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交联原的长效可注射微球封装固体分散,以提高阿里皮普拉的生物可用性

Shanglun Li¹, Xiaoxuan Ji¹, Wei Huang¹

¹School of Pharmacy, Jiangsu University, Zhenjiang 212000, China.

Journal of pharmaceutical sciences

|February 13, 2026

概括

这项研究开发了新型的可注射微球 (APZ@PVP@CC) 用于阿里皮普拉 (APZ),以改善精神分裂症治疗的遵守性. 该配方显著提高了APZ的生物可用性,并在30天内持续释放.

科学领域:

制药科学制药科学
生物材料工程生物材料工程
药物输送系统药物输送系统

背景情况:

治疗精神分裂症的口服阿里皮普拉 (APZ) 配方面临患者遵守问题的问题.
随着pH值的增加,APZ的溶解性降低,限制了肌内注射的生物可用性.
需要新的注射配方来克服这些局限性.

研究的目的:

开发一种可注射的阿里皮普拉配方 (APZ@PVP@CC) 具有增强的溶解性和生物利用性.
创建一个长效的交付系统,以改善精神分裂症管理.
为了优化APZ固体分散在交叉连接的原体微球中的制备.

主要方法:

基于聚烯 (PVP) 的优化APZ固体分散 (APZ@PVP) 使用单轴电喷.
合成交联原蛋白 (CC) 并使用同轴电喷涂涂层APZ@PVP.
使用SEM,XRD,体外释放研究和在子中的药理动力学分析进行了APZ@PVP@CC的特征化.

主要成果:

APZ@PVP固体分散显示APZ溶解度增加了15倍,并增强了体外释放.
APZ@PVP@CC显示持续释放超过30天,遵循希克森-克劳尔模型 (表面侵蚀).
药理动力学研究表明,与微晶体相比,生物可用性和30天长效释放增加了225%.

结论:

APZ@PVP@CC微球为阿里皮普拉提供了一个有前途的注射配方.
这种配方增强了APZ的生物可用性,并提供持续释放,解决了精神分裂症治疗中的合规性和有效性问题.
开发的微球代表了长期精神分裂症治疗的修改后,有效的选择.

关键词:

阿里皮普拉 (aripiprazole) 是一种药物.生物可用性生物可用性交叉连接的原蛋白.长效注射式微球长效注射式微球固体的分散固体的分散

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