乙二胺四甲叉膦酸骨靶向性异烟肼载体的研制与分子机制研究  

Preparation of Ethylenediamine Tetramethylphosphonate Bone-targeted Isoniazid Carrier and its Molecular Mechanism

作　　者：林健泽[1] 蓝涛[1] 田长庆[1] 余铮[1] 杨欣建[1] 郭伟壮[1] LIN Jian-ze;LAN Tao;TIAN Chang-qing;YU Zheng;YANG Xin-jian;GUO Wei-zhuang(The First Affiliated Hospital of Shenzhen University,Shenzhen Second People’s Hospital,Guangdong Shenzhen 518035)

机构地区：[1]深圳大学第一附属医院深圳市第二人民医院,广东深圳518035

出　　处：《深圳中西医结合杂志》2020年第10期1-4,F0003,共5页Shenzhen Journal of Integrated Traditional Chinese and Western Medicine

基　　金：深圳市科技计划项目资助课题(JCYJ20170306090836148)。

摘　　要：目的:研究乙二胺四甲叉膦酸骨靶向性异烟肼载体的研制与分子机制,为临床医学治疗脊柱结核提供参考,以提高临床治疗效果。方法:通过同位素示踪技术锝–99标记异烟肼、液相色谱–质谱连用技术检测5种一线抗结核药物、构建脊柱结核动物模型等方法。结果:计算标记率> 90 %、载药率与包封率平稳,观察体外释放情况。结论:乙二胺四甲叉膦酸骨靶向性异烟肼载体在治疗脊柱结核方面具有重要作用。Objective To study the development and molecular mechanism of bone-targeted isoniazid carrier of ethylenediamine tetramethylidenephosphonate and to provide reference for clinical treatment of spinal tuberculosis in order to improve the clinical therapeutic effect.Methods Isotope tracing technique technetium-99 Labeled isoniazid,liquid chromatography-mass spectrometry with five kinds of first-line anti-TB drugs,construction of spinal tuberculosis animal models and other methods to calculate the labeling rate.Results Drug loading rate and encapsulation efficiency(>90%),observe the release in vitro.Conclusion Ethylenediamine tetramethylenephosphonate bone-targeted isoniazid carrier plays an important role in the treatment of spinal tuberculosis.

关 键 词：脊柱结核 乙二胺四甲叉膦酸 骨靶向性 异烟肼载体 动物实验 

分 类 号：R682[医药卫生—骨科学]