SOLID DOSAGE FORM DEVELOPMENT OF GLIBENCLAMIDE-ASPARTAME COCRYSTAL USING THE SOLVENT EVAPORATION METHOD TO INCREASE THE SOLUBILITY OF GLIBENCLAMIDE

ARIF BUDIMAN; SANDRA  MEGANTARA; AYU  APRILIANI

doi:10.22159/ijap.2019v11i3.32121

Authors

ARIF BUDIMAN Department of Pharmaceutical and Technology Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran,
SANDRA MEGANTARA Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran,
AYU APRILIANI Department of Pharmaceutical and Technology Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran,

DOI:

https://doi.org/10.22159/ijap.2019v11i3.32121

Keywords:

Cocrystal, Glibenclamide, Aspartame, Solvent Evaporation

Abstract

Objective: The solubility of a drug in water plays an important role in the absorption of the drug after oral administration. Cocrystal is one method that improves the solubility of the active pharmaceutical ingredient (API). The aim of this study was to investigate the formation of a glibenclamide (GCM)-aspartame (APM) cocrystal using the solvent evaporation method and to evaluate its solubility and dissolution rate.

Methods: Molecular docking of the GCM-APM cocrystal was observed using an in silico method. The GCM-APM cocrystal (1:2) was prepared by using the solvent evaporation method. The cocrystal of GCM-APM was evaluated by the saturated solubility test and the dissolution rate test (USP type 2 apparatus). The solvent evaporation product of GCM-APM was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD).

Results: In silico study showed that the interaction of GCM-APM has hydrogen bonding and the potential to improve the solubility of GCM. Evaluation of the cocrystal of GCM-APM showed that the solubility and dissolution rate of the cocrystal are significantly increased. Characterization of FT-IR showed that no chemical reaction occurred in the GCM-APM cocrystal. The DSC analysis showed the changes in the melting point of GCM. Measurement of PXRD showed the formation of a new solid crystal phase that is different from GCM and APM.

Conclusion: GCM-APM has hydrogen bonding can improve the solubility and dissolution rate of GCM.

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