摘要
目的研制索拉非尼半乳糖神经酰胺固体脂质纳米粒(S-GC-SLN)混悬液。方法采用乳化蒸发-低温固化法制备S-GC-SLN,正交试验法优选处方,透射电镜观察形态,激光粒度测定仪测定粒径、多分散指数及Zeta电位,采用葡聚糖凝胶柱层析法与HPLC法测定包封率。结果优选处方为:索拉非尼15mg、半乳糖神经酰胺250 mg、泊洛沙姆188 350 mg、蛋黄卵磷脂450 mg。所制脂质纳米粒子为类球形实体,粒径为(186.6±2.6)nm,Zeta电位为(-46.1±2.9)mV,包封率为(83.47±1.54)%。结论乳化蒸发-低温固化法制备S-GC-SLN可行,为开发索拉非尼新制剂提供了实验依据。
Objective To prepare sorafenib galactosyceramide solid lipid nanoparticle （S-GC-SLN） suspension. Methods S-GC-SLN was prepared by emulsion evaporation-solidification at low temperature. The prescription was optimized by orthogonal test. The morphology was observed by transmission electronic microscope. The particle size, Zeta potential and polydispersity index were determined by laser granularity equipment. The encapsulation efficiency was detected by Sephadex gel chromatography and HPLC. Results The optimized prescription was as follows： 15 mg of sorafenib ,250 mg of galactosyceramide ,350 mg of poloxamer and 450 mg of egg phophatidylcholine. The S-GC-SLN was spherical shape and its size, Zeta potential and encapsulation efficiency were （ 186.6 ＋ 2.6 ） nm, （ - 46.1 _＋ 2.9） mV and （ 83.47 _＋ 1.54） %, respectively. Conclusion The emulsion evaporation-solidification at low temperature was rational. It provided experimental evidence for developing a new sorafenib preparation.
出处
《广东药学院学报》
CAS
2013年第5期474-478,共5页
Academic Journal of Guangdong College of Pharmacy
基金
湖北省科技计划软科学研究专项项目(2012FKB04439)
