5-单硝酸异山梨酯缓释胶囊的人体生物等效性Relative bioavailability of 5 ISMN sustained release capsules in normal volunteers
代宗顺,刘奕明,侯淑贤
DAI Zong shun; LIU Yi ming; HOU Shu xian (The Institute of Clinical Pharmacology in Tongji Medical University;
摘要(Abstract)：
采用GC法测定 5 单硝酸异山梨酯血浆药物浓度 ,研究 5 单硝酸异山梨酯缓释胶囊相对生物利用度和生物等效性。 18名健康志愿者随机交叉单剂量口服试验药 (T)与对照药 (R) 4 0mg ,测得Cmax分别为 (348 3± 146 8)ng/mL和 (347 9± 2 0 2 4)ng/mL ;Tmax 分别为 (4 7± 1 8)h和(4 6± 1 7)h ;AUC( 0 -n) 分别为 (3 933 2± 142 5 0 )ng h/mL和 (3 6 93 0± 12 39 5 )ng h/mL ;相对生物利用度为 (10 6 6± 16 9) %。 18名志愿者随机交叉多剂量口服T与R ,测得达稳态的Cmax分别为 (2 30 9± 72 4)ng/mL和 (190 9± 6 6 9)ng/mL ;Cmin分别为 (4 2 6± 2 3 5 )ng/mL和 (4 7 4±2 2 1)ng/mL ;AUCSS分别为 (2 939 4± 92 2 1)ng h /mL和 (2 6 6 7 4± 832 9)ng·h /mL ;DF分别为1 6± 0 4和 1 3± 0 3 ;相对生物利用度为 (111 0 2± 2 1 0 5 ) %。经生物等效性分析 ,两制剂在单剂量与多剂量条件下生物等效
To study the relative bioavailability of 5 ISMN sustained release capsules,18 healthy volunteers were given single or multiple oral dose in a randomized crossover study. The concentration of 5 ISMN in plasma was determined by GC. After a single dose (40 mg), C max of 5 ISMN were (348 3±146 8)ng/mL and(347 9±202 4)ng/mL, T max (4 7±1 8)h and (4 6±1 7)h, AUC (0- n ) (3 933 2±1 425 0)ng·h/mL and (3 693 0±1 239 5)ng·h/mL for test formulation(T) and reference formulation(R), the relative bioavailability was(106 6±16 9)%.Following the multiple dose, C max in the steady state were (230 9±72 4)ng/mL and(190 9±66 9)ng/mL, C min (42 6±23 5)ng/mL and(47 4±22 1)ng/mL,AUC SS ( 2 939 4± 922 1)ng·h/mL and(2 667 4±832 9)ng·h/mL,DF 1 6±0 4 and 1 3±0 3 for T and R, the relative bioavailability was(111 02±21 05)%. The result of the statistic analysis showed that the two preparations were bioequivalent.
关键词(KeyWords)：
5-单硝酸异山梨酯;缓释胶囊;生物利用度;气相色谱法
ISMN; sustained release capsule; bioavailability; L
基金项目(Foundation):
作者(Authors):
代宗顺,刘奕明,侯淑贤
DAI Zong shun; LIU Yi ming; HOU Shu xian (The Institute of Clinical Pharmacology in Tongji Medical University;