Hydroxytyrosol Nicotinamide Co-Crystal Stability
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Solution Overview
Problem
Hydroxytyrosol, a polyphenolic compound with strong antioxidant properties, is unstable, easily oxidized, and has a low melting point, making it unsuitable for direct use in capsules or tablets, and its embedding powders suffer from increased hygroscopicity and instability due to starch-based materials.
Innovation Solution
Formation of a co-crystal with nicotinamide through non-covalent molecular interactions, increasing the melting point and stability of hydroxytyrosol, and reducing hygroscopicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hydroxytyrosol is used directly in capsules or tablets, then the antioxidant capacity is available, but the low melting point and high hygroscopicity make it unsuitable for solid formulations
Solution Approach 1:
The patent changes the physical and chemical parameters of hydroxytyrosol by forming a co-crystal with nicotinamide. This co-crystal formation increases the melting point from 52°C to above 100°C and reduces hygroscopicity, transforming the material properties to enable solid formulation while maintaining stability.
Solution Approach 2:
The patent creates a composite material system by forming a co-crystal between hydroxytyrosol and nicotinamide. This composite structure combines the antioxidant properties of hydroxytyrosol with the stabilizing properties of nicotinamide, resulting in a material that is both stable and suitable for solid formulations.
2Reliability
If embedding powder with starch-based auxiliary materials is used to protect hydroxytyrosol, then the powder properties are improved, but the hygroscopicity is further increased
Solution Approach 1:
The patent uses nicotinamide as an intermediary substance to form a co-crystal with hydroxytyrosol. This intermediary structure protects hydroxytyrosol from direct interaction with moisture while avoiding the hygroscopic properties of starch-based materials, thereby reducing overall hygroscopicity.
3Reliability
If embedding powder is used to protect hydroxytyrosol, then the powder properties are improved, but the embedding efficiency is not high due to amphiphilic nature
Solution Approach 1:
The patent changes the molecular-level parameters by forming a co-crystal structure where hydroxytyrosol and nicotinamide are integrated at the molecular level. This co-crystal formation achieves complete incorporation of hydroxytyrosol (100% embedding efficiency) unlike conventional embedding methods that only achieve 20-30% efficiency.
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 hydroxytyrosol-nicotinamide co-crystal exhibits a significantly higher melting point, improved chemical stability, and reduced hygroscopicity, enabling its use in solid formulations like capsules or tablets.
Implementation Method 1
adding an auxiliary compound which has non-covalent bond interaction with hydroxytyrosol at the molecular level
Implementation Method 2
the melting point of hydroxytyrosol is capable of being increased at molecular level
Data Source
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AI summary
The present invention relates to the technical field of medicines, and in particular to a hydroxytyrosol nicotinamide eutectic crystal, a preparation method therefor and a composition thereof. In the hydroxytyrosol nicotinamide eutectic crystal of the present invention, a molar ratio of hydroxytyrosol to nicotinamide is 1: 1, and cell parameters are as follows: a=9.4999, b=11.8285, c=11.4439, α=90°, β=96.628°, and δ=90°. The hydroxytyrosol nicotinamide eutectic crystal of the present invention is high in melting point, does not absorb moisture and is good in stability, and the application convenience of the hydroxytyrosol is greatly improved. The composition directly prepared by means of a grinding method has the advantages of high yield and low cost, and is suitable for large-scale application.