目的制备盐酸青藤碱传递体,并进行质量评价。方法以盐酸青藤碱的包封率为指标,比较了薄膜分散法、逆相蒸发法和乙醇注入法制备的盐酸青藤碱传递体。采用均匀设计筛选逆相蒸发法制备盐酸青藤碱传递体的最佳处方,并对传递体的粒径、形态、电位和稳定性进行评价。结果逆相蒸发法制备的传递体的包封率最高。均匀设计筛选逆相蒸发法的最佳处方为:大豆磷脂与胆酸钠的质量比为200/30mg/mg,氯仿与PBS的体积比为5mL/mL,PBS的pH值为6.5,盐酸青藤碱的加入量为10mg。制得的盐酸青藤碱传递体为乳白色半透明混悬液,平均包封率为62.2%。在电镜下观察其外形呈较规则的球形或类球形,光滑且不黏连,平均粒径为96.4nm,Zeta电位为-35.93mV,于4℃下放置30d,未产生聚积或沉淀。结论盐酸青藤碱传递体的制备工艺可行,所得产品稳定,为盐酸青藤碱的临床给药提供一种新的给药系统。

Objective To prepare sinomenine hydrochloride transfersomes and evaluate their qualities.Methods Three different preparation Methodsincluding film dispersion,reverse phase evaporation,and ethanol injection Methods were compared according tO the encapsulation efficiency of transfersomes.Uniform design was applied to optimize the formulation and pharmaceutical process of reverse phase evaporation.The particle size,the appearance,the Z-potential,and the stability were also evaluated.Results The transfersomes prepared by reverse-phase evaporation method possessed the highest encap sulation efficiency.The ideal combinations of preparation and formulation were:soya lecithin/sodium cholate was 200/30 mg/mg,chloroform/PBS was 5 mL/mL,pH of PBS was 6.5,added sinomenine hydrochloride was 1 0 mg.The transfersomes obtained were milky white translucent suspension,with a mean encapsulation efficiency of 62.2% .The shape of their particles was spherical or similar to spherical under microscope,which was smooth and disconglutinated with an average diameter of 96.4 nm,and a Z-potential of-35.93 mV.Aggregation or deposition was not observed after exposure under the temperature of 4℃for 30 d.Conclusion The preparation process of sinomenine hydrochloride transfersomes is feasible,the quality of obtained transfersomes is stable.It is expected to provide a new preparation for clinical use of sinomenine hydroehloride.

湖南省教育厅资助项目(06c498)