Pterostilbene Cocrystals for Improved Water Solubility
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Solution Overview
Problem
Pterostilbene's low water solubility poses a challenge for its bioavailability, necessitating the development of more soluble solid forms to enhance pharmaceutical properties.
Innovation Solution
Formation of cocrystals with coformers capable of forming hydrogen bond interactions, such as picolinic acid, 1,4-dimethylpiperazine, and others, to improve water solubility and dissolution rate.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If pterostilbene is used in its conventional crystalline solid form, then it maintains structural stability, but its water solubility remains low which limits bioavailability
Solution Approach 1:
The patent applies cocrystal formation by combining pterostilbene with coformers (such as aromatic carboxylic acids, heterocyclic compounds, or amino acids) to create a composite solid material. This cocrystal structure maintains the stability of pterostilbene while incorporating coformers that enhance water solubility and dissolution rate, thereby improving bioavailability without sacrificing structural integrity
Solution Approach 2:
The patent changes the physical and chemical parameters of pterostilbene by forming cocrystals with different coformers, resulting in solid forms with modified solubility characteristics. By selecting appropriate coformers with specific functional groups capable of hydrogen bonding, the dissolution rate and water solubility parameters are improved while maintaining the active ingredient's stability
2Quantity of substance
If cocrystal formation is attempted to improve solubility, then water solubility and dissolution rate increase, but the process requires significant time, effort and resources to find appropriate coformers and conditions
Solution Approach 1:
The patent systematically varies parameters such as coformer selection (different functional groups), solvent types, temperature, and mixing ratios to identify optimal cocrystal formation conditions. This structured parameter exploration accelerates the discovery process by focusing on promising coformer classes rather than exhaustive screening
Solution Approach 2:
The patent uses screening methodologies and solubility assessment tools as intermediaries to evaluate potential cocrystal systems efficiently. These intermediaries provide rapid feedback on solubility improvements, allowing researchers to identify successful cocrystal formulations without extensive optimization work
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 cocrystals exhibit enhanced water solubility and bioavailability, making them suitable for pharmaceutical and dietary compositions.
Implementation Method 1
a cocrystal of pterostilbene and a coformer capable to form hydrogen bond interactions
Data Source
AI summary
The present disclosure relates to a cocrystal of pterostilbene and a coformer capable to form hydrogen bond interactions, to a process for the preparation thereof, and to its use as a medicament or a dietary supplement. The present disclosure also relates to a composition comprising the cocrystal.