Fluorinated Stilbene PET Tracer Formulation for Sterile Filtration
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current PET pharmaceutical formulations, particularly those involving lipophilic Amyloid beta ligand stilbene, face challenges with chemical stability and significant losses during sterile filtration, necessitating a formulation that maintains activity and allows for precise adjustment of doses while minimizing adsorption onto filters.
Innovation Solution
A pharmaceutical formulation comprising lipophilic Amyloid beta ligand stilbene, ethanol, polyether, ascorbic acid, and sodium ascorbate, which is chemically stable and suitable for parenteral administration, allowing for sterile filtration without significant loss of activity and reducing adsorption onto filters.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If lipophilic Amyloid beta ligand stilbene is used for PET imaging, then the pharmaceutical shows low water solubility and requires special formulation, but significant loss occurs during sterile filtration
Solution Approach 1:
The patent introduces ethanol and polyether as intermediary substances that mediate between the lipophilic stilbene compound and the aqueous environment. These intermediaries form a compatible formulation system that prevents direct interaction between the hydrophobic compound and hydrophilic filter materials, thereby reducing adsorption losses during sterile filtration while maintaining chemical stability
Solution Approach 2:
The patent changes the physical-chemical parameters of the formulation by adjusting ethanol concentration (8-25% v/v), polyether concentration (10-25% w/v), and pH (4.5-8.5). These parameter changes optimize the formulation to reduce adsorption onto sterile filters while maintaining chemical stability and solubility of the lipophilic stilbene compound
2Duration of action of stationary object
If the pharmaceutical formulation is made stable for storage, then it can be stored for at least 8 hours, but adsorption onto sterile filter increases
Solution Approach 1:
The patent creates a composite formulation system combining lipophilic stilbene, ethanol, polyether, ascorbic acid, and sodium ascorbate. This composite material system provides both long-term stability for storage and compatibility with sterile filtration, as the polyether component specifically addresses filter interaction while other components maintain chemical stability
3Ease of operation
If the PET tracer is diluted for dose adjustment, then precise dosing is needed for each patient, but the formulation must remain stable during storage
Solution Approach 1:
The patent creates a dynamic formulation system that can accommodate varying dilution ratios (within the specified concentration ranges) while maintaining stability. The formulation's ethanol and polyether components provide a flexible matrix that remains stable across different concentrations, enabling precise dose adjustment without compromising formulation integrity
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 formulation ensures chemical stability for at least 8 hours, allows precise dose adjustment, and significantly reduces adsorption during sterile filtration, enhancing the yield of radiolabeling and maintaining the pharmaceutical's effectiveness for PET imaging.
Implementation Method 1
the lipophilic Amyloid beta ligand stilbene is solubilized and stabilized by the formulation of present invention
Implementation Method 2
Ascorbic acid, and Sodium ascorbate
Data Source
AI summary
The invention is directed to formulations of lipophilic Amyloid beta ligand stilbene and more particularly to formulations which are capable to be administered parenterally e.g. intravenously, wherein the lipophilic Amyloid beta ligand stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for PET imaging of mammals pursuant to the invention.