Open AccessSTEADY-STATE PHARMACOKINETICS OF METFORMIN IN OBESE PATIENTS WITH TYPE 2 DIABETES MELLITUS: A PRELIMINARY STUDY
Author(s) -
Vitarani Dwi Ananda Ningrum,
Zullies Ikawati,
Ahmad Hamim Sadewa,
Mohammad Robikhul Ikhsan,
S Saepudin
Publication year - 2016
Publication title -
asian journal of pharmaceutical and clinical research
Language(s) - English
Resource type - Journals
eISSN - 2455-3891
pISSN - 0974-2441
DOI - 10.22159/ajpcr.2017.v10i1.15252
Subject(s) - metformin , trough (economics) , type 2 diabetes , obesity , genotype , medicine , diabetes mellitus , pharmacokinetics , pharmacology , chemistry , endocrinology , gene , biochemistry , economics , macroeconomics
Objective: This study aimed to determine the metformin plasma steady-state concentration (PSSC) either trough and peak level in Type 2 diabetesmellitus patients with obesity and the impact of SLC22A1 gene organic cation transporter 1 (OCT) rs628031 A>G on PSSC of metformin.Methods: Validated reversed-phase high-performance liquid chromatography method with ultraviolet detector was used to determine the metforminPSSC, as well as genotype variation was performed using the restriction fragment length polymorphisms-polymerase chain reaction method.Results: A total of 13 patients were recruited from five Primary Health Centers in Yogyakarta Province of Indonesia. The results showed that themeans of their trough and peak PSSC were 0.285±0.192 and 1.175±0.814 µg/ml, respectively. Only 10 patients (77%) had peak PSSC within theplasma therapeutic level (PTL) of metformin, and 14-fold variability was observed for the peak PSSC. None of the patients achieved the PTL ofmetformin with regard to their trough PSSC. The PSSC of metformin was independent of the OCT1 genotype in rs628031 (A>G) 408M/V SLC22A1.Conclusion: This study found a huge variability in the trough concentration of metformin (>100-fold) and 14-fold for the peak PSSC, and no impactof a variant of rs628013 SLC22A1 OCT1 on metformin PSSC was revealed.Keywords: Metformin, Steady-state pharmacokinetics, Obesity, Type 2 diabetes mellitus.