Study On The Solubilization Of Lappaconitine Drug And Construct A Sustained Release System

To improve the solubility of Lappaconitine (LA) and give it a sustained release effect, inclusion and microspheres technology was used and inclusion compound of lappaconitine-β-CDPH (LA-β-CDPH), microspheres of lappaconitine-p-cyclodextrin (LA-β-CDP) was prepared in this study. Inclusion compound and blank microspheres was characterized, also, the performance was studied. At the same time Drug content percency, Drug entrapment efficiency were investigated, the lappaconitine-β-cyclodextrin polymer microspheres preparation technology of infusion method was optimized through orthogonal experiment. The physiological parameters of stomach, small intestine and blood pH value were mimicked to plot the in vitro release of inclusion compound and microspheres of lappaconitine-β-cyclodextrin (LA-β-CDP), separately, the releasing mechanism of la from the microsphere and inclusion compounds was established by equation fitting of releasing kinetic model. The inclusion compound was obtained, the molecular ratio of lappaconitine to β-CDPH was1:1with a mean drug content of (27±1.1)%. The solubility increases by1.5、3.9times after LA is included with p-CDPH compared to β-CD、β-CDPL, arriving at11978mg/L. After inclusion, lappaconitine-β-CDPH had a sustained release effect on LA, achieving8h. and the water solubility were significantly improved, the appropriate condition a for preparing blank microspheres are the concentration of dissolvent alcohol is70%, the temperature of Microspheres is45℃the mass ratio between Microspheres and lappaconitine is1:1, and the time is45h, with a mean drug content of (17±1.1)%. Simultaneously, LA-β-CDPM had a sustained release effect on LA, achieving20h. Kinetics equation curve fitting of zero order release equation and Ritger-Peppas equation.The technique of preparing lappaconitine-β-CDP inclusion compound and microspheres of lappaconitine-β-cyclodextrin (LA-β-CDPM) was simple, inclusion compound could increase solubility and microspheres significantly improved sustained releas effect.