Open AccessDifference in oral absorption of ginsenoside Rg 1 between in vitro and in vivo models
Author(s) -
HAN Min,
FANG Xiaoling
Publication year - 2006
Publication title -
acta pharmacologica sinica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.514
H-Index - 90
eISSN - 1745-7254
pISSN - 1671-4083
DOI - 10.1111/j.1745-7254.2006.00303.x
Subject(s) - chemistry , bioavailability , in vivo , panax notoginseng , stomach , pharmacology , absorption (acoustics) , oral administration , small intestine , in vitro , passive transport , ginsenoside , medicine , biochemistry , membrane , pathology , biology , materials science , alternative medicine , microbiology and biotechnology , composite material , ginseng
Aim: To clarify the cause of poor oral absorption of ginsenoside Rg 1 (Rg 1 ), the active ingredient in Panax notoginseng saponins (PNS) used for treating hemorrhage. Methods: Caco‐2 cell monolayers were used as an in vitro model to study the transport mechanism of Rg 1 across the intestinal mucosa. Moreover, the serum concentration‐time profiles after peroral ( po ), intraduodenal (id), portal venous (pv) and tail venous (iv) administration of Rg 1 in rats were compared to evaluate the first‐pass effects in the stomach, intestine, and liver. Results: Up take of Rg 1 by Caco‐2 cell monolayers was temperature‐dependent, but was not influenced by cyclosporin A. The change in the apical pH produced no obvious effect on the uptake of Rg 1 . The uptake and transport of Rg1 was non‐saturable; whereas the flux from the apical compartment to the basolateral compartment (A‐B) increased in a linear manner with the increase in concentration, indicating passive transport. An apparent permeability coefficient of (2.5 9±0.17) × 10 −7 cm/s (C 0 =1 mg/mL) predicted incomplete absorption. A significant difference was ob served between the po (F po was 3.29% at a dose of 1500 mg/kg), id F id was 6.60% at a dose of 1200 mg/kg) and pv ( F PV was 50.56%) administration methods, and the barrier function of the intestine was more significant than those of the stomach and liver in the absorption process. Conclusion: Elimination in the stomach, large intestine and liver contributed to the low oral bioavailability of Rg 1 , but low membrane permeability might be a more important factor in determining the extent of absorption.