褪黑激素鼻腔给药淀粉微球的制备工艺

Studies on the preparing technique of melatonin starch microspheres for intranasal administration

目的研究褪黑激素鼻黏膜给药淀粉微球的制备工艺。方法以可溶性淀粉为载体材料 ,环己烷为油相 ,司盘 80为乳化剂 ,对苯二甲酰氯为交联剂 ,采用均匀设计法优化了空白淀粉微球的制备工艺 ,用包埋法制备了含药微球 ,考查了投药量与载药量、包封率之间的关系。并对含药微球的相关性质、体外释药及稳定性作了进一步研究。结果所得淀粉微球形态圆整 ,粒径分布在 30～6 0 μm之间 ,体外释放符合一级动力学方程 ,并具有明显的缓释作用。

Objective To investigate the preparing technique of melatonin starch microspheres for intranasal administration.Methods Using soluble starch as a carrier material,cyclohexane as the oil phase,Span-80 as an emulsifier,and paraphthaloyl chloride as a crosslinker,an uniform design method was employed to optimize the preparation process of the blank microspheres.Subsequently,melatonin starch microspheres were prepared by the embedding method and the relationship between the encapsulated drug and drug embedding ratio,as well as the encapsulated drug and drug loading ratio were investigated.Additionally,the morphology,size and size distribution of the microspheres were characterized by scanning an electron microscope and an optical microscope,respectively.In vitro drug release and the stability of the microspheres were further studied.Results The microspheres were of a spherical shape with some visible cracks on the surface.The particle size was in the range of 30～ 60 μm,an a optimal value for intranasal administration.Melatonin was released from the microspheres in a sustained manner and the release profile could be described with the first-order kinetics equation.Conclusions The optimized technique could be used to prepare melatonin starch microspheres for intranasal administration.