Stabilizing R-Phenylephrine Hydrochloride via Temperature Control
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Solution Overview
Problem
Phenylephrine hydrochloride solutions used as decongestants and pupillary dilators often degrade, losing chiral purity and becoming brown, leading to waste due to instability at standard storage conditions, which affects their effectiveness and safety for use.
Innovation Solution
A composition comprising at least 95% R-phenylephrine hydrochloride with an aqueous buffer, stored between −10 to 10°C, maintains initial chiral purity for at least 6 months, using methods such as chiral column chromatography, optical rotation, capillary electrophoresis, or Nuclear Magnetic Resonance to determine purity, and includes preservatives like benzalkonium chloride.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If phenylephrine hydrochloride solution is stored at standard conditions (20-25°C), then ease of operation is improved, but stability of the composition deteriorates (chiral purity is lost and solution turns brown)
Solution Approach 1:
The patent applies parameter changes by modifying the storage temperature parameter from standard room temperature (20-25°C) to refrigerated temperature (2-8°C). This temperature parameter change fundamentally alters the stability characteristics of phenylephrine hydrochloride, preventing degradation and chiral purity loss while maintaining the solution's therapeutic effectiveness throughout its shelf life.
2Ease of operation
If phenylephrine hydrochloride solution is stored at standard conditions (20-25°C), then ease of operation is improved, but reliability deteriorates (drug effectiveness is compromised)
Solution Approach 1:
The patent implements parameter changes by establishing a refrigerated storage temperature range (2-8°C) that preserves the drug's effectiveness. This temperature parameter modification prevents chemical degradation and maintains the pharmacological activity of phenylephrine hydrochloride, ensuring reliable therapeutic outcomes while the solution remains stable for at least 6 months.
3Stability of the object's composition
If phenylephrine hydrochloride solution is stored at lower temperatures (2-8°C), then stability of the composition is improved (chiral purity is maintained), but use of energy increases (refrigeration required)
Solution Approach 1:
The patent applies parameter changes by optimizing the storage temperature to a specific refrigerated range (2-8°C) that balances stability requirements with energy consumption. This temperature parameter selection maintains chiral purity and prevents degradation while using standard refrigerator energy levels, avoiding the need for more energy-intensive freezing or ultra-low temperature storage.
4Stability of the object's composition
If phenylephrine hydrochloride solution is stored at lower temperatures (2-8°C), then stability of the composition is improved (chiral purity is maintained), but duration of action is extended (storage life increased)
Solution Approach 1:
The patent implements parameter changes by setting the storage temperature to (2-8°C), which simultaneously achieves two objectives: maintaining chiral purity by preventing racemization and extending the storage life to at least 6 months. This temperature parameter optimization ensures both compositional stability and prolonged shelf life without requiring additional preservatives or formulation modifications.
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 solution effectively stabilizes R-phenylephrine hydrochloride, maintaining its chiral purity and potency for extended periods, ensuring consistent efficacy in applications like pupillary dilation and ocular treatments without turning brown, thus reducing waste and ensuring drug effectiveness.
Implementation Method 1
a composition comprising at least 95% R-phenylephrine hydrochloride and an aqueous buffer
Implementation Method 2
the chiral purity is determined by chiral column chromatography
Implementation Method 3
the chiral purity is determined by chiral column chromatography, optical rotation
Implementation Method 4
the chiral purity is determined by chiral column chromatography, optical rotation, capillary electrophoresis
Implementation Method 5
the chiral purity is determined by chiral column chromatography, optical rotation, capillary electrophoresis, circular dichroism, or Nuclear Magnetic Resonance
Implementation Method 6
includes preservatives like benzalkonium chloride
Data Source
AI summary
The invention is directed to methods and compositions of stabilizing phenylephrine formations. The composition has good time-dependent stability at low temperature and has no change in its outward appearance even after having been stored at least 6 months.