盐酸黄酮哌酯胶囊正常人体药代动力学和相对生物利用度研究  

THE PHARMACOKINETICS AND RELATIVE BIOAVAILABILITY OF FLAVOXATE CAPSULES IN HEALTHY VOLUNTEERS

作　　者：王建新[1,2] 陈得光[1,2] 李铜铃 黄英[1,2] 李稻[1,2] 

机构地区：[1]华西医科大学药学院 [2]华西医科大学附一院临床药理研究所

出　　处：《中国临床药理学杂志》1999年第1期48-51,67,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：本实验采用反相高效液相色谱法测定１０名健康男性志愿受试者单剂量口服２００ｍｇ盐酸黄酮哌酯胶囊和２００ｍｇ盐酸黄酮哌酯片（优必达）后，血浆中盐酸黄酮哌酯体内主要活性代谢物３－甲基黄酮－８－羧酸浓度变化情况，经３Ｐ８７药动学程序处理，以盐酸黄酮哌酯体内主要活性代谢物３－甲基黄酮－８－羧酸计的药时曲线下面积ＡＵＣ０→∞分别是：３５．９８±６．９２ｍｇ·ｈ·Ｌ－１和３３．８７±４．９７ｍｇ·ｈ·Ｌ－１，达峰时间Ｔｍａｘ分别是：０．８３±０．３５ｈ和０．９２±０．２３ｈ，峰浓度Ｃｍａｘ分别是：１３．９５±２．７８ｍｇ·Ｌ－１和１２．９８±２．６３ｍｇ·Ｌ－１。以配对Ｔ检验和双单侧Ｔ检验对上述参数进行统计分析，两种制剂的ＡＵＣ０→∞、Ｃｍａｘ和Ｔｍａｘ均无显著性差异（Ｐ＞０．０５）。说明盐酸黄酮哌酯胶囊和盐酸黄酮哌酯片为生物等效制剂。以盐酸黄酮哌酯片为标准参比制剂，盐酸黄酮哌酯胶囊以盐酸黄酮哌酯体内主要活性代谢物３－甲基黄酮－８－羧酸计的相对生物利用度为１０６．２３±５．００％。The pharmacokinetics and relative bioavailability of flavoxate (FL) capsules was studied in 10 healthy male volunteers. A single oral dose 200 mg FL of reference(tablet) or test(capsules) drugs was given to each volunteer according to an open randomized crossover design. The concentration of 3-methylflavone-8-carboxylic acid(MFCA), a main active metabolite of FL , was determined by HPLC method. The main pharmacokinetic parameters of MFCA were: AUC0→∞ 33.87±4.97 (mg·h·L-1) and 35.98±6.92 (mg·h·L-1),Tmax 0.92±0.23 h and 0.83±0.35 h, Cmax 12.98±2.63 mg·L-1 and 13.95±2.78 mg·L-1 for tablet and capsules respectively. The results of statistical analysis showed that two formulations were bioequivalent.

关 键 词：盐酸黄酮哌酯 药代动力学 相对生物利用度 

分 类 号：R983[医药卫生—药品] R969.1[医药卫生—药学]