免疫抑制剂的血药浓度变异系数过大,会增加急性排斥反应风险,进而导致移植功能丧失。他克莫司治疗指数狭窄,临床应用时其血药浓度应保持在一定范围内。他克莫司缓释胶囊剂与普通胶囊间药物浓度曲线下面积相似,但缓释胶囊的药物峰值降低。针对肝、肾移植受者的药物动力学研究显示,剂型的改变可使其获得更平稳的血药浓度,并能显著降低血药浓度变异系数。本文综述他克莫司缓释胶囊制剂特点及其临床应用。 Immunosuppressive drug concentration coefficient of variation is too large, will increase the risk of acute rejection, which led to loss of graft function. Tacrolimus therapeutic index is narrow, its clinical application of blood concentration should be maintained within a certain range. The area under the drug concentration curve for the tacrolimus sustained-release capsules was similar to that for the normal capsules, but the drug peak for the slow release capsules was reduced. Pharmacokinetics studies in liver and kidney transplant recipients have shown that changes in dosage forms result in smoother plasma concentrations and significantly lower plasma concentration variability. This article reviews the characteristics of tacrolimus sustained-release capsules and its clinical application.