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中国临床药理学与治疗学 ›› 2008, Vol. 13 ›› Issue (11): 1272-1276.

• 定量药理学 • 上一篇    下一篇

诺必擂停在大鼠和Beagle犬体内的药动学研究

陈西敬, 于雪, 任伟超, 孙伟, 卢杨, 何佳珂   

  1. 中国药科大学药物代谢研究中心, 南京 210009, 江苏
  • 收稿日期:2008-07-14 修回日期:2008-10-20 出版日期:2008-11-26 发布日期:2020-10-14
  • 作者简介:陈西敬, 男, 教授, 硕士生导师, 研究方向:药物代谢动力学。Tel:025-83271286 E-mail: chenxj@jlonline.com
  • 基金资助:
    国家自然科学基金项目(30472060); 国家863计划项目(2007AA02Z171)

Pharmacokinetics of nobiletin in rats and Beagle dogs

CHEN Xi-jing, YU Xue, REN Wei-chao, SUN Wei, LU Yang, HE Jia-ke   

  1. Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Jiangsu, China
  • Received:2008-07-14 Revised:2008-10-20 Online:2008-11-26 Published:2020-10-14

摘要: 目的: 研究诺必擂停在大鼠和Beagle 犬体内的药动学过程。方法: 通过口服和静注两种给药方式, 用高效液相色谱法测定血浆中诺必擂停的浓度。结果: 大鼠灌胃给予诺必擂停8 、16 和32 mg /kg 剂量后, 血药浓度达峰时间tmax 分别为20 、30 、30 min, 峰浓度Cmax 分别为(300 ±171) 、(468 ±122) 、(982 ±449) ng /mL, 根据血药浓度AUC 计算出的生物利用度F 为(14.6 ±2.7) %。Beagle 犬按4 mg /kg 单剂量口服给予诺必擂停片后, tmax 为(95 ±12) min, Cmax 为(436 ±88) ng /mL,生物利用度F 为(27.4 ±8.4) %。结论: 灌胃给药后诺必擂停在大鼠和Beagle 犬体内吸收较快但吸收程度较低, 该药在两种动物的药动学参数tmax 、t1 /2α和t1 /2β等存在明显的种属差异。

关键词: 诺必擂停, 大鼠, Beagle犬, 高效液相色谱法, 药代动力学

Abstract: AIM: To investigate the pharmacokinetics of nobiletin in rats and Beagle dogs. METHODS: The concentration of nobiletin in plasma was measured by HPLC after intragastric administration and intravenous injection. RESULTS: In rats, the tmax values of nobiletin by intragastric administration at doses of 8, 16 and 32 mg /kg were 20, 30 and 30 min, respectively, and the Cmax values were (300 ±171), (468 ±122) and (982 ±449) ng /mL respectively and the bioavailability was (14.6 ±2.7) %.In Beagle dogs, the tmax value of nobiletin after oral administration at a single dose of 4 mg /kg was (95 ±12) min, the Cmax value was (435.6 ±88.1) ng /mL and the bioavailability was (27.4 ±8.4) %. CONCLUSION: After oral administration, nobiletin was rapidly absorbed in rats and Beagle dogs, but had low bioavailability. The values of tmax, t1 /2α and t1 /2β were different between the two species of animals obviously.

Key words: nobiletin, rat, Beagle dog, HPLC, pharmacokinetics

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