他克莫司互变异构体的制备及其结构鉴定

Isolation and structure determination of tacrolimus tautomeric compounds

目的分离纯化他克莫司互变异构体-I和互变异构体-II,并对其结构鉴定,为他克莫司原料药及其制剂质量控制奠定基础。方法采用反相高效液相色谱方法,对原料药中的他克莫司互变异构体-I和互变异构体-II进行分离纯化,通过质谱、核磁共振等现代波谱学方法鉴定其结构。结果本文报道了采用反相高效液相色谱制备他克莫司互变异构体-I和互变异构体-II的方法,并通过多种光谱和波谱学方法鉴定了结构。结论采用反相高效液相色谱制备他克莫司互变异构体-I和互变异构体-II的方法是可行有效的,为制定产品质量标准奠定了基础。

Objective This presence study was aimed at isolation and determination of the structure of tacrolimus tautomeric compounds in order to lay a foundation for quality control of API and pharmaceutic preparation. Methods Tacrolimus tautomeric compounds were prepared by reverse phase high performance liquid chromatography methods and their structures were determined by MS and NMR. Results The method for preparation of tacrolimus tautomeric compounds by reverse phase HPLC was reported and their structures were identified on the basis of the data of NMR and MS respectively. Conclusion The method about preparation of tacrolimus tautomeric compounds by reverse phase HPLC is effective and efficient and lays a foundation for specification of API and preparation.