Transdermal Hormone Patch Without Penetration Enhancers

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Solution Overview

Problem

Transdermal systems for hormone delivery, particularly progestins like Gestodene, often require penetration enhancers that can irritate the skin and reduce stability, leading to viscosity issues and unsightly patches.

Innovation Solution

A transdermal composition without penetration enhancers, utilizing a drug-containing layer with limited solubility for Gestodene, typically up to 3% by weight, using non-polar polymers like polyisobutylenes, which ensures high release rates and skin penetration without irritation, maintaining transparency and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If penetration enhancers are incorporated into transdermal systems for hormone delivery, then skin penetration of hormones is improved, but skin irritation and stability issues occur

Engineering Contradiction:

Improveskin penetration rateVSAvoidskin irritation

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The invention extracts and eliminates penetration enhancers from the transdermal system formulation. By removing these harmful substances while maintaining effective hormone delivery through optimized adhesive polymer selection and formulation, the system achieves skin penetration without causing irritation or stability issues.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention changes the formulation parameters by selecting specific adhesive polymers with appropriate molecular weights and compositions that inherently facilitate hormone penetration without requiring additional penetration enhancers. This parameter optimization allows effective drug delivery while avoiding the harmful effects of traditional enhancers.

Inventive Principle:

Principle #35Parameter changes

2Quantity of substance

If penetration enhancers are used to achieve effective hormone delivery, then plasma concentration levels are improved, but viscosity issues and unsightly patches result

Engineering Contradiction:

Improveplasma concentration of hormoneVSAvoidformulation stability

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The invention removes penetration enhancers from the formulation, eliminating the cause of viscosity problems and appearance issues. The system achieves effective plasma concentration levels through optimized adhesive formulation that does not rely on these problematic additives.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention uses composite adhesive formulations combining specific polymer blends that work synergistically to enable hormone penetration and maintain formulation stability. The composite material approach replaces the need for penetration enhancers while maintaining effective drug delivery.

Inventive Principle:

Principle #40Composite materials

3Quantity of substance

If polar polymers are used in the adhesive layer to improve hormone solubility, then hormone delivery is enhanced, but skin irritation increases

Engineering Contradiction:

Improvehormone delivery amountVSAvoidskin irritation

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The invention changes the polymer selection parameters by opting for non-polar or less polar adhesive polymers with specific molecular weight ranges. This parameter change maintains hormone solubility and delivery effectiveness while reducing skin irritation compared to traditional polar polymer formulations.

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

Achieves therapeutically effective plasma levels of Gestodene for contraception and other applications like ovulation inhibition, pre-menstrual syndrome, and osteoporosis prevention without skin irritation or stability issues, maintaining transparency and prolonged plasma levels.

Implementation Method 1

Transdermal delivery of at least one hormone, preferably a progestin, such as a gestodene... estrogens and progestins do generally poorly penetrate the skin... achieve high release rates and skin penetration without irritation

Methodology Applied

Scientific EffectPermeation: Permeation

Implementation Method 2

utilizing a drug-containing layer with limited solubility for Gestodene, typically up to 3% by weight... maintaining transparency and stability

Methodology Applied

Scientific EffectSolubility: Solvation

Data Source

PatentUS8668925B2Transdermal delivery of hormones without the need of penetration enhancers

Publication Date: 2014.03.11 LUYE PHARMA SWITZERLAND AG

AI summary

The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). Upon administering the patch to a woman, plasma levels of at least 1.0 ng/ml of Gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.