Moxidectin Microparticles with Biodegradable Polymer for Extended Release
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Solution Overview
Problem
Existing heartworm disease preventive agents require daily or monthly administration due to short half-life, leading to potential missed doses and increased infection risk, and cause discomfort during administration.
Innovation Solution
Microparticles comprising moxidectin and a biodegradable polymer with a uniform size distribution, designed to release the drug continuously for 3 to 6 months, reducing the frequency of administration and minimizing discomfort.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If preventive agents (diethylcarbamazine, ivermectin, milbemycin, moxidectin, selamectin) are administered daily or monthly, then heartworm disease prevention effect is achieved, but administration frequency is high requiring daily or monthly dosing which increases risk of missed doses
Solution Approach 1:
The patent segments the drug delivery system into microparticles with controlled size distribution (5-50 μm) that can be administered as a single dose. The microparticles are further segmented by release rate, with fine particles (5-20 μm) releasing drug faster and coarse particles (30-50 μm) releasing slower, creating a segmented release profile that extends protection to 3-6 months.
Solution Approach 2:
The patent changes the physical parameters of the drug delivery system by controlling microparticle size distribution and using biodegradable polymers with different degradation rates. This allows the drug to be released over an extended period (3-6 months) rather than requiring daily or monthly administration, while maintaining effective concentration levels.
2Object-affected harmful factors
If microparticles with small size are used for injection, then foreign body sensation and pain are reduced, but particle size must be precisely controlled within 5-50 μm range
Solution Approach 1:
The patent controls the particle size parameter within a specific range (5-50 μm) to minimize foreign body sensation and pain during injection. The emulsion solvent evaporation method with controlled parameters (emulsifier concentration, solvent ratio, evaporation temperature) enables precise particle size control while maintaining a uniform distribution that reduces variability.
Solution Approach 2:
The microparticles are designed with a porous internal structure formed during the emulsion solvent evaporation process. This porous structure allows controlled drug release while the external smooth surface maintains small effective size for reduced foreign body sensation. The porosity enables drug diffusion without requiring large particle sizes.
3Ease of operation
If extended release microparticles are designed to maintain drug concentration for 3-6 months, then administration frequency is reduced, but the drug release mechanism must be precisely controlled
Solution Approach 1:
The microparticles utilize the self-service principle by employing biodegradable polymers that automatically degrade and release the drug over time without requiring external control mechanisms. The polymer degradation rate inherently controls the drug release profile, extending protection to 3-6 months while simplifying the overall system design. The particles self-regulate their drug release based on their composition and environmental conditions.
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 microparticles maintain effective drug concentration for an extended period, reducing the need for frequent dosing and minimizing foreign body sensation during injection.
Implementation Method 1
release the drug continuously for 3 to 6 months
Implementation Method 2
biodegradable polymer
Implementation Method 3
preparation method therefor
Data Source
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AI summary
The present invention relates to microparticles comprising moxidectin and a biodegradable polymer, wherein the microparticles comprising moxidectin have a shape allowing a moxidectin drug to be uniformly distributed in spherical biodegradable polymer particles, and the average particle diameter of the microparticles is 80-130 µm. The present invention relates to: extended release microparticles capable of continuously maintaining a heartworm disease prevention effect for 3 months to 6 months by administering microparticles comprising moxidectin; and a preparation method therefor. In addition, the present invention is prepared such that the average diameters of the particles have a predetermined micrometer size, and thus reduces a foreign body sensation and pain during administration into an animal through injection, thereby enabling administration through injection to be facilitated.