替考拉宁的快速提取纯化及其单组份制备  

Fast preparation of teicoplanin, and isolation of its five monomers

作　　者：陈丽[1] 罗婷[1] 江宁宇[1] 彭飞[1] 连云阳[1] 

机构地区：[1]福建省微生物研究所,福建省新药(微生物)筛选重点实验室,福州350007

出　　处：《中国抗生素杂志》2014年第12期905-910,共6页Chinese Journal of Antibiotics

基　　金：福建省科技计划重点项目(2012Y0078);福建省自然科学基金项目(2012J01307);福州市科技计划重点项目(2013-PT-42);国家"重大新药创制"课题(2012ZX09301002-003)

摘　　要：目的从菌株Actinoplanes teichomyceticus sp.FIM-1112发酵液中快速提取纯化替考拉宁,并建立替考拉宁5个单组份A2-1、A2-2、A2-3、A2-4和A2-5的快速制备方法。方法采用碱化、HP-20大孔树脂柱分离、沉淀、脱色、冷却沉淀等技术,快速提取纯化替考拉宁;结合制备液相色谱分离技术[制备柱Welch Column XB-C18(250mm×21.2mm i.d.,5μm),流动相A为3.2g/L Na H2PO4-乙腈(900:100);流动相B为2.75g/L Na H2PO4-乙腈(300:700),流速为10.0m L/min,检测波长为254nm]分离制备替考拉宁5个单组份。结果 A2组份的收率提高至76%,HPLC结果显示各组份的含量均符合欧洲药典标准,且各组份纯度分别为94.90%(A2-1),96.86%(A2-2),84.75%(A2-3),80.16%(A2-4)和78.59%(A2-5)。结论该提取纯化方法经过优化,简单、快速、易于操作,且首次采用制备色谱分离技术对其5个组份进行分离,可用于替考拉宁单组份的分离制备。Objective To develop a fast purification process of teicoplanin from the culture broth of Actinoplanes teichomyceticus sp. FIM-1112, and to establish an RP-HPLC method for the preparation of five monomers of teicoplanin. Methods Basification, HP-20 macroporous adsorption resin column separation, precipitation, decolorization and decontamination steps were adopted to separate and purify teicoplanin. The preparative liquid chromatography was used to isolate the five monomers, a Welch Column XB-C18 （250mm ~ 21.2mm i.d., 5~tm） was adopted, and the mobile phase was comprised of （A） 3.2g/L NaHEPO4 ： acetonitrile （900：100）, and （B） 2.75g/L NaHEPO4 ： acetonitrile （300：700）; flow rate： 10.0mL/min; injection volume： 500gL. Results The yield of A2 was greatly raised to 76%, and the HPLC results revealed that purities of the monomers were 94.90% （A2-1）, 96.86% （A2-2）, 84.75% （A2-3）, and 80.16% （A2-4） and 78.59% （A2-5）, respectively. Conclusion The extraction scheme optimized was simple, rapid and easy to operate, and this is the first time the preparation method was established to prepare the five monomers of teicoDlanin.

关 键 词：替考拉宁 提取纯化 制备液相色谱法 

分 类 号：R978[医药卫生—药品]