张强, MB, Yamamoto, HM, Aki, KH, Kubo, 廖工铁. 头孢类抗生素在水溶液中的聚合J. 药学学报, 1996, 31(4): 306-312.
引用本文: 张强, MB, Yamamoto, HM, Aki, KH, Kubo, 廖工铁. 头孢类抗生素在水溶液中的聚合J. 药学学报, 1996, 31(4): 306-312.
shu
Q Zhang, MB Yamamoto, HM Aki, KH Kubo , GT Liao, . POLYMERIZATION OF CEPHALOSPORINS IN AQUEOUS SOLUTIONJ. Acta Pharmaceutica Sinica, 1996, 31(4): 306-312.
Citation: Q Zhang, MB Yamamoto, HM Aki, KH Kubo , GT Liao, . POLYMERIZATION OF CEPHALOSPORINS IN AQUEOUS SOLUTIONJ. Acta Pharmaceutica Sinica, 1996, 31(4): 306-312.
shu

头孢类抗生素在水溶液中的聚合

POLYMERIZATION OF CEPHALOSPORINS IN AQUEOUS SOLUTION

    摘要
  • 摘要: 对7种头孢类抗生素:头孢唑肟钠(CZX),头孢噻肟钠(CTX),头孢曲松钠(CTRX),头孢替安(CTM),头孢孟多钠(CMD),头孢唑啉钠(CZL)和头孢噻吩钠(CLT)在水溶液中的聚合行为进行了研究。将头孢类抗生素的水溶液(10%～50%)在DEAE-Sephadex A-25离子交换色谱柱上,用含NaCl 0.2～3.0mol·L-1的磷酸盐缓冲液(pH 7.4～9.4),在室温下进行线性梯度洗脱,在260nm监测,收集各流分。用CD,FAB-MS和NMR等确证洗脱图谱中峰值对应的化合物,发现CMD,CZL,CLT,CTRX和CTM在实验条件下没有形成聚合物,CTX和CZX的水溶液在室温下放置几天可形成二聚物,表明分子中不含自由氨基或含有氨基,但空间或电荷位阻大时,没有聚合物形成。形成的二聚物是由于自由氨基向核进攻另一分子的β-内酰胺环,引起分子间氨解的结果。

     

    Abstract: The polymerization of 7 cephalosporins, including ceftizoxime Na (CZXj , cefotaximeNa (CTX) . ceftriaxone Na (CTRX),cefotiam 2 HCI (CTM) . eefamandole Na (CMD) i cefazolin Na(CZL) and cefalotln Na (CLT), in aqueous solution has been investigated in relation to their chemicalstructuree. The aqueous solution of cephalosporins was eluted on DEAE-Sephadex A-25 column by a lineargradient of 0.2～3.0 mol.L-1 NaCl (pH 7.4～9.4) at ambient temperatute. The ftactions werecharacterized by UV. CD, FAB-MS, and NMR spectrometries. No pelymers were observed from CTM,CTRX, CMD, CZL, and CLT solutions, while CZX and CTX were found to fotm dimers within a fewdays. The dimers were evidently confirmed to form through the intermolecular aminolysis of the β-lactamcarbonyl moiety by the NH2 group in the second molecule. However, the steric and ionic charge hindranceniay have a direct effect on the polymerization.

     

    • HTML全文
    • 参考文献(0)
    • 相关文章
    • 施引文献
  • 资源附件(0)

/

返回文章
返回