Bioequivalence of metformin hydrochloride sustained-release tablets under fed condition in healthy subjects
10.11665/j.issn.1000-5048.20220922001
- VernacularTitle:盐酸二甲双胍缓释片在健康受试者餐后条件下的生物等效性研究
- Author:
Mingli SUN
1
;
Chen LIU
;
Yali WEI
;
Qian GAO
;
Qianying LIU
;
Xinghe WANG
Author Information
1. 首都医科大学附属北京世纪坛医院
- Publication Type:Journal Article
- Keywords:
metformin hydrochloride sustained-release tablets;
pharmacokinetics;
fed;
bioequivalent
- From:
Journal of China Pharmaceutical University
2023;54(1):89-94
- CountryChina
- Language:Chinese
-
Abstract:
To evaluate bioequivalence and safety of two kinds of metformin hydrochloride sustained-release tablets (test preparation vs reference preparation) under the condition of fed and single administration.A single center, randomized, open, single-dose, two-period, two-sequence, and double-crossover design was used.32 healthy subjects took 0.5 g of test preparation or reference preparation under fed and single-dose administration.4 mL of venous blood was collected from before administration (0 h) to 1, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 9, 10, 12, 15, 24, 36 and 48 h after administration.The concentration of metformin in plasma samples was detected, and then the pharmacokinetic parameters were calculated by WinNonlin 7.0 software.When the 90% confidence intervals of cmax, AUC0-t and AUC0-∞ geometric mean ratio of test preparation and reference preparation were within 80.00%-125.00% equivalent intervals respectively, the bioequivalence of the two preparations was proved.One subject fell off due to adverse events.The main pharmacokinetic parameters of test preparation and reference preparation as follows: cmax were (0.68 ± 0.14) and (0.65 ± 0.11) mg/L, AUC0-t were (7.33 ± 1.65) and (7.00 ± 1.89) h·mg/L, AUC0-∞ were (7.39 ± 1.67) and (7.06 ± 1.91) h·mg/L, respectively.The 90% confidence intervals of the geometric mean ratio of the two main pharmacokinetic parameters were 101.45%-109.14%, 100.08%-112.32% and 100.24%-112.28%, respectively, which fell within the bioequivalence interval of 80.00%-125.00%.There were no serious adverse events and unexpected adverse events during the trial.The results show that test preparation and reference preparation are bioequivalent under fed and single-dose administration, safe and well tolerated in healthy subjects.
