Blarcamesine Salt Polymorphs for Stable Drug Formulation
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Solution Overview
Problem
There is a need for additional solid state forms of Blarcamesine HCl and other salts to improve formulation, processing, stability, and bioavailability for the treatment of Neurodegenerative and Neurodevelopmental Diseases such as Alzheimer's disease, Parkinson's disease dementia, and Rett syndrome.
Innovation Solution
The development of crystalline polymorphs of Blarcamesine salts, including HCl, HBr, Tosylate, Maleate, Camphorsulfonate, and Besylate, which can be used to prepare pharmaceutical compositions and formulations, enhancing properties such as chemical stability, dissolution profile, and shelf-life.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If additional solid state forms of Blarcamesine salts are developed, then formulation and bioavailability are improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies parameter changes by developing multiple solid state forms (polymorphs and solvates) of Blarcamesine salts with different crystal structures and physical properties. By varying parameters such as crystal packing arrangement, solvent content, and molecular orientation, the invention creates diverse solid forms that offer improved formulation options and bioavailability while maintaining a systematic approach to manufacturing through controlled crystallization processes
2Reliability
If new solid state forms are discovered, then processing characteristics and stability are improved, but research and development time increases
Solution Approach 1:
The patent applies preliminary action by systematically exploring and characterizing multiple solid state forms of Blarcamesine salts during the development phase. By pre-identifying stable polymorphs and solvates with desirable properties (improved processing characteristics and stability) before formulation development, the invention reduces later development time and ensures robustness of the final pharmaceutical product
Solution Approach 2:
The invention utilizes parameter changes by controlling crystallization conditions (temperature, solvent composition, cooling rates) to access different solid state forms. This systematic variation of parameters enables identification of stable forms with improved properties while optimizing the discovery process through structured experimentation
3Adaptability or versatility
If multiple salts and solid state forms are developed, then bioavailability and shelf-life are improved, but cost increases
Solution Approach 1:
The patent applies universality by developing a portfolio of Blarcamesine salt forms (HCl, HBr, Tosylate, Maleate, Camphorsulfonate, Besylate) and their solid state forms that can serve multiple functions: improved bioavailability, enhanced stability, optimized processing characteristics, and extended shelf-life. This multi-functional approach allows selection of appropriate forms for different pharmaceutical development stages and market needs, maximizing the value derived from development resources
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 crystalline polymorphs provide improved processing characteristics, stability, and bioavailability, making them suitable for the treatment of Neurodegenerative and Neurodevelopmental Diseases.
Implementation Method 1
The present disclosure provides crystalline polymorphs of Blarcamesine salts including Blarcamesine HCl, Blarcamesine HBr, Blarcamesine Tosylate, Blarcamesine Maleate, Blarcamesine Camphorsufonate and Blarcamesine Besylate
Data Source
AI summary
The present disclosure encompasses novel solid state forms of Blarcamesine and salts thereof, processes for preparation thereof, and pharmaceutical compositions thereof.