吗替麦考酚酯分散片在早期肾移植患者中的药动学研究

发布时间：2018-02-03 22:40

本文关键词： 超高效液相色谱法吗替麦考酚酯分散片霉酚酸肾移植药动学　出处：《中国药学杂志》2017年08期 　论文类型：期刊论文

【摘要】：目的建立测定人血浆中霉酚酸(MPA)的超高效液相色谱(UPLC)方法,研究多次口服吗替麦考酚酯(MMF)分散片在早期肾移植患者中的药动学,为该药的临床合理应用提供依据。方法 15例肾移植受者口服MMF分散片,750 mg·次~(-1),q12 h,连续服用6 d后,第7天分别于服药前及服药后0.5、1、1.5、2、3、4、6、8、10、12 h采集静脉血样2 mL,采用UPLC-UV分析方法测定MPA血浆浓度。计算主要的药动学参数。结果测定方法线性范围为0.1~40μg·mL~(-1),定量下限为0.10μg·mL~(-1),术后第7天MMF分散片的主要药动学参数AUC_(0-12 h)为(24.63±9.51)μg·h·mL~(-1),ρ_(max)为(6.51±3.27)μg·mL~(-1),t_(max)为(1.83±1.30)h,ρ_0为(1.26±0.99)μg·mL~(-1),CL为(34.66±12.45)L·h~(-1)。大部分病人在给药后4~12 h血浆MPA浓度出现第2个小峰。结论本测定方法简单、快速,适用于测定人血浆中MPA的浓度。MMF分散片在早期肾移植患者体内的药动学参数个体间变异较大,常规剂量的MMF分散片在早期肾移植患者中暴露量普遍较低,建议结合MPA-AUC_(0-12 h)值调整给药剂量。
[Abstract]:Objective to establish a high performance liquid chromatography (UPLC) method for the determination of mycophenolate mofetil (MPA) in human plasma and to study the pharmacokinetics of multiple oral mycophenolate mofetil (MMF) dispersible tablets in patients with early renal transplantation. Methods Fifteen renal transplant recipients were treated with MMF dispersible tablets (750mg 路min ~ (-1)) for 12 h for 6 days. Venous blood samples of 2 mL were collected on the 7th day before and after the treatment. The plasma concentration of MPA was determined by UPLC-UV method. The main pharmacokinetic parameters were calculated. The linear range of the method was 0.1 渭 g 路mL ~ (-1). The lower limit of quantification was 0.10 渭 g 路mL ~ (-1). The main pharmacokinetic parameters (AUC_(0-12 h) of MMF dispersible tablets were 24.63 卤9.51 渭 g 路h 路mL -1 on the 7th day after operation. 蟻 _ (max) (6.51 卤3.27) 渭 g 路mL ~ (-1)) is 1.83 卤1.30 h. 蟻 0 was 1.26 卤0.99 渭 g 路mL ~ (-1). CL was 34.66 卤12.45 L 路hm-1. The second peak of plasma MPA concentration appeared in most patients at 4h after administration. Conclusion this method is simple and rapid. [WT5HZ] [WT5BZ] [WT5 "BZ] [WT5" BZ] [WT5BZ] [WT5 "BZ]. The pharmacokinetic parameters of MPA dispersible tablets in early renal transplantation patients were significantly different from each other. The conventional dose of MMF dispersible tablets is generally low in early renal transplantation patients. It is suggested to adjust the dose combined with MPA-AUC_(0-12 value.
【作者单位】：郑州大学第一附属医院药学部;
【基金】：郑州大学第一附属医院院内青年创新基金资助项目
【分类号】：R699.2
【正文快照】： 吗替麦考酚酯(MMF)是霉酚酸(MPA)的2-乙基酯类衍生物,口服后迅速代谢为活性产物MPA从而发挥免疫抑制作用,与他克莫司、激素一起广泛应用于心、肝、肾移植术后以预防急性排异反应的发生。目前MMF主要有2种剂型在临床使用:经典的MMF胶囊和新型的MMF分散片。新型的MMF分散片在移

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