Sublingual PDE5 Inhibitor Spray for Rapid Transmucosal Absorption
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Solution Overview
Problem
Oral administration of PDE5 inhibitors like sildenafil faces challenges such as variable absorption, adverse effects, and slow onset of action, making it inefficient for treating erectile dysfunction and pulmonary arterial hypertension.
Innovation Solution
A sublingual transmucosal delivery method using a pharmaceutical composition comprising a PDE5 inhibitor, such as sildenafil mesylate, in a carrier that is soluble or forms a suspension or emulsion, providing rapid absorption and minimizing gastrointestinal adverse effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral administration is used to deliver PDE5 inhibitors, then the drug can reach the site of action, but absorption is variable and gastrointestinal adverse effects occur
Solution Approach 1:
The patent introduces a sublingual spray formulation as an intermediary delivery system that bypasses the gastrointestinal tract. The spray delivers the PDE5 inhibitor directly to the sublingual mucosa, which serves as an alternative absorption pathway, eliminating exposure to gastric acid and intestinal enzymes while providing consistent absorption through the rich vascularization of the oral mucosa.
Solution Approach 2:
The invention transitions from the conventional oral gastrointestinal absorption pathway to a trans-mucosal absorption pathway in the oral cavity. This dimensional change in the delivery route allows the drug to enter systemic circulation directly through the sublingual vessels, avoiding the harmful gastrointestinal environment while maintaining reliable and consistent drug delivery.
2Speed
If oral administration is used to deliver PDE5 inhibitors, then the drug can be delivered systemically, but the onset of action is slow
Solution Approach 1:
The sublingual spray formulation allows the PDE5 inhibitor to skip the slow processes of gastric emptying, intestinal transit, and hepatic first-pass metabolism. The drug is rapidly absorbed through the highly vascularized sublingual mucosa, rushing the active ingredient directly into systemic circulation and achieving therapeutic concentrations much faster than oral administration.
Solution Approach 2:
The spray formulation is designed to be applied directly to the sublingual area, where the drug is immediately available for absorption. This preliminary positioning of the drug at an optimal absorption site with rich blood supply ensures rapid uptake and quick onset of action, eliminating the delays associated with conventional oral delivery.
3Ease of operation
If oral tablets are used for PDE5 inhibitor delivery, then the formulation is simple, but the drug may be lost from the mouth or stomach
Solution Approach 1:
The invention replaces the mechanical swallowing action required for tablet administration with a spray delivery system that applies the drug directly to the sublingual mucosa. The spray formulation adheres to the mucosal surface, allowing absorption without requiring swallowing, thereby eliminating drug loss through vomiting or spitting while maintaining ease of administration.
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 sublingual transmucosal delivery method achieves consistent and rapid absorption of PDE5 inhibitors, reducing adverse effects and improving treatment efficacy for erectile dysfunction and pulmonary arterial hypertension.
Implementation Method 1
sublingual transmucosal delivery method achieves consistent and rapid absorption of PDE5 inhibitors
Implementation Method 2
a carrier in which said PDE5 inhibitor is soluble or forms a suspension or emulsion
Data Source
Figure 1
AI summary
The invention provides a pharmaceutical composition for the transmucosaldelivery of a PDE5 inhibitor, said composition comprising a PDE5 inhibitor and a carrier in which said PDE5 inhibitor is soluble or forms a suspension or emulsion. The invention also provides a pharmaceutical composition comprising a PDE5 inhibitor for use in inhibiting PDE activity in vivo, where in said use said composition is delivered by the transmucosal route.