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KMID : 0369819950250040323
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Jorunal of Korean Pharmaceutical Sciences
1995 Volume.25 No. 4 p.323 ~ p.330
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Synthesis and Biopharmaceutical Studies of Ceftezole Pivaloyloxymethyl ester, a Novel Prodrug of Ceftezole
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Abstract
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Ceftezole pivaloyloxymethyl ester(CFZ-PV) was synthesized to improve oral absorption and bioavailability of parent drug by esterification of ceftezole(CFZ) with chloromethyl pivalate. The successful synthesis of CFZ-PV was conformed by
spectroscopic
analysis. Partition coefficient studies showed that CFZ-PV is more lipophillic than CFZ. The pharmacokinetic characteristics of CFZ-PV and CFZ were compared following oral administrations of these compounds to rabbits The amount of CFZ in plasma
was
determined with an HPLC method. The ester compound (prodrug) was not detected in plasma following oral administration of CFZ-PV, and although CFZ-PV and not microbiological activity in vitro, the plasma taken after oral administration of CFZ-PV
had
microbiological activity. From above observations, it was noted that CFZ-PV is rapidly hydrolyzed to CFZ in the body. And the oral absorption of CFZ-PV was increased by yielding 2-fold bioavalability rather than CFZ. Therefore, CFZ-PV could be a
novel
prodrug of CFZ which can improve the oral dioavailability of CFZ.
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