ACP-2 Polymorph Crystallization for Drug Stability
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Solution Overview
Problem
There is a need for polymorphs of the A-decarbonized-5α androstane compound (ACP-2) that exhibit high crystallinity, good stability, low hygroscopicity, and are easy to prepare, in order to improve the physical and chemical properties of the drug and facilitate large-scale production.
Innovation Solution
The development of three new crystalline forms of ACP-2, specifically crystal forms I, II, and III, which are characterized by their high crystallinity, stability, low hygroscopicity, and ease of preparation, achieved through specific nucleation modes and crystallization conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polymorphs of ACP-2 are developed with high crystallinity and good stability, then the physical and chemical properties of the drug are improved, but the preparation complexity increases
Solution Approach 1:
The patent applies parameter changes by optimizing crystallization conditions including solvent selection (ethyl acetate, ethanol, isopropanol, n-butanol, or their mixtures with water), temperature control (0-25°C), and pH adjustment (pH 2-10) to obtain different polymorphic forms of ACP-2 with high stability and crystallinity while maintaining preparability
Solution Approach 2:
The patent employs preliminary action by performing pre-treatment steps including dissolving ACP-2 in specific solvents, adjusting pH to predetermined ranges, and controlling temperature before crystallization to ensure the formation of stable polymorphic forms with high crystallinity
2Object-affected harmful factors
If polymorphs with low hygroscopicity are developed, then the storage stability is improved, but the crystallization process complexity increases
Solution Approach 1:
The patent uses parameter changes by controlling crystallization temperature (0-25°C), pH (2-10), and solvent composition to produce polymorphic forms with low hygroscopicity while keeping the crystallization process simple and scalable
Solution Approach 2:
The patent employs intermediary substances (specific solvents like ethyl acetate, ethanol, isopropanol, n-butanol, or their mixtures with water) as mediators to facilitate the formation of low-hygroscopicity polymorphic forms through controlled crystallization processes
3Ease of manufacture
If simple preparation methods are used, then the ease of manufacture is improved, but the crystallinity and purity may be compromised
Solution Approach 1:
The patent applies parameter changes by using readily available solvents (ethyl acetate, ethanol, isopropanol, n-butanol, or their mixtures with water) and simple parameter adjustments (temperature 0-25°C, pH 2-10) to achieve both ease of manufacture and high crystallinity in the polymorphic forms of ACP-2
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 new crystal forms of ACP-2 enhance the physical and chemical properties of the drug, improving its druggability and suitability for large-scale production, while maintaining therapeutic efficacy for treating tumors and prostate hyperplasia.
Implementation Method 1
The present invention reports three new crystalline forms of ACP-2: crystal form I, crystal form II, and crystal form III by studying the nucleation mode and crystallization conditions of ACP-2
Implementation Method 2
the X-ray powder diffraction pattern of crystal form I comprises 3 or more 2θ values selected from the group consisting of: 7.1±0.2°, 11.7±0.2°, 13.4±0.2°, 16.0±0.2°, 17.1±0.2°, 20.9±0.2°, 21.1±0.2°, 23.4±0.2° and 28.6±0.2°
Data Source
AI summary
A polymorphic substance of a A-decarburization-5α androstane compound (ACP-2), an application thereof and a preparation method therefor are provided. Specifically, a polymorphic substance of a A-decarburization-5α androstane compound (ACP-2), a preparation method therefor and use thereof are provided.