Bioavalaibility and pharmacokinetic comparison of two formulations of metformin 850 mg tablets in healthy Colombian volunteers

Colombia Médica

Sergio Parra¹  Fanny Cuesta¹  Blanca Montoya¹  Juan Carlos Ríos¹  Rosendo Archbold¹  Victoria Eugenia Toro¹  Gloria Holguín¹  Lina Peña¹  Margarita Restrepo¹  Adriana Ruiz¹ 

关键词: Metformin;    Bioequivalence;    Bioavailability;    Pharmacokinetics;    Interchange of drugs;    Area under curve;   

DOI  :  

学科分类：医学（综合）

来源: Universidad del Valle * Facultad de Salud / Universidad del Valle, Faculty of Health

【 摘 要 】

urpose:The aim of this study was to compare the bioavailability of two formulations of metformin 850 mg tablets: Glucophage® from Merck Santè laboratories (reference product) and Metformin from Winthrop Pharmaceuticals de Colombia SA (test product) in healthy Colombian volunteers. Methods:A random, double blind, two-period, two-week wash out period, crossover study was performed in 24 healthy male and female volunteers for a single 850-mg dose of metformin tablets administrated with 240 ml of water after 12 hours of fasting. Once the drug was administrated, blood samples were collected before and within 24 hour, and plasma metformin concentration was determined by using a validated HPLC method. Pharmacokinetic parameters such as C max , AUC 0-96h , AUC 0- �?, and T maxwere determined. The formulations were considered bioequivalent if the logarithmic mean ratios of ln-transformed C maxand AUC 0- �? values were within the equivalence range of 80%-125%. Results:ANOVA analysis of the ln-transformed C maxand AUC 0- �? indicated that none of the effects examined (formulation, period, within and between-subjet variances and carry over) was statistically significant. The mean (±SD) of C max1217.38 (± 251.72) ng/ml vs. 1305.25 (± 301.06) ng/ml, AUC 0-96h1363.49 (± 315.51) ng.h/ml vs. 1584.82 (± 368.75) ng.h/ml, AUC 0- �?, 7155.75 (± 1440.74) ng.h/ml vs. 7777.08 (± 1896.49) ng.h/ml, and T max2.57 (± 0.93) h vs. 2.22 (± 0.94) h were obtained with test and reference formulations, respectively. These pharmacokinetic parameters presented differences with the results from other published papers. The 90% confidence interval of the logarithmic ratio of AUC 0- �? and C maxwas within the range of 80-125%. Conclusions:In this study in healthy Colombian volunteers, a single 850-mg dose of metformin tablet test formulation met the criteria for bioequivalence to the reference formulation based on pharmacokinetic parameters AUC 0- �? and C max .

【 授权许可】

Unknown