中国临床药理学与治疗学2017，Vol.22Issue(9)：1022-1028,7.
罗西维林注射液在中国健康受试者体内的药代动力学
Pharmacokinetics of rociverine injection in Chinese healthy volunteers
摘要
Abstract
AIM:To study the pharmacokinetics of rociverine injection in Chinese healthy volunteers.METHODS:Twelve healthy volunteers were randomly assigned and administered with single or multiple doses of 10,20 and 40 mg rociverine injection by intravenous drip infusion.The concentrations of rociverine in human plasma and urine were determined by LC-MS/MS.The main pharmacokinetic parameters were calculated by DAS software.RESULTS:The main pharmacokinetic parameters of rociverine after single dose of 10,20 and 40 mg rociverine injection were as follows:Cmax were (309.83 ±138.81),(701.42 ±226.91) and (978.73 ± 108.53) ng/mL;V were (276.50 ± 128.52),(274.88 ±114.71) and (384.13 ±149.85) L;CL were (20.23 ± 10.73),(18.68 ± 4.20) and (20.13 ± 5.73) L/h;AUC0-t were (578.17 ± 280.59),(1 082.70 ± 245.93) and (2 058.48 ± 628.33) ng · mL-1 · h;accumulative urine excretion rate of 48 h (Ae) were (0.83 ± 1.35) ％,(0.48 ± 0.28) ％,(0.39 ± 0.37) ％,respectively.The main pharmacokinetic parameters of rociverine after multiple dose of 20 mg rociverine injection were as follows:C was (79.85 ± 9.09) ng/mL;AUCss was (1 188.38 ±201.79) ng · mL-1 · h;CLss was (7.97 ± 2.55) L/h;accumulation ratio was (4.18 ± 1.43) ％,respectively.CONCLUSION:The process of rociverine in the dosage range of 10-40 mg does not show any significant departure from linear dynamic feature.There is mild accumulation after multiple dosing.Rociverine is eliminated less than 1％ from urine in parent drug.关键词
罗西维林注射液/药代动力学/单次给药/多次给药Key words
rociverine injection/pharmacokinetic/single administration/multiple administration分类
医药卫生引用本文复制引用
刘胜利,黄晓晖,高署..罗西维林注射液在中国健康受试者体内的药代动力学[J].中国临床药理学与治疗学,2017,22(9):1022-1028,7.基金项目
国家自然科学基金(81173133) （81173133）
安徽省学术技术带头人科研资助项目(2015D068) （2015D068）
