贝达奎林烟酸的配方开发,表征和评估 - - Soluplus® - - 固体分散剂
Vishwas P Pardhi1, Manisha Patel1, Keerti Jain1
1Department of Pharmaceutics, Drug Delivery and Nanomedicine Research Laboratory, National Institute of Pharmaceutical Education and Research (NIPER), Raebareli, India.
Pharmaceutical development and technology
|April 29, 2024
概括
使用基于Soluplus的固体分散剂,增强了贝达基林烟酸 (BQF) 的溶解性和生物可用性. 三级固体分散物显著改善了BQF.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 生物制药生物制药公司
背景情况:
- 贝达基林烟酸 (BQF) 具有较差的水溶性和溶解性,由于其BCSII类分类,限制了其生物利用性.
- 之前的研究使用了晶体聚合物,如Poloxamer 188用于BQF固体分散,显示了适度的可溶性改善.
- 无形聚合物为提高难溶性药物的可溶性提供了潜在的优势.
研究的目的:
- 为了增强贝达基林烟酸 (BQF) 的生物制药性质.
- 使用Soluplus®开发和描述BQF的二进制 (BSD) 和三进制固体分散 (TSD).
- 评估Soluplus®对BQF可溶性,溶解,细胞吸收和生物可用性的影响.
主要方法:
- 用Soluplus®制备BQF的二元固体分散 (BSD) 和三元固体分散 (TSD).
- 可溶性和溶解研究比较BQF,BSD和TSD.
- 固态特征 (例如,FTIR) 和Caco-2细胞系中的细胞吸收研究.
- 开发的固体分散配方的药理动力学评估.
主要成果:
- 与纯BQF相比,BQF的可溶性在BSD中增加了14.31倍,在TSD中增加了20.43倍.
- 与波洛克萨默188.8相比,Soluplus®证明了BQF的优越可溶性增强.
- 鉴定证实了BQF在固体分散中的无形状态,没有化学相互作用.
- 对于TSDs,观察到增强的细胞吸收和显著改善的药物动力学特征,包括生物可用性.
结论:
- 用无形Soluplus®配制的固体分散剂代表了改善BQF生物制药性能的有希望的策略.
- 三级固体分散 (TSD) 显示出提高BQF可溶性和生物利用性的优越潜力.
- 这种配方方法提供了一种可行的解决方案,以克服与BQF等溶解不良药物相关的生物可用性挑战.
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