大蒜素肠溶微囊的制备及其性质研究

Preparation of diallyl trisulfide enteric microcapsules and study on its characteristics

目的以肠溶材料聚丙烯酸树脂Ⅱ为囊材制备大蒜素微囊。方法采用单凝聚法制备大蒜素肠溶微囊并研究其粒径、载药量、包封率、体外释药等性质。结果经优化制得的大蒜素肠溶微囊为类圆球形颗粒,平均粒径为52.2μm,平均载药量28.97%,包封率80.74%,体外释放符合肠溶制剂的标准,对大鼠的胃黏膜几乎无刺激。在4.5×103lx照射,60℃高温及相对湿度90%条件下放置10 d,微囊的粒径分布和剩余药量无显著变化。结论制备工艺简单,所制得的大蒜素微囊具有肠溶特性。

OBJECTIVE To explore the process for preparing the diallyl trisulfide loaded microcapsules using the enteric material Eudragit L100 -55. METHODS The diallyl trisulfide enteric microcapsules were prepared by simple coacervation method. Diameter, durg loading and encapsulation efficiency and some other properties were investigated. RESULTS The diallyl trisulfide loaded microcapsules were sphere like with the mean size of 52. 2 μm, the drug loading was 28.97% and the encapsulation efficiency was 80. 74% prepared based on the optimized formulation. In vitro drug release behavior fitted to the standard of enteric preparation. And there was almost no stimulus on rat gastric mucosa. The size distribution and residual drug contents of the product, which were stored at 4500 lx, high temperature（60℃ ） and high relative humidity （90%） conditions respectively for 10 d, had no significant changes. CONCLUSION This preparation procedure is simple and the diallyl trisulfide microcapsules posses enteric characteristics.