大理学院学报：综合版
大理學院學報：綜閤版
대이학원학보：종합판
Journal of Dali University
2012年
6期
1-4
,共4页
氟哌塞吨%美利曲辛%LC-MS/MS法%药动学%生物等效性
氟哌塞噸%美利麯辛%LC-MS/MS法%藥動學%生物等效性
불고새둔%미리곡신%LC-MS/MS법%약동학%생물등효성
Flupentixol%melitracen%LC-MS/MS%pharmacokinetics%bioequivalence
目的：研究单剂量口服国产和进口氟哌噻吨美利曲辛片在健康受试者体内的药动学特征,评价其是否具有生物等效性。方法：采用随机、双交叉试验设计。22名健康男性受试者分别单次口服氟哌噻吨美利曲辛片10 mg（2片）后血浆中氟哌塞吨和美利曲辛的浓度采结果：国产和进口制剂中氟哌噻吨峰浓度Cmax分别为164.8±55.2和161.5±51.9 pg.mL-1;达峰时间Tmax用LC-MS/MS法检测,药动学参数用SigmaPLot 2001和Orign 6.0软件程序计算。分别为9.0±4.5和9.6±3.9 h,AUC0→t分别为5 622±2 243和5412±1 677 pg.h-1;美利曲辛Cmax分别为10.9±6.2和9.6±4.4 ng.mL-1;Tmax分别为4.7±0.9和4.4±1.1 h。AUC0→t分别为312±155和291±139 ng.h-1;国产及进口制剂的Cmax、AUC0→120 h、AUC0→∞等药动学参数经对数转换后的统计学处理（方差分析及双单侧t检验）,国产与进口制剂药物间差异均无统计学意义（P〉0.05）。国产制剂的相对生物利用度氟哌噻吨为103.2±19.9%,美利曲辛为107.1±14.5%（n=22）。结论：国产与进口氟哌噻吨美利曲辛片具有生物等效性。
目的：研究單劑量口服國產和進口氟哌噻噸美利麯辛片在健康受試者體內的藥動學特徵,評價其是否具有生物等效性。方法：採用隨機、雙交扠試驗設計。22名健康男性受試者分彆單次口服氟哌噻噸美利麯辛片10 mg（2片）後血漿中氟哌塞噸和美利麯辛的濃度採結果：國產和進口製劑中氟哌噻噸峰濃度Cmax分彆為164.8±55.2和161.5±51.9 pg.mL-1;達峰時間Tmax用LC-MS/MS法檢測,藥動學參數用SigmaPLot 2001和Orign 6.0軟件程序計算。分彆為9.0±4.5和9.6±3.9 h,AUC0→t分彆為5 622±2 243和5412±1 677 pg.h-1;美利麯辛Cmax分彆為10.9±6.2和9.6±4.4 ng.mL-1;Tmax分彆為4.7±0.9和4.4±1.1 h。AUC0→t分彆為312±155和291±139 ng.h-1;國產及進口製劑的Cmax、AUC0→120 h、AUC0→∞等藥動學參數經對數轉換後的統計學處理（方差分析及雙單側t檢驗）,國產與進口製劑藥物間差異均無統計學意義（P〉0.05）。國產製劑的相對生物利用度氟哌噻噸為103.2±19.9%,美利麯辛為107.1±14.5%（n=22）。結論：國產與進口氟哌噻噸美利麯辛片具有生物等效性。
목적：연구단제량구복국산화진구불고새둔미리곡신편재건강수시자체내적약동학특정,평개기시부구유생물등효성。방법：채용수궤、쌍교차시험설계。22명건강남성수시자분별단차구복불고새둔미리곡신편10 mg（2편）후혈장중불고새둔화미리곡신적농도채결과：국산화진구제제중불고새둔봉농도Cmax분별위164.8±55.2화161.5±51.9 pg.mL-1;체봉시간Tmax용LC-MS/MS법검측,약동학삼수용SigmaPLot 2001화Orign 6.0연건정서계산。분별위9.0±4.5화9.6±3.9 h,AUC0→t분별위5 622±2 243화5412±1 677 pg.h-1;미리곡신Cmax분별위10.9±6.2화9.6±4.4 ng.mL-1;Tmax분별위4.7±0.9화4.4±1.1 h。AUC0→t분별위312±155화291±139 ng.h-1;국산급진구제제적Cmax、AUC0→120 h、AUC0→∞등약동학삼수경대수전환후적통계학처리（방차분석급쌍단측t검험）,국산여진구제제약물간차이균무통계학의의（P〉0.05）。국산제제적상대생물이용도불고새둔위103.2±19.9%,미리곡신위107.1±14.5%（n=22）。결론：국산여진구불고새둔미리곡신편구유생물등효성。
Objective： To study the pharmacokinetics and bioequivalence of domestic and imported Flupentixol and Melitracen tablets in healthy subjects. Methods： Twenty-two healthy male subjects in a randomized crossover design were given a single oral dose of 10 mg domestic and imported Flupentixol and Melitraeen tablets. Plasma concentrations of the subjects were determined by liquid chromatography-tandem mass spectrometry （LC-MS/MS）. The pharmacokinetic parameters were calculated applied SigmaPLot 2001 and Origin 6.0 software. Results： The main pharmacokinetic parameters of domestic and imported Flupentixol and Melitracen were as follows. Flupentixoh Cmax were 164.8 ± 55.2 and 161.5 ±51.9 pg.mL-l; Tmax were 9.0 ± 4.5 and 9.6 ± 3.9 h; AUC0-t were 5 622 ± 2 243 and 5 412± 1 677 pg＇h-1, respectively. Melitracen： Cmax were 10.9 ± 6.2 and 9.6 ± 4.4 ng＇mL-l; were 4.7 ± 0.9 and 4.4 ± 1.1 h; AUCOwere 312± 155 and 291 ± 139 ng·h-1, respectively. The statistic analysis of two formulations was conducted by analysis of variance, two one-sided tests and confidence intervals, which demonstrated that there were no significant differences between domestic and imported formulations in main pharmacokinetic parameters （P 〉 0.05）. The mean relative bioavailability of domestic formulation of Flupentixol was 105.42 ±22.23%, and Melitracen was 107.29 ±20.40% （n=24）. Conclusion： The domestic Flupentixol and Melitracen are bioequivalent to the imported formulation.
