Treprostinil Monohydrate Stability and Static Charge Reduction
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
The anhydrous form of treprostinil is unstable at room temperature, leading to dimer formation and requiring refrigeration for storage and transport, making it difficult to handle and increasing safety risks due to static electrical charges.
Innovation Solution
The development of a stable treprostinil monohydrate form, which is prepared through recrystallization and air-drying at controlled temperatures, eliminating the need for refrigeration and reducing static charges, thereby enhancing stability and safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If the anhydrous form of treprostinil is stored at room temperature, then handling and shipping are simplified, but the compound becomes unstable and forms dimers
Solution Approach 1:
The patent applies parameter changes by modifying the molecular structure of treprostinil to create the monohydrate form (treprostinil monohydrate). This structural parameter change introduces a water molecule into the crystal lattice, which fundamentally alters the stability characteristics of the compound, allowing it to remain stable at room temperature without forming dimers.
Solution Approach 2:
The invention creates a composite material by forming a hydrate complex where treprostinil molecules are associated with water molecules in a specific crystalline structure. This composite approach combines the active pharmaceutical ingredient with water in a stoichiometric ratio, resulting in a new material form that exhibits improved stability while maintaining therapeutic activity.
2Stability of the object's composition
If the anhydrous form of treprostinil is refrigerated for storage, then chemical stability is maintained, but storage and shipping complexity increases
Solution Approach 1:
The patent applies parameter changes by modifying the molecular structure of treprostinil to create the monohydrate form (treprostinil monohydrate). This structural parameter change introduces a water molecule into the crystal lattice, which fundamentally alters the stability characteristics of the compound, allowing it to remain stable at room temperature without forming dimers.
3Object-affected harmful factors
If the anhydrous form of treprostinil is handled, then static electrical charges accumulate creating safety risks, but the monohydrate form reduces these charges improving safety
Solution Approach 1:
The patent applies parameter changes by modifying the molecular structure of treprostinil to create the monohydrate form (treprostinil monohydrate). This structural parameter change introduces a water molecule into the crystal lattice, which fundamentally alters the stability characteristics of the compound, allowing it to remain stable at room temperature without forming dimers.
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 monohydrate form of treprostinil is significantly more stable at room temperature, easier to handle, and safer to work with, allowing for improved storage, shipment, and formulation without the need for cold conditions, while maintaining high purity and therapeutic effectiveness.
Implementation Method 1
The monohydrate is stable at room temperature over a longer period of time than other forms of treprostinil
Implementation Method 2
air-drying at controlled temperatures
Data Source
Figure 1a
Figure 1b
AI summary
There is provided a stable monohydrate form of treprostinil and pharmaceutical formulation comprising the same, method of making and using the same.