印度蒂鲁奇拉帕利国家理工学院Kalaichelvi Ponnusamy团队报道了，氯唑嗪的非均相结晶对晶体物理化学性质的调节作用。相关研究成果于2024年4月11日发表在《颗粒学报》。

聚合物对晶体习性的调节是药物结晶领域的一项不断发展的研究。

该研究证明了在浓度为0.50、0.75和1.00 wt%的聚乙烯吡咯烷（PVP）存在下，在二元溶剂乙腈-乙醇（A-E（1:1））中通过非均相结晶（HC）对氯唑嗪（CHZ）的结晶习性进行改性。HC实验中的A-E（1:1）和PVP影响了晶体形状从针状变为片状，并降低了晶体尺寸，从而产生较低的纵横比（在1.5–2.3范围内）。

在PVP存在的情况下，CHZ的尺寸分布为65–78μm，这倾向于增强CHZ晶体的粉末流动能力，并且随着PVP浓度的增加，成核速率降低。研究发现尺寸减小的CHZ晶体在不同pH下的溶解度提高了1.2–1.4倍。因此，HC被认为在改变CHZ的物理化学属性方面是有效的。

附：英文原文

Title: Heterogeneous crystallization of Chlorzoxazone for modulating the physicochemical properties of crystals

Author: Kalaichelvi Ponnusamy

Issue&Volume: 2024/04/11

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.

DOI: 10.1016/j.partic.2024.03.011