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[抗银屑病药物地蒽酚和柯桠素在水体系中的化学不稳定性:氧化行为]

[Chemical instability of the antipsoriatic dithranol and chrysarobin in aqueous systems: oxidation behavior].

作者信息

Berset J D, Krebs A

机构信息

Dermatologische Klinik der Universität Bern.

出版信息

Pharm Acta Helv. 1990;65(3):66-9.

PMID:2333308
Abstract

Decomposition of dithranol (1) and chrysarobin (4) in homogeneous and heterogeneous buffer solutions (pH 7.5) were studied by means of HPLC-chromatography. Half lives of (1) under homogeneous conditions were 1 h 15 min., under heterogeneous conditions 2 h 45 min., whereas in the case of (4) 3 h and 30 min. respectively were measured. (1) was degraded to dihydroxyanthrachinon (2) and dimeric dithranol (3), the amount of (2) and (3) depending of the chosen conditions, whereas degradation of (4) under heterogeneous conditions revealed no oxidation products. On the other hand two metabolites of (4) were detected in homogeneous buffer solutions. The presenting studies clearly show the different ways of decomposition of (1) and (4) in homogeneous and heterogeneous solutions.

摘要

通过高效液相色谱法研究了在均相和非均相缓冲溶液(pH 7.5)中二羟基蒽酚(1)和柯桠素(4)的分解情况。(1)在均相条件下的半衰期为1小时15分钟,在非均相条件下为2小时45分钟,而对于(4),分别测得为3小时30分钟。(1)降解为二羟基蒽醌(2)和二聚二羟基蒽酚(3),(2)和(3)的量取决于所选条件,而(4)在非均相条件下的降解未显示出氧化产物。另一方面,在均相缓冲溶液中检测到了(4)的两种代谢产物。目前的研究清楚地表明了(1)和(4)在均相和非均相溶液中的不同分解方式。

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