对乙酰氨基酚栓剂人体相对生物利用度和生物等效性  

Assessment of the bioavailability and bioequivalence of paracetamol suppository

作　　者：郭红英[1] 王曼丽[1] 赵志刚[2] 张晋华[1] 王汝龙[1] 

机构地区：[1]北京友谊医院临床药理研究室,北京100050 [2]北京天坛医院临床药理研究室,北京100050

出　　处：《中国新药杂志》2004年第9期831-834,共4页Chinese Journal of New Drugs

摘　　要：目的：研究进口试验制剂与国产对乙酰氨基酚栓剂(参比制剂)的相对生物利用度和生物等效性。方法：采用HPLC法测定18例健康男性志愿者单次交叉直肠给予参比制剂2粒(300mg)及试验制剂2粒(250mg)后的血药浓度，经CRFB软件处理，计算其药动学参数和相对生物利用度，评价两制剂的生物等效性。结果：试验制剂和参比制剂的t1/2分别为(3．94±1.54)和(3．81±1.24)h；Tmax分别为(1．56±0．57)和(1．58±0．43)h；平均滞留时间MRT0-tn分别为(5．67±1．44)和(5．40±1．28)h；Cmax分别为(1．73±0．38)和(1．61±0．34)μg·mL-1；AUC0-tn分别为(8.01±2．20)和(7．54±1．82)μg·h·mL-1。试验品与参比品的相对生物利用度为(109．07±27．92)％，经统计学处理，试验品AUC0-t的90％置信区间为97．20％-115．85％，Cmax的90％置信区间为98．64％-116．97％。结论：两制剂生物等效。Objective:To compare the relative bioavailability and bioequivalence of paracetamol suppository imported (test) to the one locally manufactured (reference). Methods: Eighteen healthy volunteers were randomized to receive a single crossover rectal dose of test (250mg) or reference suppositories (300mg). The plasma paracetamol concentrations in both groups were determined by HPLC. Results:Based on the analysis by CRFB program, the pharmacokinetics parameters of test and reference suppositories were as follows: t1/2(3.94±1.54) vs (3.81±1.24)h; Tmax(1. 56±0.57) vs (1.58±0.43)h;MRT0-tn(5.67±1.44) vs (5.40±1.28)h;Cmax(1.73±0.38) vs (1.61±0.34)μg·mL-1; AUC0-tn(8.01±2.20) vs (7.54±1.82)h·μg·mL-1. The relative bioavailability of the test suppository was (109.07±27.92) % compared to reference suppository. The AUC0-t and Cmax of test suppository were within 97. 20%-115. 85% and 98. 64%-116. 97% of the reference suppository using the 90% confidence interval. Conclusion:The test suppository is bioequivalent to the reference suppository.

关 键 词：对乙酰氨基酚 生物等效性 相对生物利用度 栓剂 

分 类 号：R971.1[医药卫生—药品] R969.1[医药卫生—药学]