桃胶改良前后的多糖含量、功能性质以及体外释放度变化研究  

Changes of polysaccharide content, functional properties and in vitro release of peach gum before and after improvement

作　　者：蔡延渠[1] 董碧莲 朱志东 邓剑壕 刘文彬[2] 朱盛山[1] 霍务贞[1] CAI Yan-qu;DONG Bi-lian;ZHU Zhi-dong;DENG Jian-hao;LIU Wen-bin;ZHU Sheng-shan;HUO Wu-zhen(The Center for Drug Research and Development,Guangdong Pharmacological University,Guangzhou 510006,China;Guangdong Provincial Key Laboratory of Pharmaceutical Bioactive Substances,Guangdong Pharmacological University,Guangzhou 510006,China)

机构地区：[1]广东药科大学新药研发中心,广东广州510006 [2]广东药科大学广东省生物活性药物研究重点实验室,广东广州510006

出　　处：《中草药》2018年第20期4808-4815,共8页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年基金项目(81503260);国家自然科学基金面上项目(81373981)

摘　　要：目的分析桃胶改良前后的多糖含量、影响制剂的功能性质以及体外释放度变化情况,探索其变化规律,为改良桃胶作为新型缓释辅料的应用提供依据。方法将不同产地原桃胶与改良桃胶烘干、粉碎、过筛,粉末用超纯水超声溶解,采用苯酚-硫酸法结合紫外-可见分光光度法测定多糖质量分数;p H计测定胶液的酸碱度;Brookfield DV-II Pro黏度计测定胶液的动力黏度;称重法测定胶粉溶解度及溶胀度;干燥器控制法测定胶粉不同相对湿度环境下的吸湿率;体外释放度实验结合HPLC法测定喘平方胶片中3个指标成分(麻黄碱、伪麻黄碱和东莨菪碱)的体外累积释放度。结果贵州习水、江西信丰、湖北随县产原桃胶各指标为多糖质量分数为84.30%、81.52%、77.84%;1%胶溶液p H值为5.63、5.60、5.88;1%胶溶液动力黏度为30.8、28.5、25.9 m Pa·s;水中溶解度为60.8、57.5、51.2 mg/g;溶胀度为34.22%、29.66%、26.25%;12 h的相对湿度(RH)43%吸湿率为28.19%、27.02%、26.44%,RH 81%吸湿率为38.22%、35.26%、34.64%;喘平方胶片中麻黄碱、伪麻黄碱和东莨菪碱2 h的体外累积释放度为95.41%～98.84%、96.05%～97.11%、96.35%～98.21%。贵州习水、江西信丰、湖北随县产改良桃胶,各指标为多糖质量分数为96.92%、94.76%、93.65%;1%胶溶液p H值为7.07、7.08、7.12;1%胶溶液动力黏度为318.4、289.6、266.4 m Pa·s;水中溶解度为178.2、167.3、163.8 mg/g;溶胀度为84.98%、81.55%、79.82%;12 h的RH 43%吸湿率为41.22%、39.93%、39.20%,RH 81%吸湿率为60.88%、58.48%、57.17%;喘平方胶片中麻黄碱、伪麻黄碱和东莨菪碱12 h的体外累积释放度为97.88%～98.36%、97.59%～98.56%、97.72%～98.12%。结论与原桃胶相比,改良桃胶在多糖含量、溶解度、溶胀度、动力黏度、吸湿率、缓释性能等方面均显著提高,且溶液呈现中性,提示可作为新型缓释材料进一步研发、应用。Objective To analyze the difference of polysaccharides content,property characterization,and in vitro release between the original peach gum and improved peach gum,and to find the change rule,so as to provide the basis for its further application as the new delivery material.Methods The content of polysaccharides was measured by the phenol-sulfuric acid method combined with ultraviolet spectrophotometry.The p H value of liquid cement was measured by p H meter.The dynamic viscosity of liquid cement was measured by the Brookfield DV-Pro viscometer.The solubility and swelling Ⅱ ratio of rubber powder were measured by the weighing method.The moisture-absorption rate at different relative humidity of rubber powder was measured by the method of controlling humidity with the desiccator.With three index components（ephedrine,pseudoephedrine,and scopolamine） as the standards,HPLC and the release test were applied to determine the accumulated release rate of Chuanping adhesive tablets（CAT）.Results Original peach gum： In the three producing areas of Xishui in Guizhou Province,Xinfeng in Jiangxi Province,and Suixian in Hubei Province,the content of polysaccharides respectively was 84.30%,81.52%,and 77.84%.The p H value of 1% liquid cement was 5.63,5.60,and 5.88.The dynamic viscosity of 1% liquid cement was 30.8,28.5,and 25.9 m Pa·s.The solubility of rubber powder was 6.08%,5.75%,and 5.12%.The swelling ratio of rubber powder was 34.22%,29.66%,and 26.25%.The 12 h moisture-absorption rate of the improved peach gum polysaccharose at RH of 43% was 28.19%,27.02%,and 26.44%; and at RH of 81% was 38.22%,35.26%,and 34.64%.The 2 h cumulative release amount in vitro of methamphetamine,pseudoephedrine,and scopolamine of Chuanping adhesive tablets were 95.41%—98.84%,96.05%—97.11%,and 96.35%—98.21%.Improved peach gum： In the three producing areas of Xishui,Xinfeng,and Suixian,the content of polysaccharides respectively was 96.92%,94.76%,and 93.35%.The p H of 1% liquid cement was 7.10,7.08,and 7.12.The dynamic viscosity

关 键 词：原桃胶 改良桃胶 多糖 功能性质 体外释放度 缓释 辅料 苯酚-硫酸法 动力黏度 溶解度 溶胀度 吸湿率 HPLC 麻黄碱 伪麻黄碱 东莨菪碱 

分 类 号：R283.6[医药卫生—中药学]