国产氧氟沙星片剂健康人体生物等效性研究  

Bioequivalence of Domestic Ofloxacin Tablets in Chinese Healthy Volunteers

作　　者：张莉[1] 吕媛[1] 李曼宁[1] 刘燕[1] 李天云[1] 肖永红[1] 

机构地区：[1]北京大学临床药理研究所,北京100083

出　　处：《中国临床药理学杂志》2002年第5期349-353,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的:研究国产氧氟沙星片剂（泰利必妥）的相对生物利用度并求证该制剂的生物等效性。方法:22名男性健康受试者随机交叉给药,分别口服单剂量氧氟沙星国产片剂（试验制剂）及进口片剂（参比制剂）,采用反相高效液相色谱法测定血及尿药浓度,计算两者的药代动力学参数及相对生物利用度,并求证国产片与进口片的生物等效性。结果:口服氧氟沙星200mg国产及进口片剂的主要药代动力学参数t1/2分别为6.08±0.87和6.49±0.68h;tmax分别为0.86±0.26和0.88±0.34h;Cmax分别为2.61±0.53和2.75±0.52mg·L-1;AUC0-t分别为15.54±1.81和15.60±1.42mg·h·L-1;AUC0-∞分别为5.91±.78和15.97±1.40mg·h·L-1。36h平均尿药累积排泄百分率分别为75.12％±7.82％和74.77％±8.15％。经计算试验制剂（国产）对于参比制剂（进口）的平均相对生物利用度AUC0-t为99.75％±8.73％。两种片剂的AUC0-t及Cmax经对数转换后多因素方差分析结果显示,周期间及处方间均无显著性差异（P>0.05）,但个体间有显著牲差异（P<0.05）;双单侧t检验表明,InAUC0-t及InCmax的检验统计量t1、t2均大于t0.05（20）=1.725,故接受两种片剂生物等效的假设,AUC0-t90％置信区间为91.8％～105.9％,Cmax为75.0％～104.5％,根据本试验结果。The aim of this research is to study the relative bioavailability of ofloxacin tablet in Chinese healthy volunteers and to evaluate the bioequivalence. METHODS: A single oral dose 200mg of domestic and imported ofloxacin tablets was given to 22 healthy volunteers in a randomized cross-over study. The concentrations of ofloxacin in serum and urine were determined by HPLC. Results: the main pharmacokinetic parameters of two formulations ,domestic and imported tablet, were as follows: t1/2b were 6.28±0.87 and 6.49±0.68 h; tmax were 0.86±0.26and 0.88±0.34h;Cmax were 2.61±0.53 and 2.75±0.52 mg·L-1;AUC0-1 were 15.54±1.80 and 15.60±1.42 mg·h·L-1;AUC1-∞ were 15.91±1.78 and 15.97±1.40 mg·h·L-1, respectively. The 36-hour cumulative urinary excretion rate were 75.12±7.82% and 74.77±8.15%,The relative bioavailability of AUC0-t was 99.75±8.73%.The results of ANOVA and two one-sided t test statistical analysis for In AUC0-∞ and InCmax showed that two formulations were bioequivalent. The 90% confidenceinterval of AUC0-t was 91.8%-105.9% was 75.0%-104.5%, then could evaluatethe two tablets were bioequivalent. CONCLUSION: The domestic and imported ofloxacin tablets were bioequivalent.

关 键 词：氧氟沙星 片剂 人体生物等效性 生物利用度 高效液相色谱法 

分 类 号：R978.19[医药卫生—药品] R969.1[医药卫生—药学]