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中国临床药理学与治疗学 ›› 2004, Vol. 9 ›› Issue (6): 666-668.

• 研究原著 • 上一篇    下一篇

西洛他唑的高效液相色谱法测定及药动学研究

胡玉荣, 赵永星, 阿有梅, 贾欣, 尹志峰1, 刘世龙1, 乔海灵   

  1. 郑州大学药学院药理教研室, 郑州450052, 河南
  • 收稿日期:2004-03-05 修回日期:2004-04-29 发布日期:2020-11-22
  • 通讯作者: 胡玉荣, 女, 临床药理学硕士, 讲师, 研究方向:临床药理学。Tel:0371-5209010  Fax :0371-6974214  E-mai l:huyr@zzu.edu.cn
  • 作者简介:1郑州大学药学院2000 届本科生。

Determination of cilostazol in human plasma and its pharmacokinetics by HPLC

HU Yu-Rong, ZHAO Yong-Xing, A You-Mei, JIA Xin, YIN Zhi-Feng, LIU Shi-Long, QIAO Hai-Ling   

  1. Department of Pharmacology, Pharmaceutical College of Zhengzhou University, Zhengzhou 450052, Henan, China
  • Received:2004-03-05 Revised:2004-04-29 Published:2020-11-22

摘要: 目的 建立测定人血浆中西洛他唑含量的高效液相色谱(HPLC) 法, 并研究西洛他唑片在健康人体内的药动学。 方法 色谱柱为Hypersil C18 柱(4.6 mm ×200 mm, 5 μm), 流动相为乙腈-水(45∶55), 流速1.0 ml·min-1, 柱温30 ℃, 检测波长254 nm, 西洛他唑血浆样品以2 mol·L-1NaOH-无水乙醚(1∶4) 提取, 以地西泮为内标。 结果 标准曲线线性范围20 ~ 2 000 μg·L-1 (r=0.9999)。血浆中西洛他唑最低检测限为10 μg·L-1。平均提取回收率为80.2 % ±3.6 %, 平均方法回收率为97.0 % ±3.8 %, 日内RSD ≤5.8 %, 日间RSD ≤10.1 %。应用该法研究了10 例健康志愿者口服100 mg 西洛他唑后的药动学;其体内过程符合二室模型, tmax 为3.58±1.08 h, Cmax 为920 ±230 μg·L-1, AUC0-48 为11.0±3.3 mg·h-1·L-1结论 此法简便、快速, 适用于药物分析, 其药动学数据可为临床合理用药、新药研制及剂型改进提供理论依据。

关键词: 西洛他唑, 高效液相色谱法, 血药浓度, 药动学

Abstract: AIM: To establish a reversed phase highperformance liquid chromatographic method to determine cilostazol in human plasma and to study the pharmacokinetics of cilostazol in 10 healthy volunteers. METHODS: Using diazepam as the internal standard, cilostazol was extracted from human plasma with a mixture of 2mol ·L-1 NaOH-diethyl ether anhydrous (1:4).The mobile phase was acetonitrile-water (45:55), flow rate 1 ml· min-1, and the UV absorbance wavelength 254 nm.The pharmacokinetic analysis of cilostazol in 10 healthy volunteers after oral administration of 100mg was studied. RESULTS: Linear range of the standard curve was from 20 to 2 000 μg·L-1 (r=0.9999).The quantitative limit for cilostazol was 10 μg·L-1.The mean extraction recovery was 80.2 %±3.6 %.The mean analytical recovery was 97.0 % ±3.8 %.The relative standard deviation of intra-day and inter-day did not exceed 5.8 % and 10.1 %, respectively.It was found to be fitted to a twocompartment open model and its pharmacokinetic parameters were as follow:tmax 3.58 ±1.08 h, Cmax 920 ±230 μg ·L-1 AUC0-48 11.0 ±3.3 mg·h-1 ·L-1, respectively. CONCLUSION: The method is suitable for drug monitoring of cilostazol and the pharmacokinetics of cilostazol in human provides a useful index for clinical trial.

Key words: cilostazol, high-performance liquid chromatography, serum concentration, pharmacokinetics

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