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Background and Objective This study has evaluated the pharmacokinetic parameters and bioavailabilities of monotropein, kae-mpferol-3-O-glucoside, and quercetin-4’-O-glucoside after administration of MOTILIPERM in rats. Material and Methods Following the administration of MOTILIPERM, the plasma concentrations of each compound in rats were simultaneously determined by using liquid chromatography tandem mass spectrometry (LC-MS/MS). Results The pharmacokinetic parameters of monotropein in rats were AUCinf 20,020.44±3944.67 and 11,915.53±1190.91 min·ng/mL and Cmax 286.99±38.37 and 56.23±9.02 ng/mL for intravenous and oral administration, respectively. The pharmacokinetic parameters of kaempferol-3-O-glucoside in rats were AUCinf 287.86±126.17 min·ng/mL and not estimated; Cmax 5.80±1.87 and 1.24±0.41 ng/mL for intravenous and oral administration, respectively. The pharmacokinetic parameters of querce-tin-4’-O-glucoside in rats were AUCinf 511.38±248.11 and 481.44±65.72 min·ng/mL; Cmax 10.72±2.70 and 2.83±0.34 ng/mL for intravenous and oral administration, respectively. Conclusion The absolute bioavailabilities of monotropein and quercetin-4’-O-glucoside for oral administration were evaluated and calculated as 3.0 and 4.7%, respectively. The absolute bioavailability of kaemp-ferol-3-O-glucoside was not calculated because the elimination rate constant could not be estimated. These results may be applied to the basic data in a further study in order to develop functional foods or herbal medicinal products.