Novel Ascorbic Acid Co-Crystal Formulations for Improved Stability

Author:

Zhang Hui,Zeng Huahui,Li Mengfei,Song Yagang,Tian Shuo,Xiong Jing,He Lan,Liu YangORCID,Wu XiangxiangORCID

Abstract

A series of co-crystals of ascorbic acid were prepared with equimolar amounts of co-crystal formers (CCFs), including isonicotinic acid, nicotinic acid, 3,4-dihydroxybenzoic acid, 2,5-dihydroxybenzoic acid and m-hydroxybenzoic acid, by slow solvent evaporation and solvent-assisted grinding. The co-crystals were characterized by single-crystal X-ray diffraction spectroscopy, powder X-ray diffraction, IR spectroscopy, differential scanning calorimetry and thermogravimetric analysis. Molecular dynamics (MD) simulations further validated the interaction energy and the possible intermolecular hydrogen bonds among VC and CCFs. The co-crystals showed improved stability when exposed to different wavelengths of light, pH and temperatures compared to the free analogue, especially at higher pH (~9) and lower temperature (~4 °C).

Funder

National Natural Science Foundation of China

Henan Scientific and technological Innovation Talents Project

Henan Science Fund for Excellent Young Scholars

Henan Scientific Research Funding Project for Overseas Staffs 2020

Natural Science Foundation of Henan Province

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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