High Purity Cangrelor Formulation via pH Control and Lyophilization
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Solution Overview
Problem
Current pharmaceutical formulations of cangrelor often contain significant levels of impurities due to degradation during the compounding process, which can affect product stability and dosage control, and the pharmacological impact of these impurities has not been fully evaluated in clinical settings, necessitating a method to consistently produce high-purity cangrelor.
Innovation Solution
A method involving dissolving cangrelor in a solvent, adjusting the pH to between 7.0 and 9.5, and removing the solvent through lyophilization to produce high-purity cangrelor with controlled moisture levels, while incorporating pharmaceutically acceptable excipients like mannitol or sorbitol to minimize impurity levels and enhance stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If cangrelor undergoes compounding process (mixing with excipients, filtration, lyophilization), then the drug becomes usable and stable for medical applications, but significant levels of impurities are generated during the process
Solution Approach 1:
The patent applies preliminary action by adjusting the pH to between 7.0 and 9.5 before the compounding process begins. This pre-adjustment prevents degradation and impurity formation during subsequent processing steps, achieving both high purity and product stability without requiring additional purification steps afterward.
Solution Approach 2:
The patent changes the pH parameter to a specific range (7.0-9.5) and maintains it throughout the compounding process. This parameter control prevents hydrolysis of the phosphonate group and formation of degradation products, resolving the contradiction between maintaining stability during processing and preventing impurity generation.
2Productivity
If conventional compounding processes are used, then the formulation can be produced efficiently, but impurity levels remain problematic and affect dosage control
Solution Approach 1:
The patent modifies the pH parameter to a specific range (7.0-9.5) and maintains it throughout the compounding process. This parameter control prevents hydrolysis of the phosphonate group and formation of degradation products, resolving the contradiction between maintaining stability during processing and preventing impurity generation.
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
This approach consistently achieves high-purity cangrelor with impurity levels below 1.5% by weight, ensuring stability and effective dosage control, and maintaining the pH within a range that minimizes degradation, thus enhancing the pharmaceutical formulation's reliability and safety.
Implementation Method 1
mixing a pH-adjusting agent with the first solution to form a second solution, wherein the pH of the second solution is between about 7.0 and 9.5
Implementation Method 2
removing the solvent from the second solution to produce high purity cangrelor or a salt thereof under conditions wherein a level of moisture of less than about 2.0% by weight is achieved
Data Source
AI summary
The present invention relates to high purity cangrelor, pharmaceutical formulations comprising high purity cangrelor as an active ingredient, methods for preparing such compounds and formulations, and methods for using the pharmaceutical formulations in the inhibition of platelet activation and aggregation.