头孢氨噻肟的长效研究

STUDY ON PROLONGED ACTION CEFOTAXIME

头孢氨噻肟(CTX)与二苄基乙二胺醋酸盐反应,制成长效的头孢氨噻肟(头孢氨噻肟二苄基乙胺盐,BCTX)。元素分析、紫外、红外、核磁共振、质谱等证明了BCTX的结构式。BCTX微溶于水,特性溶出速度为0.183μg/ml·min.水混悬液降解符合零级动力学过程,室温分解速度常数为1.69×10^(-7)mg/ml·s.BCTX的水混悬液与CTX的水溶液家兔动力学试验表明,BCTX具有长效作用。

A prolonged action cephalosporin was prepared by the reaction of cefotaxime sodium (CTX) with N, N-dibenzylethylene diamine acetate. It is reasonable to consider the resultant as benzathine cefotaxime (BCTX) by means of elemental analysis, DSC, UV spectra, IR spectra, NMR spectra and mass spectra. In contrast to CTX, BCTX appeared to be almost insoluble in water and its intrinsic dissolution rate was 0.183μg/ml·min. The stability revealed that the degradation of BCTX suspension in water followed zero-order kinetics and the rate of degradation at room temperature was found to be 1.67×10^(-7)mg/ml·s. An in vivo test by using 12 rabbits given BCTX sttspension and CTX solution intramuscularly was conducted. The results showed that the former was longer in maintaining serum drug level than the latter.