壳聚糖游离膜在不同溶出介质中的降解性能研究

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24 h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.

Degradation property of chitosan free-film in different dissolution media

Objective Through comparing the degradation property of chitosan free-film in differerent dissolution media to screen dissolution media in vitro suitable for colon-specific delivery formulation by chi-tosan-coating. Methods Preparing the chitosan into free-film and taking the digestibility and fragmenta-tion as indices, the degradation of free-film in domestic compound pectinase, imported pectinase, panerea-tin, β-glueosidase, 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 en-zyme solution. Results Domestic compound pectinase, imported peetinase, 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.