基于多电解质的固体分散剂,以提高西尔代纳菲尔酸盐的溶解和pH独立的受控释放
Ju-Hyeong Woo1, Hai V Ngo1, Hy D Nguyen1
1College of Pharmacy, Ajou University, Suwon 16499, Republic of Korea.
Heliyon
|December 25, 2023
概括
这项研究开发了一种使用固体分散和多电静态相互作用的新型矩阵片来实现提升,pH独立的西尔德纳菲尔酸盐 (SIL) 释放. 这种方法可以改善溶解和生物可用性,使难以溶解的药物.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 西尔德纳菲尔酸盐 (SIL) 具有依赖pH值的溶解性,这对药物递送的一致性构成了挑战.
- 开发具有受控和pH独立的药物释放的口服剂型对于提高治疗疗效至关重要.
- 矩阵片为控制药物释放提供了一个多功能平台,但实现pH独立可能是复杂的.
研究的目的:
- 设计一种新型的矩阵片,用于提升西尔代纳菲尔酸盐 (SIL) 的溶解和pH独立的受控释放.
- 利用固体分散 (SD) 和多电静态相互作用来克服SIL的pH依赖性溶解度.
- 研究聚合物载体和充电聚合物在调节SIL释放中的作用.
主要方法:
- 使用各种聚合物 (poloxamer 188,poloxamer 407,Soluplus®,PVP K12,PVP K17) 通过溶剂蒸发来制备西尔德纳菲尔酸盐 (SIL) 装载固体分散剂 (SD).
- 最有效的聚合物 (Soluplus®) 被纳入一个含有奇多 (正电荷) 和Eudragit® L100 (负电荷) 的矩阵片中.
- 在不同的pH条件下 (pH1.2和pH6.8) 进行了药物释放研究,以评估溶解概况和pH依赖性.
主要成果:
- 基于Soluplus®的SDs在6小时内在pH 6.8的肠液中显著增强了SIL溶解.
- 在基于Soluplus®的SD中,发现SIL处于无形状态,有助于提高溶解度.
- 在矩阵片中,Soluplus® SDs与奇托和Eudragit® L100的组合导致了进一步调节的,受控的药物释放.
- 与pH 1.2相比,pH 6.8的电荷密度较高,由于多电静电相互作用,促进了pH独立的SIL释放.
结论:
- 使用基于Soluplus®的固体分散和多电静态相互作用的组合方法有效地改善了西尔德纳菲尔酸盐的溶解.
- 这一策略使SIL从矩阵片制剂中独立于pH值的受控释放成为可能.
- 开发的方法对设计水溶性较差的药物的矩阵片具有前景,可能会提高其生物可用性.
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