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目的 :比较苦参素片剂与胶囊剂的生物等效性。方法 :2 0名男性健康志愿者 ,双交叉于试验当日晨空腹一次口服试验制剂苦参素片、参比制剂苦参素胶囊 6 0 0mg ,于药前和药后 0 .2 5 ,0 .5 ,1.0 ,1.2 5 ,1.5 ,2 .0 ,2 .5 ,3.0 ,3.5 ,4 .0 ,5 .0 ,6 .0 ,8.0h取肘静脉血 ,高效液相色谱法测定主要成分氧化苦参碱血药浓度。氧化苦参碱血药浓度 时间数据经 3P97处理 ,得药动学参数 ,参数进行方差分析、双单侧t检验和 (1- 2α)置信区间分析 ,并计算相对生物利用度评价两种制剂的生物等效性。结果 :苦参素片和苦参素胶囊氧化苦参碱主要药代动力学参数t1/ 2 分别为 (2 .14 4± 0 .4 5 3)h和 (2 .0 6 6± 0 .4 39)h ,tmax分别为 (2 .2 75± 0 .716 )h和 (2 .175± 0 .6 5 4 )h ,Cmax分别为 (0 .384± 0 .14 4 ) μg·ml-1和 (0 .370± 0 .132 ) μg·ml-1,AUC0 -8h分别为 (1.0 98±0 .2 78) μg·ml-1·h和 (1.0 94± 0 .2 80 ) μg·ml-1·h ,AUC0 -∞ 分别为 (1.2 16± 0 .2 92 ) μg·ml-1·h和 (1.2 0 0± 0 .2 71) μg·ml-1·h。试验制剂苦参素片相对生物利用度F(以氧化苦参碱计 )为 10 0 .4 0 3%± 6 .2 81% ,两制剂具有生物等效性。结论 :苦参素片和苦参素胶囊为生物等效制剂。
Objective : To compare the bioequivalence of oxymatrine tablets and capsules. METHODS: Twenty male healthy volunteers were randomly assigned to receive oral osinol tablets and ginsenoside capsules (600 mg) from a single oral test on the morning of the day of the test. The drug was pre-dose and 0.25 post-dose. 5, 1.0, 1.2 5, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.00, 8.0h venous venous blood were taken, and the main components of oxidative bitterness were determined by HPLC. Senate blood drug concentration. Oxymatrine plasma concentration time data were processed by 3P97 to obtain pharmacokinetic parameters and parameters for analysis of variance, double unilateral t-test, and (1- 2α) confidence interval analysis, and relative bioavailability evaluation of two preparations Bioequivalence. RESULTS: The main pharmacokinetic parameters of oxymatrine (T1/2) of oxymatrine and oxymatrine capsules were (2.14 4±0.45)h and (0.66±0.4), respectively. 39) h, tmax were (2. 2 75 ± 0 .716) h and (2 .175 ± 0. 6 5 4) h respectively, and Cmax was (0.384 ± 0.144) μg·ml-1, respectively. And (0.370± 0 .132) μg·ml-1, AUC0 -8h were (1.0 98±0 .2 78) μg·ml-1·h and (1.0 94± 0 .2 80 ) μg·ml, respectively. -1 · h , AUC0 - ∞ were (1.2 16 ± 0.292) μg·ml -1 · h and (1.2 0 ± ± 0.271) μg·ml -1 · h, respectively. The relative bioavailability F (measured by oxymatrine) of the test preparation Kushenin Tablets was 100.43%±6.22%, and the two preparations were bioequivalent. Conclusion: Kushensu tablets and oxymatrine capsules are bioequivalent.