Microparticles containing moxidectin and sustained-release injection composition containing same
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Solution Overview
Problem
Conventional heartworm preventive drugs require regular administration due to their short half-life, posing a risk of missed doses and potential infection, and cause initial excessive drug release and injection site irritation.
Innovation Solution
Microparticles containing moxidectin and a biodegradable polymer with specific intrinsic viscosity and diameter, designed to sustainably release moxidectin for three months or more, maintaining effective concentration and reducing initial drug release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional heartworm preventive drugs are administered regularly every month, then heartworm infection can be prevented, but animals may still be exposed to infection risk when doses are missed and injection site irritation occurs
Solution Approach 1:
The patent encapsulates moxidectin in biodegradable polymer microparticles with controlled release properties, preparing the drug delivery system in advance to release the drug over an extended period (at least 3 months). This preliminary action of creating a sustained-release formulation eliminates the need for frequent re-injection, thereby reducing injection site irritation while maintaining reliable heartworm prevention efficacy.
2Reliability
If heartworm preventive drugs are administered monthly, then infection prevention is maintained, but administration convenience is reduced due to frequent dosing requirements
Solution Approach 1:
The patent employs a sustained-release microparticle formulation that continuously releases moxidectin over at least 3 months following a single injection. This continuous drug release maintains effective plasma concentrations throughout the period, eliminating gaps in protection that occur with monthly dosing schedules and significantly improving administration convenience while preserving prevention reliability.
3Speed
If moxidectin is released quickly after injection, then initial drug concentration is high, but excessive initial release causes injection site irritation and foreign body sensation
Solution Approach 1:
The patent utilizes biodegradable polymer microparticles that degrade in a controlled periodic manner, releasing moxidectin at a steady, moderate rate over time rather than all at once. This periodic degradation and release mechanism prevents excessive initial drug concentration at the injection site, thereby reducing irritation and foreign body sensation while still achieving the desired sustained therapeutic effect over at least 3 months.
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 provide prolonged heartworm prevention with minimal initial drug release, reducing foreign body sensation and injection site irritation, ensuring consistent drug levels for up to three months.
Implementation Method 1
a biodegradable polymer having an intrinsic viscosity of 0.1 dl/g to 1 dl/g
Implementation Method 2
releasing moxidectin sustainably over three months or more after administration
Data Source
AI summary
Embodiments relate to microparticles containing moxidectin, and a preparation method thereof. Unlike conventional heartworm prevention drugs that have a short half-life and thus require daily or monthly administration, moxidectin is continuously released for at least three months and thus the effect of preventing heartworms can be maintained for at least three months when the microparticles containing moxidectin are administered. In addition, microparticles which have a constant average diameter and a narrow diameter distribution are prepared so that initial over-release of moxidectin is prevented when the microparticles are administered, the release of the drug can be controlled to keep constant the concentration of moxidectin that is valid for at least three months, and foreign body sensation and pain can be reduced when the microparticles are applied in the form of an injection.