Sublingual Melatonin Composition with Valerenic and Carnosic Acids

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Solution Overview

Problem

Current melatonin formulations for treating insomnia and inflammatory conditions face challenges with bioavailability, onset/offset times, and side effects, and lack synergistic combinations with plant extracts to enhance therapeutic efficacy.

Innovation Solution

Development of novel compositions comprising melatonin, valerenic acid, and carnosic acid in specific molar ratios, combined with plant-derived materials like Valeriana and Rosmarinus officinalis, formulated as sublingual tablets with both immediate and controlled release components to improve bioavailability and reduce side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If melatonin is administered orally in conventional formulations, then it can treat insomnia and inflammatory conditions, but its bioavailability is poor and onset time is delayed

Engineering Contradiction:
ImprovebioavailabilityVSAvoidonset time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent uses sublingual administration as an intermediary route between oral and parenteral administration. The sublingual mucosa serves as a mediator that allows direct absorption of melatonin into the bloodstream, bypassing the gastrointestinal tract and first-pass metabolism, thereby improving bioavailability and reducing onset time compared to conventional oral formulations

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical digestion and absorption process of the gastrointestinal tract with direct mucosal absorption in the sublingual region. This substitution eliminates the need for gastric breakdown and hepatic metabolism, allowing faster and more reliable delivery of melatonin to the systemic circulation

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Reliability

If single-ingredient melatonin formulations are used, then the treatment is simple, but therapeutic efficacy is limited and side effects occur

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent merges melatonin with plant-derived extracts containing specific active compounds (such as valerenic acid from Valeriana and carnosic acid from Rosmarinus officinalis) in defined molar ratios. This combination creates a synergistic effect that enhances therapeutic efficacy for insomnia and inflammatory conditions while reducing the required dosage of each individual component, thereby minimizing side effects

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent creates a composite pharmaceutical formulation consisting of melatonin combined with plant-derived active ingredients in specific proportions. This composite material leverages the complementary mechanisms of action of its components - melatonin's circadian rhythm regulation and antioxidant effects, combined with the plant compounds' anxiolytic and anti-inflammatory properties - to achieve superior therapeutic outcomes with reduced adverse effects

Inventive Principle:
Principle #40Composite materials

3Duration of action of moving object

If prolonged-release formulations are used to extend therapeutic effect, then duration of action is improved, but peak concentration is reduced and onset time is delayed

Engineering Contradiction:
Improveduration of therapeutic effectVSAvoidonset speed
Core Design Contradiction:
Duration of action of moving objectVSSpeed

Solution Approach 1:

The patent segments the melatonin dose into two distinct formulations: an immediate-release component for rapid onset of action and a prolonged-release component for extended therapeutic effect. This segmentation allows each component to fulfill its specific function - the immediate-release portion provides quick relief of symptoms while the prolonged-release portion maintains therapeutic levels throughout the night, achieving both fast onset and long duration without compromise

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS10675269B2Compositions comprising melatonin
Publication Date: 2020.06.09 TRINUTRA LTD
  • US10675269B2 patent drawing
  • US10675269B2 patent drawing
  • US10675269B2 patent drawing

AI summary

The present invention provides a composition comprising a synergistic combination of melatonin, valerenic acid and carnosic acid. The composition may be used in the treatment and prevention of several different disorders including inflammatory conditions, sleep disorders and anxiety. The invention also relates to several dosage forms which are suitable for the delivery of the claimed composition to subjects in need of treatment therewith.