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A Potential Breakthrough in the Enhancement of Glimepiride Solubility and Dissolution Rate by Binary and Ternary Solid Dispersion Technique and In Vitro Comparison with Marketed Formulation

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Abstract

Purpose

Glimepiride, an anti-diabetic and third-generation sulfonylurea drug belonging to class II BCS (Biopharmaceutical Classification System) type, is characterized by its low solubility and high permeability. In order to increase glimepiride’s aqueous solubility and hence increase its dissolution rate, the goal of this study was to formulate the drug as binary and ternary solid dispersion employing water-soluble carriers.

Methods

Three binary solid dispersions of glimepiride were prepared by solvent evaporation technique using β-cyclodextrin with different drug carrier ratios. After optimizing the binary solid dispersion concerning solubility improvement, four different ratios of ternary solid dispersion employing polyvinylpyrrolidone K30 (PVPK30) were fabricated with the optimized solid dispersion to determine solubility and compared with marketed formulation to determine the consequence of the study. Further FTIR, XRD, and DSC studies were performed for a better understanding of the characterization of optimized solid dispersion and to know if there are any significant interactions with water-soluble carriers or with excipients.

Results

The combination of the glimepiride and β-cyclodextrin systems significantly increases the solubility and in the case of ternary solid dispersion, the solubility is increased even more. The enhancement of the solubility is influenced by the carrier’s concentration.

Conclusions

A total of four tablet formulation batches that were prepared and the explicit in vitro comparisons been carried out with commercially available immediate-release formulation, suggested that formulating glimepiride in ternary solid dispersion has enhanced the solubility and dissolution rate drastically.

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Data Availability

Data are contained within the article.

Abbreviations

T2DM:

Type II diabetes mellitus

BCS:

Biopharmaceutical classification system

BCD:

β-Cyclodextrin

PVPK30:

Polyvinylpyrrolidone K30

MCC:

Microcrystalline cellulose

SD:

Solid dispersion

PM:

Physical mixture

GLIMI:

Glimepiride

FTIR:

Fourier-transform infrared spectroscopy

MW:

Molecular weight

XRD:

X-ray diffraction

DSC:

Differential scanning calorimetry

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Acknowledgements

The authors appreciate the gift sample of glimepiride from Dr Reddy’s Laboratories Ltd. (India) and the department of Pharmaceutical Technology and department of Metallurgical and Material engineering at Jadavpur University (Kolkata-700032, India) for providing all necessary facilities. The authors are also thankful of the AICTE’s financial assistance for their work.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, Jadavpur University, 132 Raja SC Mallick Road, Jadavpur, Kolkata, 700032, West Bengal, India

    Rideb Chakraborty, Naureen Afrose & Ketousetuo Kuotsu

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  1. Rideb Chakraborty
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  2. Naureen Afrose
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  3. Ketousetuo Kuotsu
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Contributions

Conceptualization: R.C., N.A., and K.K.; methodology: R.C.; software: N.A.; validation: R.C., N.A., and K.K.; formal analysis: R.C. and N.A.; investigation: R.C.; resources: K.K.; data curation: R.C. and N.A.; visualization: R.C. and N.A.; writing—original draft preparation and review and editing: R.C.; visualization: R.C. and N.A.; supervision: K.K.; project administration: R.C., N.A., and K.K.

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Correspondence to Ketousetuo Kuotsu.

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Chakraborty, R., Afrose, N. & Kuotsu, K. A Potential Breakthrough in the Enhancement of Glimepiride Solubility and Dissolution Rate by Binary and Ternary Solid Dispersion Technique and In Vitro Comparison with Marketed Formulation. J Pharm Innov 18, 1981–1991 (2023). https://doi.org/10.1007/s12247-023-09761-2

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