口服生物可用性提高不太溶解的药物通过无形固体分散使用糖酸盐异酸盐
Eman M Mohamed1,2, Sathish Dharani1, Tahir Khuroo1
1Irma Lerma Rangel School of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, Texas, 77843-1114, U.S.A.
AAPS PharmSciTech
|September 5, 2024
概括
这项研究使用酸异酸盐 (SAIB) 开发了阿普雷皮坦的无形固体分散 (ASD),显示出可比的稳定性和生物可用性与基于HPMC的不溶性药物的配方相比.
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:
- 溶解不良的药物对生物可用性构成重大挑战.
- 无形固体分散 (ASDs) 是一种有前途的策略,可以提高药物的溶解性和吸收性.
- 甘酸异酸盐 (SAIB) 正在作为一种新的ASD配方辅助剂进行研究.
研究的目的:
- 使用SAIB开发和描述阿普雷皮坦 (APT) 的无形固体分散 (ASD).
- 评估基于SAIB的ASD的物理化学特性,稳定性和生物可用性.
- 为了比较基于SAIB的ASD配方与基于基甲基纤维素 (HPMC) 的配方.
主要方法:
- 阿普雷皮坦 (APT) ASD配方是使用溶剂蒸发方法制备的.
- 描述包括用于药物阶段分析的X射线粉末衍射 (XRPD).
- 进行了体外溶解研究,稳定性测试 (25°C/60%RH和40°C/75%RH),以及体外药理动力学研究.
主要成果:
- 在ASD中,XRPD证实了晶体阿普雷皮坦的转化为无形状态.
- 优化的SAIB配方 (F10) 呈现出超过80%的溶解,与HPMC配方 (F13) 相比.
- 两种F10和F13配方都表现出可比的稳定性,并且具有生物等价性,与晶体阿佩皮坦特相比,生物可用性显著提高 (超过两倍).
结论:
- SAIB 是一种可行的辅助剂,用于开发稳定且生物可利用的不溶性固体分散剂的不溶性药物.
- 基于SAIB的ASD配方提供了与传统基于HPMC的配方可比的性能.
- 这项研究突出了改善具有挑战性的药物化合物的口服输送的潜在新方法.
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