Colored Resin Container for Luliconazole Stability
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Solution Overview
Problem
Stable and high-concentration storage of pharmaceutical compositions containing compounds like luliconazole is challenging due to light-induced isomerization, poor solubility, and crystallization issues, which existing light-blocking containers cannot effectively address.
Innovation Solution
A resin container with a specific color range (7.0Y to 9.99Y or 7.0YR to 9.99YR hue, 1.0 to 6.0 value, and 0.5 to 7.5 chroma) combined with an N-alkyl-2-pyrrolidone-based formulation containing benzyl alcohol and diester of dibasic acid, preventing isomerization and crystallization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If light-blocking metal oxide structures are used in containers, then light stability is improved, but radical generation occurs that impairs pharmaceutical compositions
Solution Approach 1:
The patent removes light-blocking metal oxides from the container formulation and replaces them with colored resin materials that block light without generating harmful radicals. This extracts the harmful component while retaining the beneficial light-blocking function.
Solution Approach 2:
The patent introduces colored resin materials as an intermediary substance that mediates between light and the pharmaceutical composition. These resins absorb light to prevent penetration to the medication without undergoing the photochemical reactions that generate radicals, thus serving as a safe intermediary barrier.
2Quantity of substance
If high concentration of luliconazole is formulated, then antifungal effectiveness is improved, but solubility limitations and crystallization occur
Solution Approach 1:
The patent changes the chemical parameters of the formulation by selecting specific solvents (N-alkyl-2-pyrrolidones with 3-7 carbon atoms) and adjusting their molecular structure parameters. This enables the system to dissolve higher concentrations of luliconazole (up to 8% or more) while maintaining solution stability and preventing crystallization.
Solution Approach 2:
The patent creates a composite solvent system combining N-alkyl-2-pyrrolidone with other co-solvents and additives to achieve synergistic effects. This composite formulation enhances the solubility of luliconazole at high concentrations while maintaining physical stability and preventing precipitation.
3Illumination intensity
If normal light blocking means are used, then light penetration is reduced, but isomerization of luliconazole cannot be suppressed
Solution Approach 1:
The patent applies color changes principle by using colored resin materials with specific absorption characteristics. These materials are designed to absorb in the ultraviolet and visible light ranges, creating a color barrier that blocks the specific wavelengths responsible for inducing isomerization of luliconazole, thereby protecting the pharmaceutical composition's stereochemical stability.
4Productivity
If transparent solutions with high luliconazole concentration are formulated, then penetration into nail is improved, but crystallization upon application occurs
Solution Approach 1:
The patent applies preliminary action by incorporating specific solvents and stabilizers into the formulation before application. These components pre-establish a stable solvation environment that prevents crystallization during storage and upon application to the nail, ensuring the medication remains in solution form for effective penetration.
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 solution provides a stable, high-concentration pharmaceutical composition that maintains stability under storage conditions and prevents immediate crystallization on application, achieving up to 8% luliconazole concentration without significant isomerization.
Implementation Method 1
the resin container does not show permeability in measurement of the ultraviolet-visible absorbance spectrum
Data Source
AI summary
Provided is a means for stably storing a pharmaceutical composition comprising a compound represented by the General Formula (I) below and/or a salt thereof, and for providing the pharmaceutical composition to the market. A resin container colored with a color having a hue (H) within the range of 7.0Y to 9.99Y or 7.0YR to 9.99YR, value (V) within the range of 1.0 to 6.0, and chroma (C) within the range of 0.5 to 7.5, according to Munsell color coordinates, is filled with a pharmaceutical composition comprising a compound represented by the General Formula (I) and/or a salt thereof, to store the pharmaceutical composition.(wherein, in the formula, R1 and R2 each independently represent a hydrogen atom or a halogen atom)