二甲双胍丝素微球的制备工艺研究

Studies on the preparation technology of Metformin Silk Fibroin Microspheres

目的以丝素蛋白为载体,二甲双胍为模型药物,制备二甲双胍丝素微球,优选最佳制备工艺。方法以液状石蜡为油相,再生丝素溶液为水相,Span 80为乳化剂,采用乳化固化法制得二甲双胍丝素微球,应用激光粒径分布仪测定微球的粒径及其分布,单因素考察影响微球载药量和包封率的因素,并进一步采用正交实验优选微球的最佳制备工艺。结果所制得的微球圆整,微球的粒径分布在4～40μm之间。对微球载药量和包封率影响较大的因素为投药比、水油比和转速,最佳工艺条件是:投药比为7%、转速为300 rpm、水油比为11∶100,载药量可达5.8%。结论该二甲双胍丝素微球制备方法简单,无有毒有害物质加入,可在常温常压下制备,易于扩大生产。

Objective Silk fibroin（SF）as drug carrier and metformin as a model drug,to prepare metformin silk fibroin microspheres, and optimize the optimal conditions of preparation technology. Methods Liquid paraffin as oil phase,regenera- ted silk fibroin solution as water phase, Span 80 as oil soluble emulsifier,metformin SF microspheres were prepared by emul- sion solidification method,the particle diameter and its distribution were measured by Laser particle sizer, the factors that af- fected drug loading and entrapment efficiency were investigated by single factor test, then the optimal preparation technology was optimized by orthogonal test. Results The microspheres were spherical in shape, and microsphere diameters were on the order of 4 - 40 txm. The factors that greatly affected the drug loading and entrapment efficiency were the mass ratio （ metform- in/SFI ,water/oil phase ratio and rotation speed. The optimal preparation technology was obtained：the rotation speed was 300 rpm,the mass ratio was 7 % ,water/oil phase ratio was 11：100, the drug loading up to 5.8%. Conclusion This method of preparing metformin SF microsphere was simple, no potentially toxic agents, and silk fibroin microspheres could be prepared at normal temperature and pressure,and it＇s easy to expand production.