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溴甲纳曲酮水溶液降解动力学研究
引用本文:穆常让,靳文仙,王成港,王春龙. 溴甲纳曲酮水溶液降解动力学研究[J]. 中国药学杂志, 2012, 47(13): 1060-1064
作者姓名:穆常让  靳文仙  王成港  王春龙
作者单位:河南大学药学院;释药技术及药代动力学国家重点实验室;天津药物研究院
摘    要: 目的 研究溴甲纳曲酮在水溶液中的降解动力学特征,考察溴甲纳曲酮的降解影响因素,为其制剂的研究提供必要的实验结果和数据。方法 通过经典恒温实验,应用HPLC测定溴甲纳曲酮在不同温度、pH值、光照和Fe3+浓度条件下的降解动力学参数,用阿仑尼乌斯公式预测其有效期和活化能。结果 溴甲纳曲酮在水溶液中的降解反应级数为n=1,其水溶液最稳定的pH值在3.51左右;随着温度升高,溴甲纳曲酮降解速率增加,在常温水溶液中的有效期t0.9=145 d;Fe3+和光照能促进溴甲纳曲酮的降解。结论 溴甲纳曲酮在水溶液中的降解属近似一级动力学过程,降解速率与温度成正相关,pH对溴甲纳曲酮的降解有一定的影响,Fe3+和光照对溴甲纳曲酮的降解速率影响较明显。为制剂的研发提供了必要的实验结果和数据。

关 键 词:溴甲纳曲酮  降解动力学  经典恒温法  稳定性
收稿时间:2011-07-26;

Degradation Kinetics of Methylnaltrexone Bromide Aqueous Solution
MU Chang-rang,JIN Wen-xian,WANG Cheng-gang,WANG Chun-long. Degradation Kinetics of Methylnaltrexone Bromide Aqueous Solution[J]. Chinese Pharmaceutical Journal, 2012, 47(13): 1060-1064
Authors:MU Chang-rang  JIN Wen-xian  WANG Cheng-gang  WANG Chun-long
Affiliation:2,3(1.Pharmaceutical College of Henan University,Kaifeng 475001,China;2.Tianjin Institute of Pharmaceutical Research,Tianjin 300193,China;3.State Key Laboratory of Drug Delivery Technology and Pharmacokinetics,Tianjin 300193,China)
Abstract:OBJECTIVE To investigate the degradation kinetic characteristics of methylnaltrexone bromide aqueous solution and to study the factors that influence methylnaltrexone bromide degradation,thus to provide necessary data for the pharmaceutical research.METHODS Classical isothermal method was employed to evaluate the degradation kinetic profile of methylnaltrexone bromide under different temperatures,pH values,illumination and concentrations of Fe3+.The activation energy and shelf life were predicted with Arrhenius equation.RESULTS The degradation of methylnaltrexone bromide aqueous solution complied with first order kinetics.The aqueous solution was stable in an environment of pH 3.51,the higher the temperature was,the larger the degradation kinetic rate constant was.The shelf-life of the aqueous solution was 145 d at room temperature;and the illumination,as well as the existence of Fe3+ could both facilitate the degradation of methylnaltrexone bromide.CONCLUSION The degradation of methylnaltrexone bromide follows apparent first-order kinetics,and the degradation kinetic rate is affected by Fe3+ and illumination.Moreover,its degradation remarkably and positively correlates with temperature.pH also has an effect on the degradation rate.The kinetic profile provides basis for the investigation of the degradation mechanism and necessary experimental data for the future pharmaceutical research.
Keywords:methylnaltrexone bromide  degradation kinetics  classic isothermal method  stability
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