Prodrugs pp 1195-1205 | Cite as

Case Study: Cefuroxime Axetil: An Oral Prodrug of Cefuroxime

  • Tarra Fuchs
Part of the Biotechnology: Pharmaceutical Aspects book series (PHARMASP, volume V)


Cefuroxime axetil (Ceftin®, Zinnat®) was designed to be an oral form of cefuroxime (Zinacef®), a second-generation cephalosporin antibiotic available by IV and IM injection (O’Callaghan et al., 1976; Brogden et al., 1979; Emmerson, 1988). Cefuroxime is a useful antibiotic because it is a broad-spectrum antibiotic, effective against bacterial strains with β-lactamase activity (Dürckheimer et al., 1985; Kees and Grobecker, 1995). The parenteral cefuroxime, like other cephalosporins, is not orally absorbed because it contains a highly polar carboxyl group that is ionized at intestinal pH, making transport across intestinal mucosa unlikely (Foord, 1976; Tsuji et al., 1986). An attempt to deliver the free acid orally led to only 1% of the drug recovered in the urine (Foord, 1976).


Antimicrob Agent Cefuroxime Axetil Lactam Antibiotic Film Coated Tablet Ethyl Bromide 
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Copyright information

© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • Tarra Fuchs
    • 1
  1. 1.Sunesis PharmaceuticalsSouth San FranciscoUSA

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