Pharmacokinetic studies in healthy humans show that oral vildagliptin is rapidly absorbed with a bioavailability of approximately 85. The peak time is 1-2 hours after administration, the plasma half-life is 1.5-4.5 hours, and the protein binding rate is low (4-17). Its in vivo process has linear pharmacokinetic characteristics, no drug accumulation occurs after multiple oral administrations, and its pharmacokinetic parameters are not affected by food.
Vildagliptin has many metabolic pathways. Most of the drugs (55) are inactivated through liver hydrolysis (cyanohydrolysis), and the main metabolite LAY151 has no pharmacological activity. A small portion of the parent drug is metabolized by the CYP450 enzyme system. Vildagliptin is mainly excreted through urine, and urine contains 18-22 prototype drugs.
A single dose of vildagliptin (25-200mg) can quickly inhibit DPP in plasma. 4 activity, it can inhibit the activity of 90DPP4 in 30-60 minutes. The duration of DPP-4 inhibition is dose-dependent. After oral administration of 50 mg and loom mg of vildagliptin, the inhibition of DPP4 activity can reach 70 and 90% respectively within 12 hours; oral administration of 100 mg of vildagliptin can still inhibit 40% of DPP4 activity in 24 hours. No dose adjustment is required for vildagliptin in patients with abnormal hepatic function.