GC4711 Crystalline Forms Polymorph Screening

Solution Overview

Problem

There is an unmet need for crystalline forms of GC4711 and its mirror image GC4748 that exhibit improved properties for pharmaceutical compositions, such as stability and solubility, which are essential for effective drug delivery and shelf life.

Innovation Solution

The present disclosure provides polymorph screens that identify crystalline forms of GC4711 with good physical properties, including preliminary characterization of amorphous and crystalline materials, assessment of polymorphic complexity, limited characterization of observed forms, and evaluation of thermodynamic relationships between forms through competitive slurry experiments.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a crystalline form of GC4711 is selected for pharmaceutical formulation, then stability and solubility are improved, but the complexity of identifying and characterizing the appropriate polymorphic form increases

Engineering Contradiction:

ImprovestabilityVSAvoidpolymorphic complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically varying crystallization conditions (solvent type, temperature, pH, concentration) to generate and identify different polymorphic forms of GC4711. This allows selection of specific crystalline forms with optimized stability and solubility parameters for pharmaceutical formulation.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent utilizes phase transitions between different crystalline forms (polymorphs) and solvates of GC4711 to achieve desired physical properties. By controlling the phase transition during crystallization, the patent identifies forms with improved stability and solubility characteristics suitable for drug formulation.

Inventive Principle:

Principle #36Phase transitions

2Ease of operation

If a crystalline form of GC4711 is selected for pharmaceutical formulation, then solubility and bioavailability are improved, but the manufacturing process complexity increases

Engineering Contradiction:

ImprovesolubilityVSAvoidmanufacturing process complexity

Core Design Contradiction:

Ease of operationVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by systematically varying crystallization conditions (solvent type, temperature, pH, concentration) to generate and identify different polymorphic forms of GC4711. This allows selection of specific crystalline forms with optimized stability and solubility parameters for pharmaceutical formulation.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses solvents as intermediaries during the crystallization process to facilitate the formation of specific polymorphic forms. The choice of solvent acts as a mediator that influences the crystal packing and resulting physical properties, enabling control over solubility and bioavailability while managing manufacturing complexity.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Duration of action of stationary object

If extended shelf life is achieved through proper crystalline form selection, then drug stability is improved, but the time and resources required for polymorph screening increase

Engineering Contradiction:

Improveshelf lifeVSAvoidscreening time

Core Design Contradiction:

Duration of action of stationary objectVSLoss of time

Solution Approach 1:

The patent applies preliminary action by conducting comprehensive polymorph screening and characterization before final formulation development. This upfront identification of stable crystalline forms prevents later instability issues and extends shelf life, while the systematic approach minimizes total screening time through efficient experimental design.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent utilizes phase transitions between different crystalline forms (polymorphs) and solvates of GC4711 to achieve desired physical properties. By controlling the phase transition during crystallization, the patent identifies forms with improved stability and solubility characteristics suitable for drug formulation.

Inventive Principle:

Principle #36Phase transitions

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 identified crystalline forms of GC4711 demonstrate improved stability and solubility, which are critical for the formulation of pharmaceutical compositions with enhanced bioavailability and extended shelf life, while also being applicable to its mirror image GC4748.

Implementation Method 1

The present disclosure provides polymorph screens that identified crystalline forms of GC4711 with good physical properties for therapeutics

Methodology Applied

Scientific EffectCrystallisation: Crystallisation

Data Source

PatentUS20250073244A1Crystalline forms of pentaaza macrocyclic ring complex

Publication Date: 2025.03.06 BIOSSIL INC

AI summary

The present invention provides crystalline forms of a pentaaza macrocyclic ring complex according to the following formula:Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of disease states.