最后一道防线——万古霉素市售制剂的研究进展  

The last line of defense:recent advances in the research on commercial preparations of vancomycin

作　　者：汪泽卿 高凯璇 沈润溥[1] 席眉扬 吴国锋[2] 周艳艳 骆翔 WANG Zeqing;GAO Kaixuan;SHEN Runpu;XI Meiyang;WU Guofeng;ZHOU Yanyan;LUO Xiang(College of Chemistry and Chemical Engineering,Shaoxing University,Shaoxing 312000,China;Xinchang Pharmaceutical Factory,Zhejiang Medicine Co.,Ltd.,Shaoxing 312500,China)

机构地区：[1]绍兴文理学院化学化工学院,浙江绍兴312000 [2]浙江医药股份有限公司新昌制药厂,浙江绍兴312500

出　　处：《沈阳药科大学学报》2021年第1期95-101,共7页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(81602949),浙江省教育厅一般科研项目(Y201839799),绍兴文理学院校级重点科研项目(2018LG1002),2018绍兴文理学院学生科研项目。

摘　　要：目的万古霉素是一种糖肽类抗生素,因其不易产生细菌抗药性,被誉为“人类对付耐药菌株的最后一道防线”。然而,万古霉素室温下极易降解,并且口服生物利用度几乎为零。因此,本文对万古霉素降解机制和制剂研发方法进行总结。方法通过对近年来国内外50余篇万古霉素相关文献整理分析,本文主要分析了目前临床上最常用的三种万古霉素市售制剂,并对其相应的药物保护机制进行总结。结果本文从药剂学的角度阐明万古霉素制剂通过克服药物易降解、易氧化等共性技术难题,成功将万古霉素应用于临床治疗。结论通过对万古霉素结构稳定性的深入研究,将为万古霉素为代表的抗生素类药物未来制剂开发提供更为完善的理论基础和实际应用价值。Objective Vancomycin belongs to the glycopeptide drug family and has for long been regarded as“the last line of defense against drug-resistant strains”because of hardly bacterial resistance induced by vancomycin.However,vancomycin is easily degraded at room temperature,and its oral bioavailability is close to zero.Therefore,the degradation mechanisms,research and development methods of vancomycin are summarized in the review.Methods Referring more than 50 domestic and overseas vancomycin-related literatures,the review analyzes the most widely used three commercial preparations of vancomycin in clinic,and summarizes the drug protection mechanisms accordingly.Results This review elucidates that vancomycin preparations overcome common technical problems,such as degradability and oxidation,and from a pharmaceutical perspective,the vancomycin has been successfully applied in clinical treatment.Conclusion In summary,further studies on the structural stability of vancomycin will provide better theoretical basis and practical application for the future development of antibiotics represented by vancomycin.

关 键 词：万古霉素 稳定性 胶囊剂 冻干粉针剂 即用型预混万古霉素注射液 

分 类 号：R94[医药卫生—药剂学]