RESUMEN
<p><b>OBJECTIVE</b>To study the effects of different penetration enhancers on the transcutaneous permeability of lappaconitine gel in vitro and therefore to screen out the effective accelerator to enhance the permeation rate of lappaconitine.</p><p><b>METHOD</b>Using improved Franz-type diffusion cell and excised big mouse skin in vitro as transdermal barrier, the kinetics parameters such as cumulative permeation quantity, permeation rate and permeation lagged time were determined by HPLC. The enhancement ability of four different enhancers such as azone (Azone), propylene glycol (PG), oleic acid (OA) and lauryl alcohol (LA), was investigated when used either uniquely or combinatively each other at random.</p><p><b>RESULT</b>When used combinatively, Azone + PG, LA + PG, OA + PG can enhance the cumulative permeation quantity, OA + PG was the best one among them.</p><p><b>CONCLUSION</b>The selection of the best penetration enhancers provided reference for lappaconitine transdermal delivery.</p>
Asunto(s)
Animales , Femenino , Masculino , Ratas , Aconitina , Farmacocinética , Administración Cutánea , Analgésicos no Narcóticos , Farmacocinética , Azepinas , Farmacología , Dodecanol , Farmacología , Combinación de Medicamentos , Sinergismo Farmacológico , Técnicas In Vitro , Ácido Oléico , Farmacología , Propilenglicol , Farmacología , Ratas Sprague-Dawley , Absorción CutáneaRESUMEN
<p><b>AIM</b>To investigate the tissue distribution and pharmacokinetics of oridonin-solid lipid nanoparticles in animals.</p><p><b>METHODS</b>HPLC method was established to determine the concentration of oridonin in serum of rabbits and in different tissues of mice. The results after tail iv administration of oridonin and oridonin solid lipid nanoparticles were compared.</p><p><b>RESULTS</b>The relative tissue content of oridonin of solid lipid nanoparticles in the liver, spleen, lung, heart and kidney were 4.25%, 3.44%, 1.19%, 0.52% and 0.60%, respectively. The concentration-time curves of oridonin and oridonin solid lipid nanoparticles were both fitted to the three-compartment model. T(1/2)pi = 0.087 h, T(1/2)alpha = 1.65 h, T(1/2)beta = 32.36 h, V(C) = 0.66 mL.kg(-1).</p><p><b>CONCLUSION</b>Solid lipid nanoparticles could increase the hepatic and lienic targeting efficiency of oridonin in mice and improve its bioavailability. Solid lipid nanoparticles were helpful for oridonin to reach a long circulation time and were hopeful to be its novel drug carrier.</p>