盐酸青藤碱微囊的制备及其质量评价

目的研究盐酸青藤碱微囊的制备工艺,并考察其体外释药特性。方法用复凝聚法制备盐酸青藤碱微囊,以包封率为指标,用正交试验设计法对盐酸青藤碱的制备工艺进行研究,用高效液相色谱法研究制备的微囊体外释药特性,并且对其形态、稳定性等进行研究。结果盐酸青藤碱微囊的囊心囊材比、搅拌速率及成囊温度对微囊的包封率均有显著影响,当囊心与囊材比为1∶3、搅拌速率为200 r/min、成囊温度为60℃时,制得的盐酸青藤碱微囊囊形圆整光滑,囊壁清晰,粒径均匀,平均包封率可高达85%,载药量平均为16.5%,囊径为4～12μm。结论复凝聚法制备盐酸青藤碱微囊工艺简单、可靠,产品稳定性好。微囊作为一种新兴剂型,具有一定的缓释效果。

Preparation of sinomenine hydrochloride microcapsules and its quality evaluation

Objective To study the preparation technology of sinomenine hydrochloride microcapsules,then examine their in vitro release.Methods The sinomenine hydrochloride microcapsules were prepared with the complex agglutination method.The preparation technique of sinomenine hydrochloride microcapsules was optimized by orthogonal design.In vitro release of sinomenine hydrochloride microcapsules was studied by HPLC,afterwards its morphology and stability were studied.Results The encapsulation rate was significantly related to the ratio of coating material,encapsulation temperature,and stirring speed.The highest rate of production and minimum diameter of microcapsules were obtained when the ratio of coating material to sinomenine hydrochloride was 1∶3,the temperature of encapsulation was 60 ℃,and the stirring speed was 200 r/min.The obtained microcapsules were smooth round capsule-shaped,wall clear,uniform particle size,the average encapsulation rate up to 85%,the average drug loading 16.5%,and the microcapsule diameter 4—12 μm.Conclusion Complex agglutination used to prepare sinomenine hydrochloride microcapsules is simple and reliable,and its product is stable.As a new formulation,microcapsules could provide some controlled-release effect.