• 中国核心期刊(遴选)数据库收录期刊
  • 中文科技期刊数据库收录期刊
  • 中国期刊全文数据库收录期刊
  • 中国学术期刊综合评价数据库统计源期刊等

中国药物评价 ›› 2020, Vol. 37 ›› Issue (4): 291-294.

• 药品评价 • 上一篇    下一篇

头孢呋辛酯片在中国健康受试者的药动学及生物等效性研究

李敏1, 李雪2, 陈潮2, 胡利敏1, 张锁庆1, 王菊勇2*   

  1. 1. 华北制药河北华民药业有限责任公司, 河北 石家庄 052165;
    2. 上海中医药大学附属龙华医院I期临床试验研究室, 上海 200032
  • 收稿日期:2020-03-17 修回日期:2020-04-06 出版日期:2020-08-28 发布日期:2020-09-21
  • 基金资助:
    十三五“重大新药创制”科技重大专项(编号:2017ZX09304001,项目名称:恶性肿瘤等疾病示范中药新临床评价技术平台建设)

Pharmacokinetic and Bioequivalence of Cefuroxime Axetil Tablets in China Healthy Subjects

  1. 1. NCPC Hebei Huamin Pharmaceutical Co., Ltd, Hebei Shijiazhuang 052165, China;
    2. Drug Clinical Trial Institution′ LongHua Hospital Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China
  • Received:2020-03-17 Revised:2020-04-06 Online:2020-08-28 Published:2020-09-21

摘要: 目的:评价2种头孢呋辛酯片在中国健康受试者的生物等效性及安全性。方法: 按单中心、开放、随机、单次给药、两制剂、两序列、两周期、交叉试验设计。空腹和餐后条件下各入组34例受试者,随机交叉单次口服受试制剂和参比制剂125mg,用LC-MS/MS法测定血浆中头孢呋辛的浓度,用WinNonlin6.3软件计算头孢呋辛的药动学参数,并进行生物等效性评价。 结果:受试者服用受试制剂和参比制剂后,空腹组血浆中头孢呋辛的主要药代动力学参数如下:Cmax分别为(1 904.2±419.16),(1 996.4±386.55)ng·mL-1; AUC0-t分别为(5 942.884 9±1 278.885 5),(6 017.278 7±1 199.180 8)h·ng·mL-1;AUC0-∞分别为(5 997.406 3±1 267.705 5),(6 077.5767±1 196.461 9)h·ng·mL-1;餐后组血浆中头孢呋辛的主要药代动力学如下:Cmax分别为(2 223.2±467.72),(2 119.7±504.41)ng·mL-1; AUC0-t分别为(7 454.268 7±1 064.233 4),(7 471.536 4±1 030.637 7)h·ng·mL-1;AUC0-∞分别为(7 512.512 6±1 060.955 7),(7 541.289 8±1 050.708 4)h·ng·mL-1。2种制剂的Cmax、AUC0-t和AUC0-∞,经对数转换后几何均值比(90%CI)分别为空腹状态下94.96%(87.84%~102.65%),98.57%(93.98%~103.38%),98.52%(94.02%~103.24%);餐后状态下105.39%(97.51%~113.91%),99.68%(97.18%~102.24%),99.57%(97.12%~102.07%)。结论:2种头孢呋辛酯片在中国健康受试者中具有生物等效性。

关键词: font-size:medium, ">头孢呋辛酯片;中国健康受试者;药代动力学;生物等效性

Abstract: Objective: To evaluate the bioequivalence of two kinds of Cefuroxime Axetil Tablets in China healthy subjects. Methods: This was a single-center′ randomized′ open-label′single-dose′ two-period′ cross-over pharmacokinetic study. A total of 34 subjects in fasted and 24 subjects in a fed state were given single oral dose of test and reference preparation of Cefuroxime Axetil Tablets(each 125 mg), respectively. The concentration of cefuroxime in human plasma was measured by LC-MS/MS. Main pharmacokinetic parameters were calculated by using WinNonlin 6.3 software. Results: The main pharmacokinetic parameters of cefuroxime of the test and the reference preparations were as follows: the fasting state Cmax were(1 904.2±419.16), (1 996.4±386.55)ng·mL-1. AUC0-t were(5 942.884 9±1 278.885 5),(6 017.278 7±1 199.180 8)h·ng·mL-1; AUC0-∞ were((5 997.406 3±1 267.705 5),(6 077.576 7±1 196.461 9)h·ng·mL-1. The fed state Cmax were (2 223.2±467.72),(2 119.7±504.41)ng·mL-1. AUC0-t were(7 454.268 7±1 064.233 4),(7 471.536 4±1 030.637 7)h·ng·mL-1. AUC0-∞ were (7 512.512 6±1 060.955 7),(7 541.289 8±1 050.708 4)h·ng·mL-1. The geometric mean ratio(90%CI confidential interval) after logarithmic conversion for Cmax、AUC0-t and AUC0-∞ were 98. 94.96%(87.84%-102.65%), 98.57%(93.98%-103.38%), 98.52%(94.02%-103.24%) in fasting group and were 105.39%(97.51%-113.91%), 99.68%(97.18%-102.24%), 99.57%(97.12%-102.07%) in fed group. Conclusion: Two kinds of Cefuroxime Axetil Tablets are determined to be bioequivalent.
   

Key words: font-size:medium, ">Cefuroxime axetil tablets; Healthy Chinese subjects; Pharmacokinetics; Bioequivalence

中图分类号: