Ziprasidone Sulfate Polymorphs for Solubility
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Solution Overview
Problem
Current methods for preparing Ziprasidone salts, such as hydrochloride and hydrogensulfate, face challenges in achieving optimal solubility and bioavailability, leading to suboptimal pharmaceutical formulations.
Innovation Solution
Development of novel polymorphic forms of Ziprasidone sulfates with controlled crystal water content and particle size, specifically Ziprasidone sulfate and hydrogensulfate, which exhibit improved solubility and stability, enabling better bioavailability and tolerance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Manufacturing precision
If conventional concentration and recrystallization techniques are employed to prepare Ziprasidone salts, then the salts can be obtained in high purity, but the solubility and bioavailability remain suboptimal
Solution Approach 1:
The patent changes the crystal structure parameters by controlling the formation of specific polymorphic forms (monohydrate and anhydrous forms) through controlled crystallization conditions, thereby improving solubility while maintaining high purity
Solution Approach 2:
The patent utilizes phase transitions during crystallization to obtain specific polymorphic forms with optimized solubility properties, transitioning from solution to solid state in a controlled manner to achieve desired crystal structure
2Ease of manufacture
If conventional methods are used to prepare Ziprasidone salts, then the preparation process is simple, but the particle size is large resulting in reduced bioavailability
Solution Approach 1:
The patent segments the crystallization process into controlled stages, producing fine particles through controlled nucleation and growth, thereby increasing surface area and bioavailability while maintaining process simplicity
Solution Approach 2:
The patent transitions from conventional bulk crystallization to controlled fine particle formation, effectively changing the particle size dimension to optimize bioavailability without complicating the overall manufacturing process
3Stability of the object's composition
If existing Ziprasidone salts are used, then the formulations are stable, but the solubility is insufficient leading to suboptimal therapeutic effectiveness
Solution Approach 1:
The patent modifies the crystal structure parameters by forming specific polymorphic forms with optimized water content, achieving both stability and enhanced solubility simultaneously
Solution Approach 2:
The patent creates composite crystal structures (monohydrate and anhydrous forms) that combine stability and solubility properties, achieving superior performance compared to conventional salts
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 novel polymorphic forms of Ziprasidone sulfates demonstrate enhanced solubility and bioavailability, allowing for reduced drug dosages while maintaining or improving therapeutic effectiveness, thus addressing the limitations of existing formulations.
Implementation Method 1
The present invention relates to novel polymorphic forms of Ziprasidone sulfates... The present Ziprasidone sulfates may be obtained in high purity, have good stability and advantageous formulation properties
Implementation Method 2
Ziprasidone sulfates, i.e. Ziprasidone sulfate and Ziprasidone hydrogensulfate, having specific amounts of crystal water... The solubility of the compounds is on the one hand directly influenced by the content of crystal water
Implementation Method 3
The present Ziprasidone sulfates... are characterized by small average particle sizes... The solubility of the compounds is on the other hand by the low particle size
Data Source
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AI summary
The present invention relates to novel polymorphic forms of Ziprasidone sulfates Ziprasidone Hn+ X Z H2O wherein Ziprasidone is a compound of the formula; H is hydrogen; n is 1 or 2; 2- X is HSO4 - or SO4 2 -; and Z is O to 30., as well as to a process for their preparation and pharmaceutical formulations containing it. The present polymorphic forms of Ziprasidone sulfates are characterized by small average particle sizes and high solubility bestowing the compounds an improved bioavailability.