- 期刊
- OpenAccess
燒傷治療藥Silver Norfloxacin之合成及抗菌活性
Synthesis and Antibacterial Activity of Silver Norfloxacin
摘要
本研究深入探討新燒傷治療藥silver norfloxacin之合成、製劑製備及抗菌活性。燒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），指本藥具肝毒性、導致腎衰竭、價格高昂及安全性不佳，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silver norfolxacin（Ag NFLX）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Ag NFLX之優點為具有強力抗綠膿根菌活性，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。本類藥物高效、低毒，為極具開發潛能之新藥。
並列摘要
The synthesis, physicochemical properties, stability, in vitro antibacterial activity, and toxicity of silver norfloxacin (Ag NFLX; 1c) was described. Ag NFLX was redily obtained from norfloxacin (1a), a novel pyridine-carboxylic acid type antibacterial agent, by treatment with sodium hydroxide in the yield of 49.5%. The structural characterization was established by UV, IR, NMR, and elemental analysis. Ag NFLX 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, Ag NFLX exhibits superior in vitro antibacterial, notably antipseudomonal activity with low toxicity in animal study which may make Ag NFLX a valuable addition to the therapeutic armamentarium for the control of burn would sepsis in the military field.