Physicochemical and Pharmacokinetic Studies of Metformin for Development of Controlled Release Matrix Tablet: Formulation Optimization Using in silico Tools
Abstract
Metformin, taken by nearly 120 million people across the world as a treatment for type 2 diabetes, has a relatively short plasma half-life and low absolute bioavailability. In this study, physicochemical and pharmacokinetics properties of metformin have been thoroughly assayed using ADMETLab, SwissADME, SmartCYP, LigandScout web-servers and software to evaluate the effectiveness of its formulation as controlledrelease matrix tablets. The objective of the present work was to develop a formulation of an oral controlled-release (CR) metformin tablet, using hydrophilic hydroxylpropylmethylcellulose (HPMC) grades K4M and K100M polymers at different concentrations utilizing computational simulatory tools. Intestinal membrane permeability of the drug has been assayed using 2 hours simulation run with MembranePlus Software. Simulated environment generated for in silico dissolution study, using DDDPlus software, of the prepared formulations used USP Apparatus Type 2 rotating at 100 rpm. The simulation run was for 2 hours using 0.1N HCl phase followed by 8 hours with 6.8 USP Phosphate buffer phase. The results showed that drug release from the higher viscosity grade, K100M was slower as compared to the lower viscosity grade K4M at a fixed polymer concentration level. Furthermore, plasma concentration-time curves for the formulations have been generated using GastroPlus software.
Dhaka Univ. J. Pharm. Sci. 22(1): 29-42, 2023 (June)
How strong is the evidence?
Evidence Hub reads this as a simulation / modelling, done in computer models (in silico), not in people. Its evidence level is 5 of 5 (Very low · case / narrative / animal / in vitro / in silico). Case reports, narrative reviews, and animal, cell or computer-model studies give the weakest evidence for human health. Reported size: 120 participants or records.
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