Stilbene Polyphenol Co-precipitate with Lamellar Anionic Solids
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Solution Overview
Problem
Stilbene polyphenols, such as resveratrol, face limitations in bioavailability due to low water solubility and rapid degradation, leading to reduced efficacy in pharmaceutical and cosmetic applications.
Innovation Solution
A co-precipitate of stilbene polyphenols with lamellar anionic solids is formed in a hydro-alcoholic environment at alkaline pH, enhancing dissolution rate and bioavailability while maintaining photostability, suitable for various formulations across pharmaceutical, nutraceutical, and cosmeceutical fields.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If stilbene polyphenols are used in their native form, then they exhibit pharmacological activity, but they show low water solubility and reduced bioavailability
Solution Approach 1:
The patent creates a composite material by forming a co-precipitate between stilbene polyphenols and lamellar anionic solids (such as hydroxide double salts or hydrotalcites). This composite structure integrates the active polyphenol compound with a carrier material that provides improved solubility characteristics while maintaining the pharmacological activity of the original substance
Solution Approach 2:
The invention changes the physical and chemical parameters of the stilbene polyphenols by converting them from their native crystalline form into a co-precipitate form with altered surface properties and solubility characteristics. The co-precipitation process modifies parameters such as particle size, surface area, and crystal structure, thereby enhancing water solubility and bioavailability
2Duration of action of stationary object
If stilbene polyphenols are stored or exposed to light, then they remain available for use, but they exhibit rapid degradation and photostability issues
Solution Approach 1:
The lamellar anionic solids act as an intermediary protective matrix that shields the stilbene polyphenols from direct light exposure and environmental degradation factors. This carrier material serves as a barrier between the sensitive active ingredient and harmful external conditions, thereby extending shelf life and improving photostability
3Reliability
If the dissolution rate of stilbene polyphenols is increased through formulation, then bioavailability improves, but the complexity of the formulation process increases
Solution Approach 1:
The patent performs preliminary action by pre-forming the co-precipitate structure before final formulation. The active ingredient is pre-complexed with the lamellar anionic solids in a controlled co-precipitation process, creating a pre-optimized solubility-enhanced form that can be directly incorporated into final formulations without requiring additional complex solubility enhancement steps
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 co-precipitate exhibits improved bioavailability and photostability, enabling stable absorption and increased pharmacokinetic benefits, suitable for diverse applications including oral, topical, and ophthalmic preparations, with enhanced shelf life and industrial production feasibility.
Implementation Method 1
The process to obtain this product is based on the development, in hydro-alcoholic environment, of a co-precipitate as defined in claim 1
Implementation Method 2
The increased dissolution rate of the stilbene polyphenols co-precipitate, and therefore the better biovailability compared to the starting one, makes this product suitable for the preparation of formulations with improved activity and it allows its use for different applications
Data Source
Figure 1A~1B
Figure 2A~2B
Figure 2C
AI summary
In the present invention describes a new product, its applications and its method of preparation, consisting of one or more stilbene polyphenols, including resveratrol, and their derivatives and lamellar solids anionic, such as the hydrotalcites (LDHs), also known as anionic clays or lamellar double hydroxides, and salts double hydroxide (HDSs). The new product has an increased dissolution rate in acid gastric-like aqueous environment, increased bioavailability, greater photostability compared to starting stilbene poliphenols and their derivatives. The increased dissolution rate of the stilbene polyphenol co-precipitate, and therefore the better bioavailability compared to that of starting active principles, make the product suitable to the preparation of formulations with improved activity and allow for their use in different applications. Among the formulations and applications considered in the context of the present invention include those pharmaceutical, nutraceutical, dermatological, cosmeceutical, food and medical devices.