中国药房2011，Vol.22Issue(22)：2048-2050,3.
中国西部健康人群口服替诺福韦富马酸酯片的药动学研究
Pharmacokinetics of Tenofovir Disoproxil Fumarate Tablets in Healthy Volunteers from Western China
摘要
Abstract
OBJECTIVE: To study the pharmacokinetics of Tenofovir disoproxil fumarate (TDF) tablets in healthy volunteers from western China. METHODS: 24 healthy volunteers were randomly divided to 3 groups with 8 in each group. 3 groups were given 300 mg TDF tablets, 300 mg TDF tablets with 200 mg Emtricitabine tablets, 300 mg TDF tablets with high fat diet (the proportion of dietary fat was 50％ ), respectively. 2 mL of venous blood was collected at 0, 05, 0.75, 1, 1.5, 2, 3, 4,6,8, 12,24,36,48,72 h after administration, respectively. The plasma was separated to determine the concentration of tenofovir by HPLC-UV after solid phase extraction, and the pharmacokinetics parameter of tenofovir was calculated by DAS (Vet2.1.1)software. RESULTS: The main pharmacokinetic parameters of tenofovir in 3 groups were as follows: t1/2(18.78 ± 3.28)h, (12.72 ± 2.83)h,(13.08 ± 1.47)h; tmax(1.05 ± 0.16)h, (1.28 ± 0.30)h, (1.55 ± 0.37)h; cmax(290.71 ± 65.21)ng·mL-1, (420.84 ± 96.71) ng·mL-1,(429.06 ± 174.81)ng·mL-1; AUC0～72(1 871.60 ± 377.00)μg·h·L-1, (3 869.42 ± 962.85)μg·h·L-1, (3 569.47 ± 633.47)μg·h·L-1;AUC0～∞ (2 284.16 ± 373.54)μg·h·L-1, (4 107.09 ± 974.82)μg·h·L-1, (3 856.00 ± 618.39)μg·h·L-1; CL/F(2.25 ± 0.39)L·h-1·kg-1,( 1.28 ± 0.28 ) L· h- 1· kg - 1, ( 1.33 ± 0.20) L· h - 1· kg - 1. Compared with that of TDF treated group, cmax, tmax, AUC0～72 and AUC0～∞ in TDF+ emtricitabine treated group and TDF+high fat diet treated group were increased, and t1/2 were decreased. CONCLUSION:Pharmacokinetic characteristics of tenofovir disoproxil fumarate in Chinese healthy people are similar to that of the foreign crowd.High fat diet and combination with emtricitabine can change the pharmacokinetic properties of tenofovir.关键词
中国西部健康人群/替诺福韦富马酸酯/恩曲他滨/脂肪食物/药动学/高效液相色谱-紫外法Key words
Healthy volunteers from western China/ Tenofovir disoproxil fumarate/ Emtricitabine/ High fat diet/ Pharmacokinetics/ HPLC-UV分类
医药卫生引用本文复制引用
谭瑞,杨俊卿,颜波,尚京川,黄爱龙..中国西部健康人群口服替诺福韦富马酸酯片的药动学研究[J].中国药房,2011,22(22):2048-2050,3.基金项目
"艾滋病和病毒性肝炎等重大传染病防治"科技重大专项"十一五"计划(2008ZX10001-016) （2008ZX10001-016）
