Abstract：
Fenofibrate (FNF) is used to treat hyperlipidemia. However, FNF is a poorly water-soluble drug, and the dosage of commercial products is relatively high at 160 mg in a Lipidil® tablet. Therefore, this study aimed to develop an FNF-solid dispersion (SD) that solubilizes and stabilizes FNF. The melting method that uses the low melting point of FNF was employed. The dissolution percentage of FNF in the optimal formulation (SD2) increased by 1.2-, 1.3-, and 1.3-fold at 5 min compared to that of Lipidil® and increased by 2.0-, 2.1-, and 2.0-fold compared to the pure FNF in pH 1.2 media, distilled water, and pH 6.8 buffer, which included 0.025 M sodium lauryl sulfate, respectively. The SD2 formulation showed a dissolution percentage of nearly 100 % in all dissolution media after 60 min. The physicochemical properties of the SD2 formulation exhibited slight changes in the melting point and crystallinity of FNF. Moreover, the stability of the SD2 formulation was maintained for six months. In particular, it was challenging to secure stability when starch#1500 was excluded from the SD2 formulation. In conclusion, the dissolution percentage of FNF in the SD2 formulation was improved owing to the weak binding force between FNF and the excipients, stability was secured, and favorable results are expected in future animal experiments.
摘要：
非诺贝特(FNF)用于治疗高脂血症。然而,FNF是一种水溶性差的药物，在Lipidil®片剂中,商业产品的剂量相对较高,为160mg。因此,这项研究旨在开发一种溶解和稳定FNF的FNF-固体分散体（SD）。采用使用低熔点FNF的熔融方法。最佳配方（SD2）中FNF的溶出百分比增加了1.2-，1.3-,与Lipidil®相比，5分钟时增加了1.3倍，增加了2.0-，2.1-,与pH1.2介质中的纯FNF相比是2.0倍，蒸馏水,和pH6.8缓冲液，其中包括0.025M十二烷基硫酸钠，分别。SD2制剂在60分钟后在所有溶出介质中显示出近100%的溶出百分比。SD2制剂的物理化学性质表现出FNF的熔点和结晶度的轻微变化。此外，SD2制剂的稳定性维持6个月.特别是,当从SD2制剂中排除淀粉#1500时,确保稳定性是具有挑战性的。总之,由于FNF和赋形剂之间的弱结合力，FNF在SD2制剂中的溶出度得到改善，稳定性得到了保证，在未来的动物实验中有望获得良好的结果。
