通过Sepineo P600乳化剂进行局部药物递送:质学,物理稳定性和配方性能之间的关系
Abu Zayed Md Badruddoza1, Md Ikhtiar Zahid2, Taylor Walsh3
1Pharmaceutical Sciences Small Molecule, Pfizer Worldwide Research and Development, Groton, CT 06340, USA.
International journal of pharmaceutics
|May 8, 2024
概括
这项研究优化了使用Sepineo P600.00进行局部药物递送的油在水乳化剂. 较高的Sepineo P600度提高了稳定性,但由于粘度增加和离子相互作用,降低了药物释放和皮肤透率.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 局部药物输送需要具有最佳微观结构和物理稳定性的配方,以提高疗效.
- 基于乳液的凝 (乳液) 提供了改善局部药物输送的潜力.
- 控制乳化物特性对于可预测的药物释放和皮肤透至关重要.
研究的目的:
- 开发和优化油在水 (O/W) 乳化剂,以改善局部药物输送.
- 研究Sepineo P600度对乳膜微观结构,物理稳定性和质性质的影响.
- 评估含有利多卡因的乳化剂的体外药物释放和皮肤透概况.
主要方法:
- 含有2.0%重量百分比利多卡因的乳化剂配方,含有不同度的Sepineo P600 (0.75-5.0%重量百分比).
- 乳化剂的特征包括滴滴大小,物理稳定性,风湿学,体外药物释放和皮肤透.
- 分析乳化物特性与药物输送性能之间的关系.
主要成果:
- 塞皮尼奥P600度显著影响了乳膜微观结构,质和稳定性,稳定配方至少需要1.0%的重量.
- 所有配方都表现出理想的非牛顿式剪切稀释行为.
- 由Sepineo P600驱动的乳粘度和刚度增加,降低了药物释放和皮肤透率.
- 观察到利多卡因和Sepineo P600之间的离子相互作用,降低了热力学活性和皮肤流量,同时增加了聚合物度.
结论:
- 在局部应用中,Sepineo P600 能够有效地稳定乳化剂并调节其质性质.
- 乳化剂的特性,特别是质和离子相互作用,显著影响了利多卡因的局部输送.
- 这项研究通过将微观结构,稳定性和药物输送特征联系起来,为设计优化的乳化剂配方提供了洞察力.
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