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.
Highlights
Solubility is an important parameter of the absorption process of a drug in the gastrointestinal tract that affects the drug concentration that can reach the blood circulation
Increasing the dissolution rate of poorly watersoluble drugs is important in enhancing their bioavailability [2]
In the biopharmaceutical classification system (BCS), GCM is included in class II, which means it has a high permeability and a low solubility
Summary
Solubility is an important parameter of the absorption process of a drug in the gastrointestinal tract that affects the drug concentration that can reach the blood circulation. This is important because the effectiveness of a drug treatment depends on the level of drug in the blood. Drugs with poor solubility in water exhibit poor bioavailability and low dissolution rates in the drug absorption [1]. Several studies have been conducted to increase the solubility of GCM such as solid dispersion [4], surface solid dispersion, nanoparticles [5], and nanoemulsion [6]. None of these methods stably yield a solid preparation
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