[Effect of quercetin on the acyclovir intestinal absorption].
OBJECTIVE
To study the effect of quercetin on acyclovir intestinal absorption.


METHODS
The everted gut sac and in vitro intestinal absorption tests were performed. The acyclovir transport quantity was determined by HPLC method.


RESULTS
The everted gut sac study showed that quercetin significantly inhibited the function of intestinal P-glycoprotein   P-gp  . The acyclovir transport quantities from mucosa to serosa space, which incubated with 5, 10, 80 mg/L quercetin solution or 10 mg/L verapamil solution, were increased 0.3, 0.6, 1.0 and 1.0-fold higher than acyclovir alone, respectively. The transport quantity caused by inhibition of intestinal P-gp function fitted with Boltzmann equation. The in vitro intestinal absorption test indicated that the transported acyclovir from serosa to mucosa, incubated with 2, 5, 10 mg/L quercetin solution, was significantly decreased compared with acyclovir alone.


CONCLUSIONS
Quercetin can enhance acyclovir intestinal absorption by inhibiting the function of P-gp.
Yang
Zhao-gang
ZG
Department of Pharmaceutics, Peking University School of Pharmaceutical Sciences, Beijing 100083, China.
Meng
Huan
H
Zhang
Xuan
X
Li
Xiao-dan
XD
Lv
Wan-liang
WL
Zhang
Qiang
Q
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors* / Q000502:physiology; D000212:Acyclovir / Q000493:pharmacokinetics*; D000818:Animals; D001692:Biological Transport; D002851:Chromatography, High Pressure Liquid; D007408:Intestinal Absorption / Q000187:drug effects*; D008297:Male; D011794:Quercetin / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D011794:Quercetin; D000212:Acyclovir