Preparation Of Sodium New Houttuyfonate Microsphere And Preliminary Targeting Study In Mice

Objective:By controlling materials and other factors of preparation process,we in order to weaken or eliminate the adverse reaction of Sodium New Houttuyfonate;with controlling the particle size of microspheres, to reach the passive targeting effects to lung,play a better pharmacodynamics .Methods:To prepare Sodium New Houttuyfonate poly(lactic-co-glycolic acid) microspheres by solvent evaporation, and research its preparation; Establish quality control and standards of microspheres,and determinate it's drug loading and entrapment efficiency;microspheres' physical morphology and properties of powders are investigated;we study the in vitro release of microspheres with dynamic dialysis;and learn preliminary stability;by targeting experiments in mice tissues and organs,study its distribution and targeting effect.Results:We got the best prescription is: PLGA type 75:25, dosage ratio (SNH: PLGA) 1:10,oil phase volume ratio 1:20.The average drug loading of SNH-PLGA-MS is 8.31%,and the average encapsulation efficiency is 89.297%.Its surface rake 31.23°,angle of repose 26.83°,graduated bulk density of 0.475g ? mL-1,the arithmetic average particle size is 10.736μm;SNH-PLGA-MS meet the two-phase micro-vitro release kinetic equation in vitro release, SNH in vitro release with A kinetic equation.The microspheres used to low temperature (4℃) and room temperature (20-30℃) conditions;light had no significant effect on the stability of microspheres,the microspheres were not changed significantly with 60Co irradiation sterilization.It show that the microspheres distributed mainly in the lung in mice.Conclusion:Optimization of preparation technology,the encapsulation ratio of microsphere we prepared up to Pharmacopoeia standards,stability is good,with significant lung targeting.