Abstract: The absorption and metabolism of a 1-deoxynojirimycin and hydroxychalcone heterocomplex (DC-5) as a novel potent α-glucosidase inhibitor was investigated in rats. A total of four metabolites derived from DC-5 were identified in the blood of rats gavaged with DC-5 using ultra-performance liquid chromatography quadrupole time-of-flight tandem mass micrometry (UPLC-Q-TOF-MS/MS), including hydrogenated, methylated, sulfonated, and glucuronidated metabolites of DC-5. The concentration of DC-5 in the blood, heart, liver, lung, stomach and small intestine all peaked at 0.5 h after oral administration, while the peak concentration appeared at 1 h in the spleen and kidney. The peak concentration of DC-5 in the blood was 162.76 ng/mL, with a half-life in the terminal phase (T1/2) of 30.66 h and mean residence time (MRT) of 11.41 h. DC-5 was mainly excreted via feces, and a total of 2.26% of the intragastrical DC-5 was found in feces, which was significantly higher than that in urine (0.015 6%). The results of pharmacokinetics test showed that the bioavailability of DC-5 in rats was 1.47%.

Key words: α-glucosidase inhibitor; metabolism; absorption; bioavailability