塞来昔布胶囊犬口服给药的体内过程及一致性评价

中国临床药理学与治疗学 ›› 2013, Vol. 18 ›› Issue (4): 371-375.

塞来昔布胶囊犬口服给药的体内过程及一致性评价

崔涛^1,2, 高晶², 伊秀林², 曾勇², 李薇², 司端运²

¹天津中医药大学,天津 300193;
²天津药物研究院释药技术与药代动力学国家重点实验室,天津 300193

收稿日期:2012-10-19 出版日期:2013-04-26 发布日期:2013-04-26
通讯作者: 司端运,男,研究员,研究方向:药物代谢与药代动力学。Tel: 022-84845261 E-mail: ddysi@sohu.com
作者简介:崔涛,女,硕士研究生,研究方向:药代动力学。Tel: 13821697465 E-mail: cuitao2010@yahoo.com.cn

Consistency assessment and disposition in vivo after oral administration of celecoxib capsules to Beagle dogs

CUI Tao^1,2, GAO Jing², YI Xiu-lin², ZENG Yong², LI Wei², SI Duan-yun²

¹ Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China;
² State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China

Received:2012-10-19 Online:2013-04-26 Published:2013-04-26

摘要/Abstract

摘要： 目的: 建立Beagle犬血浆中塞来昔布的定量测定方法,考察Beagle犬口服塞来昔布胶囊体内药代动力学过程,并与进口的西乐葆胶囊比较,进行体内过程一致性评价。方法: 采用双周期自身交叉实验设计,8只Beagle犬分别单剂量口服西乐葆和塞来昔布胶囊,用HPLC法测定血浆中的塞来昔布浓度,以DAS 2.0 药代动力学计算程序拟合药物浓度-时间曲线,计算药动学参数和相对生物利用度。结果: 塞来昔布胶囊和西乐葆胶囊主要药代动力学参数t_max分别为(2.0±0.8)、(2.0±0.9) h、C_max分别为(902±433)、(764±295) μg/L、AUC_(0→t)分别为(10053±6100)、(9266±3967) μg·h·L^-1,差异均无统计学意义(P>0.05)。相对生物利用度为(106.0±26.7)%。结论: 塞来昔布胶囊与西乐葆胶囊的体内过程具有一致性。

关键词: 塞来昔布, 生物利用度, 高效液相色谱法

Abstract: AIM: Establish an HPLC method for the determination of celecoxib in dog plasma. Besides evaluate in vivo disposition consistency by comparing their pharmacokinetic parameters after oral administration of celecoxib capsules or Celebrex to Beagle dogs.METHODS: According to a two-period crossover design, 8 Beagle dogs received a single oral dose of test or reference capsules, respectively. The plasma concentration of celecoxib was determined by the established HPLC method. The pharmacokinetic parameters and relative bioavailability were calculated.RESULTS: The relative bioavailability of celecoxib was (106.0±26.7) %. Based on the analysis of variance, two-sided t-test and rank sum test of the pharmacokinetic parameters including t_max, C_max, and AUC_(0→t), there were no significant difference between both preparations (P>0.05).CONCLUSION: The disposition in vivo of celecoxib capsules is in consistency with that of Celebrex.

Key words: Celecoxib, Bioavailability, High performance liquid chromatography

中图分类号:

R969

崔涛, 高晶, 伊秀林, 曾勇, 李薇, 司端运. 塞来昔布胶囊犬口服给药的体内过程及一致性评价[J]. 中国临床药理学与治疗学, 2013, 18(4): 371-375.

CUI Tao, GAO Jing, YI Xiu-lin, ZENG Yong, LI Wei, SI Duan-yun. Consistency assessment and disposition in vivo after oral administration of celecoxib capsules to Beagle dogs[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2013, 18(4): 371-375.

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