摘要
目的研究国产和进口格列吡嗪控释片(降血糖药)的相对生物利用度。方法男性健康受试者随机交叉单剂(24名)、连续(22名)口服国产和进口格列吡嗪控释片,均每天5mg,共7天。用LC-MS/MS法测定血清中格列吡嗪的药物浓度,计算药代动力学参数及相对生物利用度并进行生物等效性评价。结果进口和国产制剂的主要药代动力学参数如下。单次给药:t1/2β分别为((9.12±2.73)和(8.60±4.43)h,tmax分别为(10.67±5.13)和(9.08±2.76)h,Cmax分别为(135.9±41.1)和(157.9±25.3)ng·mL-1;AUC0-48分别为(2852.0±946.6)和(3021.5±899.9)ng.h.mL-1;2种制剂AUC0-48的相对生物利用度为(109.2±28.9)%。连续给药:t1/2β分别为(11.31±3.37)和(10.97±3.49)h,tmax分别为(6.8±3.5)和(6.6±3.7)h,Cssmax分别为(187.4±54.5)和(176.0±72.3)ng·mL-1,Cssmin分别为(61.3±28.1)和(69.1±41.2)ng·mL-1,AUC0-48分别为(3495.0±1110.6)和(3488.2±1554.9)ng.h.mL-1,DF为(56.2±19.9)%和(49.7±22.5)%。2种制剂AUC0-48的相对生物利用度为(101.0±32.1)%。结论2种格列吡嗪控释片为生物等效制剂。
Objective To study the relative bioavailability and bioequivalence of two glipizide controlled - release preparations in healthy volunteers. Methods The tests were carried out according to single dosage regimen and multiple dosage regimen in a open crossover design. In single dosage regimen, 24 enrolled healthy volunteers were randomized given 5mg of test or reference preparation. In multiple dosage regimen,22 enrolled subjects were given 5 mg of test or reference preparation once daily for 7 consecutive days. LC - MS/MS was used to determine the glipizide concentration in serum. Pharmacokinetic parameters and relative bioavailability were calculated, and bioequivalence of the two preparations was evaluated. Results The main pharmacokinetic parameters were calculated as follows：In single dosage regimen, for reference and test preparations, t（1/2β） were （ 9. 12 ± 2.73 ）, （ 8.60 ± 4.43 ） h ; tmax, were （10.67 ±5.13）, （9.08±2.76）h;Cmaxwere （135.9 ±41.1）,（157.9 ±25.3）ng · mL^-1;AUC（0-48） were （2852.0 ±946.6）, （3021.5 ± 899.9）ng · h · mL^-1 ;AUC（0-∞） were （3002.4 ± 1107.6）, （3167.6 ± 1090.6） ng· h ·mL^-1 respectively. The relative bioavailability was （109.2 ±25.4）%. In multiple dosage regimen,for reference and test preparations, t（1/2β） were （11.31±3.37）, （10.97±3.49）h; t were （6.8 ±3.5）, （6.6±3.7） h; C were （187.4±54.5）, （176.0±72.3） ng. mL; CssminWere （61.3 ±28.1）, （69.1 ±41.2 ）ng·mL; AUG（0-48）were （3495.0 ±1110.6）, （3488.2±1554.9）ng·h·mL^-1;AUC（0-∞） were （3670.7±1199.7）, （3650.5 ±1599.2） ng·h·mL^-1, respeetively. The relative bioavailability was （ 101.0 ± 32.1 ） %. DF were （ 56.2 ± 19.9 ） %, （49.7 ± 22.5 ） % for referenee and test preparation, respeetively. Conclusion The two preparations were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2007年第5期348-352,共5页
The Chinese Journal of Clinical Pharmacology
