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头孢呋新(ce furoxi me)为注射用第二代头孢菌素。它体外抗菌活性很强,对肠道细菌产的β内酰胺酶稳定性高,且药代动力学特征良好。因为它在生理pH时高度离解,脂溶性差,基本上口服不吸收。头孢呋新酯(Cefuroxime axe(?)l)为头孢呋新前体药,在头孢呋新C4位羧基上发生酯化,从而提高了亲脂性,增加口服后吸收率。头孢呋新酯吸收后仅3～4分钟内在肠粘膜和门循环中迅速水解,去酯分解为头孢呋新、乙醛和乙酸。血循环中测不到头孢呋新酯原药。制剂由于曾存在一些与药物本身理化特性有关的问题,发展头孢呋新酯花了相当长的时间。
Cefloxacin is the second generation cephalosporin for injection. Its strong antibacterial activity in vitro, β-lactamase production of intestinal bacteria high stability, and good pharmacokinetic characteristics. Because it is highly hydrolysable at physiological pH, it has poor lipid solubility and is essentially not absorbed orally. Cefuroxime axe (?) L is a cefuroxime prodrug esterified at the carboxyl of cefuroxime C4, thereby increasing the lipophilicity and increasing the absorption rate after oral administration. After cefuroxime axetil absorption only 3 to 4 minutes in the intestinal mucosa and door cycle rapid hydrolysis, to ester decomposition of cefuroxime, acetaldehyde and acetic acid. Can not be measured in the blood circulation of cefuroxime axetil. Formulation Cefuroxime axetilization took considerable time because of some problems with the physical and chemical properties of the drug itself.