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一项比较性研究关于循环二烯衍生物在改善口服生物可用性埃托里可西布作为模型药物的比较研究:固体分散式快速溶解片剂的配方和评估
Doaa Elsegaie1, Mohamed A El-Nabarawi2, Hanaa Abdelmonem Mahmoud2
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Heliopolis University, Cairo 11785, Egypt.
Biomedicines
|September 28, 2023
概括
这项研究改善了埃托里可西布.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
背景情况:
- 埃托里可西布具有较差的溶解性和溶解性,限制了其治疗效果.
- 循环二烯衍生物是一种有前途的方法,可以提高难以溶解药物的可溶性.
研究的目的:
- 通过使用不同的循环二烯衍生物 (β-CD,HP β-CD,SBE β-CD) 来制备和评估埃托里可西布的固体分散剂.
- 从优化的固体分散物中制备快溶性片,并评估它们的体外和体内性能.
- 为了比较优化配方的生物利用率与市场上销售的 etoricoxib 产品.
主要方法:
- 对三种循环德克斯特林衍生物 (β-CD,HP β-CD,SBE β-CD) 的比较评价,用于埃托里可西布固体分散配方.
- 使用各种药物:载体比率 (1:1, 1:2, 1:4) 和超级分解剂 (Prosolv ODT®,F-melt® type C) 制备快速溶解片.
- 使用3^2因数设计和体外溶解试验进行优化.
- 在子模型中进行体内药理动力学研究,将优化配方 (SD-HP3) 与Arcoxia®进行比较.
主要成果:
- 优化的配方 (SD-HP3) 包含埃托利可西布:HP β-CD (1:4比) 与Prosolv ODT®和F-melt® C型混合物,达到高可取性 (0.86).
- 与Arcoxia®相比,体内研究表明SD-HP3的药理动力学参数显著增强.
- SD-HP3表现出较低的Tmax (13.3分钟),更高的Cmax (9122.156微克/毫升) 和增加的AUC,表明生物可用性得到改善.
结论:
- 埃托利可西布的固体分散与基基β-环氧化 (HP β-CD) 有效地提高了其可溶性和溶解率.
- 与SD-HP3配制的快速溶解片提供优越的药理动力学性能,与传统的市场上销售的产品相比.
- 这种方法提供了一个可行的策略,以改善口服生物可用性,像 etoricoxib 这样的溶性较差的药物.
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