Aqueous Ibuprofen Paracetamol Formulation pH Stability
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Solution Overview
Problem
Existing formulations of ibuprofen and paracetamol face challenges due to ibuprofen's poor water solubility and paracetamol's susceptibility to hydrolysis and oxidation, particularly in aqueous solutions intended for intravenous use.
Innovation Solution
A method for preparing a stable aqueous formulation of ibuprofen and paracetamol by dissolving them in an aqueous solvent with a pH of 6.0-8.0, specifically 6.3-7.3, which enhances solubility and stability, and includes the use of antioxidants like cysteine to prevent degradation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If ibuprofen is formulated in aqueous solution, then it can be administered by intravenous injection, but its poor water solubility causes precipitation and instability
Solution Approach 1:
The patent adjusts the pH parameter of the aqueous solution to a specific range (pH 7.0-7.4) to optimize ibuprofen solubility and stability. This parameter change allows the drug to remain dissolved and stable in intravenous formulation without precipitation
Solution Approach 2:
The patent introduces sodium hydroxide as an intermediary substance to adjust and maintain the pH of the solution. This mediator enables ibuprofen to remain soluble by controlling the ionization state, preventing precipitation while maintaining compatibility for intravenous administration
2Adaptability or versatility
If paracetamol is formulated in aqueous solution at pH 7, then it can be combined with ibuprofen, but paracetamol undergoes significant hydrolytic degradation
Solution Approach 1:
The patent carefully controls the pH parameter within a narrow range (pH 7.0-7.4) to balance the requirements of both drugs. This optimized pH setting minimizes paracetamol hydrolysis while maintaining ibuprofen solubility and enabling successful drug combination
Solution Approach 2:
The patent performs preliminary pH adjustment and buffering before combining the drugs, ensuring the solution is pre-conditioned to protect paracetamol from hydrolytic degradation. This preliminary action prevents degradation before it occurs during storage
3Stability of the object's composition
If antioxidants are added to prevent paracetamol oxidation, then stability improves, but toxicity concerns and formulation complexity increase
Solution Approach 1:
The patent converts the harmful effect of oxygen into a beneficial control parameter by deliberately removing oxygen from the formulation through nitrogen purging. This eliminates oxidation risk without needing to add potentially toxic antioxidants, transforming an environmental hazard into a controlled process step
Solution Approach 2:
The patent creates an inert atmosphere by purging the formulation with nitrogen gas to remove oxygen. This inert environment protects paracetamol from oxidation without requiring additional chemical antioxidants, simplifying the formulation while maintaining stability
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 method results in a stable combination of ibuprofen and paracetamol with improved compatibility, suitable for intravenous injection, maintaining stability and effectiveness over long-term storage.
Implementation Method 1
dissolving them in an aqueous solvent with a pH of 6.0-8.0, specifically 6.3-7.3, which enhances solubility and stability
Implementation Method 2
paracetamol's susceptibility to oxidation... includes the use of antioxidants like cysteine to prevent degradation
Implementation Method 3
paracetamol in aqueous solution is liable to undergo hydrolysis... The rate of degradation of paracetamol increases with increasing temperature and light. This rate is minimal at a pH in the region of 6
Data Source
AI summary
An aqueous ibuprofen and paracetamol composition has a pH 6.3-7.3. The composition can be used as a medicament, especially for the treatment of pain and/or inflammation. The composition can be formulated for intravenous injection.