Modoflaner Tablet Composition for Oral Bioavailability

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Solution Overview

Problem

Modoflaner, an arylaminobenzamide, exhibits low solubility and wettability in aqueous media due to its hydrophobicity, making it challenging to formulate into tablets, and limits its oral bioavailability, particularly in the treatment of parasitic infestations in animals.

Innovation Solution

A tablet formulation incorporating crystalline modification IV of Modoflaner with a water absorption agent and a binding agent, along with specific processing conditions, ensures even distribution and maintains favorable pharmacokinetic properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If Modoflaner is formulated as a tablet for oral administration, then it can be used for treatment and prophylaxis of parasitic infestations, but its low solubility and wettability due to hydrophobicity make granulation and tablet formation challenging

Engineering Contradiction:

Improveoral administration feasibilityVSAvoidgranulation difficulty

Core Design Contradiction:

Ease of operationVSEase of manufacture

Solution Approach 1:

The patent changes the physical and chemical parameters of the formulation by incorporating specific excipients (surfactants, co-solvents, complexing agents) that modify the solubility and wettability characteristics of Modoflaner, enabling successful granulation and tablet formation while maintaining the drug's therapeutic efficacy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite tablet formulation combining Modoflaner with multiple excipients including surfactants, co-solvents, binders, and fillers. This composite approach addresses the hydrophobicity issue by integrating materials that improve wettability and solubility while maintaining structural integrity for tablet manufacture

Inventive Principle:

Principle #40Composite materials

2Reliability

If Modoflaner is administered orally, then it can treat parasitic infestations, but its hydrophobicity limits oral bioavailability

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidoral bioavailability

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent introduces surfactants and co-solvents as intermediary substances that facilitate the interaction between the hydrophobic Modoflaner and the aqueous gastrointestinal environment. These intermediaries form micelles or solubilizing complexes that enhance drug dissolution and absorption without altering the drug's molecular structure

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physicochemical parameters of the drug delivery system by adjusting pH, adding complexing agents, and incorporating materials that change the solubility profile of Modoflaner, thereby improving its bioavailability while maintaining therapeutic reliability

Inventive Principle:

Principle #35Parameter changes

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 maintains high bioavailability and stability of Modoflaner, allowing effective treatment and prophylaxis of parasitic infestations in animals, particularly dogs and cats, by ensuring uniform distribution and retention of the crystalline form during processing and storage.

Implementation Method 1

Modoflaner shows polymorphism and can be crystallized in at least 4 different crystalline modifications and at least 3 different pseudopolymorphic forms

Methodology Applied

Scientific EffectPolymorphism:

Implementation Method 2

a tablet comprising Modoflaner, preferably crystalline modification IV of Modoflaner, and a water absorption agent

Methodology Applied

Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentUS12509425B2Tablet comprising modoflaner as an active component

Publication Date: 2025.12.30 VIRBAC SA

AI summary

The present invention relates to a crystalline modification of Modoflaner 6-fluoro-N-(3-(2-iodo-4-(perfluoropropan-2-yl)-6-(trifluoromethyl)phenylcarbamoyl)-2-fluorophenyl)nicotinamide of formula (I):