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一些1,4 - 二氢吡啶衍生物在固态下的光稳定性和辐射稳定性

Photo- and radiostability of some 1,4-dihydropyridine derivatives in the solid state.

作者信息

Marciniec Barbara, Ogrodowczyk Magdalena

机构信息

Department of Pharmaceutical Chemistry, K. Marcinkowski University of Medical Sciences, 60-780 Poznań, 6 Grunwaldzka Str., Poland.

出版信息

Acta Pol Pharm. 2003 Mar-Apr;60(2):151-5.

Abstract

The effect of UV (254 nm) and beta-irradiation at doses 10-100 kGy on physical and chemical properties of four 1,4-dihydropyridyne derivatives in the solid state (nifedipine, nitrendipine, felodipine and nimodipine) has been studied. It has been established that the irradiation causes the appearance of free radicals (EPR) and decomposition products (TLC, GC), a decrease in the melting point (DSC) and the content (GLC, IR) and an increase in microbiological purity. The changes appear faster under the effect of UV than by beta-irradiation and their intensity and character depend on the derivative and dose. The most sensitive to UV irradiation is nifedipine (about 300 times more sensitive than the most resistant nimodipine), while the most sensitive to beta-irradiation is felodipine (about twice as sensitive as the most resistant nitrendipine). The results of our study indicate that 1,4-dihydropyridyne derivatives in solid state can be safely subjected to sterilization by beta-irradiation at doses < 20 kGy.

摘要

研究了紫外线(254纳米)和剂量为10 - 100千戈瑞的β辐射对四种固态1,4 - 二氢吡啶衍生物(硝苯地平、尼群地平、非洛地平和尼莫地平)物理和化学性质的影响。已确定辐射会导致自由基的出现(电子顺磁共振)和分解产物(薄层色谱法、气相色谱法),熔点降低(差示扫描量热法)和含量减少(气相色谱法、红外光谱法),以及微生物纯度提高。在紫外线作用下变化出现得比β辐射更快,其强度和特征取决于衍生物和剂量。对紫外线辐射最敏感的是硝苯地平(比最具抗性的尼莫地平敏感约300倍),而对β辐射最敏感的是非洛地平(比最具抗性的尼群地平敏感约两倍)。我们的研究结果表明,固态的1,4 - 二氢吡啶衍生物可以安全地接受剂量<20千戈瑞的β辐射灭菌。

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