国产麦角溴烟酯缓释胶囊的相对生物利用度和生物等效性评价

RELATIVE BIOAVAILABILITY AND BIOEQUIVALENCE EVALUATION OF DOMESTIC ETICER

10名健康男性志愿者采用交叉给药方案，分别多剂量口服30mg国产和进口麦角溴烟酯纷释胶囊，用HPLC法测定代谢较快者血浆中麦角淇烟酯代谢产物Ⅱ（MDL）浓度，进行国产制剂生物利用度和生物等效性评价，其生物等效性采用方差分析和单侧t检验判定。结果表明：国产与进口胶囊达稳态后MDL血药浓度－时间曲线均符合一室模型，Cmax分别为47．41±9．77μg／L和47．88±8．46μg／L，AUC分别是754，60±96．77μg·h·L－1778．45±80．16μg·h·L-1，FI（峰谷波动）为1．70±0．05和1．68±0．08。国产麦角溴烟酯的相对生物利用度是96．94％，两种制剂的药代动力学参数经数理学统计，无显著性差异（P＞0．05）。

Ten healthy male volunteers were given orally domestic or imported eticer capsule,with a multdose of 30 mg in randomized crossover study, there were no unchanged eticer in plasma,the decision on bioequivalence and the relative bioavailability were based on the results of metabolite n (MDL) in the fast metabolizing volunteers. The plasma concentration of MDL was assayed by HPLC and the bioequivalence of the formulations was evaluated by analysis of variance and two onesided tests. the peak levels of MDL in plasma were 47. 41±9. 77 μg/ L and 47. 88 ± 8. 46 μg/ L, respectively. The areas under the drug concentration curves were 754. 60± 96. 77μg· h· L-1 and 778. 45 ± 80. 16μg· h· L-1, respectively. Peak through fluctuation(PTF) were 1. 70± 0. 05 and 1. 68 ± 0. 08respectively. The relative bioavailability of domestic capsule was 96. 94%. The results suggested the two formulations were of bioequivalence.