Dicarboxylic Acid Ester Composition for Pain and Glucose Reduction
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Solution Overview
Problem
There is a need to enhance the efficacy of dicarboxylic acid esters, including diethyl azelate, in treating pain, decreasing blood glucose levels, inhibiting hemolysis and/or associated pain induced by PLA2, PLD, and other conditions and disorders.
Innovation Solution
The use of dicarboxylic acid esters in combination with at least one solvent and at least one terpene to induce analgesic effects by disrupting lipid rafts, promoting the secretion of certain signaling molecules, and suppressing the expression of pain-related markers, thereby inhibiting localized pain and reducing glucose levels.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If dicarboxylic acid esters are used alone, then the treatment effect is limited, but the composition is simple
Solution Approach 1:
The patent combines dicarboxylic acid esters with solvents and terpenes to create a synergistic composition. The solvent enhances drug solubility and stability, while the terpene component improves skin penetration and analgesic effects, collectively boosting therapeutic efficacy beyond what the dicarboxylic acid ester could achieve alone.
Solution Approach 2:
The invention creates a composite pharmaceutical composition integrating multiple functional components: dicarboxylic acid esters as the active pharmaceutical ingredient, solvents for solubility and stability enhancement, and terpenes for penetration and synergistic analgesic effects. This composite approach optimizes both efficacy and deliverability.
2Reliability
If higher concentrations of dicarboxylic acid esters are used to improve efficacy, then the therapeutic effect increases, but the risk of side effects increases
Solution Approach 1:
The patent optimizes the concentration parameters of dicarboxylic acid esters within safe ranges (e.g., 0.1-10% w/v) and balances them with specific ratios of solvents and terpenes. This parameter optimization ensures sufficient therapeutic efficacy while maintaining safety by preventing excessive concentrations that could cause irritation or systemic toxicity.
Solution Approach 2:
The solvent and terpene components act as intermediaries that enhance the delivery and effectiveness of dicarboxylic acid esters at lower, safer concentrations. The solvent improves solubility and stability, allowing effective dosing without high concentrations, while the terpene enhances penetration and provides synergistic analgesic effects, reducing the need for high doses of the active ingredient.
3Adaptability or versatility
If dicarboxylic acid esters are administered orally, then systemic treatment is achieved, but the bioavailability is limited
Solution Approach 1:
The solvent component acts as an intermediary that enhances the bioavailability of dicarboxylic acid esters during oral administration by improving solubility in gastrointestinal fluids and facilitating absorption. The terpene component further enhances this by improving membrane penetration and reducing first-pass metabolism, collectively boosting systemic bioavailability.
Solution Approach 2:
The patent optimizes the physicochemical parameters of the composition, including pH adjustment and solubility enhancement through solvent selection, to maximize oral bioavailability. The formulation parameters are tuned to ensure stable absorption and consistent systemic delivery of the active ingredient.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The combination effectively reduces pain and glucose levels, inhibits hemolysis, and treats conditions associated with PLA2 and PLD, providing significant therapeutic benefits.
Implementation Method 1
Dimethyl sulfoxide (DMSO) is an organosulfur compound that enhances the plasma membrane permeation of drugs, DNA and other substances. Increasing concentrations of DMSO reportedly induce thinning of the plasma membrane followed by pore formation and, finally, a collapse of the bilayer.
Implementation Method 2
Terpenes also enhance skin penetration by interaction with intercellular lipids in stratum corneum, the outermost layer of the skin. Terpenes can boost the activity of both hydrophilic and lipophilic drugs even at low concentrations.
Implementation Method 3
Limonene has anti-inflammatory activity when applied to the skin and facilitates wound healing in vivo.
Implementation Method 4
Menthol can stimulate skin nociceptors, initiate release of vasodilator peptides and increase skin temperature.
Data Source
AI summary
This disclosure provides methods and compositions including dicarboxylic acid esters, and at least one solvent that is effective in enhancing the therapeutic efficacy of the dicarboxylic acid ester. In some embodiments, the composition further includes at least one terpene, and other embodiments include methods of making the compositions and uses of the compositions for treating a variety of ailments that dicarboxylic acid esters are useful in treating.