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丝裂霉素和卟吩姆在酸性溶液中的化学稳定性方面

Aspects of the chemical stability of mitomycin and porfiromycin in acidic solution.

作者信息

Underberg W J, Lingeman H

出版信息

J Pharm Sci. 1983 May;72(5):549-53. doi: 10.1002/jps.2600720518.

DOI:10.1002/jps.2600720518
PMID:6864504
Abstract

Aspects of the degradations of mitomycin and porfiromycin were studied. The initial degradation processes of the compounds in an acidic medium were investigated. Influences of pH, buffers, and other additives such as halogenides and dioctyl sodium sulfosuccinate [sodium 1,4-bis(2-ethylhexyl)sulfosuccinate] were studied. The hydrogen ion catalyzes the degradation of both the uncharged and the protonated species. Anions also promote the degradation of the compounds in an acidic medium. Rate constants for all of the catalytic reactions could be determined. From the pH profiles, after correction for buffer influences, accurate pKa values for the aziridine nitrogens could be obtained. The protective influence of the dioctyl sulfosuccinate ion could be explained. From the data obtained a plausible mechanism for the initial acidic degradation reactions was developed.

摘要

研究了丝裂霉素和卟吩姆的降解情况。研究了这些化合物在酸性介质中的初始降解过程。研究了pH值、缓冲剂以及卤化物和磺基琥珀酸二辛酯钠[1,4 - 双(2 - 乙基己基)磺酸钠]等其他添加剂的影响。氢离子催化不带电荷和质子化形式的降解。阴离子在酸性介质中也促进化合物的降解。可以确定所有催化反应的速率常数。通过pH曲线,校正缓冲剂影响后,可以得到氮丙啶氮的准确pKa值。可以解释磺基琥珀酸二辛酯离子的保护作用。根据获得的数据,提出了初始酸性降解反应的合理机制。

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