Methotrexate Oral Solution Stability Through Buffered Salt Formulation
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing Methotrexate compositions for oral administration are unsuitable for patients with swallowing difficulties and are prone to precipitation over time, necessitating a stable and palatable solution form.
Innovation Solution
A Methotrexate composition comprising a pharmaceutically acceptable salt, such as Methotrexate disodium, dissolved in an aqueous carrier with a pH range of 6-7 and a buffer system to maintain stability, including agents like Citric Acid and Sodium Phosphate, along with preservatives and flavorings to enhance palatability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If Methotrexate is formulated as an oral tablet, then it provides a stable solid dosage form, but it becomes unsuitable for patients with swallowing difficulties
Solution Approach 1:
The patent changes the physical state parameter of Methotrexate from solid tablet to liquid oral solution, making it suitable for patients with swallowing difficulties while maintaining pharmacological efficacy
Solution Approach 2:
The patent introduces buffer agents (such as citrate buffer or phosphate buffer) as intermediaries to maintain pH within a specific range (6.0-7.5), preventing Methotrexate precipitation and ensuring stability of the oral solution formulation
2Ease of operation
If Methotrexate is formulated as an oral solution, then it improves ease of administration for difficult-to-swallow patients, but it becomes prone to precipitation over time
Solution Approach 1:
The patent optimizes pH parameter to range 6.0-7.5 and controls ionic strength through buffer selection, preventing Methotrexate from precipitating while maintaining solubility and stability of the oral solution
Solution Approach 2:
Buffer agents serve as intermediaries that maintain pH stability and prevent Methotrexate precipitation, ensuring long-term physical stability of the oral solution formulation
3Stability of the object's composition
If the pH of the Methotrexate solution is lowered to prevent precipitation, then physical stability improves, but degradation increases limiting shelf life
Solution Approach 1:
The patent identifies and optimizes multiple parameters simultaneously: pH (6.0-7.5), buffer type (citrate or phosphate), and buffer concentration, achieving both physical stability and extended shelf life through coordinated parameter control
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 composition remains stable and dissolved for a prolonged period, providing a safe and easy-to-administer oral solution with increased shelf life and improved patient compliance.
Implementation Method 1
including agents like Citric Acid and Sodium Phosphate
Implementation Method 2
containing a pharmaceutically acceptable salt of Methotrexate and an aqueous carrier agent in which the Methotrexate salt is substantially or completely soluble to form an aqueous solution
Data Source
AI summary
A Methotrexate composition for oral administration is provided comprising a pharmaceutically acceptable salt of Methotrexate and an aqueous carrier agent. The Methotrexate salt is substantially or completely soluble in the aqueous carrier agent, forming an aqueous solution. There is also provided a method of manufacturing a Methotrexate composition for oral administration, comprising mixing a pharmaceutically acceptable salt of Methotrexate with an aqueous carrier agent until the Methotrexate salt is substantially or completely soluble in the carrier agent to form an aqueous solution.