Amorphous Polyphenol Solid Composition for Rapid Dissolution
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Solution Overview
Problem
Polyphenols, due to their poor water solubility, are absorbed and dissolved into body fluids at slow rates, limiting their efficient ingestion and physiological effects, despite their potential health benefits.
Innovation Solution
A solid composition comprising an amorphous poorly water-soluble polyphenol, a hydrophilic polymer such as a homopolymer or copolymer of N-vinyllactam, and a nonionic surfactant like polyglycerol fatty acid esters, which enhances the polyphenol's solubility and absorption in intestinal fluid.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If polyphenols are administered in conventional solid compositions, then the dosage form is convenient and efficient for ingestion, but the polyphenols are dissolved and absorbed into body fluid at slow rates due to poor water solubility
Solution Approach 1:
The patent changes the physical state of polyphenol from crystalline to amorphous form, which fundamentally alters its dissolution properties. The amorphous polyphenol exhibits significantly enhanced solubility and dissolution rate compared to the crystalline form, while maintaining the convenient solid composition format for oral administration
Solution Approach 2:
The patent creates a composite solid composition comprising amorphous polyphenol in combination with specific carriers or excipients. This composite structure maintains the solid dosage form convenience while the amorphous state of polyphenol within the composite enables rapid dissolution and absorption in body fluids
2Quantity of substance
If large amounts of polyphenol are ingested to achieve physiological effects, then the therapeutic effect is enhanced, but the poor water solubility limits the absorption efficiency
Solution Approach 1:
By transforming polyphenol to amorphous form, the patent dramatically improves its apparent solubility and dissolution rate. This enables more efficient absorption of the same quantity of polyphenol, or alternatively, allows administration of lower doses to achieve the same therapeutic effect, thereby improving absorption efficiency while maintaining or enhancing the quantity of absorbed substance
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 composition enables high and prolonged dissolution of polyphenols into body fluids, facilitating efficient ingestion and absorption, thereby enhancing their physiological effects.
Implementation Method 1
a solid composition comprising (1) an amorphous poorly water-soluble polyphenol... (2) a hydrophilic polymer... and (3) a nonionic surfactant... allows a polyphenol to dissolve at a high rate into the body fluid
Implementation Method 2
an amorphous poorly water-soluble polyphenol having two or more phenolic hydroxy groups in the same molecule, wherein the solubility of the polyphenol in crystalline form is 0.1 mass% or less at 25°C in pure water
Data Source
Figure 1-1~1-2
Figure 1-3~2
Figure 3~4
AI summary
An object of the present invention is to provide a polyphenol-containing solid composition that enables efficient ingestion of a polyphenol. This object can be achieved by a solid composition containing (1) an amorphous poorly water-soluble polyphenol, (2) a hydrophilic polymer, and (3) at least one nonionic surfactant selected from the group consisting of polyglycerol fatty acid esters, sucrose fatty acid esters, and lecithins.