Oltipraz Crystal Size Reduction for Solubility and Stability
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Solution Overview
Problem
Current crystalline forms of oltipraz have poor bioavailability and solubility, limiting their effectiveness in treating viral infections such as COVID-19, due to their large particle size and instability in aqueous solutions.
Innovation Solution
Formulated oltipraz compositions with controlled particle size and stabilization methods, including the use of stabilizing agents, are developed to create smaller, more stable oltipraz crystals with improved solubility and size-stability, which can be administered to enhance therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If crystalline oltipraz is used in conventional forms, then it provides basic antiviral activity, but it exhibits poor solubility and bioavailability due to large particle size
Solution Approach 1:
The patent applies segmentation by reducing the large crystalline oltipraz particles into smaller particle sizes through mechanical size reduction processes. This division of the crystalline structure into finer particles increases the surface area to volume ratio, thereby improving solubility and bioavailability while maintaining the antiviral therapeutic effect.
Solution Approach 2:
The patent changes the physical parameter of particle size from conventional large crystals to controlled fine particles within a specific size range. This parameter change optimizes both solubility and stability, resolving the contradiction between maintaining adequate particle size for stability and reducing particle size for improved solubility.
2Reliability
If crystalline oltipraz is administered, then it provides antiviral treatment, but it shows instability in aqueous solutions
Solution Approach 1:
The patent changes multiple parameters including particle size, crystal morphology, and formulation composition to achieve a stable yet soluble oltipraz formulation. By controlling particle size within specific ranges and using appropriate excipients, the patent resolves the instability-solubility contradiction.
Solution Approach 2:
The patent creates a composite formulation by combining oltipraz with specific excipients and stabilizing agents. This composite approach enhances the stability of oltipraz in aqueous solutions while maintaining its solubility and therapeutic efficacy.
3Ease of manufacture
If conventional oltipraz formulations are used, then they are simple to manufacture, but they exhibit poor bioavailability
Solution Approach 1:
The patent maintains ease of manufacture by using conventional size reduction techniques and standard pharmaceutical formulation methods. The segmentation of crystals into smaller particles can be achieved through common industrial processes, avoiding complex manufacturing steps while significantly improving bioavailability.
Solution Approach 2:
The patent optimizes particle size parameters within ranges that can be achieved through standard manufacturing processes. By selecting particle size ranges that are attainable through conventional equipment and methods, the patent improves bioavailability without compromising manufacturing simplicity.
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 formulated oltipraz compositions exhibit improved solubility and stability, reducing mucositis and reactive oxygen species, and effectively treat or prevent COVID-19 symptoms by reducing viral entry into host cells and protecting respiratory tissues.
Implementation Method 1
comprising stabilized oltipraz crystals... crystal parameters including particle size are controlled and stabilized
Implementation Method 2
comprising stabilized oltipraz crystals... size-stability in aqueous suspension
Implementation Method 3
confers cytoprotection by triggering nuclear factor related erythroid factor-2(Nrf2)-dependent gene expression
Implementation Method 4
effectively treat or prevent COVID-19 symptoms by reducing viral entry into host cells
Data Source
AI summary
This disclosure provides, among other things, formulated oltipraz compositions comprising stabilized oltipraz crystals, for use in treating a patient who has a viral infection or is at risk of incurring a viral infection. Such viral infections can include a viral infection caused by a coronavirus such as one associated with MERS or SARS, e.g., SARS-CoV-2.