芒果苷的离解常数和脂水分配系数的测定方法研究
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昆药集团股份有限公司药物研究院,云南 昆明 650100

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R284.1

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* 基金项目: 云南省重点新产品开发计划项目(2012BC008) 收稿日期: 2016 - 07 - 12 作者简介: 董知旭(1986-),男,云南墨江人,助理工程师,主要从事新药开发质量研究工作。E-mail:dongzhixu668@163.com


Study on Dissociation Constant and Oil /water Partition Coefficient of Mangiferin
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Drug Research Institute of Kunming Pharmaceutical Group Co., Ltd., Kunming 650100, China

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    摘要:

    目的〓建立芒果苷离解常数和脂水分配系数的测定方法。方法〓采用紫外分光光度法和pH-HPLC色谱法测定了芒果苷离解常数,并对两种方法进行比较;用摇瓶法—高效液相色谱(HPLC)法测定了芒果苷在正辛醇-不同pH缓冲溶液中的脂水分配系数。结果〓通过高效液相色谱(HPLC)法和紫外分光光度法对芒果苷离解常数进行测定方法研究。紫外分光光度法中,测定了芒果苷的离解常数为6.52,在高效液相色谱法中,测定了芒果苷的离解常数为6.1。采用摇瓶法—HPLC法测定了芒果苷在正辛醇-不同pH缓冲溶液中的脂水分配系数。当pH2.0~5.0时,芒果苷在正辛醇—缓冲溶液中的脂水分配系数受溶液的pH值影响不大,当pH6.70~8.18时,芒果苷的脂水分配系数大幅度减小,说明在酸性条件下,芒果苷的脂溶性增加,水溶性下降,而在碱性条件下,芒果苷的脂溶性下降,水溶性增加。结论〓用所建立的方法分别测定了芒果苷的离解常数和脂水分配系数,HPLC法准确度高,重现性好,方便简单,分析快速、准确。

    Abstract:

    Objective To establish the method of measuring dissociation constants and oil-water partition coefficients of mangiferin. Methods Comparing two measurements for dissociation constants of mangiferin, which are ultraviolet spectrophotometry and pH – HPLC. Measuring oil-water partition coefficients of mangiferin between n-octanol and different pH buffer solution by HPLC and shaking flask method. Results Studying on the HPLC and ultraviolet spectrophotometry method for the dissociation constants of mangiferin. They got almost the same results which respectively are 6.5 and 6.1. Studying on the HPLC and shaking flask method for measuring the oil-water partition coefficients of mangiferin. The oil-water partition coefficients of mangiferin were almost the same, while the pH of buffer solution was between 2.0 to 5.0. But they should recede considerably, while the pH was between 6.70 to 8.18. That means the lipid solubility of mangiferin increased and the water solubility of it decreased in acidic conditions. While that was diametrically opposite in alkaline conditions. Conclusion The Methods, which were established for measuring dissociation constants and oil-water partition coefficients of mangiferin, HPLC method were accurate, repeatable, convenient and rapid.

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