Heptyl Glucoside Transdermal Solubility and Permeability

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Solution Overview

Problem

Current transdermal drug delivery methods face challenges with the low solubility and permeability of many active pharmaceutical ingredients (APIs), often requiring high doses and using toxic or irritating chemical solubilizers and penetration enhancers.

Innovation Solution

Heptyl glucoside, a natural alkyl glycoside derived from sugar and alcohol, is used as a biobased non-ionic surfactant to enhance the solubility and skin permeability of APIs in transdermal pharmaceutical compositions, acting as both a solubilizer and penetration enhancer, allowing for complete dissolution and increased bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If chemical solubilizers and penetration enhancers are used to improve API solubility and skin permeability, then the solubility and permeability are enhanced, but the composition becomes toxic, irritating, or allergenic

Engineering Contradiction:

ImproveAPI solubilityVSAvoidtoxicity and irritation

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters by replacing traditional chemical solubilizers with heptyl glucoside, a natural alkyl glycoside with different physicochemical properties. This parameter change maintains solubility enhancement while eliminating toxicity and irritation associated with conventional agents

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses heptyl glucoside as a composite natural surfactant formed from sugar and alcohol components. This composite structure provides both solubilization and penetration enhancement capabilities while maintaining biocompatibility and safety profiles superior to synthetic alternatives

Inventive Principle:

Principle #40Composite materials

2Reliability

If high doses of APIs are used to overcome low solubility and permeability, then adequate therapeutic effect is achieved, but the dosage increases and potential side effects rise

Engineering Contradiction:

Improvetherapeutic effectVSAvoidAPI dosage

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

Heptyl glucoside acts as an intermediary substance that facilitates API delivery through the skin. By improving both solubility and permeability, it enables lower API doses to achieve the same therapeutic effect, reducing the mediator's role in enhancing bioavailability while minimizing dosage requirements

Inventive Principle:

Principle #24Intermediary (Mediator)

3Ease of operation

If traditional topical treatments are used for API delivery, then the application is simple, but the bioavailability and skin permeation are insufficient

Engineering Contradiction:

Improveapplication simplicityVSAvoidAPI bioavailability

Core Design Contradiction:

Ease of operationVSQuantity of substance

Solution Approach 1:

Heptyl glucoside performs multiple functions simultaneously: it acts as a solubilizer, penetration enhancer, and bioavailability promoter. This multi-functionality maintains the simplicity of topical application while dramatically improving API delivery efficiency and therapeutic effectiveness

Inventive Principle:

Principle #6Universality (Multi-functionality)

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

Heptyl glucoside enables effective transdermal absorption of APIs at lower doses, improving bioavailability and skin permeation without altering the pharmaceutical composition, and is suitable for various APIs and dosage forms, offering a safer and more efficient delivery method compared to traditional topical treatments.

Implementation Method 1

heptyl glucoside is: a 100% biobased non-ionic surfactant; a concentrated oil/water solubilizer

Methodology Applied

Scientific EffectSurfactant action: Surfactant

Implementation Method 2

heptyl glucoside enables the introduction of hydrophobic compounds into an aqueous medium

Methodology Applied

Scientific EffectSolubilization: Solvation

Implementation Method 3

heptyl glucoside is employed as a natural solubilizer and as a skin penetration enhancer for use in transdermal pharmaceutical compositions

Methodology Applied

Scientific EffectPermeation enhancement: Permeation

Data Source

PatentUS9750813B2Use of heptyl glucoside as skin penetration enhancer in transdermal pharmaceutical compositions

Publication Date: 2017.09.05 PROFESSIONAL COMPOUNDING CENTS OF AMERICA PCCA

AI summary

The present disclosure refers to heptyl glucoside included, as a natural solubilizer and as a skin penetration enhancer, in transdermal pharmaceutical compositions. Heptyl glucoside is a natural alkyl glycoside and a hydrotrope that improves solubility of active pharmaceutical ingredients (APIs), thereby enhancing skin permeability to APIs. Transdermal pharmaceutical compositions including heptyl glucoside allow lower APIs dosage requirements. Heptyl glucoside can be combined with at least one API and suitable ingredients to formulate transdermal pharmaceutical compositions with improved skin permeability, thereby promoting percutaneous absorption of APIs. Transdermal pharmaceutical compositions including heptyl glucoside can be formulated in a plurality of dosage forms, such as, a liquid, cream, paste, gel, lotion, patch (e.g., matrix and reservoir), tape, film former (e.g., plaster), and the like.