摘要
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 study the bioequivalence between tablet and capsule of kurorinone in healthy volunteers.Method: twenty volunteers were randomly divided into two groups(test and reference),ten in each,with double-cross experimental design.Blood amples were collected at 0, 0.25 , 0.5 , 1.0 , 1.25 , 1.5 ,2, 2.5 , 3.0 , 3.5 , 4.0 , 5.0 , 6.0 , 8.0 h after single oral dose of 600 mg tablet or capsule of kurorinone, respectively.The time-concentration of kurorinone were determined by HPLC and pharmacokinetic parameters were calculated with 3P97 practical pharmacokinetics program.Result: The pharmacokinetic parameters of kurorinone tablet and capsule were as follows: t 1/2 ( 2.144 ± 0.453 )h and ( 2.066 ± 0.439 )h,t max ( 2.275 ± 0.716 )h and ( 2.175 ± 0.654 )h,C max ( 0.384 ± 0.144 )μg·ml -1 and( 0.370 ± 0.132 )μg·ml -1 ,AUC 0-8 h ( 1.098 ± 0.278 )μg(ml·h) and ( 1.094 ± 0.280 )μg(ml·h),AUC 0-∞ ( 1.216 ± 0.292 )μg(ml·h) and( 1.200 ± 0.271 )μg(ml·h).The relative bioavailability of kurorinone tablet was ( 100.403 ± 6.281 )%.Conclusion: The statistical analysis showed that the test and reference preparations were bioquivalent.
出处
《中国药师》
CAS
2004年第8期582-584,共3页
China Pharmacist
