Avasopasem Manganese Crystalline Polymorphs for Stability and Bioavailability
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Solution Overview
Problem
There is a need for additional solid state forms of Avasopasem manganese to improve its processing properties, stability, and bioavailability for the treatment of radiation-induced severe oral mucositis, as existing forms may not adequately address these aspects.
Innovation Solution
The development of crystalline polymorphs of Avasopasem manganese, including specific forms such as AM1, AM2, AM3, AM4, AM5, and AM6, which are characterized by distinct X-ray powder diffraction patterns and can be used to prepare pharmaceutical compositions, along with processes for their isolation and formulation with pharmaceutically acceptable excipients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing solid state forms of Avasopasem manganese are used, then the basic therapeutic function is achieved, but processing properties and stability are insufficient
Solution Approach 1:
The patent applies parameter changes by discovering and utilizing different crystalline polymorphs (Form I, Form II, Form III) of Avasopasem manganese, each with distinct crystal structures and physical properties. These polymorphic forms exhibit improved stability and processing characteristics compared to the original form, directly resolving the contradiction between reliability and ease of manufacture.
Solution Approach 2:
The patent employs composite material strategies by formulating Avasopasem manganese polymorphs with various excipients and combining them into optimized pharmaceutical compositions. This approach enhances both the stability and processability of the active ingredient while maintaining its therapeutic efficacy.
2Reliability
If existing solid state forms of Avasopasem manganese are used, then the basic therapeutic function is achieved, but bioavailability is insufficient
Solution Approach 1:
The patent utilizes parameter changes by identifying crystalline polymorphs with improved dissolution profiles and bioavailability characteristics. Form I, Form II, and Form III each demonstrate enhanced pharmacokinetic properties compared to the original form, directly addressing the bioavailability limitation while providing multiple formulation options.
3Adaptability or versatility
If a single solid state form of Avasopasem manganese is used, then the formulation is simple, but the ability to optimize properties is limited
Solution Approach 1:
The patent applies segmentation by dividing Avasopasem manganese into distinct crystalline polymorphs (Form I, Form II, Form III), each with specific optimized properties. This segmentation allows formulation scientists to select the most appropriate polymorph for each specific application, enhancing adaptability while maintaining manageable complexity through clear characterization of each form.
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
These crystalline polymorphs offer improved chemical and physical stability, enhanced bioavailability, and effective treatment of radiation-induced severe oral mucositis, particularly in cases associated with head or neck cancer, by providing a range of solid state forms with varied properties.
Implementation Method 1
X-ray diffraction (XRD) pattern
Implementation Method 2
X-ray powder diffraction patterns
Implementation Method 3
thermogravimetric analysis (TGA)
Implementation Method 4
differential scanning calorimetry (DSC)
Implementation Method 5
infrared absorption fingerprint
Data Source
AI summary
The present disclosure encompasses solid state forms of Avasopasem manganese, in embodiments crystalline polymorphs of Avasopasem manganese, processes for preparation thereof, and pharmaceutical compositions thereof.