Stauntonia hexaphylla leaf extract (YRA-1909), which is widely used for the antirheumatic\nproperties, has been under phase 2 clinical trials in patients with rheumatoid arthritis since April 2017.\nLiquid chromatography-tandem mass spectrometric method while using liquidâ??liquid extraction\nwith ethyl acetate was validated for the simultaneous determination of the major active components\nof YRA-1909, including chlorogenic acid (CGA), neochlorogenic acid (NCGA), cryptochlorogenic acid\n(CCGA), and their metabolites (i.e., caffeic acid (CA), caffeic acid 3-O-glucuronide (CA-3-G), caffeic\nacid 4-O-glucuronide (CA-4-G), and ferulic acid (FA)) in rat plasma and applied to a pharmacokinetic\nstudy of YRA-1909 in rats. Seven analytes were separated on Halo C18 while using gradient\nelution of formic acid and methanol, and then quantified in selected reaction monitoring mode\nwhle using negative electrospray ionization. Following oral administration of YRA-1909 at doses\nof 25, 50, and 100 mg/kg to male Sprague-Dawley rats, CGA, NCGA, and CCGA were rapidly\nabsorbed and metabolized to CA, CA-3-G, and CA-4-G. The area under the plasma concentration-time\ncurve (AUClast) of CGA, NCGA, CCGA, and three metabolites linearly increased as the YRA-1909\ndose increased. Other pharmacokinetic parameters were comparable among three doses studied.\nAUClast values for CA, CA-3-G, and CA-4-G exceeded those for CGA, NCGA, and CCGA.
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