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題 名 | 燒傷治療藥Zinc Norfloxacin之合成及抗菌活性=Synthesis and Antibacterial Activity of Zinc Norfloxacin |
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作 者 | 李安榮; 黃文鑫; | 書刊名 | 醫學研究 |
卷 期 | 13:6 1993.05[民82.05] |
頁 次 | 頁397-404 |
分類號 | 418.2321 |
關鍵詞 | 合成; 抗菌活性; 治療藥; 燒傷; |
語 文 | 中文(Chinese) |
中文摘要 | 本研究深入探討新燒傷治療藥zinc norfloxacin之合成、製劑製備及抗菌活性。 傷燙傷是最常見的意外傷害,甚至在軍陣上影響戰力甚鉅。大範圍或深度燒傷,不僅傷口癒合緩慢,且影響皮膚外觀,若受到綠膿桿菌感染,更為燒傷病人死亡之主因。 臨床上唯一外用燒傷治療藥物,為達淨磺胺銀(silver sulfadiazine; AgSD),然本藥具肝毒性、導致腎衰竭、價格高昂及安定性不佳,且易致過敏之缺點。本研究室曾製備達淨磺胺鋅(zinc sulfadiazine; Zn(SD)₂)衍生物具優越之療效及低毒性,然其乳膏劑型之長期安定性試驗發現外觀仍不穩定,乃著手進一步探討zinc norfloxacin (Zn(NFLX)₂)是否具有強力抗菌活性及加速傷口痊癒或成本低廉之優點,以作為AgSD之取代藥物。初步結果發現Zn(NFLX)₂之優點為具有強力抗綠膿桿菌活性,療效更優於達淨磺胺鋅及達淨磺胺銀。本藥製備容易,成本低廉,適合量產。本研究室將進行與其他藥物配伍,製成各種軟膏、人造皮膚製劑等之研究。 |
英文摘要 | The synthesis, physicochemical properties, stability, intro antibacterial activity, and toxicity of zinc norfloxacin (Zn(NFLX)₂; 1d) was described. Zn(NFLX)₂ was readily obtained into two steps from norfloxacin (1a), a novel pyridine-carboxylic acid type antibacterial agent, by treatment with sodium hydroxide followed by zinc nitrate in a total yield of 23.9%. The structural characterization was established by UV, IR, NMR, and elemental analysis. Zn(NFLX)₂ possesses fairly good stability and is reasonably soluble in water which endows itself an excellent candidate in the studies of pharmaceutical dosage forms. Compared to silver or zinc sulfadiazine, Zn(NFLX)₂ exhibits superior in vitro antibacterial, notably antipseudomonal activity with low toxicity in animal study which may make Zn(NFLX)₂ a valuable addition to the therapeutic armamentarium for the control of burn wound sepsis in the military field. |
本系統中英文摘要資訊取自各篇刊載內容。