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Wolverhampton Intellectual Repository and E-Theses > Research Institutes > Research Institute in Healthcare Science > Pharmacy and Natural Products Research Group > The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.

Please use this identifier to cite or link to this item: http://hdl.handle.net/2436/29756
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Title: The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.
Authors: Chan, Kelvin C.
Liu, Zhong Qiu
Jiang, Zhi-Hong
Zhou, Hua
Wong, Yuen Fan
Xu, Hong-Xi
Liu, Liang
Citation: Journal of ethnopharmacology, 103(3): 425-432
Publisher: Amsterdam: Elsevier
Journal: Journal of ethnopharmacology
Issue Date: 2006
URI: http://hdl.handle.net/2436/29756
DOI: 10.1016/j.jep.2005.08.020
PubMed ID: 16169700
Additional Links: http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6T8D-4H4T0VC-7&_user=10&_rdoc=1&_fmt=&_orig=search&_sort=d&view=c&_acct=C000050221&_version=1&_urlVersion=0&_userid=10&md5=ba0973ce6bf98e3cac6f31b3e4fb9a4d
Abstract: Paeoniflorin and sinomenine, derived from the root of Paeonia lactiflora Pall. (family Ranunculaceae) and the stem of Sinomenium acutum Rehder & Wilson (family Menispermaceae), respectively, have been, and are currently, widely used for treatment of rheumatic and arthritic diseases in China and Japan. Our previous studies demonstrated that sinomenine could significantly improve the bioavailability of paeoniflorin in rats, but the underlying mechanisms remain unknown. The present study aims to investigate the intestinal kinetic absorptive characteristics of paeoniflorin as well as the absorptive behavior influenced by co-administration of sinomenine using an in vitro everted rat gut sac model. The results showed a good linear correlation between the paeoniflorin absorption in sac contents and the incubation time from 0 to 90 min. However, the concentration dependence showed that a non-linear correlation exists between the paeoniflorin absorption and its concentrations from 10 to 160 microM, and the absorption was saturated at about 80 microM of the drug. Sinomenine at 16 and 136 microM concentrations could significantly enhance the absorption of paeoniflorin (20 microM) by 1.5- and 2.5-fold, respectively. Moreover, two well-known P-glycoprotein inhibitors, verapamil and quinidine, could significantly elevate the absorption of paeoniflorin by 2.1- and 1.5-fold, respectively. Furthermore, sinomenine in a pattern, which influenced paeoniflorin's absorption, manifested as similar to that of P-glycoprotein inhibitors. In conclusion, sinomenine significantly enhance the intestinal absorption of paeoniflorin, subsequently improve the bioavailability of paeoniflorin. The mechanism underlying the improvement of paeoniflorin's bioavailability was proposed that sinomenine could decrease the efflux transport of paeoniflorin by P-glycoprotein.
Type: Article
Language: en
Keywords: Paeoniflorin
Sinomenine
Pharmacokinetics
Bioavailability
Herbal medicine
Chinese medicine
Traditional Chinese medicine
Chinese herbs
Medicine, Chinese Traditional
MeSH: Animals
Anti-Inflammatory Agents
Benzoic Acids
Bridged Compounds
Digoxin
Dose-Response Relationship, Drug
Drugs, Chinese Herbal
Glucosides
Intestinal Absorption
Intestines
Male
Models, Animal
Morphinans
P-Glycoprotein
Paeonia
Quinidine
Rats
Rats, Sprague-Dawley
Sinomenium
Time Factors
Verapamil
ISSN: 0378-8741
Appears in Collections: Pharmacy and Natural Products Research Group

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