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| 高效液相色谱法测定特考韦瑞的平衡溶解度和油水分配系数 | |
| 引用本文： | 于锋英,刘皈阳,梁尔光,高春生,钟武.高效液相色谱法测定特考韦瑞的平衡溶解度和油水分配系数[J].军事医学科学院院刊,2012,36(1):49-51,55. |
| 作者姓名： | 于锋英 刘皈阳 梁尔光 高春生 钟武 |
| 作者单位： | 1. 河北北方学院,河北张家口,075000;军事医学科学院毒物药物研究所,北京,100850 2. 解放军总医院附属医院,北京,100037 3. 军事医学科学院毒物药物研究所,北京,100850 |
| 基金项目： | 国家科技支撑计划资助项目（2011BAI18B01） |
| 摘 要： | 目的 用高效液相色谱法(HPLC)测定特考韦瑞(ST-246)在37℃水和不同pH缓冲液的平衡溶解度,以及在正辛醇-水/缓冲液系统的油水分配系数.方法 采用摇瓶法测定平衡溶解度,通过药物分配平衡后在油相及水相的浓度比,计算油水分配系数.结果 ST-246在37℃水的平衡溶解度为3.35 mg/L,ST-246的表观油水分配系数为230.49(lgP=2.36),在正辛醇/pH4.0缓冲液的油水分配系数最大,为779(lgP=2.89).结论 ST-246的水溶性较差,脂溶性不佳,其水中溶解度呈pH依赖性,增大pH可增加其溶解度. |
| 关 键 词： | 高效液相色谱法 特考韦瑞 平衡溶解度 油水分配系数 |
Determination of the equilibrium solubility of tecovirimat and its apparent oil/water partition coefficients using HPLC |
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| YU Feng-ying,LIU Gui-yang,LIANG Er-guang,GAO Chun-sheng,ZHONG Wu.Determination of the equilibrium solubility of tecovirimat and its apparent oil/water partition coefficients using HPLC[J].Bulletin of the Academy of Military Medical Sciences,2012,36(1):49-51,55. | |
| Authors: | YU Feng-ying LIU Gui-yang LIANG Er-guang GAO Chun-sheng ZHONG Wu |
| Institution: | 1.Hebei North College,Zhangjiakou,Hebei 075000,China;2.Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing 100850,China;3.Department of Pharmacy,Affiliated Hospital,Chinese PLA General Hospital,Beijing 100037,China) |
| Abstract: | Objective To determine the equilibrium solubility and oil/water apparent partition coefficients（lgP） of tecovirimat（ST-246） in a series of test solutions of different pH using HPLC.Methods The equilibrium solubility was determined by saturation methods,and P was calculated with the concentration ratio of the drug in oil and water phase after partition equilibrium.Results The equilibrium solubility of ST-246 is 3.35 mg/L in water at 37℃,and the oil/water lgP of ST-246 was 2.36.It has the highest partition coefficients in n-octanol/pH4.0 buffer solution system.Conclusion ST-246 has poor watersolubility and liposolubility.ST-246 is not easily soluble and a higher pH can improve its equilibrium solubility. |
| Keywords: | HPLC tecovirimat equilibrium solubility partition coefficients |
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