TY - JOUR
T1 - Effect of Excipients on the Quality of Drug Formulation and Immediate Release of Generic Metformin HCl Tablets
AU - Arafat, Mosab
AU - Sakkal, Molham
AU - Yuvaraju, Priya
AU - Esmaeil, Anna
AU - Poulose, Vijo
AU - Aburuz, Salahdein
N1 - Funding Information:
This research was funded by Al Ain University, grant number Ph2021-2-902, and by a Research Start-up grant No.: 700032854 awarded by United Arab Emirates University, UAE.
Funding Information:
We acknowledge Al Ain University for providing financial support and United Arab Emirates University for awarding Research Start-up grant No.: 700032854.
Publisher Copyright:
© 2023 by the authors.
PY - 2023/4
Y1 - 2023/4
N2 - Generic medications are bioequivalent to brand-name medications, but the quality and purity of generic medications are still debatable. The aim of this study was to compare the generic product of metformin (MET) to its branded counterpart using pure MET powder as a reference. Quality control tablet assessment and in vitro evaluation of drug release were carried out in various pH media. Additionally, several analytical methods and thermal techniques were used, namely differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier-transform infrared (FTIR), and confocal Raman microscopy. The results showed a significant difference between the two products. In terms of friability assessment, mean resistance force, and tablet disintegration, the generic MET product showed significant weight loss, higher mean resistance force, longer disintegration time, and a slower rate of drug release. In addition, DSC and TGA showed that the generic product had the lowest melting point and the least weight loss compared to the branded product and pure powder. XRD and SEM demonstrated some changes in the crystallinity structure of the molecule particles for the generic product. Additionally, FTIR and confocal Raman revealed the same peaks and band shifts in all samples, but with differences in the intensity for the generic tablet only. The observed differences could be due to the use of different excipients in the generic product. The possibility of forming a eutectic mixture between the polymeric excipient and metformin in the generic tablet was presumed, which might be attributed to alterations in the physicochemical properties of the drug molecule in the generic product. In conclusion, using different excipients might have a significant effect on the physicochemical properties of drugs in generic formulations, leading to significant changes in drug release behavior.
AB - Generic medications are bioequivalent to brand-name medications, but the quality and purity of generic medications are still debatable. The aim of this study was to compare the generic product of metformin (MET) to its branded counterpart using pure MET powder as a reference. Quality control tablet assessment and in vitro evaluation of drug release were carried out in various pH media. Additionally, several analytical methods and thermal techniques were used, namely differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier-transform infrared (FTIR), and confocal Raman microscopy. The results showed a significant difference between the two products. In terms of friability assessment, mean resistance force, and tablet disintegration, the generic MET product showed significant weight loss, higher mean resistance force, longer disintegration time, and a slower rate of drug release. In addition, DSC and TGA showed that the generic product had the lowest melting point and the least weight loss compared to the branded product and pure powder. XRD and SEM demonstrated some changes in the crystallinity structure of the molecule particles for the generic product. Additionally, FTIR and confocal Raman revealed the same peaks and band shifts in all samples, but with differences in the intensity for the generic tablet only. The observed differences could be due to the use of different excipients in the generic product. The possibility of forming a eutectic mixture between the polymeric excipient and metformin in the generic tablet was presumed, which might be attributed to alterations in the physicochemical properties of the drug molecule in the generic product. In conclusion, using different excipients might have a significant effect on the physicochemical properties of drugs in generic formulations, leading to significant changes in drug release behavior.
KW - brand-name drug
KW - generic drug
KW - in vitro evaluation
KW - metformin
KW - quality control test
KW - thermal analysis
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U2 - 10.3390/ph16040539
DO - 10.3390/ph16040539
M3 - Article
AN - SCOPUS:85154552939
SN - 1424-8247
VL - 16
JO - Pharmaceuticals
JF - Pharmaceuticals
IS - 4
M1 - 539
ER -