College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.
Arch Pharm Res. 2013 Jan;36(1):86-93. doi: 10.1007/s12272-013-0012-y.
The purpose of this study was to develop a raloxifene-loaded solid dispersion with enhanced dissolution rate and bioavailability via spray-drying technique. Solid dispersions of raloxifene (RXF) were prepared with PVP K30 at weight ratios of 1:4, 1:6 and 1:8 using a spray-drying method, and characterized by differential scanning calorimetry, X-ray powder diffraction, scanning electron microscopy, and solubility and dissolution tests. The bioavailability of the solid dispersion in rats was also evaluated compared to those of RXF powder and commercial product. Results showed that the RXF-loaded solid dispersion was in amorphous form with increased solubility and dissolution rate. The absorption of RXF from solid dispersion resulted in approximately 2.6-fold enhanced bioavailability compared to pure drug. Moreover, RXF-loaded solid dispersion gave similar AUC, C(max) and T(max) values to the commercial product, suggesting that it was bioequivalent to the commercial product in rats. These findings suggest that an amorphous solid dispersion of RXF could be a viable option for enhancing the oral bioavailability of RXF.
本研究旨在通过喷雾干燥技术制备一种载有雷洛昔芬的固体分散体,以提高其溶解速率和生物利用度。采用喷雾干燥法,以重量比为 1:4、1:6 和 1:8 将雷洛昔芬(RXF)与 PVP K30 制成固体分散体,并通过差示扫描量热法、X 射线粉末衍射、扫描电子显微镜和溶解度及溶解试验进行了表征。还比较了固体分散体在大鼠体内的生物利用度与 RXF 粉末和市售产品的生物利用度。结果表明,载有 RXF 的固体分散体呈无定形状态,溶解度和溶解速率提高。与纯药物相比,固体分散体中 RXF 的吸收使生物利用度提高了约 2.6 倍。此外,载有 RXF 的固体分散体与市售产品的 AUC、C(max)和 T(max)值相似,表明其在大鼠体内与市售产品生物等效。这些发现表明,雷洛昔芬的无定形固体分散体可能是提高雷洛昔芬口服生物利用度的一种可行选择。