摘要
目的评价国产奥氮平片在中国健康人体中的药动学及生物等效性。方法采用双周期交叉试验设计,20名健康男性受试者单次口服国产和进口奥氮平片5 mg,采用LC-MS/MS测定奥氮平血药浓度,计算两制剂的主要药动学参数和生物利用度,并进行生物等效性评价。结果国产和进口奥氮平片的主要药动学参数如下:tmax分别为(4.25±1.33)和(4.55±1.10)h,ρmax分别为(9.62±1.79)和(9.69±2.18)ng.mL-1,t1/2分别为(31.71±6.87)和(32.46±5.67)h,AUC0-t分别为(327.19±60.55)和(324.39±70.84)ng.h.mL-1,AUC0-∞分别为(354.44±74.58)和(350.70±80.94)ng.h.mL-1。受试制剂的相对生物利用度F0-t为(102.93±18.22)%,F0-∞为(103.30±20.75)%,经统计分析,各药动学参数均无显著性差异(P>0.05)。结论两种奥氮平制剂在体内过程相似,两制剂人体生物等效,临床上可以替换使用。
OBJECTIVE To study the pharmacokinetics and bioequivalence of domestic olanzapine tablets in healthy Chinese vol- unteers. METHODS A single oral dose of 5 mg olanzapine tablets was given to 20 healthy male volunteers in a randomized cross-o- ver study. The concentrations of olanzapine in plasma were determined by LC-MS/MS method. The pharmacokinetic parameters and relative bioavailability were calculated by DAS. Then the bioequivalence of two formulations was evaluated. RESULTS The pharma- eokinetic parameters of domestic and imported formulations were as follows ：tmax （4. 25 ± 1.33 ） and （4. 55 ± 1.10 ） h, Pmax （9.62 ± 1.79） and （9.69±2. 18） ng· mL^-1, t1/2 （31.71 ±6.87） and （32.46 ±5.67） h, AUC0-t（327.19±60.55） and （324.39± 70. 84） ng · h · mL^-1 , and AUC 0-∞, （354. 44 ±74. 58） and （350. 70 ± 80. 94） ng · h · mL^-1, respectively. The relative bioavail- ability was （ 102. 93 ± 18.22 ） % for F0-t, and （ 103.30 ± 20. 75 ） % for F0-∞. There was no significant difference between the two prepa- rations （ P 〉 0. 05 ）. CONCLUSION The two preparations are bioequivalent and can be prescribed interchangeably.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2012年第23期1934-1936,共3页
Chinese Pharmaceutical Journal
