摘要
目的研究奥美拉唑肠溶胶囊在人体内药动学和生物等效性。方法健康志愿者20名，随机双交叉单剂量口服通化神源药业有限公司研制的奥关拉唑肠溶胶囊（试验制剂）和海口康元制药有限公司生产的奥关拉唑肠溶胶囊（参比制剂），剂量分别为40mg．剂间间隔为1周。分别于服药后12h内多点抽取静脉血，用高效液相色谱（HPLC）法测定血浆中奥关拉唑肠溶胶囊的浓度。用DAS（Drug And Statistics，version 2．0）药动学程序计算相对生物利用度并评价两种制剂生物等效性。AUC0-12，AUC（0-inf）和Cmax经方差分析和双单侧t检验，Tmax进行秩和检验。结果单剂量口服奥关拉唑肠溶胶囊试验和参比制剂后，血浆奥关拉唑的Cmax分别为（1146．77±386．58）ng·mL%-1和（1138．93±360、90）ng·mL^-1；Tmax分别为（2．40±0、53）h和（2．28±0．44）h；AUC（0-12）分别为（4853.61±1960．52）ng·h·mL^-1和（4743．06±1740、71）ng·h·mL^-1；AUC（0-inf）分别为（5111．76±2031．72）ng·h·mL^-1和（4942．71±1833.39）ng·h·mL^-1。AUC（0-12）的90％可信区间为94．6-106．3％，AUC（0-inf）的90％可信区间为96．5—107．2％，Cmax的90％可信区间为95.9—104．3％。结论试验制剂与参比制剂的人体相对生物利用度为（101．32±14．90）％，试验制剂与参比制剂具有生物学等效性。
OBJECTIVE To study the Pharmacokinetics and Bioequivalence of Omeprazole Enteric-coated Capsules in Chinese healthy volunteers. METHODS A single oral dose （40mg of tested and reference formulation） were given to 20 healthy volunteers in a randomised crossover study. The concentrations of Trimetazidine in plasma were determined by HPLC. The pharmacokinetics parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. RESULTS After a single dose,the pharmacokinetics parameters for Trimetazidine were as follows ： Cmax were （ 1 146.77 ± 386.58 ） ng · mL^-1 and （1 138.93±360.90）ng · mL^-1; Tmax were （2.40 ±0.53）h and （2.28 ±0.44）h; AUC（0-12）were （4 853.61 ± 1 960.52） ng · h · mL^-1 and （4 743.06 ±1 740.71）ng · h · mL^-1; AUC（0-inf） were （5 111.76 ±2 031.72）ng · h · mL^-1 and （4 942.71 ± 1 833.39）ng · h · mL^-1 for tested and reference formulation respectively. The 90% confidential interval of AUC（0-12） ,AUC（0-inf） and Cmax of tested formulation were 94.6% - 106.3% , 96.5% - 107.2% and 95.9% - 104.3% respectively. CONCLUSION The relative bioavailability was （ 101. 32 ± 14. 90 ） % ; The results of the statistic analysis showed that the two formulations were bioequivalence.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2008年第3期223-226,共4页
Chinese Journal of Modern Applied Pharmacy
关键词
奥关拉唑
药动学
相对生物利用度
生物等效性
高效液相色谱法
omeprazole
pharmacokinetics
relative bioavailability
bioequivalence
high performance liquid chromatography
