Article Title

Synthesis and stability studies on a tripartite prodrug of cefuroxime


N-Cbz-tryptophan was attached to cefuroxime at its 4-COOH via L-serine methyl ester to form compound 1. This compound is designed as a tripartite prodrug of cefuroxime for oral use. The compound was stable in pH 6.5 and pH 7.4 phosphate buffer solutions. Sixty percent of this compound remained intact after incubation in a mucosal suspension prepared from rat intestine at 37°C for 2.5 hr. The stability of this compound toward intestinal degradation indicated that it might be feasible as an oral prodrug of cefuroxime. Oral bioavailability in terms of the prodrug and the released parent drug is currently being investigated.

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