格列美脲口腔崩解片正常人体生物等效性研究

Bioequivalence of Glimepiride Orally Disintegrating Tablet in Healthy Subjects

目的研究格列美脲口腔崩解片在正常人体的药代动力学及相对生物利用度。方法20名健康志愿受试者分别单剂量口服格列美脲口腔崩解片(受试制剂)和普通片(参比制剂),用高效液相色谱法测定血药浓度,以3P97计算药动学参数和生物等效性。结果受试制剂或参比制剂体内药时曲线均符合二室模型,峰浓度(Cmax)分别为(406.89±230.57)ng/mL和(409.62±231.58)ng/mL,达峰时间(Tmax)分别为(3.70±1.53)h和(3.58±1.04)h,0～t药时曲线下面积(AUC0-t)分别为(3311.60±2038.99)ng·h/mL和(3127.85±1625.64)ng·h/mL,两者药代动力学参数无显著性差异(P>0.05),受试制剂相对生物利用度为(105.87±12.92)%。结论受试制剂与参比制剂具有生物等效性。

Objective To study the relative bioavailability and pharmacokinetics of glimepiride orally disintegrating tablet in 20 healthy male volunteers. Methods A single dose of 4 mg of orally disintegrating tablets and market tablets of glimepiride were administered by randomized crossover way in 20 volunteers and the plasma concentrations of glimepiride were determined by HPLC. The pharmacokinetics parameters were calculated with 3P97 program and the bioequivalence was evaluated. Results The concentration-time curve of two preparations fitted two compartments model. The peak plasma levels （Cmax） of orally disintegrating tablet and market tablet of glimepirlde were （406.89± 230. 57） ng/mL, （409.62 ± 231.58） ng/mL, respectively. The peak time （Tmax） were （3.70 ± 1.53） h and （3.58 ± 1.04） h. And AUC（o-t） were （3 311.60 ± 2 038.99）ng · h/mL and （3 127.85 ± 1 625.64）ng · h/mL,respectively. The relative bioavailabitity of glimepiride orally disintegrating tablet was （105.87 ±12.92）%. Conclusion Glimepiride orally disintegrating tablet is bioequivalence to the market tablet of glimepiride.