Intestinal absorption of three alkaloids in Plumula Nelumbinis by rat single-pass perfusion in situ model / 中国药学杂志

ABSTRACT

OBJECTIVE: To investigate the intestinal absorption behaviors of three main active components, liensinine, isoliensinine and neferine in Plumula Nelumbinis extracts in intestine of rats. METHODS: With phenol red as the indicator, in situ single pass intestinal perfusion (SPIP) model was used and the concentrations of the alkaloids in perfusion solution in different intestinal segments (duodenum, jejunum, ileum, and colon) were determined by HPLC. RESULTS: Liensinine, isoliensinine and neferine were absorbed in whole intestinal segments with saturation phenomena. The absorption rate constant (Ka) and/or effective permeability values (Peff) of the three alkaloids mostly had significant difference (P<0.05) at middle and high concentrations of perfusion solution vs those at low concentrations. Liensinine, isoliensinine and neferine possessed better absorption in ileum and colon of intestine. The absorption in duodenum and jejunum mostly displayed no significant difference (P≤0.05). In middle concentration group (117.3 μg·mL-1), neferine was absorbed best among the three alkaloids in colon; in other intestinal sections, the Kd and Peff of the three alkaloids were sequenced as follows neferine ≤ liensinine ≤ isoliensinine. CONCLUSION: The transport mechanism of liensinine, isoliensinine and neferine in vivo may be active transport or facilitated diffusion.