Posaconazole (PSZ) is a BCS (biopharmaceutical classification system) Class II anti-fungal drug used to treat infections in immunocompromised patients. The work presented herein describes the generation of cocrystals of PSZ with 4-aminobenzoic acid (4AMB) using supercritical CO₂ as an antisolvent in GAS (Gas Antisolvent) with acetonitrile, and as a solvent in CSS (Cocrystallization with Supercritical Solvent) methods. Cocrystals of PSZ-4AMB were obtained in a 2:3 stoichiometric ratio for the first time by GAS and CSS methods, with GAS producing higher-purity samples compared to CSS method. The work presented herein investigates the influence of critical processing variables using CO₂ solvent and antisolvent crystallization methods with respect to the formation of cocrystals of PSZ-4AMB. A Design of Experiments (DoE) approach was performed to assess the outcome of PSZ-4AMB formation, impacted by processing variables such as pressure, temperature, and stirring rate using GAS and CSS methods. The resulting cocrystalline phase was identified using differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). The particle morphologies and size distributions were determined using scanning electron microscopy and automated static imaging, respectively.

泊沙康唑（PSZ）是BCS（生物药物分类系统）II类抗真菌药物，用于治疗免疫功能低下患者的感染。本文介绍的工作描述了使用超临界CO ₂作为乙腈在GAS中的反溶剂（气体反溶剂）和在CSS中作为溶剂（与超临界溶剂共结晶）使用4-氨基苯甲酸（4AMB）生成PSZ共晶体的方法。通过GAS和CSS方法首次以2：3的化学计量比获得PSZ-4AMB的共晶体，与CSS方法相比，GAS产生的样品纯度更高。本文介绍的工作使用CO ₂研究关键工艺变量的影响溶剂和反溶剂结晶方法有关PSZ-4AMB共结晶的形成。进行了实验设计（DoE）方法，以评估PSZ-4AMB形成的结果，该结果受使用GAS和CSS方法的加工变量（例如压力，温度和搅拌速率）的影响。使用差示扫描量热法（DSC）和粉末X射线衍射（PXRD）鉴定得到的共晶相。分别使用扫描电子显微镜和自动静态成像来确定颗粒的形态和尺寸分布。