| 摘要: |
| 目的：建立大鼠组织中桂利嗪的HPLC测定法，用于小剂量尾静脉注射给药后测定桂利嗪在大鼠组织中分布。方法：组织样品加NaOH碱化，以甲基叔丁基醚提取，采用Hypersil C18 柱，甲醇-水- 冰醋酸-三乙胺(70300.60.4)为流动相，254 nm波长处检测,测定了尾静脉给药2 mg/kg桂利嗪注射液后在SD大鼠心、肝、脾、肺、肾、胃、小肠、脑、脂肪、睾丸等10个组织脏器中的分布情况。结果：肝组织样品最低检测限0.02 μg/ml，线性范围0.05～2 μg/ml，小肠组织样品最低检测限0.02 μg /ml，线性范围0.05～1 μg/ml，符合生物样品分析要求。桂利嗪广泛地分布于大鼠的多个组织脏器中，其中肺部浓度最高。结论：本法简便、准确、灵敏，适合桂利嗪临床前药代动力学组织分布研究。 |
| 关键词: 桂利嗪 高压液相色谱法 组织分布 |
| DOI：10.3724/SP.J.1008.2008.00303 |
| 投稿时间：2007-09-03修订日期：2008-01-05 |
| 基金项目: |
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| HPLC in determination of tissue distribution of cinnarizine in rats |
| LIU Yan,LOU Zi-yang* |
| (Pharmaceutical Analysis Center,School of Pharmacy, Second Military Medical University, Shanghai 200433, China) |
| Abstract: |
| Objective：To develop a HPLC method for the determination of tissue distribution of cinnarizine in rats. Methods: Cinnarizine (2 mg/Kg) was injected into the tail vein of rats. Tissue sample was alkalized with sodium hydroxide solution and extracted with methyl tert-butyl ether. The separation was performed on a Hypersil C18 column using methanol-water-glacial acetic acidacid-triethylamine (70300.60.4) as the mobile phase at UV 254 nm. The distribution of cinnarizine in the heart, liver, spleen, lung, kidney, stomach, small intestine, brain, fat and testes was determined. Results: The limit of detection of cinnarizine in the hepatic tissue was 0.02 μg /ml and the linear range was 0.05-1 0 μg/ml. The limit of detection in the intestine tissue was 0.02μg /ml and the linear range was 0.05-1 μg/ml, which meets the requirement for the analysis of biological samples. Cinnarizine was extensively distributed in rat body, with highest concentration found in the lung. Conclusion: Our method is easy to perform, accurate and sensitive, which makes it suitable for preclinical pharmacokinetic research of cinnarizine. |
| Key words: cinnarizine high pressure liquid chromatography tissue distribution |
