苯溴马隆在高尿酸血症患者中的药代动力学及药效学研究
Pharmacokinetics and pharmacodynamics of benzbromarone in patients with hyperuricemia
孙丽琴 1费扬 1徐晓艳 2楼琴华1
作者信息
- 1. 杭州市富阳区第一人民医院内分泌科,浙江杭州 311400
- 2. 杭州市富阳区第一人民医院高桥分院内分泌科,浙江杭州 311400
- 折叠
摘要
目的 评价苯溴马隆在高尿酸血症(HUA)患者中的药代动力学及药效学.方法 将30例HUA患者随机分为A、B、C组,每组10例.3组分别接受单次口服苯溴马隆25、50、100 mg;B组结束单次给药试验后,继续口服苯溴马隆50 mg,每天1次,连续用药28 d.用液质联用(LC-MS/MS)法测定血浆中苯溴马隆的浓度,用全自动生化分析仪测定血清尿酸(SUA)水平.结果 单次口服苯溴马隆片在25～100 mg呈线性药代动力学特征,t1/2分别为(11.67±1.85)、(12.84±1.22)和(13.25±1.02)h;tmax分别为(2.84±0.15)、(3.07±0.18)和(3.15±0.25)h;Cmax分别为(2.21±0.85)、(2.67±0.68)和(3.25±0.72)mg·L-1;AUC0-24h分别为(14.25±3.25)、(18.20±3.34)和(19.25±3.44)mg·h·L-1.连续给药后,药物的吸收程度与速度无明显变化,在体内有蓄积;经口服苯溴马隆28 d治疗,10例HUA患者的SUA水平均显著降低,其中8例患者的SUA水平＜360 μmol·L-1.结论 单次口服苯溴马隆片在25～100 mg呈线性药代动力学特征,连续口服治疗剂量的苯溴马隆片可显著降低HUA患者SUA水平.
Abstract
Objective To evaluate the pharmacokinetics and pharmacodynamics of benzbromarone in patients with hyperuricemia(HUA).Methods Thirty patients with HUA were randomly divided into A,B and C groups,with 10 patients in each group.Three groups was given a single oral dose of benzbromarone 25,50 and 100 mg.After the single administration test,group B continued to take benzbromarone 50 mg orally once a day for 28 days.The concentration of benzbromarone in plasma was measured using liquid chromatography tandem mass spectrometry(LC-MS/MS)method,and the serum uric acid(SUA)level was measured by fully automated biochemical analyzer.Results The single oral administration of benzbromarone tablets exhibited linear pharmacokinetic characteristics within the range of 25-100 mg.The main pharmacokinetic parameters were as follows:t1/2 were(11.67±1.85),(12.84±1.22)and(13.25±1.02)h;tmax values were(2.84±0.15),(3.07±0.18)and(3.15±0.25)h;Cmax values were(2.21±0.85),(2.67±0.68)and(3.25±0.72)mg·L-1;AUC0-24h were(14.25±3.25),(18.20±3.34)and(19.25±3.44)mg·h·L-1,respectively.After continuous administration,there was no significant change in the degree and speed of drug absorption,and there was accumulation in the body.After 28 days of oral treatment with benzbromarone,the SUA levels of 10 HUA patients were significantly reduced,with 8 patients having SUA levels＜360 μmol·L-1.Conclusion A single oral dose of benzbromarone tablets exhibits linear pharmacokinetic characteristics at 25-100 mg,and continuous oral doses of benzbromarone tablets can significantly reduce SUA levels in patients with HUA.
关键词
高尿酸血症/苯溴马隆/药代动力学/药效学Key words
hyperuricemia/benzbromarone/pharmacokinetics/pharmacodynamics引用本文复制引用
基金项目
浙江省中医药科技基金(2021ZB246)
出版年
2024
国家科技期刊平台
NSTL
万方数据