一种双羟萘酸雷沙吉兰长效缓释微球及其制备方法

By preparing long-acting sustained-release microspheres of rasagiline dihydroxynaphthyl acid and polylactic acid polymers, the problems of low drug loading and unstable release of rasagiline sustained-release formulations have been solved, achieving long-acting drug release and simplifying the preparation process, making it suitable for the treatment of Parkinson's disease.

CN121754491BActive Publication Date: 2026-07-17UNIV OF JINAN

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
UNIV OF JINAN
Filing Date
2026-03-03
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing rasagiline extended-release formulations suffer from low drug loading, short release cycles, severe burst release, and complex manufacturing processes, making it difficult to meet the long-term treatment needs of Parkinson's disease patients.

Method used

Long-acting sustained-release microspheres were prepared using rasagiline dihydroxynaphthyl acid and polylactic acid polymers. The drug release rate was controlled by adjusting the proportion of low molecular weight polylactic acid and lowering the curing temperature. The preparation process was simplified by using a single emulsion solvent evaporation method.

Benefits of technology

It achieves high drug loading and high encapsulation efficiency, stable drug release, and a release cycle of up to four weeks, making it suitable for industrial production, reducing biocompatibility risks, and expanding the scope of clinical application.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明涉及药物制剂技术领域,具体公开了一种双羟萘酸雷沙吉兰长效缓释微球及其制备方法,所述长效缓释微球包含双羟萘酸雷沙吉兰和聚乳酸类聚合物,其具有良好的缓释效果。所述制备方法是首先将雷沙吉兰制成双羟萘酸盐以降低雷沙吉兰的溶解度;在所述长效缓释微球的制备过程中,通过调节低分子量聚乳酸的比例以实现对药物释放速率的调控,且通过降低固化温度以减少药物突释现象,该制备工艺适合工业化放大生产。最终获得的长效缓释微球组合物可用于制备治疗帕金森病的药物。
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