中华心血管病杂志
中華心血管病雜誌
중화심혈관병잡지
Chinese Journal of Cardiology
2012年
12期
1041-1044
,共4页
刘文芳%李静%马长生%林阳%杨克旭%所伟%吴伟%赵桂平
劉文芳%李靜%馬長生%林暘%楊剋旭%所偉%吳偉%趙桂平
류문방%리정%마장생%림양%양극욱%소위%오위%조계평
曲美他嗪%血药浓度%药代动力学
麯美他嗪%血藥濃度%藥代動力學
곡미타진%혈약농도%약대동역학
Trimetazidine%Plasma concentration%Pharmacokinetics
目的 研究国产盐酸曲美他嗪胶囊与进口盐酸曲美他嗪片在中国健康男性中单次空腹给药的药代动力学和生物等效性.方法 24名健康男性受试者随机交叉单次口服两种盐酸曲美他嗪制剂20 mg,给药前和给药后按时采集静脉血,以高效液相色谱串联质谱(HPLC-MS/MS)法测定血浆中曲美他嗪的浓度,用WinNonlin 6.2.1计算药动学参数并进行生物等效性评价.结果 盐酸曲美他嗪受试制剂和参比制剂的药动学参数分别为Cmax(70.9±15.3)、(66.4±13.8) μg/ml,tmax (1.70±0.72)、(1.85±0.55)h,t1/2z(4.70±1.75)、(4.77±1.96)h,AUC0-24h(481±176)、(469±171)μg·h-1.ml-1,AUC0-∞(511±189)、(500±188)μg·h.m1-1.受试制剂和参比制剂Cmax和AUC0-24h比值的90％可信区间分别为101.9％ ～ 112.5％和99.4％ ～ 104.9％.以AUC0-24h计算,受试制剂对参比制剂的相对生物利用度为(102.2±8.3)％.结论 国产盐酸曲美他嗪胶囊与进口盐酸曲美他嗪片生物等效.
目的 研究國產鹽痠麯美他嗪膠囊與進口鹽痠麯美他嗪片在中國健康男性中單次空腹給藥的藥代動力學和生物等效性.方法 24名健康男性受試者隨機交扠單次口服兩種鹽痠麯美他嗪製劑20 mg,給藥前和給藥後按時採集靜脈血,以高效液相色譜串聯質譜(HPLC-MS/MS)法測定血漿中麯美他嗪的濃度,用WinNonlin 6.2.1計算藥動學參數併進行生物等效性評價.結果 鹽痠麯美他嗪受試製劑和參比製劑的藥動學參數分彆為Cmax(70.9±15.3)、(66.4±13.8) μg/ml,tmax (1.70±0.72)、(1.85±0.55)h,t1/2z(4.70±1.75)、(4.77±1.96)h,AUC0-24h(481±176)、(469±171)μg·h-1.ml-1,AUC0-∞(511±189)、(500±188)μg·h.m1-1.受試製劑和參比製劑Cmax和AUC0-24h比值的90％可信區間分彆為101.9％ ～ 112.5％和99.4％ ～ 104.9％.以AUC0-24h計算,受試製劑對參比製劑的相對生物利用度為(102.2±8.3)％.結論 國產鹽痠麯美他嗪膠囊與進口鹽痠麯美他嗪片生物等效.
목적 연구국산염산곡미타진효낭여진구염산곡미타진편재중국건강남성중단차공복급약적약대동역학화생물등효성.방법 24명건강남성수시자수궤교차단차구복량충염산곡미타진제제20 mg,급약전화급약후안시채집정맥혈,이고효액상색보천련질보(HPLC-MS/MS)법측정혈장중곡미타진적농도,용WinNonlin 6.2.1계산약동학삼수병진행생물등효성평개.결과 염산곡미타진수시제제화삼비제제적약동학삼수분별위Cmax(70.9±15.3)、(66.4±13.8) μg/ml,tmax (1.70±0.72)、(1.85±0.55)h,t1/2z(4.70±1.75)、(4.77±1.96)h,AUC0-24h(481±176)、(469±171)μg·h-1.ml-1,AUC0-∞(511±189)、(500±188)μg·h.m1-1.수시제제화삼비제제Cmax화AUC0-24h비치적90％가신구간분별위101.9％ ～ 112.5％화99.4％ ～ 104.9％.이AUC0-24h계산,수시제제대삼비제제적상대생물이용도위(102.2±8.3)％.결론 국산염산곡미타진효낭여진구염산곡미타진편생물등효.
Objective To compare the pharmacokinetics and bioequivalence between domestic hydrochloric trimetazidine capsules and imported hydrochloric trimetazidine tablets in healthy male Chinese volunteers after single oral administration.Methods A single oral dose (test and reference formulations) was given to 24 healthy male Chinese subjects according to an open randomized crossover design.The blood samples were collected before and after administration.Plasma trimetazidine concentration was determined by HPLC-MS/MS.The pharmacokinetic parameters were calculated by WinNonlin Ver 6.2.1 software.Results The main pharmacokinetic parameters of domestic and imported formulation of trimetazidine were similar:Cmax(70.9 ± 15.3),(66.4 ± 13.8) μg/ml; tmax(1.70 ± 0.72),(1.85 ± 0.55) h; t1/2z(4.70 ±1.75),(4.77 ± 1.96)h; AUC0-24h(481 ± 176),(469 ± 171)μg· h·ml-1; AUC0-∞(511 ±189),(500 ± 188) μg · h · ml-1.The estimated 90％ CIs for the ratio of C and AUC0-24 h were also similar:101.9％-112.5％ and 99.4％-104.9％.The relative bioavailability of domestic formulation was (102.2 ± 8.3) ％.Conclusion The results demostrats that the domestic hydrochloric trimetazidine capsules and imported hydrochloric trimetazidine tablets are bioequivalent.
