国际医学寄生虫病杂志
國際醫學寄生蟲病雜誌
국제의학기생충병잡지
INTERNATIONAL JOURNAL OF MEDICAL PARASITIC DISEASES
2015年
2期
77-81
,共5页
涂珍%陶奕%姜斌%马玉凤%张皓冰
塗珍%陶奕%薑斌%馬玉鳳%張皓冰
도진%도혁%강빈%마옥봉%장호빙
氯硝柳胺%表面活性剂%平衡溶解度
氯硝柳胺%錶麵活性劑%平衡溶解度
록초류알%표면활성제%평형용해도
Niclosamide%Surfactant%Equilibrium solubility
目的 测定氯硝柳胺在不同水相介质、表面活性剂及有机溶剂中的平衡溶解度,为氯硝柳胺的含量测定、药代动力学的研究以及新剂型的设计等提供依据. 方法 采用高效液相色谱(high performance liquid chromatography,HPLC)法测定温度为25℃和37℃时氯硝柳胺在不同水相介质如生理盐水、5％葡萄糖溶液、PBS (pH7.4)缓冲液和去离子水中的平衡溶解度.比较表面活性剂聚山梨酯80 (tween-80)、十二烷基硫酸钠(SDS)和司盘80 (span-80)对氯硝柳胺平衡溶解度的影响,并测定氯硝柳胺在石油醚、四氢味喃等15种常见有机溶剂中的平衡溶解度. 结果 氯硝柳胺在生理盐水、5％葡萄糖溶液、PBS (pH7.4)缓冲液和去离子水中的平衡溶解度均较低,25℃下依次为(0.249 7±0.005 3)、(0.232 0±0.001 2)、(0.552 2±0.005 0)、(0.233 9±0.000 6) μg/ml,37℃下依次为(0.313 2±0.014 5)、(0.253 3±0.005 9)、(1.2540±0.008 6)、(0.270 5±0.001 9) μg/ml.不同表面活性剂对氯硝柳胺的增溶能力为tween-80＞SDS＞span-80.氯硝柳胺在有机溶剂中的平衡溶解度比水性介质大,其中在四氢呋喃中最大,为(743 7.03±94.40) μg/ml,在石油醚中最小,为(50.67 ±0.66)μg/ml. 结论 氯硝柳胺水溶性差,非离子型表面活性剂tween-80可显著增加其溶解能力,在某些有机溶剂如四氢呋喃和丙酮中的平衡溶解度较大.
目的 測定氯硝柳胺在不同水相介質、錶麵活性劑及有機溶劑中的平衡溶解度,為氯硝柳胺的含量測定、藥代動力學的研究以及新劑型的設計等提供依據. 方法 採用高效液相色譜(high performance liquid chromatography,HPLC)法測定溫度為25℃和37℃時氯硝柳胺在不同水相介質如生理鹽水、5％葡萄糖溶液、PBS (pH7.4)緩遲液和去離子水中的平衡溶解度.比較錶麵活性劑聚山梨酯80 (tween-80)、十二烷基硫痠鈉(SDS)和司盤80 (span-80)對氯硝柳胺平衡溶解度的影響,併測定氯硝柳胺在石油醚、四氫味喃等15種常見有機溶劑中的平衡溶解度. 結果 氯硝柳胺在生理鹽水、5％葡萄糖溶液、PBS (pH7.4)緩遲液和去離子水中的平衡溶解度均較低,25℃下依次為(0.249 7±0.005 3)、(0.232 0±0.001 2)、(0.552 2±0.005 0)、(0.233 9±0.000 6) μg/ml,37℃下依次為(0.313 2±0.014 5)、(0.253 3±0.005 9)、(1.2540±0.008 6)、(0.270 5±0.001 9) μg/ml.不同錶麵活性劑對氯硝柳胺的增溶能力為tween-80＞SDS＞span-80.氯硝柳胺在有機溶劑中的平衡溶解度比水性介質大,其中在四氫呋喃中最大,為(743 7.03±94.40) μg/ml,在石油醚中最小,為(50.67 ±0.66)μg/ml. 結論 氯硝柳胺水溶性差,非離子型錶麵活性劑tween-80可顯著增加其溶解能力,在某些有機溶劑如四氫呋喃和丙酮中的平衡溶解度較大.
목적 측정록초류알재불동수상개질、표면활성제급유궤용제중적평형용해도,위록초류알적함량측정、약대동역학적연구이급신제형적설계등제공의거. 방법 채용고효액상색보(high performance liquid chromatography,HPLC)법측정온도위25℃화37℃시록초류알재불동수상개질여생리염수、5％포도당용액、PBS (pH7.4)완충액화거리자수중적평형용해도.비교표면활성제취산리지80 (tween-80)、십이완기류산납(SDS)화사반80 (span-80)대록초류알평형용해도적영향,병측정록초류알재석유미、사경미남등15충상견유궤용제중적평형용해도. 결과 록초류알재생리염수、5％포도당용액、PBS (pH7.4)완충액화거리자수중적평형용해도균교저,25℃하의차위(0.249 7±0.005 3)、(0.232 0±0.001 2)、(0.552 2±0.005 0)、(0.233 9±0.000 6) μg/ml,37℃하의차위(0.313 2±0.014 5)、(0.253 3±0.005 9)、(1.2540±0.008 6)、(0.270 5±0.001 9) μg/ml.불동표면활성제대록초류알적증용능력위tween-80＞SDS＞span-80.록초류알재유궤용제중적평형용해도비수성개질대,기중재사경부남중최대,위(743 7.03±94.40) μg/ml,재석유미중최소,위(50.67 ±0.66)μg/ml. 결론 록초류알수용성차,비리자형표면활성제tween-80가현저증가기용해능력,재모사유궤용제여사경부남화병동중적평형용해도교대.
Objective To determine the equilibrium solubility of niclosamide in different aqueous mediums,surfactants and organic solvents,thus providing further basis for the content determination,pharmacodynamics study and the design of new dosage forms of the drug.Methods High performance liquid chromatography was used to detect the equilibrium solubility of niclosamide in different aqueous mediums such as saline,5％ glucose solution,pH7.4 phosphate buffer and deionized water at 25 ℃ and 37 ℃.The effect of different surfactants including polysorbate 80(tween-80),sodium dodecyl sulfate(SDS) and sorbitane monooleate (span-80) on the equilibrium solubility of niclosamide were studied at the same time,and the equilibrium solubilities of niclosamide in some common organic solvents,e.g.petroleun ether,tetrahydrofuran were determined.Results Niclosamide was poorly soluble in aqueous mediums.The equilibrium solubilities of niclosamide in saline,5％ glucose solution,pH7.4 phosphate buffer and deionized water were (0.249 7±0.005 3),(0.232 0±0.001 2),(0.552 2±0.005 0),(0.233 9±0.000 6) μg/ml at 25 ℃ and (0.313 2±0.014 5),(0.253 3± 0.005 9),(1.254 0±0.008 6),(0.270 5±0.001 9) μg/ml at 37 ℃,respectively.The solubilizing power of different surfactants were tween-80＞SDS＞span-80.The equilibrium solubility of niclosamide in organic solvents was greater than that in aqueous mediums.Among them,the equilibrium solubility was the highest in tetrahydrofuran and the lowest in petroleum ether,which was(743 7.03±94.40) μg/ml and (50.67±0.66) μg/ml,respectively.Conclusion Niclosamide is a hydrophobic drug.The non-ionic surfactant polysorbate 80 can significantly increase the solubility of the drug.The equilibrium solubility is higher in some organic solvents such as tetrahydrofuran and acetone.
