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高效薄层色谱法测定人血浆中西替利嗪及其在药代动力学研究中的应用。

High-performance thin-layer chromatography for the determination of cetirizine in human plasma and its use in pharmacokinetic studies.

作者信息

Pandya K K, Bangaru R A, Gandhi T P, Modi I A, Modi R I, Chakravarthy B K

机构信息

Research & Development Centre, Cadila Laboratories Ltd, Ahmedabad, India.

出版信息

J Pharm Pharmacol. 1996 May;48(5):510-3. doi: 10.1111/j.2042-7158.1996.tb05963.x.

DOI:10.1111/j.2042-7158.1996.tb05963.x
PMID:8799876
Abstract

A rapid and sensitive high-performance thin-layer chromatography (HPTLC) assay has been developed for the measurement of cetirizine in human plasma and its utility for pharmacokinetic study has been evaluated. In the proposed HPTLC method, protein-bound cetirizine was freed by proteolysis of plasma proteins by incubating the plasma with 0.35% pepsin and then extracting with 2 mL pH 5.0 phosphate buffer, followed by 4 mL chilled chloroform. The chloroform layer was separated and concentrated. An aliquot of the extract was then spotted on precoated silica-gel 60 F254 plates using a Camag Linomat IV autosampler. Quantification was with the help of a dual-wavelength TLC scanner. The proposed method had a recovery of 98% and the lowest amount of cetirizine that could be detected was 50 ng. The method was applied for the determination of the plasma levels and pharmacokinetic parameters of cetirizine after oral administration of two marketed preparations in healthy volunteers and the pharmacokinetic parameters determined by the proposed method were in agreement with previously reported values.

摘要

已开发出一种快速灵敏的高效薄层色谱(HPTLC)分析法,用于测定人血浆中的西替利嗪,并评估了其在药代动力学研究中的效用。在所提出的HPTLC方法中,通过将血浆与0.35%胃蛋白酶孵育使血浆蛋白水解,从而释放结合蛋白的西替利嗪,然后用2 mL pH 5.0的磷酸盐缓冲液萃取,接着用4 mL冷冻氯仿萃取。分离并浓缩氯仿层。然后使用Camag Linomat IV自动进样器将一份萃取液点样于预涂硅胶60 F254板上。借助双波长TLC扫描仪进行定量分析。所提出的方法回收率为98%,可检测到的西替利嗪最低量为50 ng。该方法用于测定健康志愿者口服两种市售制剂后血浆中西替利嗪的水平和药代动力学参数,所测定的药代动力学参数与先前报道的值一致。

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