Pharmacokinetic Study of Ceftriamidine Sodium for Injection in Chinese Healthy Volunteers

Background: MRSA and PRSP resistance has surged over 30 years, threatening clinical outcomes; China-developed cefathiamidine sodium, with enhanced pharmacokinetics, offers potent activity against these Gram-positive pathogens. Objectives: This study evaluates the pharmacokinetic profile of injectable ceftriamidine sodium in healthy volunteers and compares its pharmacokinetics with those of cefathiamidine. Materials and Methods: This clinical trial was a randomized and controlled study. The ceftriamidine sodium group (administered ceftriamidine sodium or placebo) employed a double-blind design with multiple administrations and dose escalation, whereas the cefathiamidine group (administered cefathiamidine) utilized an open-label design with single and multiple continuous administrations. The clinical trial involved ceftriamidine sodium at doses of 3.0 and 4.0 g, corresponding to cefathiamidine doses of 0.5 and 2.0 g. Volunteers received the corresponding drug infusions as per the protocol, and a series of blood samples were collected at specified time points for pharmacokinetic analysis. Results: In the 3.0 and 4.0 g dose groups of ceftriamidine sodium, the t1/2, Tmax, and Cmax were 1.98–2.11 h, 0.50 h, and 321.14–448.80 μg/mL, respectively. Upon reaching steady state after multiple doses of 3.0–4.0 g, no significant drug accumulation was observed. Following multiple administrations of cefathiamidine at 0.5 and 2.0 g, the peak time at steady state was 0.50 h, t1/2 was 1.26–1.17 h, and Cmax was 48.11–194.40 μg/mL. Conclusion: The half-life of ceftriamidine sodium (1.98–2.11 h) is almost twice as long as that of cefathiamidine (1.17–1.26 h), indicating its pharmacokinetic superiority in reducing the frequency of administration.