Oil-Based Suspension for Triazine and Cyclodepsipeptide Delivery

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Solution Overview

Problem

There is a need for pharmaceutical preparations that effectively combine triazines and anthelmintic cyclodepsipeptides for oral use in animals, where the triazines must be systemically available to target parasitic protozoa while the depsipeptides act locally in the intestine to avoid systemic entry and side effects.

Innovation Solution

A formulation containing micronized triazines with a particle size of ≤15 μm and anthelmintic cyclodepsipeptides in an oil base, ensuring the triazines are available systemically and the depsipeptides act locally in the intestine, with a preferred combination of toltrazuril and emodepside in a suspension with an oil base, thickeners, antioxidants, and preservatives.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If triazines are administered orally to treat parasitic protozoa, then systemic availability is achieved, but the risk of side effects increases

Engineering Contradiction:

Improveeffectiveness against parasitic protozoaVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent divides the treatment into two separate components: triazines for systemic action against protozoa and depsipeptides for local intestinal action against nematodes. This segmentation allows each active ingredient to target its specific parasite type with optimized dosing, reducing unnecessary systemic exposure and side effects

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent uses an oil-based suspension formulation as an intermediary delivery system that enables controlled release and absorption of triazines into the bloodstream while maintaining depsipeptides in the intestinal lumen. The formulation acts as a mediator that achieves systemic availability of triazines while preventing premature systemic absorption of depsipeptides

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If depsipeptides are administered systemically, then broad-spectrum anthelmintic activity is achieved, but side effects increase due to unnecessary systemic exposure

Engineering Contradiction:

Improveanthelmintic activityVSAvoidside effects from systemic exposure

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing the formulation so that depsipeptides act locally in the intestinal lumen where nematodes reside, rather than distributing systemically. The oil-based suspension maintains depsipeptides in the gastrointestinal tract for direct contact with intestinal parasites, achieving effective local concentration while minimizing systemic exposure and associated side effects

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent extracts the intestinal action component from systemic anthelmintic treatment by using depsipeptides that remain in the gastrointestinal tract. This extraction of local intestinal activity separates the function of treating intestinal nematodes from systemic circulation, reducing unnecessary systemic exposure

Inventive Principle:

Principle #2Taking out (Extraction)

3Adaptability or versatility

If both triazines and depsipeptides are formulated together, then combined anti-protozoal and anthelmintic activity is achieved, but formulation complexity increases

Engineering Contradiction:

Improvecombined anti-protozoal and anthelmintic activityVSAvoidformulation complexity

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent creates a universal oil-based suspension formulation that simultaneously delivers both triazines and depsipeptides for combined anti-protozoal and anthelmintic activity. This multi-functional formulation consolidates what would otherwise require separate treatments into a single oral dose, achieving versatility without proportionally increasing complexity

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent merges two separate therapeutic agents (triazines and depsipeptides) into a single oil-based suspension formulation. By combining both active ingredients in one vehicle with compatible excipients, the patent achieves broad-spectrum parasitic coverage while simplifying administration compared to separate treatments

Inventive Principle:

Principle #5Merging (Combining)

4Reliability

If triazines are micronized to improve dissolution, then absorption is enhanced, but manufacturing precision requirements increase

Engineering Contradiction:

Improveabsorption and dissolutionVSAvoidparticle size control

Core Design Contradiction:

ReliabilityVSManufacturing precision

Solution Approach 1:

The patent changes the physical parameter of triazine particle size through micronization, reducing the d90 to ≤15 μm. This parameter change significantly improves dissolution rate and absorption of the poorly water-soluble triazine compounds. The specification provides clear particle size guidelines that balance manufacturing feasibility with therapeutic effectiveness

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP2405893B1Oil-based composition comprising anti-protozoal trazines and anthelminthic cyclodepsipeptides

Publication Date: 2015.04.22 BAYER INTPROP GMBH

AI summary

The present invention relates to an oil-based preparation containing a triazine effective against parasitic protozoa and an anthelmintic cyclodepsipeptide, which is suitable in particular for oral application of the combination of active agents in animals.