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中国临床药理学与治疗学 ›› 2005, Vol. 10 ›› Issue (3): 302-305.

• 研究原著 • 上一篇    下一篇

RP-HPLC法测定Beagle 犬血浆中烟酸浓度及烟酸药代动力学研究

黄敏文, 王广基, 孙建国, 顾轶   

  1. 中国药科大学药代动力学重点实验室, 南京210038, 江苏
  • 收稿日期:2004-12-14 修回日期:2005-02-15 出版日期:2005-03-26 发布日期:2020-11-18
  • 通讯作者: 王广基, 男, 教授, 博士生导师, 从事药物代谢动力学研究。Tel:025-83271544 E-mail:gjwang@cpu.edu.cn
  • 作者简介:黄敏文, 女, 硕士研究生, 研究方向:药物代谢动力学。Tel:025-85391035 E-mail:hmw0126@126.com
  • 基金资助:
    国家863 计划资助项目(No2003AA2Z347A);江苏省药物代谢动力学重点实验室资助项目(NoBM2001201)

Determination of sustained-release niacin formulation by RP-HPLC in dog plasma and its pharmacokinetic study

HUANG Min-wen, WANG Guang-ji, SUN Jian-guo, GU Yi   

  1. Key Laboratory of Pharmacokinetics, China Pharmaceutical University, Nanjing 210038, Jiangsu, China
  • Received:2004-12-14 Revised:2005-02-15 Online:2005-03-26 Published:2020-11-18

摘要: 目的:建立RP-HPLC 法测定血浆中烟酸的药物浓度, 并将建立的方法应用于Beagle 犬测定烟酸缓释片的血药浓度, 计算其药代动力学参数和相对生物利用度。方法:0.1 ml 血浆样品经乙腈沉淀蛋白后直接进样;流动相为乙腈-水相(8∶92), 水相含10 mmol°L-1 磷酸二氢钾, 用磷酸调pH 值至4.0, 流速为1.0 ml°min-1;色谱柱为汉邦科技LichrospherC18 (5 μm, 250 mm×4.6 mm I.D.), 检测波长为263 nm。6 只Beagle 犬随机交叉口服500 mg 复方洛伐烟酸缓释片和500 mg 标准参比烟酸普通片后, 用RP-HPLC 法测定血浆中烟酸的药物浓度。结果:分析方法符合生物样品分析要求。Beagle 犬单剂量口服复方洛伐烟酸缓释片500 mg 后, 估算的末端相t1 2为1.3±1.2 h, Tmax 为2.3±0.8 h, Cmax 为35.3±4.9 mg°L-1, MRT 为3.5±0.6 h。复方洛伐烟酸缓释片的AUC、Cmax 明显低于烟酸普通片(P<0.05)。经配对t 检验分析显示复方洛伐烟酸缓释片Tmax 明显长于普通片(P<0.05)。结论:单剂量口服复方洛伐烟酸缓释片后, 测得的Cmax 和AUC 与烟酸普通片均有显著性差异, 受试缓释片的Tmax 长于参比普通片,Cmax 低于参比普通片, 说明受试缓释片无突释现象, 有一定的缓释效果。

关键词: 烟酸, 缓释片, RP-HPLC, 药代动力学, 相对生物利用度

Abstract: AIM: To establish a simple RP-HPLC method for the determination of niacin in dog plasma and calculate the relative bioavailability and the pharmacokinetic parameters of sustained-release niacin formulation. METHODS: Niacin was extracted from dog plasma with perchloric acid.The RP-HPLC was performed on a Lichrospher C18 column (5 μm, 250 mm×4.6 mm I.D.) with mobile phase of acetonitrile-10 mmol°L-1 monopotassium phosphate (8∶92, v/v), and the pH of the water phase was adjusted to 4.0 with phosphoric acid at flow rate of 1.0 ml°min-1.Niacin was detected by UV absorbance at 263 nm.Single dose of sustained-release niacin formulation (500 mg)and rapid-release niacin formulation (500 mg)were given to six Beagle dogs.RESULTS: The t1 2, Tmax, Cmax and MRT of niacin in the sustained release formulation were 1.25±1.15 h, 2.3±0.8 h, 35.3±4.87 mg°L-1 and 3.45±0.55 h, respectively.The Tmax of sustained-release niacin formulation is significantly longer than that of the conventional niacin tablet (P<0.05), the Cmax was significantly lower than that of the conventional niacin tablet (P<0.05). CONCLUSION: This method is simple, accurate, sensitive and applicable for pharmacokinetic study of niacin. The relative bioavailability is (40.7±8.6)% in the sustained- release formulation.

Key words: niacin, sustained-release formulation, RP-HPLC, pharmacokinetics, relative bioavailability

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