Betteridge R F, Land C P, Bosanquet A G
Bath Cancer Research Unit, Royal United Hospital, Combe Park, Bath BA1 3NG, UK.
J Pharm Biomed Anal. 1988;6(6-8):875-8. doi: 10.1016/0731-7085(88)80104-3.
A high-performance liquid chromatographic method has been developed to investigate the stability of solutions of flavone-8-acetic acid (LM975) during preparation and storage. LM975 (20 microg ml(-1) in PBS) was found to be completely stable for 10 days at 80 degrees C as long as light was rigorously excluded. The drug showed no significant adsorption to containers of different materials or to two filtration units tested. Drug degradation did occur however, on exposure to light. In normal laboratory light the t(0.95) (5% degraded) was 30.3 min, in intense natural light (laboratory window sill) the t(0.95) was 3.3 min and in intense artificial light (100 W bulb at 10 cm) the t(0.95) was 13.8 min. NMR and mass spectral analysis of the isolated degradation product implied the formation of the decarboxylated product, 8-methyl flavone. It is suggested that care be taken to exclude light during the preparation, storage and infusion of solutions of flavone-8-acetic acid.
已开发出一种高效液相色谱法来研究黄酮 - 8 - 乙酸(LM975)溶液在制备和储存过程中的稳定性。发现LM975(在PBS中浓度为20μg ml⁻¹)在80℃下只要严格避光可完全稳定10天。该药物对测试的不同材料容器或两种过滤装置均无明显吸附。然而,药物在光照下确实会发生降解。在正常实验室光照下,t(0.95)(降解5%)为30.3分钟,在强烈自然光下(实验室窗台)t(0.95)为3.3分钟,在强烈人造光下(10厘米处100瓦灯泡)t(0.95)为13.8分钟。对分离出的降解产物进行核磁共振和质谱分析表明形成了脱羧产物8 - 甲基黄酮。建议在黄酮 - 8 - 乙酸溶液的制备、储存和输注过程中注意避光。