Phenylephrine Liquid Composition pH Stabilization

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Solution Overview

Problem

Formulating stable liquid compositions for respiratory illness treatment is challenging due to the instability of pharmaceutical actives like phenylephrine, which degrades in the presence of oxygen, aldehydes, and certain acids, leading to issues such as discoloration and precipitation in combination with other actives.

Innovation Solution

The development of liquid compositions comprising phenylephrine and acetaminophen with a defined pH range of 6.5 to 7.5, being substantially free of aldehydes, and incorporating optional components like buffers, non-aldehydic aesthetic agents, and metal chelators to enhance stability and aesthetic appeal.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If phenylephrine is formulated in liquid composition with other pharmaceutical actives, then the composition can treat multiple respiratory symptoms, but phenylephrine degrades and precipitates out of solution

Engineering Contradiction:
Improvetreatment of multiple respiratory symptomsVSAvoidphenylephrine stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent adjusts the pH parameter of the liquid composition to a specific range (pH 5.0-7.5, preferably pH 6.0-7.0) to optimize phenylephrine stability. This parameter change prevents degradation and precipitation while maintaining the composition's ability to treat multiple respiratory symptoms through combination with acetaminophen and other actives.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If phenylephrine is exposed to oxygen and aldehydes in liquid solution, then the composition remains in solution form, but phenylephrine degrades and discoloration occurs

Engineering Contradiction:
Improveliquid solution formVSAvoiddegradation and discoloration
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent creates a protective chemical environment by controlling pH and eliminating aldehydes from the composition. This inert-like environment protects phenylephrine from oxidation and degradation by oxygen and aldehydes, preventing discoloration while maintaining the liquid solution form for ease of administration.

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

Solution Approach 2:

The patent converts the potentially harmful interaction between phenylephrine and oxygen/aldehydes into a beneficial stable formulation by adjusting pH to 5.0-7.5. At this optimized pH, the composition actually enhances phenylephrine stability despite the presence of oxygen, turning a harmful interaction into a stable, long-lasting liquid product.

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

3Stability of the object's composition

If phenylephrine is formulated with citric acid to adjust pH, then the composition achieves desired pH level, but phenylephrine degradation is accelerated

Engineering Contradiction:
ImprovepH controlVSAvoidphenylephrine degradation
Core Design Contradiction:
Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent extracts or removes citric acid from the formulation to eliminate the harmful degradation effect. Instead of using citric acid for pH adjustment, the patent employs alternative buffering systems that maintain pH 5.0-7.5 without causing phenylephrine degradation, thereby separating the pH control function from the degradation-causing citric acid.

Inventive Principle:
Principle #2Taking out (Extraction)

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 achieve enhanced stability and effectiveness in treating respiratory illness symptoms, maintaining phenylephrine's stability and preventing degradation, while providing a stable and aesthetically acceptable product form.

Implementation Method 1

The compositions have a pH of from 6.5 to 7.5

Methodology Applied
Scientific EffectpH buffering:

Implementation Method 2

incorporating optional components like buffers, non-aldehydic aesthetic agents, and metal chelators to enhance stability

Methodology Applied
Scientific EffectMetal chelation:

Data Source

PatentEP2012765B2Liquid compositions comprising phenylephrine and acetaminophen and their use for the treatment of respiratory illness
Publication Date: 2018.04.11 PROCTER & GAMBLE CO

AI summary

Disclosed are compositions including phenylephrine, its salts, and mixtures thereof, in combination with acetaminophen; and optionally in combination with additional pharmaceutical actives. The compositions have a pH of about 6.5 to about 7.5 and may be substantially free of aldehydes. The invention also provides a method of stabilizing phenylephrine. Also disclosed are methods of treating respiratory illness through administration of a composition comprising phenylephrine, its salts, and mixtures thereof, in combination with acteaminophen; and optionally in combination with additional pharmaceutical actives, wherein the composition has a pH of from about 6.5 to about 7.5 and may be substantially free of aldehydes.