DHODH Inhibitor Polymorph X-Ray Diffraction
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Solution Overview
Problem
Existing DHODH inhibitors face challenges in achieving stable crystalline forms with optimal pharmacological function for treating viral diseases and autoimmune disorders.
Innovation Solution
A stable crystalline polymorph of the DHODH inhibitor 2-(3,5-difluoro-3′-methoxybiphenyl-4-ylamino)nicotinic acid, characterized by a specific X-ray powder diffraction pattern, is developed, offering excellent stability and pharmacological efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a DHODH inhibitor is developed for treating viral and autoimmune diseases, then pharmacological efficacy is improved, but achieving stable crystalline forms with optimal properties becomes difficult
Solution Approach 1:
The patent applies parameter changes by modifying the crystalline structure parameters of the DHODH inhibitor through identification of specific polymorph forms. The dominant stable pharmaceutical polymorph (DSP) is characterized by specific X-ray diffraction patterns with peaks at defined 2-theta angles, representing optimized crystal lattice parameters that simultaneously achieve stability and pharmacological efficacy.
Solution Approach 2:
The patent employs composite material principles by creating a specific polymorphic form that combines molecular arrangement stability with pharmacological activity. The DSP polymorph represents a composite state where the crystalline lattice structure is optimized to maintain both physical stability and biological function.
2Ease of manufacture
If different polymorphs are identified, then physical properties such as solubility and dissolution rates improve, but selecting the dominant stable pharmaceutical polymorph becomes complex
Solution Approach 1:
The patent applies the extraction principle by isolating and identifying the specific dominant stable pharmaceutical polymorph from among multiple possible polymorphic forms. The DSP is extracted as the preferred form based on its superior stability characteristics, simplifying the selection process despite the existence of multiple polymorphs.
Solution Approach 2:
The patent uses parameter changes to differentiate and select the DSP among polymorphs by establishing specific X-ray diffraction parameters (peak positions at 2-theta angles) as identification criteria. This parameter-based characterization simplifies polymorph selection and quality control.
3Stability of the object's composition
If the crystal lattice organization is modified, then physical properties like density and melting point change, but maintaining pharmacological function becomes challenging
Solution Approach 1:
The patent applies parameter changes by systematically evaluating different crystal lattice parameters (molecular arrangement, density, melting point) to identify the polymorph form that optimally balances physical stability with pharmacological function. The DSP represents the optimized parameter set.
Solution Approach 2:
The patent employs composite material principles by creating a polymorphic form that integrates stable crystal lattice organization with preserved pharmacological activity. The DSP polymorph represents a composite state where structural stability and biological function coexist.
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 polymorph exhibits high stability and effective pharmacological function, making it suitable for treating viral diseases and autoimmune disorders with minimal off-target effects.
Implementation Method 1
characterized by an X-ray powder diffraction pattern comprising the following peaks in terms of degrees of 2-theta at approximately: 9.129±0.1, 17.375±0.1, 20.708±0.1, 25.274±0.1, 26.488±0.1 and 29.041±0.1
Data Source
AI summary
The present disclosure relates to physical forms of a DHODH inhibitor, such as a stable crystalline form of and compositions comprising the same. Also provided is the use of the physical form (such as a polymorph) or composition thereof in treatment, such as the treatment of a viral disease or an autoimmune disease or disorder.