Acrylic Acid Derivative Crystal Forms for Stable Solid Dosage
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Solution Overview
Problem
The existing compound of formula I, an acrylic derivative used as an estrogen receptor down-regulator, is in an amorphous form with unsatisfactory stability and granularity, making it unsuitable for solid preparation processes such as tablets or capsules.
Innovation Solution
Development of crystal forms A, B, C, D, E, F, G, and H of the compound of formula I, each with specific X-ray powder diffraction patterns and thermal characteristics, along with preparation methods using solvents and conditions to achieve stable monohydrate or solvate forms.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If the compound is in amorphous form, then it can be prepared easily, but its stability and granularity are unsatisfactory
Solution Approach 1:
The patent changes the physical state parameter of the compound from amorphous to crystal form by controlling crystallization conditions. This transformation improves stability and granularity while maintaining preparability through controlled solvent selection and temperature management during the crystallization process.
Solution Approach 2:
The patent utilizes phase transition from amorphous solid to crystal solid through controlled crystallization. By managing the phase change process using appropriate solvents and temperature conditions, the compound achieves improved stability and granularity while remaining manufacturable.
2Ease of manufacture
If the compound is in amorphous form, then preparation is simple, but it is unsuitable for solid preparation processes
Solution Approach 1:
The patent changes the physical parameters (crystallinity, granularity) of the compound to make it suitable for solid preparation processes. The crystal form with improved granularity and morphology enables the compound to be effectively used in tablets and capsules while maintaining ease of preparation through controlled crystallization.
Solution Approach 2:
The patent employs phase transition to transform the compound from amorphous to crystal form, enhancing its adaptability for solid preparation processes. The crystallization process creates particles with improved morphology and granularity that are suitable for pharmaceutical formulation while keeping the preparation process simple.
3Stability of the object's composition
If multiple crystal forms are developed, then stability and formability are improved, but the complexity of preparation methods increases
Solution Approach 1:
The patent explores multiple crystal forms by varying physical parameters such as solvent type, temperature, and pH. Each crystal form is achieved through systematic parameter adjustment, providing improved stability and formability options while maintaining relatively simple preparation methods through controlled crystallization processes.
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 crystal forms provide improved stability and suitability for pharmaceutical formulations, enabling effective treatment of estrogen receptor-mediated diseases like breast and ovarian cancers by enhancing the compound's formability and therapeutic efficacy.
Implementation Method 1
Development of crystal forms A, B, C, D, E, F, G, and H of the compound of formula I, each with specific X-ray powder diffraction patterns and thermal characteristics, along with preparation methods using solvents and conditions to achieve stable monohydrate or solvate forms.
Implementation Method 2
preparation methods using solvents and conditions to achieve stable monohydrate or solvate forms
Data Source
AI summary
Crystal forms A, B, C, D, E, F, G and H of a compound represented by formula I and a preparation method therefor, as well as medical uses for the various crystal forms and advantages thereof in various aspects.