Perampanel long-acting controlled release microsphere and preparation method thereof

The preparation of long-acting controlled-release microspheres of perampanel using microfluidic technology solves the problems of encapsulation efficiency and particle size uniformity of existing microspheres, achieving long-acting sustained release and precise controlled release, thus meeting the needs of long-acting drug use and prevention of abuse.

CN121401239APending Publication Date: 2026-01-27四川迈可隆生物科技有限公司
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Patent Information

Application Number
CN202511902659.0
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-06-06
Publication Date
2026-01-27

AI Technical Summary

Technical Problem

The existing perampanel microspheres have large differences in encapsulation efficiency and poor particle size uniformity, making it difficult to achieve stable commercial production. In addition, the existing dosage forms have high dosing frequency, poor administration convenience, and large fluctuations in blood drug concentration, which cannot meet the needs of long-acting controlled release and prevention of abuse.

Method used

Long-acting controlled-release microspheres of perampanel were prepared using a microfluidic method. By adjusting the ratio of the internal and external phase solutions, and using PLGA and surfactants, the release rate and particle size uniformity of the microspheres were controlled. By combining different PLGA molecular weights, long-acting sustained release was achieved.

Benefits of technology

It achieves uniform size and quality stability of microspheres, precise controlled release, and sustained release period of several weeks to several months, reducing the risk of side effects and meeting the needs of long-acting medication and prevention of abuse.

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Abstract

The invention belongs to the field of medicines, and particularly relates to a perampanel long-acting controlled-release microsphere and a preparation method thereof. The invention aims to provide a long-acting and precise controlled-release perampanel microsphere which is prepared from an internal phase solution and an external phase solution by adopting a microfluidic method, wherein the internal phase solution comprises perampanel and a derivative thereof, PLGA (poly (lactic-co-glycolic acid)) and a good solvent of the perampanel and the derivative thereof; the external phase solution comprises a surfactant, a good solvent of the surfactant, and an internal phase solvent. According to the perampanel long-acting sustained and controlled release microspheres, the PLGA microspheres prepared through microfluidics are very uniform, can stably release drugs and have highly-stable repeatability and regularity, the perampanel-PLGA sustained release microspheres prepared through the microfluidics technology are combined with a customization strategy to be very promising, related microsphere products are also beneficial to transformation, and the perampanel long-acting sustained and controlled release microspheres are suitable for industrial production. The method is an effective solution.
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Citation Information

Patent Citations

  • Perampanel long-acting sustained-release microsphere, preparation method and sustained-release injection

    CN117530933A