Aqueous Ophthalmic Composition Foam Reduction via Additive Mediation

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Solution Overview

Problem

Aqueous ophthalmic compositions containing polyoxyethylene castor oil and polyethylene glycol monostearate tend to foam easily, making it difficult to distinguish foreign matter and prolonging production steps such as dissolution check and foreign matter detection.

Innovation Solution

Incorporating sesame oil, castor oil, vitamin A, or chlorobutanol into the composition to reduce foaming and accelerate defoaming, thereby improving production efficiency and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If polyoxyethylene castor oil and polyethylene glycol monostearate are added to dissolve components with low water solubility, then dissolution capability is improved, but foaming increases and defoaming time is prolonged

Engineering Contradiction:
Improvedissolution capabilityVSAvoiddefoaming time
Core Design Contradiction:
Quantity of substanceVSLoss of time

Solution Approach 1:

The patent introduces a third substance as an intermediary to mediate between the surfactants (which cause foaming) and the aqueous environment. This intermediary substance modifies the foam properties by interacting with the surfactant molecules, reducing foam stability and accelerating defoaming while preserving the surfactants' dissolution function.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical composition parameters of the ophthalmic solution by adding specific substances that alter the foam's physical and chemical properties. This modifies the surface tension dynamics and foam film stability, causing foam to disappear faster without affecting the surfactants' ability to dissolve lipophilic components.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If polyoxyethylene castor oil and polyethylene glycol monostearate are added to dissolve components with low water solubility, then dissolution capability is improved, but foam generation increases making foreign matter detection difficult

Engineering Contradiction:
Improvedissolution capabilityVSAvoidforeign matter detection
Core Design Contradiction:
Quantity of substanceVSDifficulty of detecting and measuring

Solution Approach 1:

The patent introduces a third substance as an intermediary to mediate between the surfactants (which cause foaming) and the aqueous environment. This intermediary substance modifies the foam properties by interacting with the surfactant molecules, reducing foam stability and accelerating defoaming while preserving the surfactants' dissolution function.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the harmful effect of foam (which obscures foreign matter detection) into a beneficial effect by selecting substances that cause rapid foam collapse. The foam that initially causes detection problems quickly disappears, actually helping to clear the view for foreign matter detection while maintaining the necessary dissolution capability.

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

3Quantity of substance

If polyoxyethylene castor oil and polyethylene glycol monostearate are added to dissolve components with low water solubility, then dissolution capability is improved, but production efficiency decreases due to prolonged dissolution check and foreign matter detection

Engineering Contradiction:
Improvedissolution capabilityVSAvoidproduction efficiency
Core Design Contradiction:
Quantity of substanceVSProductivity

Solution Approach 1:

The patent introduces a third substance as an intermediary to mediate between the surfactants (which cause foaming) and the aqueous environment. This intermediary substance modifies the foam properties by interacting with the surfactant molecules, reducing foam stability and accelerating defoaming while preserving the surfactants' dissolution function.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent enables the production process to skip or rush through the foam-related delays by causing foam to collapse rapidly. This reduces or eliminates the need to wait for foam to naturally dissipate before proceeding with dissolution checks and foreign matter detection, thereby accelerating production throughput.

Inventive Principle:
Principle #21Skipping (Rushing through)

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 addition of these components significantly reduces foaming and defoaming time, enhances antimicrobial effectiveness, stabilizes tear films, and improves the composition's ability to spread lipid layers, making it suitable for use in eye drops and contact lens care solutions.

Implementation Method 1

A surfactant can be given as an example of the solubilizing agents used in the field of ophthalmology. It is known that polyoxyethylene castor oil is a nonionic surfactant and is added to an aqueous ophthalmic composition for helping dissolution of other components

Methodology Applied
Scientific EffectSurfactant: Surfactant

Implementation Method 2

Vitamins A have been added to an ophthalmic composition ever before for purposes such as reducing eyestrain by promoting eye cell metabolism and respiration, and exhibiting anti-inflammatory action (Patent Literature 3). Chlorobutanol is also known as an additive for an aqueous ophthalmic composition.

Methodology Applied
Scientific EffectAntimicrobial action: Preservative

Data Source

PatentUS9427473B2Aqueous ophthalmic composition
Publication Date: 2016.08.30 ROHTO PHARM CO LTD
  • US9427473B2 patent drawing

AI summary

The present invention relates to an aqueous ophthalmic composition comprising (A) polyoxyethylene castor oil, (B) polyethylene glycol monostearate, and (C) at least one member selected from the group consisting of sesame oil, castor oil, vitamin A, and chlorobutanol.