国产甲磺酸左旋氧氟沙星片生物等效性评价  

BIOEQUIVALENCE ASSESSMENT OF DOMESTIC LEVOFLOXACIN MESYLATE TABLET

作　　者：张贵军[1] 李可欣[1] 刘蕾[1] 孙春华[1] 宋友华[1] 

机构地区：[1]卫生部北京医院

出　　处：《中国临床药理学杂志》1999年第1期33-35,44,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：１０名健康男性志愿者采用交叉给药方案，分别单剂量口服２００ｍｇ国产甲磺酸左旋氧氟沙星片及进口左旋氧氟沙星片，进行国产制剂的相对生物利用度研究。用ＨＰＬＣ法测定血清及尿中左旋氧氟沙星药物浓度，血药浓度－时间数据经３Ｐ８７程序自动拟合，符合二室模型。试验结果表明：单次口服２００ｍｇ国产甲磺酸左旋氧氟沙星片与进口左旋氧氟沙星片后，达峰时间分别是１．２５±０．２６ｈ和１．４０±０．２１ｈ，峰浓度分别是２．８７±０．２３ｍｇ·Ｌ－１和２．８４±０．２２ｍｇ·Ｌ－１，０～２４ｈ的药时曲线下面积分别为２１．１５±２．１８ｍｇ·ｈ·Ｌ－１和２１．６９±１．８８ｍｇ·ｈ·Ｌ－１。其主要药代动力学参数经方差分析和双单侧Ｔ检验，无显著性差异（Ｐ＞０．０５），两种制剂具有生物等效性。国产甲磺酸左旋氧氟沙星片的相对生物利用度为９７．９０％。２４ｈ的尿药排泄率为６９．６８％。The pharmacokinetics of levofloxacin was determined following a single oral dose of 200 mg given to each 10 healthy volunteers in an open randomized crossover study. The levofloxacin concentration in serum and urine was measured by HPLC. The pharmacokinetic parameters were calculated on the basis of two compartment models by using 3P87 program. Tmax of domestic levofloxacin mesylate and imported levofloxacin were 1.25±0.26 h and 1.40±0.21 h, Cmax 2.87±0.23 mg·L-1 and 2.84±0.22 mg·L-1, AUC0-24 21.15±2.18 mg·h·L-1 and 21.69 ±1.88 mg·h·L-1, respectively. The pharmacokinetic parameters obtained from our studies showed no significant difference between two products(P>0.05). The urinary recovery rates(0-24 h) were 69.68%.The relative bioavailability of domestic tablet to imported tablet was 97.90%,so it demonstrated that both formations were bioequivalence.

关 键 词：左旋氟氧沙星 药代动力学 生物等效性 甲磺酸 

分 类 号：R978.19[医药卫生—药品] R969.1[医药卫生—药学]