Delayed-Release Melatonin Granules for Fast Sleep Onset and Overnight Action

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Solution Overview

Problem

Conventional melatonin formulations exhibit rapid release and metabolism due to the short half-life of the melatonin molecule, leading to supraphysiological levels and failing to replicate the natural circadian rhythm, necessitating a composition that provides a controlled, prolonged release for effective treatment of sleep disorders.

Innovation Solution

A granulate comprising melatonin, sodium alginate, and calcium lactate, prepared through a process involving wet granulation and sequential coating with calcium lactate and sodium alginate, ensuring a sustained release of melatonin.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate-release melatonin formulations are used, then the onset of action is fast, but the duration of action is too short to maintain sleep throughout the night

Engineering Contradiction:
Improveonset of actionVSAvoidduration of action
Core Design Contradiction:
SpeedVSDuration of action of moving object

Solution Approach 1:

The melatonin formulation is divided into multiple granules with different release characteristics (immediate-release and delayed-release). This segmentation allows the medication to provide both rapid onset through immediate-release granules and sustained duration through delayed-release granules, resolving the contradiction between fast action and long-lasting effect.

Inventive Principle:
Principle #1Segmentation

2Duration of action of moving object

If extended-release formulations are used to prolong duration of action, then sleep maintenance is improved, but the onset of action becomes delayed

Engineering Contradiction:
Improveduration of actionVSAvoidonset of action
Core Design Contradiction:
Duration of action of moving objectVSSpeed

Solution Approach 1:

The formulation separates extended-release functionality into distinct delayed-release granules that coexist with immediate-release granules. This allows the extended-release component to provide prolonged duration without delaying the onset, as the immediate-release granules act first.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent combines immediate-release and delayed-release granules in a single pharmaceutical composition. This merging of different release mechanisms in one formulation simultaneously achieves fast onset and prolonged duration of action.

Inventive Principle:
Principle #5Merging (Combining)

3Duration of action of moving object

If multiple separate medications are used to achieve both immediate and delayed release effects, then duration and onset requirements are met, but the device complexity and dosing regimen increase

Engineering Contradiction:
Improveduration of actionVSAvoidcomplexity of dosing regimen
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent merges multiple functional granules (immediate-release and delayed-release) into a single pharmaceutical composition that can be administered as one dose. This eliminates the need for multiple separate medications and complex dosing regimens while maintaining the dual benefit of fast onset and prolonged duration.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The single pharmaceutical composition performs multiple functions: it provides both immediate and delayed release of melatonin, simplifying the treatment into a universal solution that replaces multiple separate medications.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP4504155B1Delayed-release granulates of melatonin, combinations comprising melatonin, pharmaceutical compositions and dietary supplements containing them, and their use in the treatment of insomnia and for the reduction of the time required to fall asleep
Publication Date: 2026.05.06 S I I T SRL
  • EP4504155B1 patent drawingFigure 1
  • EP4504155B1 patent drawingFigure 2A~2B

AI summary

It is an object of the present invention a delayed-release melatonin granulate, pharmaceutical compositions and dietary supplements comprising said granulate and their use in the treatment of sleep disorders and for the reduction of the time required to fall asleep, particularly of primary insomnia. It is also an object of the present invention to a combination consisting of melatonin, sodium alginate and calcium lactate and its use in the treatment of sleep disorders, particularly primary insomnia.