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Exploring potential coformers for oxyresveratrol using principal component analysis
Passaporn Ouiyangkul1, Vimon Tantishaiyakul2, Namon Hirun3
1Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai 90112, Thailand.
Oxyresveratrol (OXY) cocrystals with nicotinamide (NCT) and proline (PRO) were successfully formed, significantly enhancing OXY
Area of Science:
- Pharmaceutical Science
- Materials Science
- Chemical Engineering
Background:
- Oxyresveratrol (OXY) has limited pharmaceutical applications due to poor solubility and bioavailability.
- Cocrystal formation is a promising strategy to enhance the solubility of poorly soluble active pharmaceutical ingredients.
Purpose of the Study:
- To select suitable coformers for Oxyresveratrol (OXY) using principal component analysis (PCA).
- To prepare and characterize OXY cocrystals with selected coformers.
- To evaluate the impact of cocrystal formation on OXY's solubility and dissolution properties.
Main Methods:
- Principal component analysis (PCA) was used to screen coformers based on physicochemical properties.
- Cocrystals were prepared using the liquid-assisted grinding method.
- Cocrystals were characterized using thermal analysis, X-ray diffraction, FTIR, and Raman spectroscopy.
Main Results:
- PCA identified nicotinamide (NCT) and proline (PRO) as suitable coformers for OXY.
- OXY-NCT and OXY-PRO cocrystals were successfully synthesized, exhibiting distinct thermal and diffraction patterns compared to OXY.
- Spectroscopic analysis confirmed specific interactions (hydrogen bonding and π-π interactions) involved in cocrystal formation.
- Both OXY-NCT and OXY-PRO cocrystals demonstrated significantly improved solubility and dissolution rates compared to OXY alone.
Conclusions:
- PCA is an effective tool for coformer selection in cocrystal development.
- Cocrystal formation with NCT and PRO successfully enhanced OXY's solubility and dissolution.
- These findings suggest potential pharmaceutical applications for OXY cocrystals.
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