Rapid dissolving high potency danazol powders produced by spray freezing into liquid process.
Rapid dissolving high potency danazol powders produced by spray freezing into liquid process.
复制标题
DOI：
10.1016/j.ijpharm.2003.11.003
复制
发表时间：
2004-03
影响因子：
5.8
通讯作者：
Jiahui Hu;K. Johnston;R. Williams
中科院分区：
文献类型：
--
作者：
Jiahui Hu;K. Johnston;R. Williams
本研究的目的是探讨使用有机溶剂在喷雾冷冻成液（SFL）颗粒工程过程中，快速溶解的高效达那唑粉末，并检查其粒径，表面积和溶解速率。SFL微粉化达那唑/PVP K-15产生的最大药物效力为91%。XRD分析表明，高效SFL粉末中达那唑为无定形。SEM照片显示，SFL达那唑/PVP K-15纳米聚集体具有多孔结构，由许多直径约100 nm的光滑初级纳米粒子组成。SFL达那唑/PVP K-15高效粉末的比表面积在28- 115 m2/g的范围内。SFL粉末表现出显著增强的溶出速率。微粉化原料达那唑的溶出速率较慢，2 min内仅溶出30%。然而，对于SFL高效粉末，95%的达那唑仅在2 min内溶解。SFL方法提供了一种高效的方法来生产包含在具有快速溶解速率的较大结构化聚集体中的高效达那唑纳米颗粒，并且特别适用于含有水溶性差的药物的递送系统。
The objective of this study was to investigate the use of organic solvents in the spray freezing into liquid (SFL) particle engineering process to make rapid dissolving high potency danazol powders and to examine their particle size, surface area and dissolution rate. The maximum drug potency produced was 91% for SFL micronized danazol/PVP K-15. XRD indicated that danazol in the high potency SFL powders was amorphous. SEM micrographs revealed that the SFL danazol/PVP K-15 nanostructured aggregates had a porous morphology and were composed of many smooth primary nanoparticles with a diameter of about 100nm. Surface areas of SFL danazol/PVP K-15 high potency powders were in the range of 28–115m2/g. The SFL powders exhibited significantly enhanced dissolution rates. The rate of dissolution of micronized bulk danazol was slow; only 30% of the danazol was dissolved in 2min. However, 95% of danazol was dissolved in only 2min for the SFL high potency powders. The SFL process offers a highly effective approach to produce high potency danazol nanoparticles contained in larger structured aggregates with rapid dissolution rates, and is especially applicable to delivery systems containing poorly water soluble drugs.