多潘立酮-卡波姆胃内黏附微丸的制备及体外评价

Preparation of domperidone-carbopol gastric mucoadhesive pellets and in vitro evaluation

为制备多潘立酮胃内黏附型缓释微丸,并对其体外释放行为及体外的黏附性能进行考察,以卡波姆、羟丙基纤维素和PVP为主要黏附材料,以30%(质量分数)的NaCl水溶液作为润湿剂制备软材,采用挤出-滚圆法制备微丸。以释放度和体外的黏附性为评价指标,采用正交设计,优选出最佳处方,并进行最佳处方的验证,卡波姆、羟丙基纤维素及PVP的质量比为80∶80∶15。体外实验数据表明,多潘立酮胃内黏附型缓释微丸具有较好的黏附和缓释效果。本研究处方工艺简便,重现性良好,适合工业化生产。

To prepare gastric mucoadhesive pellets of domperidone and study the release behaviour and adhesive in vitro,carbopol,hydroxypropyl cellulose（HPC） and PVP are used as the main adhesive materials,30% NaCl（mass ratio） solution is used to be a wetting agent of soft wood,and extrusion-spheronization method is used to prepare pellets.Taking adhesion in vitro and sustained release behavior of the pellets as indicators,through orthogonal design,we optimized and verified the best prescription.The mass ratio of carbopol,hydroxypropyl cellulose（HPC） and PVP is 80∶80∶15.In vitro test data show that domperidone adhesion sustained-release pellets have good adhesion and release effect.The formulation and process developed in the study is convenient,repeatable and suitable for mass production.