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固体自乳化素载体用于改善simvastatin口服生物可用性

Han Li¹, Haixia Sun², Yanbing Zhao³

¹Intervention and Cell Therapy Center, Peking University Shenzhen Hospital, Shenzhen Peking University-The Hong Kong University of Science and Technology Medical Center, Shenzhen, PR China; The GBA National Institute for Nanotechnology Innovation, Guangdong Cannano Anew Medicine Co., Ltd, 136 Kaiyuan Avenue, Guangzhou 510700, PR China.

International journal of biological macromolecules

|April 15, 2024

概括

一种新型的素稳定固体自我乳化载体 (Cas-SSE) 显著提高了simvastatin (SV) 的口服生物可用性,simvastatin是一种不溶于水的药物. 这种输送系统为改善药物吸收和疗效提供了一个有希望的方法.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
生物相容性材料生物相容性材料

背景情况:

辛巴斯塔丁 (SV) 对于控制胆固醇和预防心血管疾病至关重要.
SV具有较差的水溶性和较低的口服生物可用性 (<5%),限制了其治疗效果.
固体自乳化系统比液体乳液提供更高的稳定性,以提高药物的溶解性和生物可用性.

研究的目的:

开发和评估一种用素稳定的固体自我乳化载体 (Cas-SSE),以改善simvastatin的溶解性和口服生物利用性.
为优化Cas-SSE系统的配方和乳化过程.
为了比较Cas-SSE与常规simvastatin片的性能.

主要方法:

使用配方选择和乳化过程优化来创建Cas-SSE.
在体外药物释放研究中,使用人工肠液进行了实验.
进行了避免肠囊实验和体内药理学研究,以评估药物吸收和生物可用性.

主要成果:

与口服药片相比,Cas-SSE显著提高了simvastatin在体外释放的速度.
发现某些水溶性分散剂 (如基乙烯粉) 阻碍了药物吸收.
药物动力学研究表明,没有分散剂的Cas-SSE比SV片获得了相对更高的生物可用性 (184.1%的SV,284.5%的simvastatin酸).

结论:

开发的素稳定固体自乳化载体 (Cas-SSE) 有效地提高了simvastatin的溶解性和口服生物可用性.
Cas-SSE是一个有希望的,生物相容的药物输送平台,用于水溶性较差的药物.
缺乏特定的分散剂对于最大限度地提高Cas-SSE系统提供的生物可用性至关重要.

关键词:

生物可用性生物可用性氨酸 (casein) 是一种氨酸.西姆瓦斯塔丁是一种固体自乳化药物输送系统固体自乳化药物输送系统

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