Combined-Release Gamma-Hydroxybutyrate Derivative for Stable Plasma Levels

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Solution Overview

Problem

Existing treatments for narcolepsy and associated symptoms like excessive daytime sleepiness and fatigue do not effectively manage the pharmacokinetics of γ-hydroxybutyrate, leading to suboptimal therapeutic outcomes.

Innovation Solution

Pharmaceutical compositions comprising an immediate and modified release component of 4-((L-valyl)oxy)butanoic acid, which are designed to provide a therapeutically effective amount for treating narcolepsy and related conditions, ensuring controlled release and absorption of γ-hydroxybutyrate.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate release formulation is used, then rapid onset of action is achieved, but short duration of therapeutic effect occurs

Engineering Contradiction:

Improveonset of actionVSAvoidduration of therapeutic effect

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The formulation is divided into two distinct components: an immediate release component containing 4-((L-valyl)oxy)butanoic acid for rapid absorption and onset of action, and a modified release component providing sustained release for extended duration. This segmentation allows each component to fulfill its specific function independently, resolving the contradiction between rapid onset and prolonged duration.

Inventive Principle:

Principle #1Segmentation

2Duration of action of moving object

If modified release formulation is used, then extended duration of therapeutic effect is achieved, but delayed onset of action occurs

Engineering Contradiction:

Improveduration of therapeutic effectVSAvoidonset of action

Core Design Contradiction:

Duration of action of moving objectVSSpeed

Solution Approach 1:

The patent combines immediate release and modified release formulations into a single composite product containing both 4-((L-valyl)oxy)butanoic acid components. This merging allows the patient to receive both the rapid onset from the immediate release component and the extended duration from the modified release component simultaneously, resolving the contradiction between delayed onset and prolonged duration.

Inventive Principle:

Principle #5Merging (Combining)

3Duration of action of moving object

If multiple dosing is used, then extended duration of coverage is achieved, but patient compliance decreases

Engineering Contradiction:

Improveduration of therapeutic effectVSAvoidpatient compliance

Core Design Contradiction:

Duration of action of moving objectVSEase of operation

Solution Approach 1:

By combining immediate release and modified release formulations into a single dosing regimen, the patent enables extended duration of therapeutic effect through one administration rather than requiring multiple doses throughout the day. This single-dose composite formulation maintains sustained plasma levels while simplifying the dosing schedule, thereby improving patient compliance.

Inventive Principle:

Principle #5Merging (Combining)

Data Source

PatentEP4308086B1Pharmacokinetics of combined release formulations of a gamma-hydroxybutyric acid derivative

Publication Date: 2025.10.15 XWPHARMA LTD

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AI summary

Pharmaceutical compositions comprising an immediate release component comprising 4-((L- valyl)oxy)butanoic acid and a modified release component comprising 4-((L-valyl)oxy)butanoic acid and the pharmacokinetics of 4-((L-valyl)oxy)butanoic acid and γ-hydroxybutyrate following oral administration of the pharmaceutical compositions is disclosed.