STABILITY OF ASPIRIN IN DIFFERENT MEDIA
STABILITY OF ASPIRIN IN DIFFERENT MEDIA
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DOI：
10.1002/jps.2600720914
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发表时间：
1983-01-01
影响因子：
3.8
通讯作者：
NIAZI, S
中科院分区：
文献类型：
--
作者：
BAKAR, SK;NIAZI, S
阿司匹林在各种水、有机和生物介质中迅速水解。研究了在进行药代动力学研究的生物体液分析过程中阿司匹林在与其接触的介质中的分解情况。这些介质包括水、水-聚乙二醇400、水-甲醇-乙酸、磷酸盐缓冲液、来自对照大鼠和禁水36小时的大鼠的新抽取的血液和血浆，以及用乙腈沉淀的血液。还研究了分解随温度和 pH 值的变化。在所研究的各种溶剂系统中，阿司匹林在水-聚乙二醇（4:1，v/v [vol/vol]）中最稳定，这为制备静脉注射剂提供了极好的介质。剂型。磷酸盐缓冲液显示出对阿司匹林水解的显着催化作用。当温度升至 37°C 时，阿司匹林的水解增加了 5 倍以上。从22.5°C开始。阿司匹林在大鼠血液中的水解速度比血浆中的水解速度快13倍，血液中的平均半衰期为.apprx。 13分钟这给阿司匹林处置动力学研究带来了重大问题。收集后立即将血样与两倍体积的乙腈混合，然后离心，得到血浆-乙腈混合物，其中未观察到血细胞裂解。
Aspirin rapidly hydrolyzes in various aqueous, organic and biological media. The decomposition of aspirin in the media that comes in contact with it during analysis in biological fluids for pharmacokinetic studies was investigated. These media included water, water-polyethylene glycol 400, water-methanol-acetic acid, phosphate buffer, freshly drawn blood and plasma from control rats and rats deprived of water for 36 h, and blood precipitated with acetonitrile. The decomposition as a function of temperature and pH was also studied. Of the various solvent systems studied, aspirin was the most stable in water-polyethylene glycol (4:1, v/v [vol/vol]), which provides an excellent medium for preparation of i.v. dosage forms. Phosphate buffer showed significant catalysis of aspirin hydrolysis. A more than 5-fold increase in the hydrolysis of aspirin was noted when the temperature was raised to 37.degree. from 22.5.degree.. The hydrolysis of aspirin in rat blood was 13 times faster than that in plasma, with an average half-life in blood of .apprx. 13 min. This creates significant problems in aspirin disposition kinetic studies. Mixing the blood sample immediately after collection with twice the volume of acetonitrile and then centrifuging gives a plasma-acetonitrile mixture in which no lysis of blood cells is observed.