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
Objective: To investigate the intestinal absorption of silybin-phospholipid complex by the whole and different segments of rat's intestine. Methods: An in situ intestinal perfusion model was employed in the present research; and absorption percent and intestinal wall permeability coefficient (Ke) were taken as indices. HPLC method was used to determine the concentrations of silybin and phenol red in the perfusate to calculate the absorption indices. Results: The absorption of silybinphospholipid complex was a first-order process, about 70% of it was absorbed after 6 h, with the absorption rate constants(Ka) being (0.193 ± 0.012) h-1. The absorption rate and Ke for silybin-phospholipid complex were similar between different intestinal segments (Duodenum, Jejunum, Ileum, and Colon) (P>0.05). Conclusion, Silybin-phospholipid complex can be absorbed in the whole intestinal segments.
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.
