Aprepitant Emulsion Formulation Without Ethanol for Stable Injection

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Solution Overview

Problem

Existing aprepitant emulsions for parenteral administration suffer from stability issues and require high ethanol concentrations, making them unsuitable for patients intolerant to ethanol.

Innovation Solution

An emulsion comprising aprepitant, an emulsifier, polyethylene glycol, and water, with a pH of 8.0 to 9.0, that is substantially free of ethanol, and a preparation method involving mixing and sterilization steps.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If a high concentration of ethanol is added to the emulsion, then the solubility of aprepitant is improved, but the emulsion becomes unsuitable for ethanol-intolerant patients and stability deteriorates

Engineering Contradiction:

Improveethanol concentrationVSAvoidemulsion stability

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The invention extracts ethanol from the emulsion formulation, completely replacing it with polyethylene glycol as the injection agent. This removes the harmful substance (ethanol) while maintaining the necessary solubility and stability functions through the alternative agent (polyethylene glycol), thereby resolving the contradiction between ethanol concentration and emulsion stability.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention changes the chemical parameter of the injection agent from ethanol to polyethylene glycol. This parameter substitution fundamentally alters the formulation composition, enabling the emulsion to achieve both stability and suitability for ethanol-intolerant patients without relying on ethanol concentration.

Inventive Principle:

Principle #35Parameter changes

2Stability of the object's composition

If the pH of the emulsion is adjusted to 8.0 to 9.0, then the stability of the emulsion is improved, but the complexity of formulation increases

Engineering Contradiction:

Improveemulsion stabilityVSAvoidformulation complexity

Core Design Contradiction:

Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The invention optimizes the pH parameter within the specific range of 8.0 to 9.0, which has been determined to provide optimal stability for the aprepitant emulsion. This parameter optimization balances stability improvement with formulation simplicity, as the pH adjustment is achieved through standard pharmaceutical practices without requiring complex additional components.

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

The emulsion achieves enhanced stability and can be administered to ethanol-intolerant patients without ethanol, maintaining aprepitant solubility and stability during storage.

Implementation Method 1

mixing aprepitant with polyethylene glycol to produce a drug phase

Methodology Applied

Scientific EffectSolvation: Solvation

Implementation Method 2

an emulsion including: aprepitant; an emulsifier; an oil; polyethylene glycol; and water

Methodology Applied

Scientific EffectEmulsion: Emulsion

Data Source

PatentUS12611410B2Emulsion, injection agent, and emulsion preparation method

Publication Date: 2026.04.28 Q P CORP

AI summary

The present invention relates to an emulsion including aprepitant, an emulsifier, an oil, polyethylene glycol, and water, without substantial addition of ethanol.