Pharmacokinetics of Tenofovir Disoproxil Fumarate Tablets in Healthy Volunteers from Western China

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, 0.5, 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(Ver2.1.1)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±63.21)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.