水蛭抗凝活性组分黏附微丸的制备及体外释放行为考察

Preparation of adhesive pellets of effective anticoagulant components from hirudio and their in vitro release

目的:研究水蛭抗凝活性组分黏附微丸的制备方法,并对其体外黏附性及释放行为进行考察,为水蛭抗凝活性组分口服制剂的研究与开发提供实验依据。方法:以微晶纤维素、乳糖为填充剂,利用挤出滚圆机制备含药微丸;外层通过包衣锅包裹10%羟丙甲纤维素(K15M)制备黏附层;采用离体黏附模型及二喹啉甲酸(BCA)法测定黏附微丸的黏附性及溶出度。结果:所制备的水蛭抗凝活性组分黏附微丸圆整度好,大小均匀,黏附百分率(B%)为(89.58±2.73)%,体外溶出符合规定。结论:该工艺切实可行,制得黏附微丸黏附力适中,溶出效果理想,可提高药物在胃肠道内的滞留时间,有效提高药物的生物利用度。

Objective： To prepare adhesive pellets of effective anticoagulant components from hirudio,and investigate in vitro release characters and adhesiveness of the pellets,providing the experiment basis for the study and development of the oral preparation.Methods： Micro-crystalline cellulose and lactose were used as the bulking agents,and the medicated pellets were prepared by spheronization of extruded masses.The outer adhesive spheres were prepared by using coated pot with 10 percent HPMC（K15M）.The BCA method and in vitro adhesive analogue were adopted to determine release behavior of the adhesive pellets and their adhesiveness.Results： The adhesive percentage of the prepared pellets was（89.58±2.73）% with good spherical degree and homogeneity.The release behavior of the adhesive pellets accorded with designed regulation.Conclusion： The adhesive pellets produced by this method have a perfect adhesiveness and good release behavior,which could improve the residence time in gastrointestinal tract and increase bioavailability.