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一项使用在线多维色谱法对不同阿司匹林制剂进行的比较生物利用度研究。

A comparative bioavailability study of different aspirin formulations using on-line multidimensional chromatography.

作者信息

Sagar K A, Smyth M R

机构信息

School of Chemical Sciences, Dublin City University, Ireland.

出版信息

J Pharm Biomed Anal. 1999 Nov;21(2):383-92. doi: 10.1016/s0731-7085(99)00177-6.

Abstract

A multi-dimensional column chromatographic method employing UV spectrometric detection was optimised and successfully used in a comparative bio-availability study of aspirin obtained from different commercially available oral dosage forms. Sample clean-up was achieved by on-line solid-phase extraction. In this study, the bioavailability of aspirin was compared in plain aspirin tablets, chewed tablets, effervescent tablets and Enteric-coated aspirin tablets. Blood samples were taken at frequent intervals after single dosing in ten healthy volunteers, the plasma samples were first treated with physostigmine sulphate to minimise enzymatic hydrolysis of aspirin to salicylate. The results showed the measured Tmax, Cmax, and AUC was significantly higher for soluble aspirin than for the other formulations and the t1/2 was shorter. This indicates the rapid absorption of aspirin from a soluble formulation compared with that from the other formulations. These differences suggest that the soluble formulation could be the aspirin of choice to treat patients suspected to be at high risk of myocardial infarction. The method performs, in a single step, an efficient extraction and clean-up of aspirin from human plasma. The calibration graph was linear over the calibration range 0.2-12 microg ml(-1) plasma with a limit of detection of 0.1 microg ml(-1). The intra- and inter-assay coefficients of variation were less than 6% and the recoveries ranged from 86 to 98%. The proposed method combines the advantages of being simple and selective in the presence of other potential interfering drugs and is suitable for routine analyses to obtain valuable information about the clinical effects of the drug and its use in prevention treatments of acute myocardial infarction. The whole procedure takes 7 min and is in agreement with other conventional methods.

摘要

采用紫外光谱检测的多维柱色谱法得到优化,并成功用于比较不同市售口服剂型阿司匹林的生物利用度研究。通过在线固相萃取实现样品净化。本研究比较了普通阿司匹林片、咀嚼片、泡腾片和肠溶阿司匹林片中阿司匹林的生物利用度。在10名健康志愿者单次给药后,频繁采集血样,血浆样品首先用硫酸毒扁豆碱处理,以尽量减少阿司匹林酶解为水杨酸。结果显示,可溶性阿司匹林的实测Tmax、Cmax和AUC显著高于其他剂型,t1/2较短。这表明与其他剂型相比,可溶性制剂中的阿司匹林吸收迅速。这些差异表明,可溶性制剂可能是治疗疑似心肌梗死高危患者的首选阿司匹林。该方法在一步操作中即可从人血浆中高效萃取和净化阿司匹林。校准曲线在校准范围0.2 - 12 μg ml(-1)血浆内呈线性,检测限为0.1 μg ml(-1)。批内和批间变异系数均小于6%,回收率在86%至98%之间。所提出的方法结合了在存在其他潜在干扰药物时简单且具选择性的优点,适用于常规分析,以获取有关药物临床效果及其在急性心肌梗死预防治疗中应用的有价值信息。整个过程耗时7分钟,与其他传统方法一致。

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