中文摘要：

Scopoletin 是拥有许多药理学活动的活跃香豆素，包括 anti-hyperuricemic 效果，但是与差的溶解度。改进它的口头的 bioavailability，我们试图包含 scopoletin 进 Soluplus 微粒(基于 Soluplus 的 scopoletin 微粒， Sco 女士) 并且评估了 Sco-Ms.Sco 女士的 hypouricemic 行动用一个薄电影的水和方法被准备。Sco 女士与 59.4 灭敬整祬戠潬正摥 ? 噓木椭摮 ' 讚?的一种平均尺寸显示了近球形的形状 ?? 桰獯桰牯汹瑡潩 ? 猠杵敧瑳湩 ? 桴瑡 ??? ‵捡楴杮甠獰牴慥? 景 ?? 愠摮瀠??偁欠湩獡 e

英文摘要：

Scopoletin is an active coumarin possessing a variety of pharmacological activities, including anti-hyperuricemic effect, but with poor solubility. To improve its oral bioavailability, we attempted to encapsulate scopoletin into Soluplus micelles （Soluplus-based scopoletin micelles, Sco-Ms） and evaluated the hypouricemic action of Sco-Ms. Sco-Ms were prepared using a thin-film hydration method. Sco-Ms displayed near spherical shapes with an average size of 59.4±2.4 nm （PDI=0.08＋0.02）. The encapsulation efficiency of scopoletin was 87.3%±1.5% with a loading capacity of 5.5%±0.1%. Sco-Ms were further characterized using transmission electron microscopy, powder X-ray diffraction, Fourier transform infrared techniques and scanning electron microscopy. After oral administration in rats, Sco-Ms exhibited significantly improved absorption in each intestinal segment compared to free scopoletin, with the duodenum and jejunum being the main absorption regions. In rats administered Sco-Ms （at an equivalent dose of free scopoletin of 100 mg/kg, po）, the AUC0-∞ and Cm,x of Sco-Ms were 4.38- and 8.43-fold, respectively, as large as those obtained following administration of free scopoletin. After oral administration in rats, Sco-Ms did not alter the tissue distributions of scopoletin, but significantly increased the scopoletin levels in the liver. In potassium oxonate-induced hyperuricemic mice, oral administration of Sco-Ms （at an equivalent dose of free scopoletin of 300 mg/kg） reduced the serum uric acid concentration to the normal level. The results suggest that Soluplus-based micelle system greatly improves the bioavailability of poorly water-soluble drugs, such as scopoletin, and represents a promising strategy for their oral delivery.