钠基蒙脱土对桑叶生物碱部位中1-脱氧野尻霉素的缓释研究  

Sustained-Release Effect of Na-Montmorillonite on 1-Deoxynojirimycin in Alkaloid Fraction of Mulberry Leaf Extract

作　　者：邓超[1] 刘芳[1] 曾光尧[1] 周应军[1] 

机构地区：[1]中南大学药学院,长沙410013

出　　处：《中国药学杂志》2016年第8期639-644,共6页Chinese Pharmaceutical Journal

基　　金：国家科技"十一五"重大专项-新药创制项目(2009ZX09102-110)

摘　　要：目的考察钠基蒙脱土(Na-montmorillonite,Na-MMT)对桑叶提取物中1-脱氧野尻霉素(1-deoxynojirimycin,DNJ)是否存在缓释效果。方法在搅拌条件下使其进入钠基蒙脱土层间,从而制备1-脱氧野尻霉素-蒙脱土复合物。通过计算钠基蒙脱土对1-脱氧野尻霉素的载药量来选择合适的吸附时间、温度、投料比,并对该条件下制备的1-脱氧野尻霉素-蒙脱土复合物进行体外实验,评价缓释效果。结果当钠基蒙脱土用量为5.00 g,桑叶提取物用量16.00 g(1-脱氧野尻霉素含量25.1%),在100℃下,于1 000 m L去离子水中搅拌1 h时,可制得1-脱氧野尻霉素载药量为111.64 mg·g-1的1-脱氧野尻霉素-蒙脱土复合物。所制备的1-脱氧野尻霉素-蒙脱土复合物在纯净水、磷酸二氢钠缓冲液(p H 7.4)、0.1 mol·L-1盐酸溶液中均能快速释放,且溶液体积越大,1-脱氧野尻霉素释放率越高。结论钠基蒙脱土对1-脱氧野尻霉素具有缓释效果,可以用于1-脱氧野尻霉素缓释制剂的研究。OBJECTIVE To investigate the sustained-release ability of Na-montmorillonite（ Na-MMT） on 1-deoxynojirimycin（ DNJ） in mulberry leaf extract（ MLE）. METHODS In order to prepare DNJ-MMT composite,DNJ was intercalated into the interlayer of MMT by stirring. Time and temperature for adsorption and ratio of DNJ to MMT were determined by calculating the loading of DNJ,then in vitro release experiment was carried out to estimate the sustained-release characteristics of DNJ-MMT. RESULTS DNJMMT composite with a drug loading of 111. 64 mg·g^- 1was obtained by stirring 5. 00 g Na-MMT and 16. 00 g MLE containing 4 016. 0mg DNJ in 1 000 mL deionized water at 100 ℃ for 1 h. The composite released DNJ quickly in water,potassium phosphate buffer（ p H7. 4）,and 0. 1 mol·L^- 1hydrochloric acid solution. With the increasing of volume of hydrochloric acid solution,the release ratio of DNJ also increased correspondingly. CONCLUSION The sustained-release effect of Na-MMT on DNJ is proved. Na-MMT can be used for study of DNJ sustained-release preparations.

关 键 词：蒙脱土 桑叶提取物 1-脱氧野尻霉素 高效液相色谱法 缓释制剂 

分 类 号：R944[医药卫生—药剂学]