免疫抑制剂细胞内浓度测定的研究进展  

Research progress on determination of intracellular concentration of immunosuppressant

作　　者：邵琨[1] 陈冰[2] 周佩军[1] Shao Kun;Chen Bing;Zhou Peijun(Transplantation Ward of Urology,Ruijin Hospital Affiliated to Shanghai Jiao Tong University School of Medicine,Shanghai 200025,China)

机构地区：[1]上海交通大学医学院附属瑞金医院泌尿外科移植病区,200025 [2]上海交通大学医学院附属瑞金医院药剂科,200025

出　　处：《器官移植》2021年第4期489-495,共7页Organ Transplantation

基　　金：国家自然科学基金(81973387)。

摘　　要：细胞外浓度测定作为目前器官移植临床免疫抑制剂治疗药物监测(TDM)的主要手段,与免疫抑制剂药效之间的相关性不理想。随着液相质谱技术的广泛应用,免疫抑制剂细胞内浓度检测技术逐渐成熟。由于细胞内浓度测定可直接检测靶细胞内的药物暴露水平,理论上能更好地反映免疫抑制剂的药效。本文总结了免疫抑制剂细胞内浓度测定的历史与现状,着重介绍免疫抑制剂细胞内浓度的测定方法及其与药效的相关性。免疫抑制剂细胞内浓度测定具有较好的临床应用价值,值得推广。Currently,extracellular concentration measurement is the major approach of therapeutic drug monitoring(TDM)of clinical immunosuppressant in organ transplantation.Its correlation with the efficacy of immunosuppressant remains elusive.With widespread application of liquid chromatography,the detection technology of intracellular concentration of immunosuppressant is gradually mature.Theoretically,it may more accurately reflect the efficacy of immunosuppressant due to that the level of drug exposure in target cells can be directly measured.In this article,the history and present situation of the determination of intracellular concentration of immunosuppressant were summarized,and the association between the determination methods of intracellular concentration of immunosuppressant and drug efficacy was emphatically analyzed.Detection of intracellular concentration of immunosuppressant possesses better application value in clinical practice,which is worthy of promotion in clinical settings.

关 键 词：器官移植 免疫抑制剂 治疗药物监测 药代动力学 药效学 高效液相色谱法 液相色谱-串联质谱法 外周血单个核细胞 哺乳动物雷帕霉素靶蛋白 

分 类 号：R617[医药卫生—外科学] R969[医药卫生—临床医学]