Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, Beijing, 100191, China.
AAPS PharmSciTech. 2018 Feb;19(2):934-940. doi: 10.1208/s12249-017-0905-z. Epub 2017 Oct 27.
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.
在这里，选择中孔硅（Sylysia 350）作为中孔材料，羟丙基甲基纤维素（HPMC）作为结晶抑制剂，别嘌醇（FBT）作为模型药物，分别制备了 FBT-Sylysia-HPMC 纳米基质（FBT@SHN）。对 FBT@SHN 的体外和体内特性进行了研究。结果表明，FBT@SHN 中的 FBT 呈无定形形式。FBT@SHN 中 FBT 的溶解度和溶解速率显著提高。与 FBT 混悬剂相比，FBT@SHN 中 FBT 的口服生物利用度提高了 5.8 倍。该纳米基质可用作提高口服生物利用度的药物传递平台。
