Assessment of Pharmacokinetics and Bioequivalence of Metoclopramide in Healthy Volunteers

[Objective]To study the pharmacokinetics parameters and bioavailability of metoclopramide tablets. [Methods]A cross-over, randomized study was performed in 24 healthy male volunteers receiving a single oral dose of 2×10 mg of the tested or the referenced metoclopramide tablets. A sensitive and specific HPLC-MS method was developed to measure the concentration of metoclopramide in plasma. The pharmacokinetics parameters were analyzed by two one-side t test to determine the bioequivalence of the two preparations. [Results]The main pharmacokinetics parameters AUC0→24、AUC0→∞、tmax、Cmax 、t1/2 of the tested and referenced preparations were as follows: 184.7±40.1 mg/(h·L) and 174.9±36.5 mg/(h·L),208.6±49.6 mg/(h·L) and 189.1±36.9 mg/(h·L),1.6±0.8 h and 1.2±0.4 h,24.5±4.3 mg/L and 24.4±4.4 mg/L,6.3±2.0h and 5.0±1.2h. The relative bioavailability of metoclopramide was 106.2±12.8%.[Conclusion]The tested and the referenced preparations are bioequivalent.