[Absorption of extractive Radix Paeoniae Alba in rat everted gut sacs and its interaction with P-glycoprotein].
OBJECTIVE
To research the intestinal absorption characteristics of paeoniflorin in extractive Radix Paeoniae Alba in the different intestinal segment, and the interaction with P-glycoprotein.


METHODS
Paeoniflorin, a representative component in extractive Radix Paeoniae Alba, on the intestinal absorption was studied in vitro using everted gut sacs model and detected by HPLC method. The absorption characteristics was evaluated by the absorption parameter.


RESULTS
The absorption of paeoniflorin was linearity at different intestine segment and dose, and the square of regrees correlation coefficient exceed 0.9 (R2 > 0.9), which consistent with zero order rate process. The Kalpha of paeoniflorin showed a dose-dependent increase along with the raised dose of extractive Radix Paeoniae Alba, indicated it was a mechanism of passive absorption. The absorption rate was jejunum > ileum > colon. Verapamil (100 micromol x L(-1)), a inhibitor of the P-glycoprotein, can remarkable increase the absorption of the paeoniflorin in ileum (P < 0.05). After administer the extractive Radix Paeoniae Alba for 5 days, the extraction of Rho123 is significantly increase in ileum (P < 0.01).


CONCLUSIONS
The intestinal absorption of paeoniflorin is zero order rate process and passive absorption. Paeoniflorin is a substrate of P-glycoprotein, and extractive Radix Paeoniae Alba could induce the expression of the P-glycoprotein.
Dong
Yu
Y
Institute of Chinese Materia Medica, Guang'anmen Hospital, Beijing 100053, China.
Zhang
Yingfeng
Y
Yang
Qing
Q
Li
Yujie
Y
Zhu
Xiaoxin
X
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000818:Animals; D001565:Benzoates / Q000302:isolation & purification / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D001952:Bridged-Ring Compounds / Q000302:isolation & purification / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000302:isolation & purification / Q000378:metabolism* / Q000493:pharmacokinetics* / Q000494:pharmacology; D041981:Gastrointestinal Tract / Q000187:drug effects* / Q000378:metabolism*; D005960:Glucosides / Q000302:isolation & purification / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D039821:Monoterpenes; D029596:Paeonia / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D014700:Verapamil / Q000494:pharmacology; D006027:Glycosides
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D001565:Benzoates; D001952:Bridged-Ring Compounds; D004365:Drugs, Chinese Herbal; D005960:Glucosides; D039821:Monoterpenes; D014700:Verapamil; C015423:peoniflorin; D006027:Glycosides