Melatonin Aqueous Solution Stability and Taste Optimization
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Solution Overview
Problem
Current melatonin pharmaceutical formulations lack stability and pleasant taste, which affects patient compliance and increases the risk of microbial contamination.
Innovation Solution
Oral pharmaceutical aqueous solutions comprising melatonin, benzyl alcohol, an anti-oxidant, a sweetening agent, and optionally a flavor, which provide chemical and microbiological stability while maintaining a pleasant taste, using a composition that includes melatonin, benzyl alcohol, sodium ascorbate, sucralose, and strawberry flavor.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If melatonin is formulated in aqueous solution without adequate stabilizers and preservatives, then the formulation is simple and easy to manufacture, but the formulation lacks stability and is susceptible to microbial contamination
Solution Approach 1:
The patent combines multiple components (melatonin, benzyl alcohol, propylene glycol, antioxidants, sweetening agents, and flavors) into a composite aqueous formulation. This composite approach provides both stability and microbiological protection while maintaining ease of manufacture through a single-step aqueous dissolution process.
Solution Approach 2:
Benzyl alcohol serves as an intermediary substance that provides dual functionality: it acts as a preservative to prevent microbial contamination and as a solubility enhancer for melatonin. This intermediary component resolves the contradiction by adding minimal complexity while significantly improving reliability.
2Reliability
If benzyl alcohol is used at high concentrations to ensure antimicrobial efficacy, then microbiological stability is improved, but the taste becomes unpleasant and patient compliance decreases
Solution Approach 1:
The patent optimizes the concentration parameter of benzyl alcohol to a specific range (1-10 mg/ml) that provides sufficient antimicrobial efficacy while maintaining acceptable taste. This parameter optimization resolves the contradiction by finding the optimal balance point between reliability and ease of operation.
Solution Approach 2:
The formulation combines benzyl alcohol with sweetening agents and flavors to create a composite taste profile. This composite approach masks the unpleasant taste of benzyl alcohol while preserving its antimicrobial efficacy, thereby improving patient compliance without sacrificing reliability.
3Device complexity
If melatonin is formulated without antioxidants, then the formulation is simpler, but melatonin degradation occurs and chemical stability is compromised
Solution Approach 1:
Antioxidants serve as intermediary substances that protect melatonin from oxidation and degradation. These intermediaries prevent chemical reactions that would compromise melatonin stability, resolving the contradiction by adding minimal complexity while significantly improving compositional stability.
4Ease of operation
If the formulation uses multiple excipients to improve taste and stability, then patient compliance and stability are improved, but the risk of microbial contamination increases due to higher water content
Solution Approach 1:
Benzyl alcohol acts as an intermediary preservative that counteracts the increased microbial contamination risk associated with high water content formulations. This intermediary component enables the use of multiple excipients for improved taste and stability while simultaneously protecting against microbial contamination.
Solution Approach 2:
The formulation creates a composite system where multiple excipients (sweetening agents, flavors, antioxidants) work together with benzyl alcohol to provide both improved patient compliance and microbiological protection. This composite approach resolves the contradiction by integrating multiple functions into a single stable formulation.
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 achieves over 95% retention of melatonin and benzyl alcohol stability, prevents microbial contamination, and ensures a pleasant taste, enhancing patient compliance and safety by maintaining high antimicrobial efficacy and stability for up to 3 months at +40 °C.
Implementation Method 1
from 1 to 10 mg/ml of benzyl alcohol, propylene glycol... prevents microbial contamination... maintaining high antimicrobial efficacy
Implementation Method 2
an anti-oxidant... achieves over 95% retention of melatonin and benzyl alcohol stability
Implementation Method 3
The activity of melatonin at the MT1, MT2 and MT3 receptors is believed to contribute to its sleep-promoting properties
Implementation Method 4
others are due to its role as a pervasive and powerful antioxidant, with a particular role in the protection of nuclear and mitochondrial DNA
Data Source
AI summary
Oral pharmaceutical aqueous solutions comprising melatonin, from 1 to 10.0 mg/ml of benzyl alcohol, propylene glycol, an anti-oxidant and a sweetening agent. Said compositions for use as a medicament and for use in the prevention and/or treatment of insomnia, sleep disorders, jet lag disorders.