Topical Pain Compositions Stabilizing Magnesium Salts

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Solution Overview

Problem

Current topical pain relief compositions face challenges in stability, particularly with high magnesium salt concentrations, leading to phase separation and instability in emulsions, which affects their long-term effectiveness and usability.

Innovation Solution

The development of topical compositions combining magnesium salts, cannabinoids, and additional analgesic agents like methyl salicylate and menthol, formulated as stable water-in-oil or oil-in-water emulsions, which maintain stability even at high magnesium concentrations and relative humidity, allowing for effective pain relief.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high magnesium salt concentrations are used in topical compositions, then pain relief effectiveness is improved, but emulsion stability deteriorates leading to phase separation

Engineering Contradiction:
Improvepain relief effectivenessVSAvoidemulsion stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent modifies the chemical composition parameters by introducing specific emulsifiers (polysorbates, sorbitan esters) and adjusting the ratio of aqueous to oily phase components. This allows the formulation to maintain emulsion stability even at high magnesium salt concentrations (e.g., magnesium chloride, magnesium sulfate) that would otherwise cause phase separation.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite topical composition combining multiple functional components: magnesium salts (for pain relief), cannabinoids (for analgesic effect), additional analgesics (methyl salicylate, menthol), and specialized emulsifiers. This composite structure enables simultaneous achievement of high effectiveness and stability by having each component serve its specific function while working synergistically.

Inventive Principle:
Principle #40Composite materials

2Duration of action of stationary object

If topical compositions are formulated for long-term stability, then storage durability is improved, but formulation complexity increases

Engineering Contradiction:
Improvestorage durabilityVSAvoidformulation complexity
Core Design Contradiction:
Duration of action of stationary objectVSDevice complexity

Solution Approach 1:

The patent introduces emulsifiers as intermediary substances that mediate between the aqueous phase (containing magnesium salts) and the oily phase (containing cannabinoids and other analgesics). These emulsifiers form stable interfacial films that prevent phase separation during storage, thereby achieving long-term stability without requiring overly complex formulation strategies.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent optimizes specific formulation parameters including the concentration ranges of emulsifiers (e.g., 0.1-10% polysorbates), the ratio of oil to water phases, and the selection of specific magnesium salt types. By carefully controlling these parameters within defined ranges, the formulation achieves robust long-term stability while maintaining reasonable formulation simplicity.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If multiple active ingredients are combined for enhanced pain relief, then therapeutic effectiveness is improved, but risk of adverse interactions increases

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidadverse interactions
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines multiple active ingredients with complementary mechanisms of action: magnesium salts (muscle relaxant, anti-inflammatory), cannabinoids (CB1/CB2 receptor agonists for pain modulation), methyl salicylate (COX inhibitor), and menthol (cooling analgesic). This merging of ingredients with different mechanisms reduces the risk of adverse interactions compared to using high doses of a single agent, while providing synergistic pain relief.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent applies the principle of local quality by having each active ingredient target specific pain pathways and receptors locally at the application site. Magnesium salts affect muscle relaxation locally, cannabinoids target cannabinoid receptors in peripheral nerves, methyl salicylate acts on local inflammatory mediators, and menthol activates TRP channels for localized cooling effect. This distributed local action reduces systemic adverse interactions while maintaining strong therapeutic effectiveness.

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS20230302028A1Pain-relieving topical compositions
Publication Date: 2023.09.28 INNOCAN PHARMA LTD

AI summary

Described herein are compositions for topical use comprising active agents to provide pain relief. The compositions comprise a magnesium salt, a cannabinoid and at least one additional topical analgesic agent. Additionally described herein are methods for treating pain comprising administering to a person in need thereof a composition comprising a pharmaceutically effective amount of a cannabinoid, a magnesium salt and at least one of: methyl salicylate, and menthol.