The preparation and characteristics of febuxostat SiO2 solid dispersions

doi:10.5246/jcps.2014.07.061

Journal of Chinese Pharmaceutical Sciences ›› 2014, Vol. 23 ›› Issue (7): 463-470.DOI: 10.5246/jcps.2014.07.061

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The preparation and characteristics of febuxostat SiO2 solid dispersions

Wending Song¹, Ruo Du¹, Ping Song¹, Ting Zhong¹, Weiqiang Zhang¹, Yang Zhao¹, Chao Wang¹, Xuan Zhang^1,2*, Qiang Zhang^1,2

1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Sciences Center, Beijing 100191, China
2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Sciences Center, Beijing 100191, China

Received:2014-05-05 Revised:2014-05-14 Online:2014-07-18 Published:2014-05-31
Contact: Tel.: +86-10-82805928, Fax: +86-10-82805928
Supported by:
National Natural Science Foundation of China (Grant No. 81172992) and the National Basic Research Program of China (Grant No. 973 Program 2009CB930300) and Innovation Team of Ministry of Education (Grant No. BMU20110263).

Abstract

Abstract:

In the present research, we selected Sylysia as a porous material and febuxostat (FBT) as model drug to prepare the FBT SiO₂ solid dispersions using a solvent evaporation method. We firstly established an HPLC method for determining FBT in our prepared FBT SiO₂ solid dispersions. And then, the characteristics of FBT SiO₂ solid dispersions were investigated, including differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscope (SEM), particle size and distribution. The solubility and dissolution of FBT SiO₂ solid dispersion were also evaluated. The results of DSC and PXRD showed that the FBT existed in an amorphous state in FBT SiO₂ solid dispersions. The SEM and particle size results indicated that the shape and average particle size of FBT SiO₂ solid dispersions was similar to the Sylysia. The solubility and dissolution of FBT in FBT SiO₂ solid dispersions were significantly enhanced compared with the pure FBT. In conclusion, we successfully prepared FBT SiO₂ solid dispersions to increase the solubility and dissolution rate of the poorly water-soluble FBT.

Key words: Febuxostat, Sylysia, Solid dispersion, Solubility and dissolution

CLC Number:

R943

Supporting:

Wending Song, Ruo Du, Ping Song, Ting Zhong, Weiqiang Zhang, Yang Zhao, Chao Wang, Xuan Zhang, Qiang Zhang. The preparation and characteristics of febuxostat SiO2 solid dispersions[J]. Journal of Chinese Pharmaceutical Sciences, 2014, 23(7): 463-470.

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The preparation and characteristics of febuxostat SiO2 solid dispersions

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