Oral Plant-Based Formulations Using SNAC for Rapid Absorption

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Solution Overview

Problem

Oral administration of plant-based compounds, such as THC, often results in slow onset and low bioavailability due to poor aqueous solubility and first-pass hepatic metabolism, leading to delayed therapeutic effects.

Innovation Solution

Incorporating N-acylated fatty amino acids, such as SNAC, into oral formulations to enhance absorption and bioavailability by improving water solubility and gastrointestinal penetration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If plant-based compounds are administered orally in traditional formulations, then they are easy to administer, but the onset of action is slow and bioavailability is low

Engineering Contradiction:
Improveease of administrationVSAvoidonset of action time
Core Design Contradiction:
Ease of operationVSLoss of time

Solution Approach 1:

The patent uses SNAC (sodium N-acetylglucosaminyl-L-alanine) as an intermediary substance that facilitates the absorption of poorly water-soluble plant-based compounds across the gastrointestinal membrane. SNAC acts as a carrier that temporarily binds to the hydrophobic compound, enabling it to traverse the aqueous environment of the GI tract and reach systemic circulation more rapidly, thereby reducing onset time while maintaining oral administration convenience.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical-chemical parameters of the formulation by combining the plant-based compound with SNAC, which alters the solubility and membrane permeability characteristics of the active ingredient. This parameter change enables faster dissolution and absorption in the gastrointestinal tract, accelerating the onset of action without sacrificing the ease of oral dosing.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If plant-based compounds are administered orally in traditional formulations, then they are easy to administer, but bioavailability is low due to poor aqueous solubility and first-pass metabolism

Engineering Contradiction:
Improveease of administrationVSAvoidbioavailability
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

SNAC serves as a mediator that protects the plant-based compound from degradation during GI transit and enhances its transport across the intestinal epithelium. The SNAC-compound complex bypasses some of the limitations of first-pass metabolism by facilitating rapid absorption into the portal circulation, increasing the fraction of the administered dose that reaches systemic circulation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite formulation consisting of the plant-based compound combined with SNAC. This composite material exhibits enhanced pharmacokinetic properties compared to the pure plant compound, including improved water solubility, increased membrane permeability, and reduced metabolic degradation, thereby increasing overall bioavailability while maintaining oral administration.

Inventive Principle:
Principle #40Composite materials

3Ease of operation

If plant-based compounds are administered orally, then they avoid invasive delivery methods, but absorption is limited by poor water solubility

Engineering Contradiction:
Improvenon-invasive deliveryVSAvoidabsorption reliability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

SNAC acts as a reliable intermediary that consistently enhances the absorption of hydrophobic plant-based compounds across the gastrointestinal barrier. By forming a stable complex with the active ingredient, SNAC ensures predictable and reliable absorption kinetics, making oral delivery as reliable as invasive methods for these compounds.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation modifies the solubility parameters of the plant-based compound through interaction with SNAC, transforming it from a poorly water-soluble substance into a formulation with enhanced aqueous solubility. This parameter change ensures reliable dissolution and absorption in the GI tract, maintaining the advantages of non-invasive oral delivery.

Inventive Principle:
Principle #35Parameter changes

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 use of N-acylated fatty amino acids significantly reduces the time to onset of action and increases peak concentrations, achieving faster and more effective therapeutic effects compared to traditional oral formulations.

Implementation Method 1

Incorporating N-acylated fatty amino acids, such as SNAC, into oral formulations to enhance absorption and bioavailability by improving water solubility

Methodology Applied
Scientific EffectSolubility enhancement: Solvation

Implementation Method 2

Incorporating N-acylated fatty amino acids, such as SNAC, into oral formulations to enhance absorption and bioavailability by improving gastrointestinal penetration

Methodology Applied
Scientific EffectPenetration enhancement: Permeation

Data Source

PatentUS11246852B2Fast-acting plant-based medicinal compounds and nutritional supplements
Publication Date: 2022.02.15 SPOKE SCIENCES INC
  • US11246852B2 patent drawing
  • US11246852B2 patent drawing
  • US11246852B2 patent drawing

AI summary

Plant-based medicinal compounds or nutritional supplements in various carrier combinations are described. The carriers can include N-acylated fatty amino acids, penetration enhancers, and/or various other beneficial carriers. The plant-based composition/carrier combinations can create administration benefits.