a Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals , Zhejiang University of Technology , Hangzhou , PR China.
J Microencapsul. 2018 Aug;35(5):454-466. doi: 10.1080/02652048.2018.1526339. Epub 2018 Dec 27.
The research aimed to prepare febuxostat (FEB) solid dispersion through solvent evaporation. Optimised solid dispersion composed of FEB, polyvinylpyrrolidone (PVP K30) and poloxamer at a ratio of 1:3:3 was characterised. Powder X-ray diffraction (XRD) and differential scanning calorimetry (DSC) indicated FEB was transformed from crystalline into the amorphous state in solid dispersion and scanning electron microscopy (SEM) revealed the morphology. Fourier transform infrared spectroscopy (FT-IR) suggested the interactions formed between FEB and polymers. A remarkable increase was observed of the optimised formulation in saturation solubility, dissolution studies (96.17 ± 0.79% in pH 6.0), and bioavailability (C 18.25 ± 2.44 vs. 7.72 ± 0.48 μg/mL and AUC 53.62 ± 7.63 vs. 34.76 ± 2.45 μg·h/mL). Besides, the FEB solid dispersion showed great stability after 90 days storage. Thus, the present study supports the rationality of PVP K30 and poloxamer188 as co-carriers for the preparation of FEB solid dispersion.
本研究旨在通过溶剂蒸发法制备非布司他（FEB）固体分散体。对由 FEB、聚乙烯吡咯烷酮（PVP K30）和泊洛沙姆以 1:3:3 的比例组成的优化固体分散体进行了表征。粉末 X 射线衍射（XRD）和差示扫描量热法（DSC）表明 FEB 在固体分散体中从结晶态转变为无定形态，扫描电子显微镜（SEM）揭示了其形态。傅里叶变换红外光谱（FT-IR）表明 FEB 与聚合物之间形成了相互作用。优化配方的饱和溶解度、溶解研究（在 pH 6.0 下为 96.17±0.79%）和生物利用度（C 18.25±2.44 与 7.72±0.48μg/mL 和 AUC 53.62±7.63 与 34.76±2.45μg·h/mL）均显著提高。此外，FEB 固体分散体在 90 天储存后表现出良好的稳定性。因此，本研究支持 PVP K30 和泊洛沙姆 188 作为制备 FEB 固体分散体的共载体的合理性。
