Aripiprazole Formulations for Rapid Intramuscular Injection

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Solution Overview

Problem

Existing methods for administering antipsychotic drugs like aripiprazole suffer from poor patient compliance due to once-a-day dosing schedules and moderate to severe tissue irritation from intramuscular and subcutaneous injections, necessitating improved delivery methods that enhance compliance and minimize injection site reactions.

Innovation Solution

A rapid injection rate of at least 0.3 mL/s is used for intramuscular administration of a pharmaceutical composition comprising 24-30% aripiprazole, 0.3-0.4% sorbitan laurate, and 0.1-0.3% polysorbate 20, which minimizes needle clogging and injection site reactions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If intramuscular injection is used to improve patient compliance and reduce dosing frequency, then compliance is improved, but tissue irritation and injection site reactions occur

Engineering Contradiction:

Improvepatient complianceVSAvoidtissue irritation

Core Design Contradiction:

Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent changes the physical parameters of the injection process by administering the formulation at a rapid injection rate (at least 0.3 mL/s), which transforms the injection from a slow process that causes tissue irritation to a rapid process that minimizes irritation while maintaining compliance benefits

Inventive Principle:

Principle #35Parameter changes

2Object-affected harmful factors

If slow injection rate is used to minimize tissue irritation, then injection site reactions are reduced, but needle clogging occurs

Engineering Contradiction:

Improveinjection site reactionsVSAvoidneedle clogging

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent inverts the conventional approach by using a rapid injection rate instead of a slow rate, which counterintuitively reduces both needle clogging and injection site reactions simultaneously through the specific formulation characteristics

Inventive Principle:

Principle #13The other way round (Inversion)

3Reliability

If rapid injection rate is used to prevent needle clogging, then injection reliability is improved, but pain intensity and tissue irritation increase

Engineering Contradiction:

Improveinjection deliveryVSAvoidpain intensity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical composition parameters by incorporating specific surfactants (sorbitan laurate and polysorbate 20) in optimized concentrations that allow rapid injection delivery while minimizing pain and tissue irritation through reduced surface tension and improved tissue compatibility

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250108047A1Aripiprazole formulations having increased injection speeds

Publication Date: 2025.04.03 ALKERMES PHARMA IRELAND LTD

AI summary

The present invention relates to pharmaceutical compositions comprising a compound of Formula (I) that are useful for the intramuscular delivery of antipsychotic drugs using rapid injection rates.