一种新型重氮丙啶基苯醌的稳定性指示高效液相色谱法及溶液稳定性
Stability-indicating HPLC assay and solution stability of a new diaziridinyl benzoquinone.
作者信息
Cheung A P, Struble E, Nguyen N, Liu P
机构信息
SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94205, USA.
出版信息
J Pharm Biomed Anal. 2001 Mar;24(5-6):957-66. doi: 10.1016/s0731-7085(00)00566-5.
RH1, 3-methyl-6-hydroxymethyl-2,5-diaziridinyl-1,4-benzoquinone, is a NQO1 (NAD(P)H quinone oxidoreductase) directed anti-tumor agent. It is designed as a water soluble analog of MeDZQ (3,6-dimethyl-2,5-diaziridinyl-1,4-benzoquinone) and is a drug candidate for clinical evaluation. A HPLC assay has been developed for its analysis. The assay is sensitive (ldl<0.2 ng), precise (rsd<1%), linear (r(2)=0.9997), accurate (error<0.6%), and stability-indicating. Using the developed assay, aqueous stability of RH1 has been evaluated. Both aziridine rings in MeDZQ are known to be easily hydrolyzable in aqueous solutions, however, hydrolysis of the second aziridine ring in RH1 appears inhibited.
RH1，即3-甲基-6-羟甲基-2,5-二氮丙啶基-1,4-苯醌，是一种由NQO1（NAD(P)H醌氧化还原酶）介导的抗肿瘤药物。它被设计为MeDZQ（3,6-二甲基-2,5-二氮丙啶基-1,4-苯醌）的水溶性类似物，是一种有待临床评估的候选药物。已开发出一种用于其分析的高效液相色谱法。该方法灵敏（检测限<0.2纳克）、精确（相对标准偏差<1%）、线性良好（r(2)=0.9997）、准确（误差<0.6%）且具有稳定性指示作用。利用所开发的方法，对RH1的水溶液稳定性进行了评估。已知MeDZQ中的两个氮丙啶环在水溶液中易于水解，然而，RH1中第二个氮丙啶环的水解似乎受到抑制。
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