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新型五环吡咯并醌类抗癌化合物GR63178A在水溶液和生物流体中的稳定性。

Stability of GR63178A, a novel pentacyclic pyrroloquinone anticancer compound, in aqueous solutions and biological fluids.

作者信息

French R C, Cummings J, Nicolson M, Smyth J F

机构信息

Imperial Cancer Research Fund, Medical Oncology Unit, Western General Hospital, Edinburgh, UK.

出版信息

J Pharm Pharmacol. 1993 Jan;45(1):10-5. doi: 10.1111/j.2042-7158.1993.tb03670.x.

DOI:10.1111/j.2042-7158.1993.tb03670.x
PMID:8094437
Abstract

The effect of temperature, pH, light, drug concentration and aeration on the stability of aqueous solutions of GR63178A, a novel anticancer compound, has been investigated. The effect of light upon the stability of GR63178A in a clinical infusion system and in biological fluids, has also been investigated. A high performance liquid chromatographic assay was used to separate the parent compound from a number of degradation products. Data presented here demonstrate that GR63178A is stable in aqueous solutions at normal ambient temperatures in neutral or alkaline pH ranges. The compound is unstable when exposed to light (t1/2 3.2-233 min) and shows an inverse relationship between concentration and rate of degradation. The drug is also unstable under acidic conditions, but shows a more limited spectrum of degradation products than those arising from photolysis.

摘要

已对温度、pH值、光照、药物浓度和通气对新型抗癌化合物GR63178A水溶液稳定性的影响进行了研究。还研究了光照对GR63178A在临床输液系统和生物流体中稳定性的影响。采用高效液相色谱分析法将母体化合物与多种降解产物分离。此处呈现的数据表明,GR63178A在中性或碱性pH范围内的正常环境温度下在水溶液中稳定。该化合物在光照下不稳定(半衰期为3.2 - 233分钟),且降解速率与浓度呈反比关系。该药物在酸性条件下也不稳定,但与光解产生的降解产物相比,其降解产物谱更有限。

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引用本文的文献

1
The comparative disposition of the pyrolloquinone GR63178A and its 9-hydroxy metabolite GR54374X in sensitive and resistant mouse colon adenocarcinoma.吡咯并醌GR63178A及其9-羟基代谢物GR54374X在敏感和耐药小鼠结肠腺癌中的比较分布。
Cancer Chemother Pharmacol. 1993;32(2):156-61. doi: 10.1007/BF00685620.