Minoxidil Release Composition for Extended Dermal Flux

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Solution Overview

Problem

Conventional twice-daily administration of minoxidil for hair growth is unnecessary and can cause systemic side effects, as it results in higher dosages than required for therapeutic efficacy.

Innovation Solution

A method of topical minoxidil administration using a release composition with glycerin and an emulsifying non-ionic surfactant, such as polysorbate, to achieve a dermal flux of at least 1.5 μg/cm²/hour for 17-27 hours with a reduced daily dose of 2-20 mg, allowing for once-daily application and extended therapeutic action.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional twice-daily minoxidil administration is used, then therapeutic efficacy for hair growth is achieved, but systemic side effects increase and dosage complexity increases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the minoxidil delivery into two distinct components: an aqueous release composition (glycerin + polysorbate) applied first, followed by the minoxidil solution. This segmentation allows the release composition to control the rate and duration of minoxidil delivery, extending therapeutic action to 17-27 hours and enabling once-daily dosing while reducing peak concentrations that cause systemic side effects

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The aqueous release composition acts as an intermediary between the minoxidil solution and the scalp. When layered together, the release composition mediates the dermal flux of minoxidil, controlling its absorption rate and extending its presence on the scalp for 17-27 hours. This intermediary mechanism reduces the need for frequent high-dose applications, thereby reducing systemic side effects while maintaining therapeutic efficacy

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If conventional twice-daily minoxidil administration is used, then therapeutic efficacy is maintained, but treatment complexity and patient burden increase

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidadministration frequency
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent achieves continuous useful action by formulating a system that maintains therapeutic minoxidil levels on the scalp for 17-27 hours through the interaction of the release composition and minoxidil solution. This extended duration of action allows patients to apply the treatment only once daily, eliminating the need for twice-daily applications and significantly improving ease of operation and patient adherence while maintaining therapeutic efficacy

Inventive Principle:
Principle #20Continuity of useful action

3Reliability

If higher minoxidil dosage is administered, then therapeutic efficacy is improved, but systemic side effects increase

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidminoxidil dosage
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent changes the temporal parameters of minoxidil delivery by using the aqueous release composition to extend the duration of action from conventional short-duration multiple applications to a sustained 17-27 hour release profile. This parameter change allows the same therapeutic effect to be achieved with lower total daily dosage (2-20 mg) administered once daily, rather than higher dosages split into multiple applications, thereby reducing systemic side effects while maintaining efficacy

Inventive Principle:
Principle #35Parameter changes

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

This regimen reduces systemic side effects and maintains therapeutic efficacy with lower dosages, enhancing medication adherence by allowing a single daily application while achieving equivalent results to conventional twice-daily administration.

Implementation Method 1

a release composition that mediates a dermal flux of minoxidil of at least 1.5 μg minoxidil/cm2 skin area/hour for a time of from 17 to 27 hours

Methodology Applied
Scientific EffectDermal flux: Permeation

Implementation Method 2

an emulsifying non-ionic surfactant, such as polysorbate

Methodology Applied
Scientific EffectEmulsification: Emulsion

Implementation Method 3

topically applying minoxidil to a skin region susceptible to induction of hair growth

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentUS10342872B2Pharmacokinetically extended action topical hair growth formulation, and administration method
Publication Date: 2019.07.09 CELMATRIX CORP
  • US10342872B2 patent drawing

AI summary

A method of inducing hair growth by topical administration of minoxidil is described, including topically applying minoxidil to a skin region susceptible to induction of hair growth, wherein the applied minoxidil is administered to the skin region (i) in a formulation comprising a release composition that mediates a dermal flux of minoxidil of at least 1.5 μg minoxidil/cm2 skin area/hour for a time of from 17 to 27 hours, at an applied dose of from 2 to 20 mg minoxidil to said skin region, and with a period of from 16 to 30 hours before any subsequent reapplication of the formulation, or (ii) subsequent to administration to the skin region of said release composition so that the sequentially applied minoxidil and release composition together mediate the dermal flux of minoxidil of at least 1.5 μg minoxidil/cm2 skin area/hour for a time of from 17 to 27 hours, at an applied dose of from 2 to 20 mg minoxidil to said skin region, and with a period of from 16 to 30 hours before any subsequent sequential reapplication of the minoxidil and release composition.