健康志愿者中格列吡嗪片剂的相对生物利用度

Bioavailability of glipizide tablet in healthy male volunteers

目的:研究两种格列吡嗪片剂在13名男性健康志愿者体内的生物利用度.方法:同体交叉试验后,用反相高效液相色谱-紫外检测法检测血浆中格列吡嗪的浓度.药一时数据用3P87程序拟合,按一室模型计算药物动力学参数.结果:研制品片剂的AUC、C_(max)、t_(max)、T_(1/2)分别为(18.598±5.569)(h·μg)/ml、(2.382±0.873)μg/ml、(2.285±0.499)h.和(3.41±0.932)h;对照品片剂分别为(20.183±6.191)(h·μg)/ml、(2.635±0.840)μg/ml、(2.187±0.458)h和(3.269±0.975)h.研制品片剂的相对生物利用度为93%.两种片剂的所有药物参数经统计学(NDST软件)处理均无显著性差异(P>0.05),用双向单侧t检验对其主要药物动力学参数进行检验.结论:两种格列吡嗪片剂具有生物等效性.

AIM: To study pharmacokinetics and bioavailability of glipizide tablets in 13 healthy male volunteers. METHODS : According to the crossover design, each volunteer was orally given 5 mg glipizide tablets, and the plasma concentrations were determined by re-versed phase high performance liquid chromatography. Pharmacokinetic parameters were ob-tained using 3P87 program,and were calculated on the basis of an open single compartment model. RESULTS :The pharmacokinetic parameters of gilipizide(developed) were : AUC,c_(max), t_(max),t_(1/2) were (18. 598 ± 5. 569) (h · μg)/ml, (2. 382 ± 0. 873)ng/ml, (2. 285 ± 0. 499)h and ( 3. 410 ± 0. 932 ) h, respectively. The pharmacokinetic parameters fo glipizide (controlled) AUC were: (20. 183 ± 6. 191) (h · μg)/ml,c_(max) (2. 635 ± 0. 840)μg/ml.t_(max) (2. 187 ± 0. 458)h and T1/2(3. 269 ± 0. 975)h. There were no significant differences in all pharmacokinetic pa-rameters between 2 formulations (P>0. 05). The relative bioavailabitity of developed formu-lation was 93%. CONCLUSION :The result shows that 2 formulations are of bioequivalence.