对帕克利塔克塞尔波洛克萨默188固体分散剂的微观结构,溶解速率和口服生物利用度的评估
Yao Liu1, Yong Zhang1, Qiuli Yan1
1Medical College, Qinghai University, Xining, 810001, Qinghai, People's Republic of China.
Drug delivery and translational research
|August 14, 2023
概括
这项研究使用喷雾干燥,用波洛克萨默188制造帕克利塔塞尔固体分散剂 (SD),显著改善药物的溶解性和口服生物可用性. 与原始药物相比,帕克利塔塞尔固体分散的溶解率和血液度要高得多.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 材料科学 材料科学 材料科学
背景情况:
- 帕克利塔塞尔 (PTX) 溶解度差限制了其口服生物可用性和临床使用.
- 固体分散 (SD) 是一种可行的策略,可以提高难溶性药物的可溶性.
- 作为PTX SD的载体,Poloxamer 188 (P188),一种triblock共聚物,正在被探索.
研究的目的:
- 通过喷雾干燥使用Poloxamer 188 (P188) 制备帕克利塔塞尔固体分散剂 (SD).
- 评估准备好的PTX SD的微观结构,体外溶解和药理动力学特性.
- 评估基于P188的SD的潜力,以改善帕克利塔塞尔口服生物可用性.
主要方法:
- 使用喷雾干燥技术,用波洛克萨默188 (P188) 制备了帕克利塔塞尔固体分散剂 (SD).
- 描述包括微观结构分析和体外溶解研究,使用三个不同的模型.
- 进行了药理动力学研究,以评估PTX SD的体内性能.
主要成果:
- 在P188共聚合物中发现了无形状态的帕克利塔塞尔 (PTX),显示出良好的混合性.
- 来自SD的PTX在体外溶解率明显高于来自物理混合物 (PM) 和原始药物.
- 药理动力学分析显示,与活性药物成分 (API) 相比,PTX SD的AUC增加了6倍,Cmax增加了约20倍.
结论:
- 使用波洛克萨默188 (P188) 的喷雾干燥的帕克利塔塞尔固体分散剂 (SD) 有效地增强了药物的溶解.
- 在P188矩阵内PTX的无形状态是提高溶解度的关键.
- 这些发现表明,通过基于P188的固体分散技术,巴克利塔塞尔口服生物可用性显著改善.
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