Microdialysis, a sampling method for pharmacokineticsââ?¬â??pharmacodynamics (PKââ?¬â??PD)\nmodeling in preclinical and clinical studies, is a convenient in vivo sampling technique. Geniposide\n(GE), an iridoid glycoside compound, is the major active ingredient of Gardenia jasminoides Ellis fruit\nwhich has an anti-inflammatory effect. In this study, an articular cavity microdialysis sampling system\nfor adjuvant arthritic (AA) rats was established to study the effect of GE on the release of prostaglandin\nE2 (PGE2) in AA rats induced by Freundââ?¬â?¢s complete adjuvant (FCA). An UHPLC-MS/MS method\nwas developed to determine the concentrations of GE and PGE2 in the dialysate. Through the\ndetermination of drug concentrations and PGE2 efficacy levels in the dialysate, the developed\nmethods were successfully applied to set up concentrationââ?¬â??time and effectââ?¬â??time profiles followed\nby PKââ?¬â??PD modeling of GEââ?¬â?¢s effect on decreasing PGE2 release after oral administration of GE.\nThe effect was well described by the developed PKââ?¬â??PD modeling, indicating that GE may play an\nanti-inflammatory role via decreasing AA-induced elevated PGE2 levels. In the selection of suitable\nendogenous small molecules as effect markers, the establishment of AA rat joint-cavity microdialysis\nis an attractive technique for rational PKââ?¬â??PD studies.
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