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

被引:2
作者
Weecharangsan, Wanlop [1 ]
Lee, Robert J. [2 ]
机构
[1] Srinakharinwirot Univ, Fac Pharm, Dept Pharmaceut Technol, Nakhonnayok 26120, Thailand
[2] Ohio State Univ, Coll Pharm, Div Pharmaceut & Pharmacol, Columbus, OH 43210 USA
来源
AAPS PHARMSCITECH | 2024年 / 25卷 / 07期
关键词
Surface solid dispersion; Trehalose dihydrate; Spray drying; Dissolution rate; Crystalline; BIOAVAILABILITY; MECHANISMS;
D O I
10.1208/s12249-024-02941-4
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
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页数:10
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