Study on Pharmacokinetics and Bioequivalence of Glipizide Tablets by HPLC-MS in Healthy Volunteers

OBJECTIVE To develop an accurate and sensitive HPLCMS method for determining glipizide in human plasma and to study pharmacokinetics and relative bioavailability of glipizide in healthy Chinese volunteers. METHODS A single oral dose of 10 mg tested or standard glipizide tablets was given to 18 healthy volunteers in a randomized crossover study.Glipizide concentration in plasma was determined by LC-MS after liquid-liquid extraction.A reversed phase C_(18) column(Kromasil,4.6 mm×150 mm,5 μm)was used and the mobile phase was methanol-water-formic acid(75∶25∶0.625).The pharmacokinetics and bioavailability were studied.RESULTS The detection limit of glipizide in plasma was 20 μg·L~(-1) and a good lineaity was obtained over the range of 20～5 000 μg·L~(-1).The relative standard deviation of with-day and between-day was less 10%.The pharmacokinetics parameters of tested and standard formulations: t_(max)(2.4±0.9) and(2.1 ±1.0) h,ρ_(max)(1.2±0.3) and(1.3 ±0.4) mg·L~(-1),t_(1/2)(5.6 ±2.2) and(5.1 ±1.6) h,AUC_(0～t)(7.6±2.9) and(7.5±3.1) mg·h·L~(-1),AUC_(0～∞)(8.4 ±3.3) and(8.1±3.3) mg·h·L~(-1),the relative bioavailability of tested to stardand tablets was(102.3±23.7)%.CONCLUSION The results demonstrate that two preparations are bioequivalent.