Sublingual Tadalafil Formulation for Rapid Bioavailability

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Solution Overview

Problem

Existing oral phosphodiesterase type 5 (PDE5) inhibitors for erectile dysfunction (ED) face challenges such as long onset of action, high first-pass metabolism, low bioavailability, and inconvenience due to the need for administration with water and discretion, especially in men with comorbidities like depression and embarrassment.

Innovation Solution

Development of stable, concentrated, and palatable pharmaceutical formulations for buccal and sublingual administration containing tadalafil or its derivatives, combined with solvents like propylene carbonate and ethanol, allowing discreet and convenient delivery of PDE5 inhibitors, along with additional therapeutic agents for comorbidities.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If oral phosphodiesterase type 5 (PDE5) inhibitors are administered conventionally, then the treatment can be delivered systemically, but the onset of action is long and bioavailability is low due to high first-pass metabolism

Engineering Contradiction:

Improveonset of actionVSAvoidbioavailability

Core Design Contradiction:

SpeedVSReliability

Solution Approach 1:

The patent extracts the active ingredient tadalafil from conventional oral tablet form and delivers it directly to the sublingual mucosa, bypassing the gastrointestinal tract and hepatic first-pass metabolism. This extraction of the drug from its traditional delivery system resolves the contradiction by enabling rapid onset while maintaining high bioavailability through direct mucosal absorption.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces a sublingual solution formulation as an intermediary delivery system between the oral route and systemic circulation. This liquid formulation allows the drug to dissolve in saliva and be absorbed directly through the highly vascularized sublingual mucosa, serving as an effective mediator that bypasses first-pass metabolism while achieving rapid systemic delivery.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If oral formulations are used, then the treatment can be administered conveniently, but the administration requires water and discretion due to embarrassment

Engineering Contradiction:

Improveconvenience of administrationVSAvoidembarrassment and social stigma

Core Design Contradiction:

Ease of operationVSObject-generated harmful factors

Solution Approach 1:

The patent employs a small-volume sublingual solution that can be administered discreetly without requiring water or special equipment. The formulation is designed to be applied and absorbed quickly in private moments, eliminating the need for conspicuous pill-taking rituals and reducing the embarrassment associated with conventional oral medication administration.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

3Reliability

If conventional oral therapy is used, then the treatment can be delivered, but the patient compliance is reduced due to long onset time and need for water administration

Engineering Contradiction:

Improvepatient complianceVSAvoidtime required for administration

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The sublingual solution formulation is prepared in advance as a ready-to-use liquid that can be applied immediately without requiring water or complex administration steps. This preliminary preparation of the drug in an optimized delivery form eliminates delays associated with conventional oral administration and improves patient compliance through simplified, faster use.

Inventive Principle:

Principle #10Preliminary action

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 formulations provide rapid bioavailability, improved patient compliance, and reduced side effects by avoiding gastrointestinal absorption, offering a convenient and effective treatment for ED and associated conditions with enhanced bioavailability and cost savings.

Implementation Method 1

pharmaceutical formulations suitable for buccal and/or sublingual administration containing a phosphodiesterase type 5 (PDE5) inhibitor... by avoiding gastrointestinal absorption

Methodology Applied

Scientific EffectMucosal absorption: Absorption (physical)

Implementation Method 2

stable, concentrated, and palatable pharmaceutical formulations... containing tadalafil or its derivatives, combined with solvents like propylene carbonate and ethanol

Methodology Applied

Scientific EffectDissolution: Solvation

Data Source

PatentUS12599554B2Pharmaceutical formulations comprising tadalafil

Publication Date: 2026.04.14 KYDES PHARMACEUTICALS LLC

AI summary

Provided are stable, concentrated, and palatable solutions suitable for sublingual and/or transurethral administration containing tadalafil, with or without other active ingredients to address comorbidities, in a liquid vehicle or solvent selected from propylene carbonate, 2-pyrrolidone, dimethyl isosorbide, dimethyl acetamide, n-methyl-2-pyrrolidone, ethanol, water, oleic acid, and isopropyl myristate. The solutions have low irritancy for sublingual tissues and a-are compatible with commercial atomizers. The invention is further directed to methods of treating male erectile dysfunction and/or comorbidities by administering an effective amount of the pharmaceutical formulations comprising tadalafil, with or without other active ingredients, to a patient in need of such treatments.