水凝和油凝制剂的DecapeptideCetrorelix酸盐用于鼻腔的管理
Philipp Wissel1, Matthias Rischer2, Gert Fricker1
1Heidelberg University, Institute for Pharmacy and Molecular Biotechnology, 69120 Heidelberg, Germany.
概括
通过使用新的oleogel和hydrogel配方实现了Cetrorelix酸盐 (CxAc) 的鼻腔注射. 水凝在老鼠中显示出有前途的吸收和生物可用性,这表明了非侵入性药物输送的潜力.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 生物材料是一种生物材料.
背景情况:
- 酸 (CxAc) 通常通过侵入性途径使用.
- 开发像CxAc这样的的非侵入性输送方法对于患者的遵守性和治疗疗效至关重要.
- 油凝和水凝配方为鼻腔递送提供了潜在的矩阵.
研究的目的:
- 开发和表征油凝和水凝配方,用于Cetrorelix酸盐 (CxAc) 的鼻服.
- 评估这些鼻腔配方的体外特性和体内药理动力学.
- 评估这些配方作为侵入性CxAc管理的非侵入性替代品的潜力.
主要方法:
- 使用多孔的二氧化载体,麻油,Labrafil®和Aerosil®来制备油凝.
- 使用奇托和波洛克萨默407与溶解CxAc.Ac一起制备水凝.
- 试验室表征包括风湿学,粘附和药物释放研究.
- 在鼻子注射后在雄性Wistar大鼠中进行体内药理动力学评估.
主要成果:
- 两种配方均表现出粗热性行为和良好的凝形成/粘合性质.
- 奥莱格尔显示CxAc释放时间长 (>20小时),受孔直径的影响.
- 水凝在体外释放速度更快,但在体内达到更高的Cmax和AUC0→24h,绝对生物利用率为5.3%.
- 药理动力学研究证实,这两种配方在24小时内吸收了.
结论:
- 开发的油凝和水凝配方适用于鼻腔CxAc输送.
- 水凝配方由于有利的药理动力学和生物可用性,显示出CxAc的非侵入性鼻腔输送的巨大潜力.
- 对于临床应用,需要进一步开发水凝配方.
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