Torasemide Composition Stability via Organic Solvent
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Solution Overview
Problem
Torasemide compositions have a narrow therapeutic margin and low stability in aqueous solutions, leading to undesirable effects and limited dosing flexibility, with existing solutions failing to provide stable, multi-use compositions with antimicrobial properties suitable for both human and veterinary use.
Innovation Solution
An aqueous composition with at least 30% organic solvent by weight, such as propylene glycol, is developed, offering improved physical, chemical, and antimicrobial stability over a wider pH range, allowing for multi-use and precise dosing control, suitable for both oral and parenteral administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If torasemide is formulated in aqueous solution, then it can be administered by oral or parenteral route, but it has low stability and narrow therapeutic margin
Solution Approach 1:
The patent uses a composite solvent system combining water with organic solvents (polyethylene glycol, polypropylene glycol, glycerol, propylene glycol, ethanol, or propanol) to create a stable aqueous composition that maintains torasemide solubility and therapeutic efficacy while improving stability for multi-use administration
2Quantity of substance
If pH is adjusted to 9.3-9.9 with organic solvent below 20%, then torasemide solubility is improved, but stability is insufficient and antimicrobial protection is lacking
Solution Approach 1:
The patent optimizes multiple parameters simultaneously: increases organic solvent content to 20-70% (w/w), adjusts pH to 7.5-10.0, and selects specific buffer systems to achieve both improved solubility and enhanced stability with antimicrobial properties for multi-use
Solution Approach 2:
The composition uses a composite system combining water, organic solvents, buffers (phosphates, citrates, acetates, carbonates, bicarbonates, borates), and optional preservatives to achieve synergistic effects for stability and antimicrobial protection
3Measurement precision
If dose is adjusted for narrow therapeutic margin, then treatment precision is improved, but dosing flexibility for different body weights is limited
Solution Approach 1:
The stable, multi-use composition allows dynamic dose adjustment by withdrawing variable volumes from the same composition using syringes or dosing devices, enabling precise dosing for different body weights and therapeutic requirements without preparing multiple fixed-dose formulations
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 composition maintains stability for at least 24 months, reduces the need for antimicrobial preservatives, and allows for flexible dosing adjustments based on body weight, enhancing treatment efficacy and reducing costs.
Implementation Method 1
An aqueous composition including torasemide and at least one organic solvent, in a percentage by weight of at least 30%
Data Source
AI summary
An aqueous composition including torasemide and at least one organic solvent, to a bottle or container including the composition, and to a kit including the bottle or container and a device for delivery of the composition (for example a syringe).A use of at least one organic solvent for increasing the stability and/or the antimicrobial properties of a composition including torasemide.A method for preparing the composition.