Cocrystals of carbamazepine: Structure, mechanical properties, fluorescence properties, solubility, and dissolution rate--颗粒学报PARTICUOLOGY

Ouyang, J., Liu, L., Li, Y., Chen, M., Zhou, L., Liu, Z., . . . Shehzad, H. (2024). Cocrystals of carbamazepine: Structure, mechanical properties, fluorescence properties, solubility, and dissolution rate. Particuology, 90, 20-30. https://doi.org/10.1016/j.partic.2023.11.016

Cocrystals of carbamazepine: Structure, mechanical properties, fluorescence properties, solubility, and dissolution rate

Jinbo Ouyang^a *, Lishan Liu^a, Yin Li ^b *, Mingyang Chen^c, Limin Zhou ^a, Zhirong Liu^a, Li Xu^a, Hamza Shehzad^a

a School of Chemistry and Materials Science, East China University of Technology, Nanchang 330013, China
b School of Physics and Materials Science, Nanchang University, Nanchang 330013, China
c School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China

10.1016/j.partic.2023.11.016

Volume 90, July 2024, Pages 20-30

Received 29 September 2023, Revised 7 November 2023, Accepted 19 November 2023, Available online 28 November 2023, Version of Record 17 December 2023.

E-mail: oyjb1001@163.com; liyin@ncu.edu.cn

Highlights

• Six cocrystals of carbamazepine were synthesized, and their structures were determined.

• Carbamazepine cocrystals possess better fluorescence performance than themselves.

• The dissolution rate of carbamazepine was enhanced by forming cocrystals.

• The mechanical property of carbamazepine was improved via cocrystal formation.

Abstract

Carbamazepine (CBZ) is an anticonvulsant with very low water solubility, presenting as a white crystalline powder with poor mechanical properties and is hard to bend. To enhance CBZ's physicochemical properties, such as water solubility and mechanical properties, we selected six cocrystal coformers (CCFs): nicotinamide (NIC), benzamide (BZM), salicylic acid (SCA), fumaric acid (FMA), trimesic acid (TMA), and hesperetin (HPE). Six CBZ cocrystals were successfully prepared using the solution method. Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and single crystal X-ray diffraction (SCXRD) were used to characterize the crystal structures and gain comprehensive insights into the six cocrystals. The mechanical, fluorescence, and solubility properties of the six cocrystals were tested. The results reveal that most of the prepared cocrystals exhibit improved water solubility and mechanical properties when compared to CBZ. Among them, the dissolution rate of cocrystals excluded from CBZ-HPE has increased by an average of 3 or 4 times compared to CBZ, while CBZ-HPE exhibits superior mechanical properties. Moreover, all six cocrystals possess better fluorescence performance than CBZ. We thoroughly evaluated the mechanical properties of the cocrystals through both experimental and theoretical approaches. This work provides a new direction for studying drug cocrystals to improve the physicochemical properties of drugs.

Graphical abstract

Keywords

Carbamazepine; Cocrystal; Mechanical properties; Fluorescence performance; Dissolution rate

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