Edonentan Crystalline Form 4 Ocular Treatment
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Solution Overview
Problem
Current treatments for glaucoma, diabetic retinopathy, retinal vein occlusion, and retinopathy of prematurity are inadequate in effectively reducing incidence and severity, with limited options for addressing high blood pressure and vascular issues contributing to these ocular diseases.
Innovation Solution
The use of Edonentan crystalline forms, specifically anhydrous crystalline Form 4, which has a unique X-ray powder diffraction pattern and high stability, is administered to ocular tissues to treat glaucoma, diabetic retinopathy, retinal vein occlusion, and retinopathy of prematurity, improving tissue perfusion and reducing intraocular pressure and neovascularization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for ocular diseases, then treatment options are available, but effectiveness in reducing incidence and severity is inadequate
Solution Approach 1:
The patent changes the physical-chemical parameters of the active compound by discovering and utilizing a new crystalline form (Form 4) with distinct X-ray diffraction patterns and stability characteristics. This parameter change in the compound's physical state improves its stability and bioavailability, thereby enhancing treatment effectiveness while maintaining therapeutic versatility
Solution Approach 2:
The patent creates a composite pharmaceutical composition that combines the active compound in its specific crystalline Form 4 with excipients and formulation components. This composite approach optimizes the drug's stability, solubility, and bioavailability properties, resolving the contradiction between reliable treatment effectiveness and versatile treatment options
2Stability of the object's composition
If Edonentan crystalline forms are used, then stability and bioavailability are enhanced, but manufacturing complexity increases
Solution Approach 1:
The patent applies preliminary action by pre-establishing the specific crystalline Form 4 through controlled crystallization processes during drug development. By determining the optimal crystallization conditions and parameters in advance, the manufacturing process becomes more predictable and controllable, reducing actual manufacturing complexity while ensuring compound stability
Solution Approach 2:
The patent utilizes parameter changes in the crystallization process (temperature, solvent composition, pH, addition rate) to control the formation of the desired crystalline Form 4. By optimizing these parameters, the manufacturing process achieves both high stability of the crystalline form and reasonable ease of production
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
Edonentan crystalline forms effectively reduce intraocular pressure, improve retinal and optic nerve head perfusion, and decrease neovascularization, providing therapeutic benefits for these ocular diseases by stabilizing the compound and enhancing its bioavailability.
Implementation Method 1
having an X-ray powder diffraction pattern comprising at least three characterization peaks, in terms of 2θ, selected from peaks at 5.6±0.2°, 11.4±0.2°, 17.7±0.2°, 19.3±0.2°, 21.1±0.2°, and 21.9±0.2°
Data Source
AI summary
The present disclosure relates to the discovery that certain ocular diseases may be treated using Edonentan crystalline forms. Specific Edonentan crystalline form can be used alone or in combination with an intra-ocular pressure (TOP) reducing agent, a neuroprotective agent, or an anti-VEGF agent. Using Edonentan crystalline forms, alone or in combination with an additional agent, provides increased perfusion to the retina or reduced TOP in certain ocular diseases and reduces damage to retinal cells.