,Jiangsu,China 3 Institute of Clinical Pharmacology,Medical College of Nanchang University,Nanchang 330006,Jiangxi,China 4 Department of Clinical Medicine,Jiangxi College of TCM,Nanchang 330004,Jiangxi,China 

会议名称：《中国药理学会临床药理学专业委员会会议暨第十次全国临床药理学学术会议》

会议日期：2007年

学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

关 键 词：population pharmacokinetic(PPK) pharmacodynamic traditional Chinese medicine(TCM) dosage regimen optimization 

摘      要：AIM:Pharmacokinetic and pharmacodynamic profiles of Xuesaitong injection in cerebral ischemic patients are in- vestigated in order to optimize dosage regimen of muhiple constituent TCM in clinic. METHODS:63 patients were studied in our protocol. Enumeration and measurement data of all patients were collected during our *** samples were col- lected for two times at different time after intravenous infu- sion Xuesaitong injection at the dosage of 800 mg/kg for two *** of Xuesaitong injection in plas- ma,prothrombin time(PT),thrombin time(TT),activat- ed partial thromboplastin time(APTT)and fibrinogen(Fib) were *** and SAAM Ⅱ were employed for the simulation of PPK parameters and time-course fit- ting of Xuesaitong injection in cerebral ischemic patients. RESULTS:Population pharmacokinetic(PPK)parame- ters of Xuesaitong injection obtained as follow:CL:1.5 L·h(-1)·kg(-1),CL:13.0 L·h(-1)·kg(-1),k:0.1136/ h,k:0.9848 /h,k:0.2057 /***-individual variability were 36.3 %,17.8 %,1.0% and 60.3 %. Residual variability was 8.67%.Age,stature,gender of patients showed no correlation with the prolong ratio of PT (PT%),TT(TT%),APTT(APTT%)and inhibit ratio of Fib(Fib%)whereas dosage(weight),infusion ratio anti concentration of Xuesaitong injection in plasma were marked correlation to PT%,TT%,APTT% and Fib%. Correlation coefficient between dosage,infusion ratio, plasma concentration to PT%,TT%,APTT% and Fib% were 0.598,0.551,0.590,0.505;0.204,0.401, 0.348,0.403 and 0.560,0.436,0.593,O.351,re- spectively.P value was less than 0.01 or *** pharmacological effect obtained when Xuesaitong injection was administered as follow:Dosage was of 12.0-17.0 mg/kg,infusion ratio was of 10.0-18.0 mg/min and plasma concentration was of 25.0-35.0 μg/*** course of Xuesaitong injection in cerebral ischemic patients was successfully predicted and simulated results suggested that better effects were obtained at the dosage of 800- 1200 mg/d than 200-40