Cariprazine Embonate Crystal Forms for Long-Acting Stability

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Existing pharmaceutical formulations of pharmaceutically acceptable salts of cariprazine lack solubility, stability, and are unsuitable for long-acting administration, leading to poor patient compliance due to frequent dosing requirements.

Innovation Solution

Development of cariprazine embonate in various crystalline forms, prepared through neutralization reactions with embonic acid, offering low solubility and high stability suitable for sustained-release preparations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If cariprazine hydrochloride is used as the pharmaceutical salt, then the solubility is improved, but the stability deteriorates due to rapid dissociation into free base in pH 6.5 buffer

Engineering Contradiction:

ImprovesolubilityVSAvoidstability

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent changes the chemical parameter of the pharmaceutical salt from hydrochloride to embonate, which fundamentally alters the dissociation behavior and stability profile while maintaining adequate solubility for therapeutic use

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The embonate salt acts as an intermediary form that provides both solubility and stability, mediating between the soluble but unstable hydrochloride form and the stable but insoluble free base form

Inventive Principle:

Principle #24Intermediary (Mediator)

2Duration of action of moving object

If cariprazine is administered as oral preparation requiring daily intake, then the plasma concentration can be maintained, but the patient compliance deteriorates due to frequent administration

Engineering Contradiction:

Improveplasma concentration maintenanceVSAvoidpatient compliance

Core Design Contradiction:

Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent uses an excessive amount of cariprazine embonate in the injection formulation to achieve sustained release over multiple weeks, eliminating the need for daily administration and significantly improving patient compliance

Inventive Principle:

Principle #16Partial or excessive action

Solution Approach 2:

The sustained-release injection provides continuous therapeutic action over several weeks through controlled release from the depot formulation, replacing the discontinuous daily oral dosing regimen

Inventive Principle:

Principle #20Continuity of useful action

3Quantity of substance

If existing cariprazine salts with high solubility are used, then the dissolution is improved, but the suitability for long-acting administration deteriorates

Engineering Contradiction:

ImprovesolubilityVSAvoidlong-acting administration suitability

Core Design Contradiction:

Quantity of substanceVSDuration of action of stationary object

Solution Approach 1:

The patent optimizes the solubility parameter to an intermediate level that is sufficient for therapeutic effect but low enough to enable sustained-release formulation, achieving both dissolution and long-acting characteristics

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 cariprazine embonate crystalline forms provide improved stability and solubility characteristics, facilitating long-acting sustained-release formulations with enhanced clinical efficacy and commercial viability.

Implementation Method 1

conducting a reaction (e.g., a neutralization reaction) of the cariprazine free base with embonic acid to give the pharmaceutical salt of cariprazine

Methodology Applied

Scientific EffectNeutralization reaction: Chemical Bonding

Data Source

PatentEP4206191B1Pharmaceutically acceptable salt of cariprazine and crystal form thereof, and preparation method therefor and use thereof

Publication Date: 2025.12.17 SHANGHAI BOCIMED PHARMA CO LTD

Figure 1~2
Figure 3~4
Figure 5

AI summary

Disclosed are a pharmaceutically acceptable salt of cariprazine, a preparation method therefor, a pharmaceutical composition containing same, and the use thereof. The pharmaceutically acceptable salt of cariprazine is a salt formed from the free base of cariprazine and an organic acid having six or more carbon atoms, and has relatively good solubility and stability, thereby having a good marketization prospect.