Abstract: A randomized, open, fasting, single dose, two sequence, two cycle and double cross administration trial design was adopted. Took the test or reference efavirenz tablets of 200 mg orally in a single time. The plasma concentration of efavirenz in healthy subjects was determined by LC-MS/MS. WinNonLin8.1 software was used to calculate the main pharmacokinetic parameters of efavirenz and to evaluate the bioequivalence. The main pharmacokinetic parameters within 72 h: t_max were 2.574 ±0.871 and 2.808 ±0.912 h; C_max were 1 586.732 ±424.538 and 1 549.518 ±366.086 ng·mL^-1; AUC_{0-72 h} were 28 464.672 ±5 682.518 and 27 828.826 ±5 082.487 h·ng·mL^-1; t_1/2 were 63.524 ±26.037 and 58.748 ±20.950 h; λ_z were 0.013 ±0.006 and 0.013 ±0.005 h^-1. The main bioequivalence indicators were as follows: The 90% confidence interval of C_max was 95.62%-107.15%, and the geometric mean ratio was 101.22%; The 90% confidence interval of AUC_{0-72 h} was 100.43%-104.38%, and the geometric mean ratio was 102.38%. The results showed that the main pharmacokinetic parameters of the test drug and the reference drug were similar, and the two preparations had bioequivalence. This human bioequivalence clinical study was approved by the drug clinical trials ethics committee of the Second Hospital of Anhui Medical University (ethics approval No.: YW2021-110).