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桑树乳汁中含有的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,进行桑树乳汁和DNJ缓释颗粒体外、体内药物释放与降血糖效果试验,探究二者临床应用是否具有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,DNJ可以维持6~8 h不被完全降解代谢,桑树乳汁中的DNJ也可以维持3 h以上不被完全降解,而DNJ标准品仅能维持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的效果。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。
1-deoxynojirimycin (DNJ) contained in mulberry milk belongs to the α-glucosidase inhibitor. Since DNJ has a relatively short half-life in mammals, the continuous control of blood sugar is affected. Kunming rats and mice were used as experimental animals to test the in vitro and in vivo drug release and hypoglycemic effects of mulberry milk and DNJ sustained-release granule respectively to explore whether the clinical application of the two drugs has a sustained effect on blood glucose control. The drug release characteristics test showed that DNJ sustained-release particles prepared in slow release in vitro and in vivo in vitro, DNJ can be maintained 6 ~ 8 h is not completely degraded metabolism, DNJ mulberry milk can also be maintained above 3 h is not completely degraded , While DNJ standard can only maintain 1 h is not completely degraded. Hypoglycemic effect test showed that DNK sustained-release granule was significantly inhibited by DNJ sustained-release granule after twice in Kunming mice, while the effects of mulberry milk on mice with elevated blood glucose were also obvious. However, DNJ standard No significant effect of inhibiting blood sugar. The results suggest that both DNJ sustained-release granule and mulberry milk can delay the release of DNJ in and out of animals and prolong the residence time of DNJ in vivo, and thus continue to inhibit the increase of blood glucose.