Terconazole Composition Citric Acid Crystallization Inhibition
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Solution Overview
Problem
Terconazole's low solubility in water makes it difficult to obtain stable aqueous solutions at therapeutic concentrations, leading to the presence of terconazole crystals, which are undesirable for effective treatment of vaginal yeast infections.
Innovation Solution
An aqueous terconazole composition with at least 0.4% by weight terconazole dissolved in water, incorporating a terconazole crystallization-inhibiting amount of citric acid, along with optional viscosity modifying agents, to create stable solutions free from crystals at ambient temperature, suitable for vaginal application.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If terconazole is dissolved in water at therapeutic concentrations, then the solution provides effective treatment of vaginal yeast infections, but terconazole crystals form due to low solubility
Solution Approach 1:
The patent introduces citric acid as an intermediary substance that mediates between terconazole and water. Citric acid forms a complex with terconazole that is soluble in water, preventing crystal formation while maintaining therapeutic concentrations. This intermediary approach allows high terconazole concentrations to be achieved without the harmful crystallization that would otherwise occur.
Solution Approach 2:
The patent changes the chemical parameters of the solution by adjusting pH and adding citric acid. By modifying these parameters, the solubility of terconazole is enhanced and crystal formation is prevented. The citric acid alters the chemical environment to create a stable aqueous solution at therapeutic concentrations.
2Productivity
If terconazole cream is used for treatment, then vaginal yeast infections are treated, but rapid release of terconazole is not achieved
Solution Approach 1:
The patent changes the physical state of terconazole from solid cream to dissolved aqueous solution. This parameter change enables rapid release by ensuring terconazole is already in molecular form, ready for immediate absorption, rather than requiring gradual dissolution from a cream base.
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 rapid and nearly complete release of terconazole, achieving high concentrations required for effective pathogen killing, outperforming commercial products by releasing over 90% of terconazole within five hours and all within ten hours, while maintaining stability without crystal formation.
Implementation Method 1
a terconazole crystallization-inhibiting amount of citric acid
Implementation Method 2
viscosity modifying agents, such as thickeners, can be included in the compositions of the invention to provide gels
Data Source
AI summary
An aqueous terconazole composition comprises at least about 0.4 percent by weight of terconazole dissolved in water, and a terconazole crystallization-inhibiting amount of citric acid. The composition is free from terconazole crystals at an ambient temperature of about 20.degree. C. Methods of preparing the composition are also described. The compositions provide for improved therapeutic release of terconazole.