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. 2018 Feb;19(2):934-940.
doi: 10.1208/s12249-017-0905-z. Epub 2017 Oct 27.

Improving Solubility and Oral Bioavailability of Febuxostat by Polymer-Coated Nanomatrix

Yi-Fan Yin  1   2 , Yang Guo  1   2 , Wen-Ding Song  1   2 , Xiao-Chuan Duan  1   2 , Xiu-Chai Zheng  1   2 , Ting Zhong  1   2 , Shuang Zhang  1   2 , Xin Yao  1   2 , Mei-Qi Xu  1   2 , Qiang Zhang  1   2   3 , Xuan Zhang  4   5
Affiliations

Improving Solubility and Oral Bioavailability of Febuxostat by Polymer-Coated Nanomatrix

Yi-Fan Yin et al. AAPS PharmSciTech. 2018 Feb.

Abstract

Here, the mesoporous silica (Sylysia 350) was selected as mesoporous material, hydroxypropyl methylcellulose (HPMC) was selected as crystallization inhibitor, and febuxostat (FBT) was selected as model drug, respectively. The FBT-Sylysia-HPMC nanomatrix (FBT@SHN) was prepared. The characteristics of FBT@SHN were investigated in vitro and in vivo. Our results indicated that the FBT in FBT@SHN was in amorphous form. The solubility and dissolution of FBT in FBT@SHN were significantly increased. The oral bioavailability of FBT in FBT@SHN was greatly improved 5.8-fold compared with that in FBT suspension. This nanomatrix could be used as a drug delivery platform for improving the oral bioavailability.

Keywords: HPMC; febuxostat; nanomatrix; oral bioavailability.

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