Utidelone Semihydrate Crystal Form for Stable Cancer Drug Storage
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Solution Overview
Problem
Existing Utidelone crystal forms lack stability and bioavailability, affecting the efficacy of pharmaceutical compositions for treating various cancers.
Innovation Solution
Development of a stable Utidelone semihydrate crystal form, prepared by crystallization in specific solvents, exhibiting high stability and bioavailability, characterized by X-ray diffraction and DSC analysis.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If Utidelone is stored under high humidity and temperature conditions, then the drug can be stored in various environments, but the stability and efficacy of the drug deteriorate
Solution Approach 1:
The patent applies parameter changes by modifying the crystalline structure parameters of Utidelone to create a stable polymorphic form. The stable crystal form has specific lattice parameters and molecular packing arrangements that resist degradation under high humidity and temperature conditions, thereby maintaining drug stability while enabling flexible storage environments
Solution Approach 2:
The patent creates a composite crystalline structure where Utidelone molecules are arranged in a specific polymorphic configuration with particular intermolecular interactions. This composite arrangement at the molecular level provides enhanced stability against environmental factors while maintaining the drug's therapeutic properties
2Ease of manufacture
If conventional crystal forms are used, then the manufacturing process is simple, but the stability under high humidity and temperature deteriorates
Solution Approach 1:
The patent modifies crystallization parameters including solvent composition, temperature profiles, and pH conditions to obtain the stable polymorphic form of Utidelone. These parameter changes enable the formation of the stable crystal structure through relatively simple crystallization processes that can be implemented in conventional manufacturing settings
3Productivity
If unstable crystal forms are used, then the drug can be produced quickly, but the bioavailability and efficacy deteriorate
Solution Approach 1:
The patent applies preliminary action by pre-establishing the stable polymorphic form through optimized crystallization conditions before drug production and storage. This preliminary establishment of the stable crystal structure ensures that subsequent production and storage processes maintain bioavailability without requiring additional stabilization steps, thus preserving both productivity and efficacy
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 Utidelone semihydrate crystal maintains stability under high humidity and temperature conditions, ensuring long-term storage and effective pharmaceutical compositions for treating cancers.
Implementation Method 1
A stable Utidelone semihydrate crystal form is developed through crystallization in a solvent mixture of n-heptane and tetrahydrofuran or dichloromethane
Implementation Method 2
Utidelone semihydrate crystal (crystal form A)... in which 4 Utidelone molecules and 2 water molecules are contained
Data Source
AI summary
A polycrystal form of Utidelone, particularly relating to a semi-hydrated crystal form (A) of Utidelone, a preparation method therefor and a use of crystal Utidelone in preparation of a pharmaceutical composition, especially the use in preparation of a pharmaceutical composition for inhibiting tumor growth and treating solid tumors of mammals, especially human. The provided crystal form is stable and resistant to high temperature and high humidity, and the preparation method is diversified and simple, and is suitable for industrialized production of new medicines.