Preparation of Poly( lactide-co-glycolide)Microspheres Containing Total Alkaloids of Panzeria alaschanica / 中国药房

ABSTRACT

OBJECTIVE:To optimize the formulation and technology of poly(lactide-co-glycolide)(PLGA)microspheres con-taining total alkaloids of Panzeria alaschanica,and to prepare microspheres and conduct quality investigation. METHODS:PLGA microspheres containing total alkaloids of P. alaschanica (PTPM) was prepared by double emulsion-solvent evaporation method. The formulation of microspheres was optimized by L9(34) orthogonal design using mass concentration of PLGA,PVA concentra-tion,ratio of water phase to oil phase as factor,drug-loading amount,encapsulation efficiency,yield as index. The morphology, particle size and drug release of microspheres were all investigated. RESULTS:The optimal formulation was as follows as the mass concentration of PLGA 200 mg/ml,the concentration of PVA 2%,and the water phase-oil phase ratio 15. In validation test,aver-age encapsulation efficiency was(83.2±2.4)%,average drug-loading amount(4.16±0.17)%,average yield(86.7±3.6)%,and comprehensive score (95.7 ± 4.4)%;all RSDs were lower than 5.0%(n=3). Prepared microspheres were spherical with smooth surface and uniform particle size. The average particle size was(22.3±2.4)μm and accumulative release rate of 24 h was(82.3± 3.5)%,which conformed to first-order release model(r=0.972 4). CONCLUSIONS:Optimized technology is stable. Prepared mi-crospheres show good sustained-release property,and fit to quality requirements.