Heterogeneous crystallization of Chlorzoxazone for modulating the physicochemical properties of crystals--颗粒学报PARTICUOLOGY

Natarajan, D., Ponnusamy, K., & Thota Karunakaran, R. (2024). Heterogeneous crystallization of Chlorzoxazone for modulating the physicochemical properties of crystals. Particuology, 91, 249-259. https://doi.org/10.1016/j.partic.2024.03.011

Heterogeneous crystallization of Chlorzoxazone for modulating the physicochemical properties of crystals

Dhayananth Natarajan, Kalaichelvi Ponnusamy^*, Radhakrishnan Thota Karunakaran

Department of Chemical Engineering, National Institute of Technology, Tiruchirappalli, 620 015, Tamilnadu, India

10.1016/j.partic.2024.03.011

Volume 91, August 2024, Pages 249-259

Received 22 December 2023, Revised 2 February 2024, Accepted 18 March 2024, Available online 11 April 2024, Version of Record 16 April 2024.

E-mail: kalai@nitt.edu

Highlights

• Chlorzoxazone (CHZ) crystal habit modification is achieved by heterogeneous crystallization (HC).

• CHZ crystals obtained in the presence of polyvinylpyrrolidine acquire a small plate-shaped.

• The size reduction of CHZ crystal improves the powder flow-ability.

• The size-reduced CHZ crystal tends to increases the surface area, and solubility.

• HC enhances the solubility, and pharmaceutical attributes of CHZ.

Abstract

The polymer on modulating the crystal's habit is an evolving research in pharmaceutical crystallization. This study demonstrates the crystal habit modification of chlorzoxazone (CHZ) by heterogeneous crystallization (HC) in the binary solvent acetonitrile-ethanol (A-E (1:1)) in the presence of polyvinylpyrrolidine (PVP) at concentrations of 0.50, 0.75, and 1.00 wt%. The A-E (1:1) and PVP in HC experiments influenced to change the shape of crystals from needle to plate shape and reduced the crystal size producing a lower aspect ratio (in the range of 1.5–2.3). In the presence of PVP, the CHZ size distribution is 65–78 μm which tends to enhance the powder flow-ability of CHZ crystals and as the PVP concentration increases, the nucleation rate decreases. The solubility of size-reduced CHZ crystals at different pH is found to be improved by 1.2–1.4 times. Hence, HC is deemed effective in modifying the physicochemical attributes of CHZ.

Graphical abstract

Keywords

Chlorzoxazone; Polyvinylpyrrolidine; Heterogeneous crystallization; Crystal habit modification; Aspect ratio

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