ABSTRACT
OBJECTIVE:To study the absorption features of Silymarin enteric coated-polyllactic-co-glycolic acid (PLGA) nanoparticles in rat in situ intestine perfusion model and colonic adenoma Caco-2 cell model. METHODS:HPLC method was used to determine the content of silymarin. The absorption rate constant(Ka)and apparent absorption coefficient(Kapp)of Silymarin sus-pension,Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were investigated in duodenum,jejunum, ileum and colon of rat in situ intestine perfusion model;the apparent permeability coefficient (Papp) of those drugs containing low-concentration,medium-concentration and high-concentration(20,40,60 μg/mL)of silymarin in Caco-2 cell model were also investigated. RESULTS:Compared with Silymarin suspension,Ka and Kapp of Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were all increased in duodenum,jejunum,ileum and colon(P0.05). CONCLUSIONS:Silymarin enteric coated-PLGA nanoparticles can effectively increase the intestinal ab-sorption,cellular uptake and transmembrane transport rate of silymarin.
ABSTRACT
To investigate the absorption kinetics characteristics of icariin for various intestinal segments.Methods: To establish the situ intestinal perfusion model and to study the absorption of icariin for various intestinal segments.Results: Icariin was metabolized quickly in the four intestinal segments.The permeability coefficient(P*eff) were(4.27?0.28),(5.25?0.17),(1.99?0.09),(0.80?0.03) at duodenum,jejunum,ileum,colon,respectively.Icariside can be detected in the four intestine segments in rats by HPLC.Conclusion: Icariin is metabolized into icariside,and then icariside can be absorbed.