Acyclovir Hyaluronic Acid Topical Composition Pain Relief

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Solution Overview

Problem

Current treatments for Herpes simplex labialis and genitalis infections, such as those containing acyclovir, do not effectively address pain symptoms and promote re-epithelialization after blister bursting and scab formation, leading to prolonged discomfort and risk of bacterial or fungal infections.

Innovation Solution

Topical pharmaceutical compositions comprising acyclovir at 2-8% w/w and hyaluronic acid sodium salt with a molecular weight of 160-200 kDa, in the form of sticks, O/W emulsions, or vaginal pessaries, which provide pain relief and enhance re-epithelialization by interacting with pain-mediating receptors and maintaining active ingredient persistence.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If acyclovir is used to treat Herpes simplex infections, then antiviral activity is improved, but pain relief and re-epithelialization are insufficient

Engineering Contradiction:
Improveantiviral activityVSAvoidpain relief efficacy
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent combines acyclovir (antiviral agent) with hyaluronic acid (pain relief and tissue repair agent) in a single topical composition. This merging of two distinct therapeutic functions into one formulation resolves the contradiction by simultaneously providing antiviral activity and pain relief with re-epithelialization promotion, eliminating the need for separate treatments.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The topical composition is designed to perform multiple functions: antiviral action (acyclovir), pain relief (hyaluronic acid), and promotion of re-epithelialization (hyaluronic acid). This multi-functional formulation addresses the limitation of acyclovir alone by incorporating substances that provide additional therapeutic benefits without compromising the primary antiviral effect.

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

2Object-affected harmful factors

If blisters burst during Herpes simplex infection, then viral release is reduced, but pain increases and re-epithelialization is delayed

Engineering Contradiction:
Improveviral spreadVSAvoidhealing speed
Core Design Contradiction:
Object-affected harmful factorsVSProductivity

Solution Approach 1:

The patent applies the composition prophylactically at the first sign of herpes outbreak, before blisters form or burst. The hyaluronic acid creates a protective film that prevents blister rupture and reduces pain from the outset. This preliminary action prevents the harmful sequence of blister bursting that leads to increased pain and delayed healing, while simultaneously promoting faster re-epithelialization.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent converts the harmful effect of blister bursting into a beneficial outcome by using hyaluronic acid to manage the bursting process. When blisters do burst, the hyaluronic acid formulation reduces pain and promotes rapid re-epithelialization, transforming what would be a harmful event (painful rupture with delayed healing) into a controlled process with minimal discomfort and faster recovery.

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

3Reliability

If topical compositions are applied frequently for prolonged treatment, then antiviral efficacy is maintained, but patient comfort and adherence decrease due to prolonged pain

Engineering Contradiction:
Improveantiviral efficacyVSAvoidpatient adherence
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

By combining acyclovir with hyaluronic acid in a single formulation, the patent addresses both antiviral efficacy and pain relief simultaneously. This eliminates the need for patients to tolerate prolonged pain while maintaining antiviral treatment, thereby improving comfort and likelihood of adherence to the treatment regimen.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent converts the harmful prolonged pain associated with frequent topical applications into a beneficial experience by incorporating hyaluronic acid's analgesic and soothing properties. Patients experience pain relief rather than discomfort during application, making frequent applications more acceptable and improving overall adherence.

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

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 compositions offer rapid and significant pain reduction, improved re-epithelialization, and prolonged antiviral activity, reducing the risk of secondary infections and enhancing patient comfort, particularly for immunodepressed individuals.

Implementation Method 1

hyaluronic acid in the form of sodium salt with a molecular weight of between 160 and 200 kDa... which provide pain relief and enhance re-epithelialization by interacting with pain-mediating receptors

Methodology Applied
Scientific EffectReceptor interaction:

Implementation Method 2

HA plays a crucial role in the tissue repair process, firstly from the structural standpoint (by organising the extracellular matrix and regulating its hydration), and secondly as a substance that stimulates a wide range of processes in which it acts directly and/or indirectly (clot formation, phagocyte activity, fibroblast proliferation, neovascularisation, re-epithelialisation, etc.)

Methodology Applied
Scientific EffectTissue repair:

Implementation Method 3

Said medicament exercises an intense antiviral activity; it inhibits viral replication, preventing or greatly slowing the progress of the infection

Methodology Applied
Scientific EffectViral replication inhibition:

Data Source

PatentEP2771013B1Topical pharmaceutical compositions comprising acyclovir and hyaluronic acid
Publication Date: 2016.07.13 FIDIA FARM SPA
  • EP2771013B1 patent drawingFigure 1~2
  • EP2771013B1 patent drawingFigure 3~4
  • EP2771013B1 patent drawing

AI summary

The present invention relates to topical painkilling pharmaceutical compositions containing acyclovir and a hyaluronic acid salt, and the use thereof.