Abstract: AIM: To evaluate the pharmacokinetics of multiple-dose Ceftriaxone/Sulbactam (4:1) injection in Chinese health volunteers.METHODS: The serum samples and urine samples of 12 healthy volunteers were collected after injecting 2.50 g Ceftriaxone/Sulbactam (4:1) injection for 7 days.RESULTS: All health volunteers were well tolerated.The pharmacokinetic parameters were calculated by DAS software.The average of C_max was 202.60 ±26.31 mg·L ^-1, C_av was 60.65 ±8.85 mg·L ^-1, AUC_ss was 1455.68 ±212.41 mg·L ^-1 ·h, DF was 3.36 %, FI was 96.77 %.The 72 h cumulative urinary excretion rate of Ceftriaxone was 43.61 %±10.23 % and the 12 h cumulative urinary excretion rate of Sulbactam was 71.61 %±10.06 %.CONCLUSION: 2.50 g multiple-dose Ceftriaxone Sulbactam (4:1) injection is well tolerated in the health volunteers.According to the results of pharmacokinetic parameters, there is no pharmacokinetic change between the two drugs from the compound preparation, and there is no drug interaction between them.

Key words: Ceftriaxone/Sulbactam (4:1) injection, pharmacokinetics, HPLC, multiple-dose