目的通过对比壳聚糖游离膜在不同酶液中的降解性能,筛选适宜于壳聚糖包衣结肠定位制剂体外的溶出介质。方法将壳聚糖制备成游离膜,以膜消化率、易碎性为评价指标,对其在复合果胶酶、进口果胶酶、胰酶、β-葡萄糖苷酶、大鼠结肠内容物等中的降解进行考察,并采用电镜扫描技术对变异性较大的膜表面性状进行观察,最终确定对壳聚糖降解最敏感酶液。结果大鼠结肠内容物、复合果胶酶、进口果胶酶对壳聚糖游离膜均有不同程度的降解,其中大鼠结肠内容物降解性能最强,游离膜在该介质中24h后成碎片,且膜表面最为粗糙;而游离膜对β-葡萄糖苷酶和胰酶不敏感。结论通过游离膜降解试验,明确了壳聚糖的敏感酶类,为结肠定位制剂体外溶出介质的选择提供了科学的依据。

Objective Through comparing the degradation property of chitosan free-film in different dissolution media to screen dissolution media in vitro suitable for colon-specific delivery formulation by chitosan-coating.Methods Preparing the chitosan into free-film and taking the digestibility and fragmentation as indices,the degradation of free-film in domestic compound pectinase,imported pectinase,pancreatin,β-glucosidase,and rat colon contents were investigated.Aslo by electron microscopic observation to study film surface character on the great degrees of variation and finally determine the most sensitive enzyme solution.Results Domestic compound pectinase,imported pectinase,and rat colon contents could degrade chitosan free-film in different degrees,where the rat colon contents was the most in which the free-film could be degraded into small pieces after 24 h and the surface was the most roughening,while the free film was not sensitive in pancreatin and β-glucosidase.Conclusion By the degradation experiment of free-film,the sensitive enzyme on chitosan could be made clear by strong pertinency so as to provide the scientific basis for the selection of dissolution media in vitro on colon-specific delivery formulation.

国家科技支撑计划项目(2006BA09B08-14);四川省中医药管理局专项资助项目(200615)