Compound slow-release implant of naltrexone and risperidone, preparation method therefor, and use thereof
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Solution Overview
Problem
Existing drug delivery systems for naltrexone and risperidone have short half-lives, leading to frequent administration, plasma concentration peaks and troughs, adverse reactions, and safety issues due to high magnesium content and poor process operability.
Innovation Solution
A compound sustained-release implant with a specific mass ratio of naltrexone to risperidone (20-30):1, using degradable materials with controlled molecular weights and a lubricant, prepared through a W/O/O/W and O/W emulsion process, and irradiation to achieve synchronous release and improve safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If conventional preparations are used to administer naltrexone and risperidone, then the drugs can be easily administered, but the plasma drug concentration shows obvious peak-trough effects and requires frequent administration
Solution Approach 1:
The patent segments the drug delivery system into a bi-layered implant structure with an inner layer containing naltrexone and an outer layer containing risperidone. Each layer has controlled porosity and degradation characteristics, allowing the drugs to be released separately and simultaneously maintain stable plasma concentrations without frequent re-administration.
2Reliability
If a large amount of magnesium stearate is added to achieve synchronous release of naltrexone and risperidone, then the release synchronization is improved, but the magnesium ion content exceeds the safety limit and causes adverse reactions
Solution Approach 1:
The patent extracts and removes magnesium stearate from the formulation entirely. Instead, it uses a bi-layered structure with controlled porosity and degradation of polymer matrices to achieve synchronous release of both drugs without relying on magnesium stearate, thereby eliminating magnesium ion toxicity while maintaining release synchronization.
Solution Approach 2:
The patent introduces polymer matrices (such as PLGA, PLA, or PCL) as intermediary materials that control drug release through their degradation rates and porosity characteristics. These polymer intermediaries replace magnesium stearate's release-control function while being biocompatible and degradable, enabling synchronous release without toxic magnesium ion accumulation.
3Reliability
If polymer solution with high viscosity is used for spray coating, then the coating effect is improved, but the process operability deteriorates
Solution Approach 1:
The patent changes the physical parameters of the coating solution by adjusting viscosity, solvent composition, and concentration to optimize both coating quality and sprayability. This allows the polymer coating to be applied uniformly while maintaining good process operability during manufacturing.
4Object-affected harmful factors
If the implant structure is simplified with fewer excipients, then the safety is improved, but the release control capability may deteriorate
Solution Approach 1:
The patent uses composite polymer materials (combinations of different biodegradable polymers with distinct degradation rates and mechanical properties) to achieve both release control and minimal excipient content. The composite structure allows precise control of drug release kinetics while maintaining implant integrity and reducing the need for additional excipients that could cause side effects.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The implant provides stable plasma drug concentration, reduces side effects, and ensures uniform release of naltrexone and risperidone, improving compliance and safety by minimizing magnesium stearate content and enhancing compressibility.
Implementation Method 1
a degradable material A, a degradable material B
Implementation Method 2
prepared through a W/O/O/W and O/W emulsion process
Data Source
AI summary
Disclosed is a compound sustained release implant of naltrexone and risperidone, and a preparation method and application thereof, which belong to the technical field of implant preparation. The naltrexone compound sustained-release implant includes naltrexone, risperidone, a degradable material A, a degradable material B, an additive and a lubricant. By controlling a mass ratio of naltrexone to risperidone to be (20-30):1, a weight-average molecular weight of the degradable material A to be 10-15 W, and a weight-average molecular weight of the degradable material B in risperidone microspheres to be 2 W-4 W, the compound sustained release implant of naltrexone and risperidone can not only effectively inhibit amphetamine type drug relapse and reduce side effects of risperidone, but also realize the synchronous release of naltrexone and risperidone.