酒石酸双氢可待因/对乙酰氨基酚片在健康人体内的生物等效性  

BIOEQUIVALENCE OF PARACETMOL AND DIHYDROCODEINE TARTRATE TABLETS IN CHINESE HEALTHY VOLUNTEERS

作　　者：刘丽京[1] 孙莉[1] 邓艳萍[1] 

机构地区：[1]北京大学中国药物依赖性研究所,北京100191

出　　处：《中国药物依赖性杂志》2015年第2期112-115,共4页Chinese Journal of Drug Dependence

摘　　要：目的:研究对乙酰氨基酚/酒石酸双氢可待因片在健康志愿者中的生物利用度和生物等效性。方法:22例健康志愿者随机单盲、单剂量、双周期两制剂交叉口服国产制剂(试验制剂)与进口制剂(参比制剂),剂量为酒石酸双氢可待因20 mg,对乙酰氨基酚1000 mg,用高效液相色谱法测定10个时间点的血药浓度,采用3P97程序计算主要药代动力学参数和相对生物利用度,并评价两种制剂生物等效性。结果:单剂量口服试验制剂与进口标准参比制剂后,血浆中双氢可待因的AUC0-12分别为399.51 ng·h·ml-1±67.94 ng·h·ml-1和415.10 ng·h·ml-1±68.31 ng·h·ml-1,Cmax分别为78.08 ng·ml-1±28.18 ng·ml-1和79.73 ng·ml-1±24.35 ng·ml-1,Tmax分别为0.98 h±0.61 h和1.20 h±0.64 h。对乙酰氨基酚的AUC0-12分别为59.41μg·h·ml-1±16.78μg·h·ml-1和58.21μg·h·ml-1±17.07μg·h·ml-1,Cmax分别为15.98μg·ml-1±5.25μg·ml-1和15.89μg·ml-1±6.30μg·ml-1,Tmax分别为0.93 h±0.65 h和1.15 h±0.81 h。相对生物利用度分别为97.2%±14.4%和102.7%±8.3%。试验药双氢可待因和对乙酰氨基酚的AUC0-t90%可信限分别为91.5%-101.2%和99.8%-105.1%,Cmax90%可信限分别为85.6%-109.8%和93.8%-111.4%。结论:两种制剂生物等效。Objective：To study the bioequivalence of paracetamol and dihydrocodeine tartrate tablets in healthy volunteers. Methods：A single oral dose of the test and the reference preparations were given to 22 healthy volunteers in a randomised crossover study. The concentrations of dihydrocodeine and paracetamol in plasma were determined by HPLC, respectively. The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of dihydrocodeine and paracetamol were evaluated by 3p97 program. Results：After a single dose,the pharmacokinetic parameters for dihydrocodeine were as follows： AUC0-12 were 399.51 ng· h · ml^-1± 67.94 ng · h· ml^-1and 415.10 ng · h·ml^-1±68.31 ng· h· ml^-1,Cmax were 78.08 ng· ml^-1±28. 18 ng · ml^-1 and 79.73 ng± ml^-1±24.35 ng· ml^-1, Tmax were 0. 98 h ±0. 61 h and 1.20 h ±0.64 h for the test and the reference preparations,respectively. The pharmacokinetic parameters for paracetamol were as follows： AUC0_12 were 59.41μg · h· ml^-1± 16. 78μg· h· ml^-land 58. 21μg· h· ml^-1±17. 07μg ·h · ml^-1 ,Cmax were 15.98μg · ml^-1 ±5.25 μg· ml^-1 and 15.89 μg · ml^-1 ±6.30 μg · ml^-1,Tmax were 0.93 h±0. 65 h and 1.15 h±0. 81 h for the test and the reference preparations, respectively. The relative bioavailability were 97.2% ±14.4% and 102. 7% ± 8.3%. AUC0-t, of dihydrocodeine and paracetamol were within 91.5% - 101.2% and 99. 8% - 105. 1% ,Cmax of dihydrocodeine and paracetamol were within 85. 6% - 109. 8% and 93.8% - 11 . 4 % for the 90% confidence interval, respectively. Conclusion ：The test preparation is bioequivalent to the reference preparation.

关 键 词：酒石酸双氢可待因 对乙酰氨基酚 生物等效性 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学] R971.1[医药卫生—药学]