Surface Solid Dispersion of Ketoconazole on Trehalose Dihydrate using Spray Drying to Achieve Enhanced Dissolution Rate

IF 4.3 3区材料科学 Q1 ENGINEERING, ELECTRICAL & ELECTRONIC ACS Applied Electronic Materials Pub Date : 2024-09-23 DOI:10.1208/s12249-024-02941-4

Wanlop Weecharangsan, Robert J. Lee

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Abstract

Ketoconazole (K) is a poorly water-soluble drug that faces significant challenges in achieving therapeutic efficacy. This study aimed to enhance the dissolution rate of ketoconazole by depositing spray-dried ketoconazole (SK) onto the surface of ground trehalose dihydrate (T) using spray drying. Ketoconazole-trehalose surface solid dispersions (SKTs) were prepared in ratios of 1:1 (SK1T1), 1:4 (SK1T4), and 1:10 (SK1T10), and characterized them using particle size analysis, scanning electron microscopy, powder X-ray diffraction, and in vitro dissolution studies. Results showed that the dissolution rates of the dispersions were significantly higher than those of pure ketoconazole, with the 1:10 ratio showing the highest dissolution rate. The improved dissolution was attributed to the formation of a new crystalline phase and better dispersion of ketoconazole particles. These findings suggest that the surface solid dispersion approach could be a valuable method for enhancing the bioavailability of poorly water-soluble drugs.

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利用喷雾干燥法将酮康唑表面固体分散在二水曲哈洛糖上以提高溶解率

酮康唑（K）是一种水溶性较差的药物，在实现疗效方面面临巨大挑战。本研究旨在通过喷雾干燥法将喷雾干燥的酮康唑（SK）沉积在磨碎的二水曲哈洛糖（T）表面，从而提高酮康唑的溶出率。研究人员以 1:1 (SK1T1)、1:4 (SK1T4) 和 1:10 (SK1T10) 的比例制备了酮康唑-曲哈洛糖表面固体分散体（SKTs），并利用粒度分析、扫描电子显微镜、粉末 X 射线衍射和体外溶解研究对其进行了表征。结果表明，分散体的溶出率明显高于纯酮康唑，其中 1:10 比率的溶出率最高。溶出率的提高归因于新晶相的形成和酮康唑颗粒的更好分散。这些研究结果表明，表面固体分散方法是提高水溶性差药物生物利用度的重要方法。

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