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桑乳汁和1-脱氧野尻霉素缓释颗粒的药物释放和降血糖效果试验

Controlled-release granules research of mulberry latex and 1-deoxynojirimycin(DNJ)pharmacokinetic

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【作者】 苏维磊杨晶盛琳波苏超张敏娟焦峰

【Author】 SU Wei-Lei;YANG Jing;SHENG Lin-Bo;SU Chao;ZHANG Min-Juan;JIAO Feng;Northwest A&F University;

【机构】 西北农林科技大学

【摘要】 桑叶乳汁中含有的1-脱氧野尻霉素(DNJ)属于α-糖苷酶抑制剂,由于DNJ在哺乳动物体内的半衰期比较短,影响到了对血糖的持续控制效果。分别以昆系大鼠、小鼠为实验动物,进行桑叶乳汁和DNJ缓释颗粒体外、体内药物释放与降血糖效果试验,探究二者能否在临床应用提高对血糖的持续控制效果。药物释放特性试验表明,制备的DNJ缓释颗粒在体内和体外的释放速度最慢,可以维持6~8 h不被完全降解代谢;桑树乳汁也可以维持3h以上不被完全降解;而对照组的标准品DNJ仅能维持1 h不被完全降解。降血糖效果试验表明,昆系小鼠2次灌胃蔗糖后给予DNJ缓释颗粒均有明显抑制血糖升高的作用,桑树乳汁抑制小鼠血糖升高的作用也较为明显,而DNJ标准品则无明显抑制血糖升高效果。研究结果提示:DNJ缓释颗粒和桑树乳汁均可以延缓DNJ在动物体内外的释放,从而延长DNJ在体内的存留时间,起到持续抑制血糖升高的效果。

【Abstract】 1-deoxynojirimycin(DNJ) in mulberry latex belongs to potent α- glucosidase inhibitors. Because its half-life in vivo is relatively short, DNJ can affects the sustainable control effect on blood glucose results. In this experiment, we use the Kunming rats and mice as experimental animals, and do the research related to the effects of the release of mulberry latex and DNJ in vitro and in vivo and its hypoglycemic effects to explore whether two of them can be used to improve continuous control effect on blood glucose in the clinical application. The experiment of drug release properties showed that the release rate of controlled-release granules was the slowest in vivo and in vitro, and cannot be degraded entirely in 6-8h while the mulberry latex in controlled-release granules cannot be degraded entirely in 3h,and the counterpart-standards-can only controlled-release in 1h. Finally, we verified the effect of lowering blood glucose by experiments in vivo of the Kunmingmice which were given sucrose of DNJ controlled-release granule after 2 times of intragastrically administered, the results show the controlled-release granules group had significant inhibitory effect for high blood glucose after intragastric administration of sucrose, and the mulberry latex also had a obvious effect, but the standard group had no significant inhibition effect; these results indicate that both of the DNJ controlled-release granules and mulberry latex can retard DNJ released in vitro and in vivo of animals, which, extend the retention time of DNJ, provides a prolonged hypoglycemic effect.

【基金】 陕西省科技统筹创新工程计划项目(No.2014KTCL02-01);现代农业产业技术体系建设专项(No.CARS-22);西北农林科技大学推广专项(No.XTG2013-40);陕西省茧丝绸行业发展专项(No.2014-27)
  • 【会议录名称】 全国蚕桑资源多元化利用学术研讨会论文集
  • 【会议名称】全国蚕桑资源多元化利用学术研讨会
  • 【会议时间】2014-12-04
  • 【会议地点】中国浙江湖州
  • 【分类号】R285.5
  • 【主办单位】中国蚕学会、国家蚕桑产业技术体系
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