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隐丹参酮单剂量和多剂量给药在大鼠体内药代动力学研究
  • ISSN号:1674-070X
  • 期刊名称:湖南中医药大学学报
  • 时间:2015
  • 页码:1-5
  • 分类:R285.5[医药卫生—中药学;医药卫生—中医学] R969.1[医药卫生—药理学;医药卫生—药学]
  • 作者机构:[1]上海中医药大学附属曙光医院临床药理科,上海201203
  • 相关基金:十二五重大新药创新《创新药物研究开发技术平台建设》(2012ZX09303009-001); 国家自然科学基金资助项目(81173118); 上海市中医临床重点实验室项目(C10d Z2220200)
  • 相关项目:基于代谢/转运与级联的隐丹参酮吸收屏障及保护机制
中文摘要:

目的评价单剂量和多剂量灌胃隐丹参酮(Cryptotanshinone,CTS)的药动学特征。方法将20只SD雄性大鼠随机分为单剂量组(隐丹参酮10 mg/kg,1 d)、多剂量组(隐丹参酮10 mg/kg,每天1次,连续10 d)给予灌胃后,用LC-MS/MS法测定血浆中隐丹参酮的浓度。血药浓度数据用DAS 2.0药代动力学软件处理,按两室模型拟合并求算药代动力学参数。结果隐丹参酮单剂量给药后,Cmax为(12.16±14.11)ng/m L,Tmax为(2.88±2.56)h,T1/2为(3.70±3.50)h,MRT为(6.69±0.54)h,AUC0~24为(58.40±25.73)ng·h/m L;多剂量给药后,Cav为(1.95±0.61)ng/m L,Tmax为(3.20±2.08)h,T1/2为(7.12±5.06)h,AUCss为(46.74±14.51)ng·h/m L,DF为2.42±0.28。单剂量和多剂量的AUC0~24、Tmax、T1/2差异无统计学意义。结论隐丹参酮长期给药后无蓄积风险。

英文摘要:

Objective To evaluate the pharmacokinetic properties of cryptotanshinone (CTS) with single and multiple doses administration in SD rats. Methods Totally 20 male SD rats were randomly divided into 2 groups: the single-dose group (CTS 10 mg/kg, 1 d) and multiple-dose group (CTS 10 mg/kg, once a day, 10 consecutive days). The CTS concentration in plasma was detected by LC-MS/MS method. The data of plasma concentration was processed by DAS 2.0 software and the pharmaeokinetic parameters were calculated according to a two-compartment open model. Results The pharmacokinetic parameters obtained from the single-dose study were as follows: Cmax was (12.16±14.11) ng/mL, Tmax was (2.88±2.56) h, T1/2 was (3.70±3.50) h, MRT was (6.69±0.54) h and AUC0-24 was (58.40±25.73) ng.h/mL; The pharmacokinetic parameters obtained from the multiple-dose study were as follows: Cav was (1.95±0.61) ng/mL, Tmax was (3.20±2.08) h, T1/2 was (7.12±5.06) h, AUC was (46.74±14.51) ng-h/mL and DF was 2.42±0.28. There was no significant difference in AUC0-24, Tmax and T1/2 of single and multiple doses. Conclusion There was no risk of accumulation after long-term administration with cryptotanshinone.

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期刊信息
  • 《湖南中医药大学学报》
  • 中国科技核心期刊
  • 主管单位:湖南省教育厅
  • 主办单位:湖南中医大学
  • 主编:黄惠勇
  • 地址:湖南长沙岳麓区含浦科教园区学士路300号湖南中医药大学含浦校区
  • 邮编:410208
  • 邮箱:xuebaotcm@126.com
  • 电话:0731-88458339 88458340
  • 国际标准刊号:ISSN:1674-070X
  • 国内统一刊号:ISSN:43-1472/R
  • 邮发代号:42-64
  • 获奖情况:
  • 2004,2006,2008年连续三次荣获全国高校两年评比一...,2005年被评为湖南省十佳科技期刊,连续三次被评为全国高校优秀自然科学学报,2009年全国高校科技期刊编辑质量优秀奖,2011年荣获湖南省新闻出版局"第五届十佳科技期刊"称号
  • 国内外数据库收录:
  • 美国化学文摘(网络版),中国中国科技核心期刊
  • 被引量:10690