SOLID DOSAGE FORM DEVELOPMENT OF GLIBENCLAMIDE WITH INCREASING THE SOLUBILITY AND DISSOLUTION RATE USING COCRYSTALLIZATION

  • Arif Budiman Department of Pharmaceutic and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran
  • Sandra Megantara bDepartment of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran
  • Putri Raraswati Department of Pharmaceutic and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran
  • Tazyinul Qoriah Department of Pharmaceutic and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran

Abstract

Objective: The aim of this study was to develop a solid dosage form of glibenclamide with increasing the solubility properties of glibenclamide with cocrystallization method.

Methods: Virtual screening was performed to investigate the interaction between glibenclamide and a co-former. Saccharin, the selected co-former, then co-crystallized with glibenclamide with equimolar ratios of 1:1 and 1:2 using the solvent evaporation method. Further characterization was performed using an infra-red (IR) spectrophotometer, differential scanning calorimetry (DSC), and powder x-ray diffraction (PXRD).

Results: Co-crystals of 1:2 equimolar ratio were more highly soluble compared to pure glibenclamide (30-fold for 12 h and 24-fold for 24 h). The dissolution rate had also increased from 46.838% of pure glibenclamide to 77.655% of glibenclamide co-crystal in 60 min. There was no chemical reaction observed during the co-crystallization process based on the IR spectrum. However, there was a new peak in the X-Ray diffractogram and a reduction of melting point in the DSC curve, indicating the formation of co-crystals.

Conclusion: The optimal co-crystal ratio of glibenclamide-saccharin was found to be 1:2, which was successful in improving the solubility of glibenclamide.

Keywords: Glibenclamide, Co-crystal, Saccharin, Dissolution

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Budiman, A., Megantara, S., Raraswati, P., & Qoriah, T. (2018). SOLID DOSAGE FORM DEVELOPMENT OF GLIBENCLAMIDE WITH INCREASING THE SOLUBILITY AND DISSOLUTION RATE USING COCRYSTALLIZATION. International Journal of Applied Pharmaceutics, 10(6), 181-186. https://doi.org/10.22159/ijap.2018v10i6.29257
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