他克莫司缓释胶囊药物动力学特征及其临床意义

Pharmacokinetics of tacrolimus sustained release capsule and its clinical application

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。

The severe variation of immunosuppressor blood concentration in organ transplantation can increase the risk of acute rejection and lead to the function of transplanted organ loss. Tacrolimus, as an immunosuppressor with narrow therapeutic index should be kept a certain range of plasma concentration. Compared with the general tacrolimus capsule, tacrolimus sustained release capsule has similar drug concentration, but the drug peak concentration is decreased. The pharmacokinetic study of the liver and kidney transplant recipients shows that the sustained released formulation can make the blood drug concentration more stable and less variation. This review focuses on the characteristics and clinical application of tacrolimus sustained release capsules.