奥硝唑胶囊人体药代动力学及生物等效性研究

Study of the Pharmacokinetics and Bioequivalance of Ornidazole Capsules andImported Ornidazole Tablets in Healthy Volunteers

目的:研究国产奥硝唑胶囊在人体内的药代动力学参数和生物等效性.方法:18名健康男性志愿者随机交叉口服国产奥硝唑胶囊1.5g和进口奥硝唑片1.5g,采用HPLC法测定给药后不同时间点血浆奥硝唑的浓度,评价两种制剂的生物等效性.结果:两种制剂的血药浓度曲线均符合二室模型,主要药代动力学参数:t1/2(β)分别为16.08±2.32h和15.85±2.26h,Tmax分别为1.75±0.49h和1.75±0.48h,Cmax分别为21.94±3.31mg·L-1和22.58±5.94mg·L-1AUC0～72分别为446.50±55.14mg·h·L-1和433.31±58.52mg·h·L-1,AUC0～∞分别为465.22±56.73mg·h·L-1和451.67±57.97mg·h·L-1.国产奥硝唑胶囊的相对生物利用度为103.52%±6.59%,两种制剂主要药代动力学参数均无显著性差异(P>0.05).结论:双单侧t检验结果提示,国产奥硝唑胶囊和进口奥硝唑片具有生物等效性.

OBJECTIVE:To study the pharmacokinetic profiles and bioequivalenceof ornidazole in healthy volunteers. METHODS: l.5g single oral dose of domesticornidazole capsules and imported ornidazole tablets were given to l8 healthyvolunteers in an open randomized crossover. Ornidazole concentrations in plasmawere determined by HPLC method. The pharmacokinetic parameters as well asrelative bioavailability were measured. RESULTS: The concentration-time curves ofcapsules and tablets ornidazole were conformed to a two-compartment model witha lag time. The pharmacokinetic parameters of capsules and tablets ornidazole wereas follows:t(1/2)(β),were l6.08±2.32h and l5.85±2.26h;Tmax were l.75±0.49h andl.75±0.48h;Cmax were 2l.94±3.3lmg.L-1 and 22.58±5.94 mg.L-1;AUC0~∞ were 456.22±446.50±55.l4mg.h.L-1 and 433.3l±58.52 mg.h.L-1;AUC0~∞co were 465.22±56.73mg.h.L-1and 45l .67±57.97mg.h.L-1, respectively. There were nosignificant difference between the two formulations (P>0.05). The relativebioavailability of ornidazole capsule was l03.52%±6.59%. CONCLUSION: Theresult of the statistical analysis showed that the two formulations werebioequivalent.