Viloxazine Modified-Release Formulations for High-Dose Bioavailability

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Solution Overview

Problem

Viloxazine presents challenges for developing an extended release formulation due to its high therapeutic dose, weakly basic nature, and high in vivo clearance rate, which existing technologies have not effectively addressed.

Innovation Solution

Modified release formulations of viloxazine, including extended and pulsatile release formulations, utilizing a combination of extended release (XR) and delayed release (DR) components, with specific release rate controlling compounds and enteric coatings, to achieve controlled drug release profiles.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If viloxazine is administered as immediate release formulation with high therapeutic dose, then therapeutic efficacy is achieved, but gastrointestinal and neurological side effects increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidgastrointestinal and neurological side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent divides the single high dose into multiple smaller doses administered at different times (immediate release component plus extended release component), segmenting the total therapeutic load to reduce peak concentration-related side effects while maintaining overall efficacy

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The formulation employs periodic release patterns with immediate release followed by extended release, creating a controlled temporal distribution of drug administration that sustains therapeutic levels while reducing peak adverse effects

Inventive Principle:

Principle #19Periodic action

2Productivity

If viloxazine is administered as extended release formulation, then dosing frequency is reduced, but maximum steady state plasma concentration is lower

Engineering Contradiction:

Improvedosing frequencyVSAvoidmaximum steady state plasma concentration

Core Design Contradiction:

ProductivityVSQuantity of substance

Solution Approach 1:

The patent combines immediate release and extended release components in a single formulation, merging the rapid absorption benefit of IR with the sustained release advantage of XR to achieve both reduced dosing frequency and adequate peak concentrations

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The immediate release component provides preliminary rapid absorption to achieve peak plasma concentration quickly, followed by the extended release component that maintains therapeutic levels over time, ensuring both fast onset and sustained efficacy

Inventive Principle:

Principle #10Preliminary action

3Ease of operation

If viloxazine is administered as extended release formulation, then once or twice daily administration is achieved, but bioavailability is reduced

Engineering Contradiction:

Improveadministration frequencyVSAvoidbioavailability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The formulation merges immediate release and extended release mechanisms to ensure that a significant portion of the drug is absorbed rapidly (maintaining bioavailability) while the extended release portion sustains therapeutic levels, achieving both ease of administration and reliable efficacy

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The patent modifies the release rate parameters by incorporating different release mechanisms (immediate and extended) with different dissolution characteristics, controlling the rate and extent of drug absorption to maintain bioavailability while enabling once or twice daily dosing

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250367208A1Formulations of viloxazine

Publication Date: 2025.12.04 SUPERNUS PHARMACEUTICALS INC

AI summary

Modified release formulations of viloxazine and methods of administering the same are disclosed. High-drug load formulations of viloxazine are further disclosed.