Sildenafil Citrate Liquid Solution for Enhanced Bioavailability
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Sildenafil citrate has low bioavailability due to its low solubility in water and high presystemic elimination, leading to reduced oral bioavailability and delayed onset of therapeutic effects, as well as potential side effects from existing solid or suspension formulations.
Innovation Solution
Sildenafil citrate is dissolved in a liquid carrier comprising water and one or more alcohols, such as ethanol, at concentrations of 7 mg/ml or higher, which can be administered orally or buccally, using a nebulizer or metered dose inhaler, to enhance bioavailability and reduce dosage requirements.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If sildenafil citrate is administered in traditional tablet or suspension forms, then the formulation is stable and easy to manufacture, but the bioavailability is low and the onset of therapeutic effects is delayed
Solution Approach 1:
The patent changes the physical state of sildenafil citrate from solid (tablet) or suspension to liquid solution form. This parameter change enables faster absorption and onset of action while maintaining stability through specific formulation components like edetate disodium and controlled packaging conditions.
Solution Approach 2:
The invention creates a composite liquid formulation by dissolving sildenafil citrate in a carrier solution containing edetate disodium and other stabilizing agents. This composite approach enhances bioavailability while preventing degradation, resolving the contradiction between improved efficacy and formulation stability.
2Reliability
If sildenafil citrate is dissolved in water at high concentrations, then the bioavailability increases and dosage is reduced, but the solubility is insufficient
Solution Approach 1:
The patent introduces edetate disodium as an intermediary substance that facilitates the dissolution of sildenafil citrate in aqueous carrier solutions. This chelating agent acts as a mediator to enhance solubility, enabling high-concentration formulations with improved bioavailability without compromising dissolution capacity.
3Ease of manufacture
If solid formulations of sildenafil citrate are used, then the manufacturing is simple, but the presystemic elimination is high and side effects occur
Solution Approach 1:
The invention transitions from solid tablet formulations to liquid solution formulations, fundamentally changing the physical state parameter. This change reduces presystemic elimination and associated side effects while maintaining manufacturing feasibility through straightforward dissolution processes and stable shelf-life characteristics.
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 form of sildenafil citrate achieves increased bioavailability, faster onset of therapeutic effects, and reduced side effects by allowing for lower doses to achieve the same therapeutic effect, compared to traditional tablet or suspension forms.
Implementation Method 1
Sildenafil citrate is dissolved in a liquid carrier comprising water and one or more alcohols, such as ethanol
Data Source
AI summary
A pharmaceutical composition comprising a liquid carrier comprising water and at least 35% of ethanol and sildenafil citrate dissolved in said liquid carrier at a concentration of at least 7 mg/ml.