| 引用本文: | 张青铃,杨艳希,罗友华,许光辉,杨辉,戚欢阳,贾玉龙,黄亦琦.化学药品对照品的吸湿性、溶解性与比表面积相关性研究[J].中国现代应用药学,2020,37(11):1343-1349. |
| ZHANG Qingling,YANG Yanxi,LUO Youhua,XU Guanghui,YANG Hui,QI Huanyang,JIA Yulong,HUANG Yiqi.Study on the Correlation Among Hygroscopicity, Solubility and Specific Surface Area of the Chemical Reference[J].Chin J Mod Appl Pharm(中国现代应用药学),2020,37(11):1343-1349. |
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| 化学药品对照品的吸湿性、溶解性与比表面积相关性研究 |
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张青铃1,2, 杨艳希1,2,3, 罗友华1,2, 许光辉2, 杨辉2, 戚欢阳2, 贾玉龙2, 黄亦琦2
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1.福建中医药大学药学院, 福州 350122;2.厦门市医药研究所, 厦门市天然药物研究与开发重点实验室, 福建 厦门 361008;3.厦门医学院药学系, 福建 厦门 361023
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| 摘要: |
| 目的 初步研究药物（化学药品对照品）吸湿性、溶解性与其比表面积的相关性。方法 分析《化学药品对照品图谱集—动态水分吸附》中631种药物的水分吸附动力学图，把图中相对湿度80%放置180 min的最大吸湿率（质量变化率）、比表面积、水溶性、乙醇溶解性输入Excel表，分析药物平均吸湿率、平均比表面积、水溶性、乙醇溶解性、水和乙醇中相同溶解性的相关性；分析极具引湿性药物的吸湿官能团及放湿情况；初步比较含不同吸湿官能团的药物吸湿性强弱。结果 631种药物比表面积为0~396.11 m2·g-1、吸湿率为0.02%~81.00%。药物平均吸湿率与平均比表面积、水溶性、吸湿官能团均正相关，与乙醇溶解性、水和乙醇相同溶解性的相关性较复杂。吸湿官能团可能包括氨基、羟基、羧基、钠盐、钾盐、铵盐、硅酸铝、寡糖等20种，药物吸湿后在低相对湿度环境中会发生不放湿、部分放湿、完全放湿等现象。药物溶解性与平均比表面积关系：水中略溶以上负相关，以下正相关；乙醇中微溶以上不相关，以下负相关。结论 化学药品对照品的吸湿性、溶解性与比表面积具有相关性，为药物防潮工艺和难溶性药物溶出度提高技术提供参考。 |
| 关键词: 化学药品对照品 动态水分吸附 吸湿性 吸湿官能团 比表面积 溶解性 相关性 |
| DOI：10.13748/j.cnki.issn1007-7693.2020.11.012 |
| 分类号:R917 |
| 基金项目:福建省医学创新课题立项（2016-CXB-16）；厦门市卫生和计划生育委员会资助（厦卫科教[2016]469号）；厦门市科技惠民项目（3502Z20164084） |
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| Study on the Correlation Among Hygroscopicity, Solubility and Specific Surface Area of the Chemical Reference |
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ZHANG Qingling1,2, YANG Yanxi1,2,3, LUO Youhua1,2, XU Guanghui2, YANG Hui2, QI Huanyang2, JIA Yulong2, HUANG Yiqi2
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1.College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, China;2.Xiamen Key Laboratory of Natural Medicine Research and Development, Xiamen Medicine Institute, Xiamen 361008, China;3.Department of Pharmacy, Xiamen Medical College, Xiamen 361023, China
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| Abstract: |
| OBJECTIVE To preliminarily study the correlation among the hygroscopicity, solubility and specific surface area of drug (chemical reference). METHODS The moisture adsorption kinetics of the 631 drugs in the Chemical Reference Map Set-Dynamic Water Adsorption was analyzed, and the maximum hygroscopic rate (rate of mass change), specific surface area, water solubility and ethanol solubility of RH80% after 180 min was input into Excel formats. The relationship of the average moisture absorption rate, average specific surface area, solubility in aqua, solubility in ethanol was analyzed. The hygroscopic functional groups of hygroscopic drugs and moisture release behavior were analyzed. The hygroscopic strength of different hygroscopic functional groups was preliminarily compared. RESULTS The specific surface area of the 631 drugs was 0-396.11 m2·g-1, the moisture absorption rate was 0.02%-81.00%. The average moisture absorption rate of the drug was positively correlated with the average specific surface area, water solubility and hygroscopic functional groups, while the correlation between the average hygroscopic rate and the solubility of ethanol, the same solubility in water and ethanol was complicated. There might be 20 hygroscopic functional groups including amino, hydroxyl, carboxyl, sodium, potassium, ammonium, aluminum silicate, oligosaccharide, etc. The appearance was observed that the drug might do not liberate moisture, liberate moisture partially or liberate moisture completely in a low relative humidity environment after moisture absorption. The relationship between drug solubility and average specific surface area:when the water solubility was more than slightly soluble, the correlation was negative, whereas showed positive correlation. When the ethanol solubility was above the slightly soluble, the correlation was not correlated, and below, negative correlation. CONCLUSION There is a correlation between the hygroscopicity, solubility and specific surface area of the chemical reference, which provides a reference for the moisture-proof process of drugs and the technology to improve the dissolution of insoluble drugs. |
| Key words: chemical reference dynamic vapor sorption hygroscopicity hygroscopic functional group specific surface area solubility correlation |
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