Scholarlink

<p>Cocrystals are multicomponent structures combining at least two substances in a shared crystalline lattice through non-covalent bonding. Cocrystallization offers improved physicochemical and stability properties, and compressed carbon dioxide (CO<sub>2</sub>) poses an innovative route for cocrystal synthesis. In this study, the gas antisolvent (GAS) method with CO<sub>2</sub> was explored to reproduce the vitamins C (ascorbic acid, ASC) and B<sub>3</sub> (nicotinamide, NIC) cocrystal. Cocrystallization screenings were conducted at varying ASC to NIC molar ratios (1:1, 1:2. 1:3, and 2:1), and cocrystal formation was verified via comparative analysis of GAS, conventional liquid-assisted grinding (LAG) and physical mixtures of ASC and NIC by PXRD DSC, and FTIR. GAS produced a pure powder of the polymorph (Form I) of the ASC-NIC (1:1) cocrystal for all initial molar ratios, except at 2:1, that revealed a cocrystal with excess ASC, as confirmed by PXRD and DSC. DSC also confirmed that cocrystals were thermally stable until their melting temperature. GAS-cocrystals (1:1) were purer than those obtained by LAG, and the yield for the two methods was comparable. SEM confirmed the needle-like morphology and smaller particle size of GAS-cocrystals compared to pure ASC and NIC. The GAS process maintained the antioxidant potential of pure ASC and as a cocrystal with NIC at neutral pH. At acidic pH (1.0), cocrystals exhibited significantly improved antioxidant activity than pure ASC. Cocrystallization of vitamins C and B<sub>3</sub> by GAS produced cocrystals with a distinct morphology and enhanced antioxidative properties under acidic conditions, indicating a potential to be explored in targeted applications such as gastric cancer treatment.</p> Graphical abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Synthesis of ascorbic acid-nicotinamide cocrystals by the gas antisolvent (GAS) method with CO2: identification, polymorphism control, and antioxidant power

  • 期刊论文

  • 发表日期：

    2025年8月8日

查看全文
  • Clóvis Antônio Balbinot Filho,
  • Jônatas Lopes Dias,
  • Evertan Antonio Rebelatto,
  • Marcelo Lanza

摘要

Cocrystals are multicomponent structures combining at least two substances in a shared crystalline lattice through non-covalent bonding. Cocrystallization offers improved physicochemical and stability properties, and compressed carbon dioxide (CO2) poses an innovative route for cocrystal synthesis. In this study, the gas antisolvent (GAS) method with CO2 was explored to reproduce the vitamins C (ascorbic acid, ASC) and B3 (nicotinamide, NIC) cocrystal. Cocrystallization screenings were conducted at varying ASC to NIC molar ratios (1:1, 1:2. 1:3, and 2:1), and cocrystal formation was verified via comparative analysis of GAS, conventional liquid-assisted grinding (LAG) and physical mixtures of ASC and NIC by PXRD DSC, and FTIR. GAS produced a pure powder of the polymorph (Form I) of the ASC-NIC (1:1) cocrystal for all initial molar ratios, except at 2:1, that revealed a cocrystal with excess ASC, as confirmed by PXRD and DSC. DSC also confirmed that cocrystals were thermally stable until their melting temperature. GAS-cocrystals (1:1) were purer than those obtained by LAG, and the yield for the two methods was comparable. SEM confirmed the needle-like morphology and smaller particle size of GAS-cocrystals compared to pure ASC and NIC. The GAS process maintained the antioxidant potential of pure ASC and as a cocrystal with NIC at neutral pH. At acidic pH (1.0), cocrystals exhibited significantly improved antioxidant activity than pure ASC. Cocrystallization of vitamins C and B3 by GAS produced cocrystals with a distinct morphology and enhanced antioxidative properties under acidic conditions, indicating a potential to be explored in targeted applications such as gastric cancer treatment.

Graphical abstract