北方药学
北方藥學
북방약학
JOURNAL OF NORTH PHARMACY
2013年
7期
4-5
,共2页
许文东%杨玉琼%杜松%黄翔
許文東%楊玉瓊%杜鬆%黃翔
허문동%양옥경%두송%황상
曲美他嗪%药代动力学%生物等效性%生物利用度%LC-MS
麯美他嗪%藥代動力學%生物等效性%生物利用度%LC-MS
곡미타진%약대동역학%생물등효성%생물이용도%LC-MS
Trimetazidine%Pharmacokinetics%Bioequivalence Bioavailability%LC-MS
目的：研究盐酸曲美他嗪片的人体生物利用度和生物等效性。方法：22名男性健康受试者，随机双交叉口服剂量为20mg的受试制剂和参比制剂，采用LC-MS法测定血浆中盐酸曲美他嗪的浓度，使用DAS2.1.1软件对各药代动力学参数进行计算，同时对其生物等效性进行统计分析。结果：22名健康受试者服用20mg盐酸曲美他嗪片受试制剂和参比制剂的Cmax分别为（42.64±17.00）ng/ml和（41.32±19.66）ng/ml，Tmax分别为（2.2±1.5）h和（2.7±1.7）h，AUC0-t分别为（418.1±177.4）ng·h/ml和（397.8±147.1） ng·h/ml，AUC0-∞分别为（428.5±181.1）ng·h/ml和（407.9±150.5）ng·h/ml，t1/2分别为（5.9±1.6）h和（5.6±1.3）h。受试制剂中曲美他嗪Cmax的90%置信区间为参比制剂的100.1%～111.1%，AUC0-t的90%置信区间为参比制剂的97.0%～111.9%，AUC0-∞的90%置信区间为参比制剂的96.9%～111.9%。以AUC0-t计算，受试制剂中曲美他嗪的相对生物利用度为（105.9±18.6）%。结论：两制剂具有生物等效性。
目的：研究鹽痠麯美他嗪片的人體生物利用度和生物等效性。方法：22名男性健康受試者，隨機雙交扠口服劑量為20mg的受試製劑和參比製劑，採用LC-MS法測定血漿中鹽痠麯美他嗪的濃度，使用DAS2.1.1軟件對各藥代動力學參數進行計算，同時對其生物等效性進行統計分析。結果：22名健康受試者服用20mg鹽痠麯美他嗪片受試製劑和參比製劑的Cmax分彆為（42.64±17.00）ng/ml和（41.32±19.66）ng/ml，Tmax分彆為（2.2±1.5）h和（2.7±1.7）h，AUC0-t分彆為（418.1±177.4）ng·h/ml和（397.8±147.1） ng·h/ml，AUC0-∞分彆為（428.5±181.1）ng·h/ml和（407.9±150.5）ng·h/ml，t1/2分彆為（5.9±1.6）h和（5.6±1.3）h。受試製劑中麯美他嗪Cmax的90%置信區間為參比製劑的100.1%～111.1%，AUC0-t的90%置信區間為參比製劑的97.0%～111.9%，AUC0-∞的90%置信區間為參比製劑的96.9%～111.9%。以AUC0-t計算，受試製劑中麯美他嗪的相對生物利用度為（105.9±18.6）%。結論：兩製劑具有生物等效性。
목적：연구염산곡미타진편적인체생물이용도화생물등효성。방법：22명남성건강수시자，수궤쌍교차구복제량위20mg적수시제제화삼비제제，채용LC-MS법측정혈장중염산곡미타진적농도，사용DAS2.1.1연건대각약대동역학삼수진행계산，동시대기생물등효성진행통계분석。결과：22명건강수시자복용20mg염산곡미타진편수시제제화삼비제제적Cmax분별위（42.64±17.00）ng/ml화（41.32±19.66）ng/ml，Tmax분별위（2.2±1.5）h화（2.7±1.7）h，AUC0-t분별위（418.1±177.4）ng·h/ml화（397.8±147.1） ng·h/ml，AUC0-∞분별위（428.5±181.1）ng·h/ml화（407.9±150.5）ng·h/ml，t1/2분별위（5.9±1.6）h화（5.6±1.3）h。수시제제중곡미타진Cmax적90%치신구간위삼비제제적100.1%～111.1%，AUC0-t적90%치신구간위삼비제제적97.0%～111.9%，AUC0-∞적90%치신구간위삼비제제적96.9%～111.9%。이AUC0-t계산，수시제제중곡미타진적상대생물이용도위（105.9±18.6）%。결론：량제제구유생물등효성。
Objective:To study the relative bioavailability and bioequivalence of domestic trimetazidine hydrochloride tablets in healthy subjects. Methods:In a randomized two-period reference and test crossover study,22 healthy male volunteers were given a single oral dose of 20 mg trimetazidine hydrochloride. The concentration of trimetazidine hydrochloride in plasma were determined by LC-MS. The pharmacokinetic parameters were processed by DAS propram for statistic analysis.Results:The pharmacokinetic parameters of the test and reference tablets were as follows:Cmax were(42.64±17.00)ng/ml and(41.32±19.66)ng/ml;Tmax were(2.2±1.5)h and(2.7 ±1.7)h;AUC0-t were(418.1±177.4)ng·h/ml and(397.8±147.1)ng·h/ml; AUC0-∞were(428.5±181.1)ng·h/ml and(407.9±150.5)ng·h/ml;t1/2 were (5.9±1.6)h and (5.6±1.3)h,respectively. The 90% confidential interval of Cmax,AUC0-t and AUC0-∞of tested formulation were 100.1%~111.1%,97.0%~111.9% and 96.9%~111.9%,respectively. The relative bioavailability of the test preparations was (105.9± 18.6)%.Conclusion:The domestic trimetazidine tablets are bioequivalent to the imported trimetazidine hydrochloride tablets.
