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題名 | Synthesis and Stability Studies on a Tripartite Prodrug of Cefuroxime=含絲胺酸及色胺酸之Cefuroxime先驅藥的合成及安定性研究 |
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作者姓名(中文) | 李嘉帥; 辜頌惟; 呂益慧; 王惠珀; | 書刊名 | 藥物食品分析 |
卷期 | 5:3 1997.09[民86.09] |
頁次 | 頁185-191 |
分類號 | 418.41 |
關鍵詞 | Cefuroxime三元式先驅藥; 絲胺酸; 色胺酸; 合成; 腸液中之安定性; Cefuroxime; Tryptophan; Tripartite prodrug; Stability; |
語文 | 英文(English) |
中文摘要 | Cefuroxime為臨床上廣為使用之β-lactam類抗生素,然其缺點為口服生體可用率 低,僅能打針。加上其體內分布體積小、腎臟清除率高,致體內半衰期為1.1小時。本研究 以研發可口服吸收之Cefuroxime先驅藥為目標,設計合成一含有絲胺酸及色胺酸之三元式 先驅藥1。期以先驅藥之脂溶性增加而成為口服劑型,並藉由色胺酸之高蛋白吸附力而減緩 Cefuroxime腎臟清除速率。化合物1之合成係由色胺酸與絲胺酸接合之雙 3藉由絲胺酸 雙 肱了之-OH基接到cefuroxime之4-COOH基形成酯類先驅藥。先驅藥1在pH6.5及pH7.4 磷酸緩衝溶液中陣搖90分鐘後,分別只有1.6%及23%分解。化合物1在以離體大鼠小腸製 備之腸膜中培養2.5小時後,仍可偵測到60%。此化合物在模擬腸液中之安定性將作為我們 進一步測試該藥生體可用率以及評估其作為cefuroxime口服先驅藥之基礎。 |
英文摘要 | N-Cbz-tryptophan was arrached 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 muscal suspension prepared from rat intestine at 37 ℃ 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. . |
本系統之摘要資訊系依該期刊論文摘要之資訊為主。