摘要
目的:建立人血浆中罗红霉素高效液相色谱-质谱联用测定法(HPLC-MS),研究罗红霉素胶囊的生物等效性。方法:采用双交叉试验设计,血样用乙酸乙酯-异丙醇(95:5)混合液提取,HPLC-MS分离测定,根据血药浓度-时间数据估算主要药动学参数和相对生物利用度,评价生物等效性。结果:罗红霉素两制剂的t1/2分别为(9.2±3.7)和(9.3±4.0)h,Tmax分别为(2.1±0.6)和(2.1±0.8)h,Cmax分别为(11823.0±3157.0)和(11856.0±2970.0)ng/ml,AUC0-t分别为(148800.0±42312.0)和(136443.0±39653.0)ng·h/ml。AUC0-∞分别为(162808.0±48977.0)和(149650.0±48077.0)ng·h/ml。受试制剂的相对生物利用度为(111.2±22.9)%。受试制剂AUC0-t和Cmax的90%置信区间为参比制剂相应参数的100.9%～117.8%和91.3%～107.4%,符合生物等效性指导原则。结论:本法简便,灵敏准确。罗红霉素两制剂生物等效。
Objective：To establish high-performance liquid chromatography mass spectrometry （HPLC-MS） method for the quantitative determination of roxithromycin in human plasma,and to study the bioequivalence of roxithromycin. Methods： Two-way crossover trial was performed. The plasma samples were extracted with ethyl acetate-isopropanol mixed liquor （95：5） and determined by HPLC-MS. The main pharmacokinetic parameters and relative bioavailability were estimated by plasma concentration-time data,and the bioequivalence was evaluated. Results： The parameters of roxithromycin for test and reference formulations were as follows： t1/2,9.2±3.7 h and 9.3±4.0 h;Tmax,2.1±0.6 h and 2.1±0.8 h;Cmax,11 823.0±3 157.0 ng/ml and 11 856.0±2 970.0 ng/ml;AUC0-t,148 800.0±42 312.0 ng·h·ml^-1 and 136 443.0±39 653.0 ng·h·ml^-1;AUC0-∞,162 808.0±48 977.0 ng·h·ml^-1 and 149 650.0±48 077.0 ng·h·ml^-1. The relative bioavailability of the test formulation was 111.2%±22.9%. The 90% confidence intervals were 100.4%~110.4% for AUC0→t and 100.9%~116.2% for Cmax,which were conformed to the bioequivalence guideline. Conclusion： HPLC-MS method used in the study is sensitive,accurate,and convenient. These 2 formulations of roxithromycin are bioequivalent.
出处
《中国医科大学学报》
CAS
CSCD
北大核心
2007年第4期429-431,共3页
Journal of China Medical University
关键词
罗红霉素
高效液相色谱-质谱联用
生物等效性
roxithromycin
high-performance liquid chromatography mass spectrometry
bioequivalence
