Short-Acting and Long-Acting Hypnotic Agent Combination for Sleep Disorders

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Solution Overview

Problem

Current hypnotic agents either fail to induce or maintain restful sleep effectively without negatively impacting wakefulness periods, and there is a need for a combination that synergistically enhances sleep quality without adverse effects on waking phases.

Innovation Solution

A combination of a short-acting hypnotic agent and a long-acting hypnotic agent, where the short-acting agent is released immediately or over a prolonged period, and the long-acting agent is released immediately, creating a synergistic effect to improve sleep quality and duration without negatively affecting wakefulness.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If a short-acting hypnotic agent is administered, then sleep induction is improved, but sleep maintenance capability deteriorates

Engineering Contradiction:
Improvesleep induction speedVSAvoidsleep maintenance duration
Core Design Contradiction:
SpeedVSDuration of action of moving object

Solution Approach 1:

The patent combines a short-acting hypnotic agent (zolpidem, zaleplon, or zopiclone) with a long-acting hypnotic agent (eplivanserin, gaboxadol, or pregabalin) into a single pharmaceutical composition. This merging allows the short-acting component to rapidly induce sleep while the long-acting component sustains sleep maintenance, thereby resolving the contradiction between sleep induction speed and sleep maintenance duration.

Inventive Principle:
Principle #5Merging (Combining)

2Duration of action of moving object

If a long-acting hypnotic agent is administered, then sleep maintenance is improved, but sleep induction speed deteriorates

Engineering Contradiction:
Improvesleep maintenance durationVSAvoidsleep induction speed
Core Design Contradiction:
Duration of action of moving objectVSSpeed

Solution Approach 1:

The pharmaceutical composition merges a long-acting hypnotic agent (eplivanserin, gaboxadol, or pregabalin) with a short-acting hypnotic agent (zolpidem, zaleplon, or zopiclone). The long-acting component ensures sustained sleep maintenance while the short-acting component provides rapid sleep induction, thereby resolving the contradiction between sleep maintenance duration and sleep induction speed.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If high doses of hypnotic agents are administered, then sleep quality is improved, but adverse effects on wakefulness periods worsen

Engineering Contradiction:
Improvesleep qualityVSAvoidadverse effects on wakefulness
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the dosing parameters by administering low doses of both short-acting and long-acting hypnotic agents in combination, rather than high doses of a single agent. The short-acting agent is administered at 0.5-10 mg and the long-acting agent at 1-30 mg, creating a synergistic effect that improves sleep quality while minimizing adverse effects on wakefulness periods through reduced individual dosages.

Inventive Principle:
Principle #35Parameter changes

4Ease of operation

If a single hypnotic agent is administered, then treatment simplicity is improved, but sleep quality and duration deteriorate

Engineering Contradiction:
Improvetreatment simplicityVSAvoidsleep quality
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent merges multiple hypnotic agents with different durations of action into a single pharmaceutical composition that can be administered as one tablet or capsule. This maintains treatment simplicity while achieving superior sleep quality and duration through the synergistic combination of short-acting and long-acting components, eliminating the need for multiple separate medications.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP1919473B1Combination of a long-acting hypnotic agent and a short-acting hypnotic agent and therapeutic use of same
Publication Date: 2012.12.05 SANOFI SA(FR)

AI summary

The invention relates to the combination of: a short-acting hypnotic agent which is selected from among a modulator of receptors GABA-A, a benzodiazepine, a phenothiazine, a melatonin derivative and a melatonin receptor agonist; and a long-acting hypnotic agent which is selected from among a modulator of receptors GABA-A, a benzodiazepine, an antagonist of receptors 5HT2A and a calcium ion modulator, for the treatment of sleep disorders. The invention also relates to galenic formulations containing said combination.