非布司他在高尿酸血症伴慢性肾病患者中的药代动力学及药效学研究

发布时间：2018-01-15 03:33

本文关键词：非布司他在高尿酸血症伴慢性肾病患者中的药代动力学及药效学研究　出处：《中国临床药理学杂志》2015年13期 　论文类型：期刊论文

【摘要】：目的评价非布司他在高尿酸血症伴慢性肾病患者中的药代动力学及药效学。方法 18名进行血液透析的慢性肾病患者随机分为A、B、C 3组,每组6人。A、B、C组分别接受单次空腹口服非布司他片40,80,120 mg;B组结束单次给药试验后,继续空腹口服非布司他80 mg,每天1次,连续用药28 d。用LC-MS/MS法测定血浆中非布司他的浓度,用全自动生化分析仪测定血清尿酸值。结果单次空腹口服非布司他片40,80,120 mg后的主要药代动力学参数分别如下,t1/2分别为(3.98±1.45),(4.63±1.37),(4.27±1.33)h;tmax分别为(0.97±0.39),(1.22±0.46),(1.35±0.37)h;Cmax分别为(1626.33±342.97),(2669.27±384.91),(3904.83±835.98)ng·m L-1;AUC0-24 h分别为(4324.32±976.87),(8415.4±1965.9),(12979.6±3788.5)ng·m L-1·h。连续给药(80 mg,qd×28 d)后,药物的吸收程度和速度无明显变化,在体内无蓄积;28 d治疗期间,6名高尿酸血症伴慢性肾病患者的血尿酸水平均显著降低,其中5名患者低于6 mg·d L-1。结论单次空腹口服非布司他片在40~120mg呈线性药代动力学特征,连续口服治疗剂量的非布司他片可显著降低高尿酸血症伴慢性肾病患者的血尿酸水平。
[Abstract]:Objective to evaluate the pharmacokinetics and pharmacodynamics of Festa in patients with hyperuricemia and chronic nephropathy. Methods 18 patients with chronic nephropathy undergoing hemodialysis were randomly divided into three groups. Each group (n = 6) was treated with a single fasting oral dose of non-busulta tablets (40 / 80) and 120 mg / g respectively in group C (n = 6). After the single trial, group B continued to take 80 mg of non-buflast once a day on an empty stomach for 28 days. The concentration of non-buflast in plasma was determined by LC-MS/MS method. Results the main pharmacokinetic parameters were as follows: the serum uric acid level was determined by automatic biochemical analyzer. T 1 / 2 was 3.98 卤1.45 and 4.63 卤1.37 respectively 4.27 卤1.33h. The tmax was 0.97 卤0.39 and 1.22 卤0.46, respectively. The tmax was 1.35 卤0.37h. The Cmax was 1626.33 卤342.97 ng 路ml ~ (-1), respectively. The Cmax was 3904.83 卤835.98 ng 路ml ~ (-1), and the Cmax was 2669.27 卤384.91 卤3904.83 卤835.98 ng 路mL ~ (-1), respectively. The AUC0-24 h was 4324.32 卤976.87 (8415.4 卤1965.9). After 12979.6 卤3788.5 ng 路mL ~ (-1) 路h ~ (-1), the absorption degree and speed of the drug did not change significantly after the continuous administration of 80 mg / g QD 脳 28 d. There is no accumulation in the body; The serum uric acid levels in 6 patients with hyperuricemia and chronic nephropathy decreased significantly during 28 days of treatment. Five of them were less than 6 mg 路d ~ (-1) 路L ~ (-1). Conclusion the pharmacokinetic characteristics of a single fasting oral Festa tablet at 40 ~ 120mg / d were linear. Continuous oral administration of non-buprofloxacin significantly decreased serum uric acid levels in patients with hyperuricemia and chronic nephropathy.
【作者单位】：珠海市人民医院药学部;遵义医学院第五附属(珠海)医院肾内科;
【分类号】：R969.1
【正文快照】： 黄好武1,黄颖斌2,黄欢文2,周春仲1,林佩清1,(1.珠海市人民医院药学部,广东珠海519000;2遵义医学院第五附属(珠海)医院肾内科,广东珠海519000)HUANG Hao-wu1,HUANG Ying-bin2,HUANG Huan-wen2,ZHOU Chun-zhong1,LIN Pei-qing1(1.Department of Pharmacy,People'sHospital of Zh

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