Piper longum L. Extract for Overactive Bladder via Receptor Modulation

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for voiding dysfunction, such as overactive bladder, are often ineffective and associated with adverse effects, necessitating the development of novel alternatives that can safely and effectively manage symptoms like frequent urination, urgency incontinence, and nocturia.

Innovation Solution

A pharmaceutical and health functional food composition utilizing an extract of Piper longum L., which inhibits muscarinic M3 and M2 receptors and acts as an agonist of the β3-adrenergic receptor, thereby increasing micturition interval, decreasing micturition pressure, and enhancing bladder capacity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments for overactive bladder are used, then voiding dysfunction symptoms are addressed, but adverse effects such as thirst, constipation, blurred vision, and acute urinary retention occur

Engineering Contradiction:
Improveeffectiveness in treating voiding dysfunctionVSAvoidadverse effects including thirst, constipation, blurred vision, and acute urinary retention
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and utilizes specific natural compounds (piperine from black pepper and piperlongumine from long pepper) that selectively target overactive bladder symptoms through specific receptor mechanisms, avoiding the broad anticholinergic effects that cause adverse symptoms. This extraction of specific active ingredients from natural sources provides targeted therapy without the harmful side effects of conventional broad-spectrum medications.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent employs piperine and piperlongumine as intermediary substances that mediate between the patient's condition and the desired therapeutic effect. These compounds act as selective modulators of bladder muscle contraction through specific receptor interactions (muscarinic and adrenergic receptors), serving as a bridge that achieves symptom relief without triggering the harmful cascades associated with conventional anticholinergic drugs.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If existing medications are administered, then some symptom relief is achieved, but drug compliance is lowered due to adverse effects

Engineering Contradiction:
Improvepatient compliance and quality of lifeVSAvoidadverse effects reducing drug compliance
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent converts the potentially harmful broad anticholinergic action into a beneficial selective mechanism by utilizing natural compounds that specifically target bladder overactivity while sparing other anticholinergic effects. The harmful property of broad anticholinergic blockade is transformed into a benefit through selective receptor interaction, maintaining compliance while achieving therapeutic effect.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent changes the therapeutic parameter from broad anticholinergic blockade to selective receptor modulation by piperine and piperlongumine. This parameter change shifts the mechanism from non-selective inhibition to targeted action on specific muscarinic and adrenergic receptors in the bladder, improving compliance by eliminating the adverse effects that currently reduce drug adherence.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If the bladder contracts abnormally to store urine, then frequent urination occurs, but quality of life is significantly lowered

Engineering Contradiction:
Improvebladder storage functionVSAvoidimpact on quality of life including restricted beverage intake and frequent toilet visits
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the bladder control mechanism into specific receptor pathways (muscarinic M3/M2 and adrenergic beta3 receptors) that can be selectively modulated. By targeting these specific segments of the neural control system rather than applying broad suppression, the treatment restores normal bladder storage function while avoiding the quality-of-life deteriorating effects of conventional therapy.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent utilizes natural compounds with multiple pharmacological activities that collectively address various aspects of overactive bladder pathology. Piperine and piperlongumine work through multiple mechanisms including receptor modulation, antioxidant effects, and anti-inflammatory properties, providing comprehensive treatment that improves both bladder function and overall quality of life.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP3120859B1Composition for preventing, treating, and alleviating urinary disturbances, containing piper longum l. extract
Publication Date: 2023.05.24 DONG WHA PHARM CO LTD
  • EP3120859B1 patent drawingFigure 1
  • EP3120859B1 patent drawingFigure 2
  • EP3120859B1 patent drawingFigure 3

AI summary

The present invention relates to a pharmaceutical composition for preventing or treating voiding dysfunction and a health functional food for preventing or improving of voiding dysfunction, comprising extract of Piper Longum L. as an active ingredient. The extract of Piper Longum L. according to the present invention is not only harmless, but also has outstanding effects of preventing, treating and improving voiding dysfunction by being involved in various mechanisms related to voiding dysfunction simultaneously so that it may increase a micturition interval, decrease a micturition pressure, increase a bladder capacity, inhibit detrusor contraction and induce relaxation of detrusor.