Enteric-Coated Ashwagandha Extract for Bioavailability

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Solution Overview

Problem

Ashwagandha extracts contain alkaloids and withanolide aglycones that are toxic and reduce the bioactivity of withanolide glycosides when ingested, leading to ineffective bioavailability and bioactivity, especially in acidic environments of the stomach.

Innovation Solution

An enteric-coated Ashwagandha extract composition is developed, enriched with withanolide glycosides and saponins, with reduced alkaloids, withanolide aglycones, and oligosaccharides, which protects withanolide glycosides from hydrolysis in acidic conditions, allowing them to be released and absorbed in neutral/alkaline pH environments of the gastrointestinal tract, enhancing bioavailability and bioactivity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Ashwagandha extract is administered in acidic environment (stomach), then the extract is released, but withanolide glycosides undergo hydrolysis and convert to toxic withanolide aglycones, reducing bioactivity

Engineering Contradiction:

ImprovebioavailabilityVSAvoidhydrolysis in acidic environment

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

An enteric coating layer is introduced as an intermediary between the Ashwagandha extract and the acidic gastric environment. This coating acts as a protective mediator that prevents direct contact between the withanolide glycosides and stomach acid, thereby preventing hydrolysis while still allowing release in the neutral/alkaline environment of the intestine.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The enteric coating provides preliminary protection against the harmful acidic environment before the extract is exposed to it. By pre-establishing a protective barrier, the coating prevents the unwanted hydrolysis reaction from occurring in the first place, ensuring the withanolide glycosides remain intact until they reach the appropriate pH environment.

Inventive Principle:

Principle #9Preliminary anti-action

2Reliability

If conventional Ashwagandha extract is used, then the extract contains all natural components, but toxic alkaloids and withanolide aglycones reduce the overall bioactivity

Engineering Contradiction:

ImprovebioactivityVSAvoidtoxic alkaloids and withanolide aglycones

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The extraction process is modified to selectively remove toxic components (alkaloids and withanolide aglycones) from the Ashwagandha extract while retaining the beneficial withanolide glycosides and saponins. This selective extraction eliminates the harmful factors that reduce bioactivity.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The extraction parameters (solvent type, temperature, pH, extraction time) are optimized to change the selectivity of the extraction process. By adjusting these parameters, the process preferentially extracts toxic alkaloids and aglycones while leaving the active glycosides and saponins in the residue, thereby enriching the extract in beneficial components.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If enteric coating is applied to protect withanolide glycosides, then bioavailability increases, but the device complexity increases due to coating requirements

Engineering Contradiction:

ImprovebioavailabilityVSAvoidenteric coating process

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

A thin film enteric coating is applied to the Ashwagandha extract particles or tablets. This flexible shell provides the necessary protection against acidic hydrolysis while maintaining a relatively simple structure that does not significantly increase device complexity. The coating can be applied using standard pharmaceutical coating techniques.

Inventive Principle:

Principle #30Flexible shells and thin films

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 enteric-coated Ashwagandha extract composition exhibits enhanced antistress, immunomodulatory, antidiabetic, and anti-inflammatory activities at lower dosages, improving sleep quality and endurance, with increased bioavailability of withanolide glycosides, demonstrating improved therapeutic efficacy.

Implementation Method 1

protects withanolide glycosides from hydrolysis in acidic conditions

Methodology Applied

Scientific EffectHydrolysis: Hydrolysis

Implementation Method 2

allowing them to be released and absorbed in neutral/alkaline pH environments

Methodology Applied

Scientific EffectpH-dependent release:

Data Source

PatentUS11638738B2Process to enhance the bioactivity of Ashwagandha extracts

Publication Date: 2023.05.02 ANTONY BENNY

AI summary

The invention relates to an extract of Ashwagandha that exhibit enhanced bioactivity and bioavailability comprising of enriched withanolide glycosides and saponins; with negligible amount of alkaloids, withanolide aglycones and oligosaccharides. The extract as disclosed prepared from root, stems, leaves and whole plant of Ashwagandha further shows improved immunomodulatory activity, anti-inflammatory activity, anti stress activity, antidiabetic activity and sleep quality. The disclosure also provides a method of improving bioactivity of withanolide glycosides even at lower doses, by the administration of an enteric coated formulation of extract of Ashwagandha to humans. The enteric coating protects the composition from hydrolysis in the acidic environment of the stomach to release the withanolide glycoside in neutral/alkaline pH in gastrointestinal tract (GIT) thus enhancing the absorption. Further the process of preparation of the extract of Ashwagandha enriched with withanolide glycosides and saponins are disclosed along with various formulations.