Study on intestinal absorption mechanism and kinetics of dauricine in rats with in situ single-pass perfusion model / 中国药学杂志

ABSTRACT

OBJECTIVE: To investigate the absorption characteristics of dauricine in rat intestine. METHODS: In situ single-pass perfusion model was used and the concentrations of dauricine in perfusate were determined by HPLC. The effects of perfusion rates, intestinal segments and drug concentrations on the intestinal absorption of dauricine were studied. RESULTS: The absorption rate and absorption degree of dauricine increased with the perfusion rates(0.1, 0.2 and 0.4 mL · min-1)(P0.05); at high, middle and low concentrations, the drug absorption rate constants(Ka) were (2.36±0.0073) × 10-2, (3.73 ± 0.0052) × 10-2 and(5.62 ± 0.0136) × 10-2 min-1, respectively, the apparent permeation coefficients(P.,) were(2.02±0.0002) × 103, (3.10±0.0007) × 10-3 and (5.31±0.0010) × 10-3 cm · min-1, respectively, the absorption percentages(P%) were 8.66%, 10.17% and 19.06%, respectively, and the accumulate absorption amount and accumulate absorption percentages of different concentrations at different time were very low. CONCLUSION: The absorption degree of dauricine increases with perfusion rates; there is no specific absorption site in the whole rat intestinal tract; the absorption of dauricine is very poor and the active transport is involved in the absorption mechanism of dauricine.