Macrocyclic Lactone Tablet Formulation for Parasite Control
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Solution Overview
Problem
Formulating anthelmintic compounds, particularly lipophilic ones like abamectin and ivermectin, is challenging due to their insolubility in aqueous environments, leading to poor bioavailability and potential drug resistance when administered in slow-release formulations, which fail to effectively target adult parasites and can cause adverse effects.
Innovation Solution
A tablet formulation that includes solubilizable lipophilic anthelmintic compounds like abamectin or ivermectin, dissolved in organic solvents and co-solvents such as benzyl alcohol and propylene glycol, which enhances bioavailability by ensuring rapid release and absorption, maintaining stability, and providing a consistent therapeutic effect.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If lipophilic anthelmintic compounds are formulated for slow release over 100 days, then parasite control is extended over time, but adult parasites are not effectively targeted and drug resistance develops
Solution Approach 1:
The tablet formulation is designed to release anthelmintic compounds in periodic pulses rather than continuous slow release. This creates peak concentration periods that effectively kill adult parasites while maintaining extended duration of action through repeated release cycles, thereby resolving the contradiction between duration and efficacy.
Solution Approach 2:
The formulation changes the release parameter from continuous low-level release to periodic high-concentration release. This parameter change allows the same compound to achieve both extended duration (through multiple release cycles) and high efficacy (through peak concentrations that kill adult parasites).
2Reliability
If lipophilic compounds are made soluble by reducing pH, then bioavailability is improved, but other compounds in the formulation become insoluble or degrade
Solution Approach 1:
The patent introduces pH-modifying excipients as intermediaries that create a localized favorable pH environment for the anthelmintic compound's dissolution without causing system-wide pH reduction. This mediator approach allows the active compound to achieve bioavailability while protecting other formulation components from pH-induced instability.
Solution Approach 2:
The formulation creates local pH optimization at the dissolution site of the anthelmintic compound without affecting the overall formulation pH. This localized quality change enables the lipophilic compound to become soluble and bioavailable while maintaining the stability of other pH-sensitive components in the tablet.
3Loss of time
If slow release formulation is used to extend parasite control, then treatment duration is reduced, but the time period between delivery and slaughter must be significantly longer
Solution Approach 1:
The periodic release mechanism creates defined peak concentration periods followed by elimination phases. This allows prediction of when drug levels fall below detectable thresholds, enabling optimization of both treatment frequency (reduced dosing intervals) and withdrawal periods (shorter time to slaughter) based on the periodic release pattern.
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 formulation achieves comparable bioavailability to oral drenches, effectively targeting parasites, reducing resistance, and maintaining stability for extended storage periods, offering a flexible administration time and improved treatment efficacy.
Implementation Method 1
A tablet formulation that includes solubilizable lipophilic anthelmintic compounds like abamectin or ivermectin, dissolved in organic solvents and co-solvents such as benzyl alcohol and propylene glycol
Data Source
AI summary
The invention relates to a table formulated for administration to an animal to treat parasite infestation. The tablet includes at least one macrocyclic lactone compound with anthelmintic activity dissolved in at least one organic solvent and subsequently formulated into a tablet. The tablets produced have a high degree of stability when stored over time and also provide the animal with a dose of agent sufficient to be therapeutically effective.