Desoximetasone Liquid Formulation Oxidation Control
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Solution Overview
Problem
Current formulations of desoximetasone and isopropyl myristate suffer from oxidation issues, leading to the formation of oxidized impurities, which exceed acceptable thresholds even when stored under inert conditions, making them unsuitable for long-term use in treating skin conditions like psoriasis.
Innovation Solution
A stable liquid formulation comprising desoximetasone, isopropyl myristate, and a C2-C4 alcohol, combined with a stabilizing agent such as mineral oil or a propellant, to reduce the formation of oxidized impurities below 1 wt% even under accelerated storage conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If desoximetasone and isopropyl myristate are combined in a liquid formulation, then the formulation provides effective treatment for skin conditions, but oxidized impurities form and exceed acceptable thresholds during storage
Solution Approach 1:
The patent introduces a stabilizing agent as an intermediary substance that prevents direct oxidation of desoximetasone by isopropyl myristate or atmospheric oxygen. This mediator absorbs or neutralizes oxidative stress, protecting the active ingredient while allowing the formulation to maintain its therapeutic function throughout storage.
Solution Approach 2:
The patent creates an inert chemical environment within the formulation by selecting oxidatively stable components and configuring the composition to minimize oxygen exposure. The specific ratios of isopropyl myristate, C2-C4 alcohol, and stabilizing agent establish a chemically protective matrix that prevents oxidation without compromising therapeutic efficacy.
2Duration of action of stationary object
If the formulation is stored under inert conditions, then oxidation is reduced, but oxidized impurities still exceed thresholds making the product unsuitable for long-term use
Solution Approach 1:
The patent applies preliminary protective action by incorporating the stabilizing agent into the formulation before storage begins. This preemptive measure establishes chemical protection against oxidation from the outset, preventing impurity formation during the entire storage period rather than attempting to address oxidation after it occurs.
Solution Approach 2:
The patent modifies the chemical parameters of the formulation by selecting specific concentrations of stabilizing agents and adjusting the ratio of isopropyl myristate to C2-C4 alcohol. These parameter changes optimize the formulation's resistance to oxidation, enabling long-term stability while maintaining therapeutic effectiveness.
3Stability of the object's composition
If antioxidants are added to prevent oxidation, then stability improves, but the formulation complexity increases
Solution Approach 1:
The patent achieves multi-functionality by selecting stabilizing agents that simultaneously protect against oxidation and maintain the physical properties of the formulation. These agents provide both chemical stability and formulation integrity, eliminating the need for separate protective measures and simplifying the overall composition.
Solution Approach 2:
The patent creates a composite formulation system where isopropyl myristate, C2-C4 alcohol, and stabilizing agent work synergistically. This composite approach distributes the stabilization function across multiple components rather than relying on a single antioxidant, achieving enhanced stability while maintaining formulation simplicity through functional integration.
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 formulation maintains stability and minimizes oxidized impurity formation, ensuring the product remains effective and commercially viable for treating skin conditions like psoriasis and atopic dermatitis.
Implementation Method 1
a stable liquid formulation comprising desoximetasone, isopropyl myristate, a C2-C4 alcohol and a stabilizing agent... reduced oxidized impurity (17-carboxy-9α-fluoro-11β-hydroxy-16α-methyl-androsta-1,4-diene-3 -one)
Data Source
AI summary
The present invention relates to a stable liquid formulation comprising desoximetasone, isopropyl myristate, a C2-C4 alcohol and a stabilizing agent. Specifically, the present invention provides a liquid formulation comprising: a) about 0.01 wt % to about 2.5 wt % desoximetasone; b) about 10 wt % to about 70 wt % isopropyl myristate; c) about 20 wt % to about 70 wt % C2-C4 alcohol; and d) a stabilizing agent selected from the group consisting of an oleaginous vehicle and a propellant, wherein the stabilizing agent is in an amount sufficient to reduce the formation of less than about 1 wt % 17-carboxy-9α-fluoro-11β-hydroxy-16α-methyl-androsta-1,4-diene-3-one under an accelerated storage condition.