In order to improve the solubility properties of BCS class II drug itraconazole, fast dissolving oral polymeric film formulations based on itraconazole nanocrystals were produced. Drug nanocrystals were manufactured by the wet pearl milling technique. In polymeric film formulations, hydroxypropyl methyl cellulose (HPMC) was used as a film forming polymer, and glycerin was used as a plasticizer. For nanocrystal suspensions and film formulations, thorough physicochemical characterization was performed, including particle sizing and size deviation, film appearance, weight variation, thickness, folding endurance, drug content uniformity, disintegration time, and dissolution profile. After milling, the nanoparticles were 369 nm in size with a PI value of 0.20. Nanoparticles were stable and after redispersion from film formulations, the particle size remained almost the same (330 nm and PI 0.16). The produced films were flexible, homogeneous, fast disintegrating, and drug release rate from both the nanosuspension and film formulations showed immediate release behavior. Based on the study, the film casting method for production of itraconazole nanocrystal based immediate release formulations is a good option for improved solubility.

中文翻译：

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伊曲康唑纳米晶体基聚合物薄膜制剂的生产，可立即释放药物

为了改善BCS II类药物伊曲康唑的溶解性，制备了基于伊曲康唑纳米晶体的快速溶解的口服聚合物膜制剂。药物纳米晶体通过湿珠磨技术制备。在聚合物膜配方中，羟丙基甲基纤维素（HPMC）用作成膜聚合物，甘油用作增塑剂。对于纳米晶体悬浮液和薄膜制剂，进行了彻底的理化表征，包括颗粒大小和尺寸偏差，薄膜外观，重量变化，厚度，耐折性，药物含量均匀性，崩解时间和溶出度。研磨后，纳米粒子的尺寸为369 nm，PI值为0.20。纳米粒子稳定，并且从薄膜配方中重新分散后，粒径几乎保持不变（330 nm和PI 0.16）。所产生的膜是柔性的，均匀的，快速崩解的，并且纳米悬浮液和膜制剂的药物释放速率均显示出立即释放行为。基于该研究，用于生产伊曲康唑纳米晶体速释制剂的薄膜流延方法是提高溶解度的好选择。