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    The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.

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    Authors
    Chan, Kelvin C.
    Liu, Zhong Qiu
    Jiang, Zhi-Hong
    Zhou, Hua
    Wong, Yuen Fan
    Xu, Hong-Xi
    Liu, Liang
    Issue Date
    2006
    
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    Show full item record
    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.
    Citation
    Journal of ethnopharmacology, 103(3): 425-432
    Publisher
    Amsterdam: Elsevier
    Journal
    Journal of ethnopharmacology
    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
    Type
    Journal article
    Language
    en
    ISSN
    0378-8741
    ae974a485f413a2113503eed53cd6c53
    10.1016/j.jep.2005.08.020
    Scopus Count
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    Research Institute in Healthcare Science

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