One of the conventional methods of alleviating the problem of poor drug solubility is the particle size reduction. The efficiency of this approach depends on successful formulation suppressing the drug agglomeration. The aim of this study was to circumvent the dissolution problems of model hydrophobic meloxicam drug (MLX) by using liquid media of different wetting capacity to comminute and formulate a rapidly dissolving carrier system without the use of surfactants. Micro-suspensions of MLX were prepared by ball milling, using water or n-Heptane as a liquid medium. The suspensions were used as granulation liquids to formulate granulate from microcrystalline cellulose and lactose mixture. The release kinetics from prepared granulates were studied using the USP-4 dissolution apparatus. Micro-suspensions prepared via wet milling in non-water liquid media exhibited a massive improvement of release rate compared with source meloxicam and they outperformed their water-milled counterparts. The release rates from those formulations, despite not comprising any surfactant, were comparable to those obtained by different authors using surfactant stabilized nanosuspension formulations. Thus, they can present an interesting formulation alternative for hydrophobic drugs that are dissolution limited.

中文翻译：

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具有在不同液体介质中的微悬浮液制备的具有增强的释放性和水润湿性的美洛昔康载体系统。

减轻药物溶解度差的问题的常规方法之一是减小粒径。这种方法的效率取决于抑制药物聚集的成功配方。这项研究的目的是通过使用不同润湿能力的液体介质粉碎和配制快速溶解的载体体系而不使用表面活性剂来解决模型疏水性美洛昔康药物（MLX）的溶解问题。使用水或正庚烷作为液体介质，通过球磨制备MLX的微悬浮液。将该悬浮液用作制粒液体，以由微晶纤维素和乳糖混合物配制颗粒。使用USP-4溶出度仪研究了制备颗粒的释放动力学。与源美洛昔康相比，在非水液体介质中通过湿磨制备的微混悬液显示出较大的释放速率改善，其性能优于水磨对映体。尽管不包含任何表面活性剂，但这些制剂的释放速率与不同作者使用表面活性剂稳定的纳米悬浮液制剂获得的释放速率相当。因此，它们可以为溶解受限的疏水性药物提供有趣的制剂替代方案。