格列吡嗪2种片剂的药物动力学和人体生物利用度比较

目的 :考察 2种格列吡嗪片剂在正常人体的药物动力学 ,评价其生物等效性。方法 :8名健康受试者随机自身交叉口服格列吡嗪片A(爱宝 )和格列吡嗪片B(金晓 )各 10mg ,用反相HPLC内标法测定经时血药浓度。结果 :HPLC测定的线性范围2 0～ 10 0 0 μg·L- 1(r =0 .9995) ;回收率 99.70 %～10 6 .34% ;天内精密度为 3.0 9%～ 6 .83% ;天间精密度为 2 .2 2 %～ 4 .13%。格列吡嗪片A和片B的Cmax为 (555± 173) μg·L- 1和 (552± 86 ) μg·L- 1;Tmax为 (1.1± 0 .2 )h和 (1.6± 0 .3)h ;T12 为 (4 .6±1.2 )h和 (4 .2± 0 .6 )h ;AUC0 -T为 (2 876± 4 6 8) μg·L- 1·h- 1和 (310 4± 582 ) μg·L- 1·h- 1。方差分析示T12 ,AUC0 -T和Cmax差异无显著意义 (P >0 .0 5) ,片A的Tmax显著小于片B(P <0 .0 1)。结论 :2种格列吡嗪片具有生物等效性。

Comparison of pharmacokinetics and bioavailability of two kinds of glipizide tablets in healthy volunteers

AIM: To compare the relative bioavailability and evaluate the bioequivalant of two glipizide tablets in healthy volunteers man (tablet A was made by Farmitalia Carloerba, tablet B was made by Hannan Willine Pharmaceutical LTD. of P.R. China). METHODS: The relative bioavailability test was carried out in eight healthy volunteers(male) by orally administration 10 mg of glipizide tablets (A or B) on random cross method. A reverse phase high pressurre liquid chromatography(HPLC) was used to determinate plasma glipizide. RESULTS: The HPLC method had a linear concentration range from 20-1000 μg·L -1 ( r =0.9995), the recoveries varied from 99.70%-106.34%, and RSD was 3.09%-6.83% within a day, 2.22%-4.13% out of days. The results of a relative bioavailability test between tablet A and B were that C max was (555± s 173)μg·L -1 and (552±86)μg·L -1 respectively, T max (1.1±0.2)h and (1.6±0.3)h, T 12 (4.6± 1.2 )h and (4.2±0.6)h, AUC 0-T (2876±468)μg·h·L -1 and (3104±582)μg·L -1 ·h -1 . C max , T 12 and AUC 0-T of two formulations had not significant differences( P >0.05). T max of two tablets had significant differences( P <0.01). It meant tablet A had a shorter peak trough time than tablet B. CONCLUSION: Two kinds of glipizide tablets were bioequivalent. Graduate (College of Pharmacy, Shanghai Medical University)