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KMID : 0369819940240040265
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Jorunal of Korean Pharmaceutical Sciences
1994 Volume.24 No. 4 p.265 ~ p.271
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Development of Cefazolin Prodrug for Oral Administration - Synthesis , Partition Coefficient and Antibacterial Activity of Cefazolin Ethoxycarbonylethyl Ester -
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정영국/Jung YG
범진필/최준식/이진환/Burm JP/Choi JS/Lee JH
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Abstract
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Cefazolin ethoxycarbonylethyl ester (CFZ-ET) was synthesized to improve oral absorption and bioavailability of the parent drug by esterification of sodium cefazolin (CFZ-Na). The successful synthesis of CFZ-ET was identified with analysis of UV spectra, FT-lR spectra and NMR spectra. Partition coefficient studies showed that CFZ-ET was more lipophilic than CFZ-Na and the ester was hydrolyzed into the parent drug in vivo. Although CFZ-ET did not have antimicrobial activity in vitro, the plasma taken after the oral administration of CFZ-ET had antimicrobial activity. Based on above observations, CFZ-ET might be rapidly hydrolyzed to CFZ in the body. Therefore, it may be concluded that CFZ-ET could be a novel prodrug of CFZ which can improve the bioavailability of CFZ-Na.
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KEYWORD
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Cefazolin ethoxycarbonylethyl ester, Sodium cefazolin, Prodrug, Partition coefficients, Antimicrobial activity
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