Enteric-Coated Oxygen-Generating Particles for Gut Microbiota Modulation

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Solution Overview

Problem

Current treatments for metabolic disorders such as obesity, metabolic syndrome, and cardiovascular disease lack effective and safe medication options, with existing microbiome modulation approaches like probiotics and antibiotics showing limited targeted efficacy and safety concerns.

Innovation Solution

Administering an effective amount of agents that increase oxygen tension and/or redox potential and/or pH in the colon using a multiparticulate pharmaceutical preparation, specifically enteric-coated particles encapsulated in a capsule or sachet, to modify the gut microbiome, thereby managing weight and treating metabolic disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the coating thickness is increased to reliably coat the capsule junction, then the enteric properties are improved, but the capsule fails to open and release API in vivo

Engineering Contradiction:

Improveenteric propertiesVSAvoidcapsule opening

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The invention divides the capsule into multiple segments or zones with different coating thicknesses. The coating is applied thicker at the cap-body junction to ensure enteric resistance, while maintaining thinner coating at other areas to allow proper opening and release of active pharmaceutical ingredient (API) in vivo.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention applies different coating qualities to different locations of the capsule. Specifically, the cap-body junction receives enhanced coating thickness to ensure reliable enteric properties at this critical failure point, while the rest of the capsule surface maintains sufficient but not excessive coating to preserve opening functionality.

Inventive Principle:

Principle #3Local quality

2Ease of operation

If the coating thickness is decreased to enable capsule opening, then the ease of operation is improved, but the enteric properties are compromised at the capsule junction

Engineering Contradiction:

Improvecapsule openingVSAvoidenteric properties

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The coating is segmented into zones of different thicknesses, with the critical cap-body junction receiving thicker coating for enteric reliability, while other areas have thinner coating to facilitate proper capsule opening and API release.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention implements local quality enhancement by applying thicker coating specifically at the cap-body junction where enteric failure is most likely to occur, while maintaining adequate but not excessive coating thickness elsewhere to preserve capsule opening capability.

Inventive Principle:

Principle #3Local quality

3Adaptability or versatility

If conventional microbiome modulation approaches are used, then the treatment options are available, but the targeted efficacy and safety profile are unfavorable

Engineering Contradiction:

Improvetreatment optionsVSAvoidtargeted efficacy

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The invention uses oxygen-generating agents as intermediaries to indirectly modulate the microbiome. Instead of directly administering probiotics or antibiotics, the agents generate oxygen in the colon, creating an environment that selectively promotes beneficial aerobic bacteria while suppressing harmful anaerobic bacteria, thereby achieving targeted efficacy with improved safety.

Inventive Principle:

Principle #24Intermediary (Mediator)

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

This approach effectively reduces harmful bacterial types and increases beneficial bacterial types in the colon, leading to weight management and improved metabolic health by modifying the colon environment, as demonstrated by increased aerobic bacteria and decreased Firmicutes abundance.

Implementation Method 1

If coating thickness is too low, then the capsules fail to reliably show enteric properties (they open in acidic conditions)

Methodology Applied

Scientific EffectEnteric coating resistance:

Implementation Method 2

a high coating thickness also leads to a non-functional formulation, because the capsules fail to open and release API in vivo

Methodology Applied

Scientific EffectpH-dependent dissolution:

Data Source

PatentUS11311573B2Pharmaceutical preparations and methods to manage weight and to modulate the gut microbiota

Publication Date: 2022.04.26 LPOXY THERAPEUTICS INC

AI summary

A pharmaceutical preparation, comprising: A) A plurality of particles, each particle comprising: 1) a core comprising at least one agent that increases oxygen tension and/or redox potential and/or pH in the colon of a subject following administration to the subject, and 2) an enteric coating encasing the core; and B) a capsule or sachet encasing the plurality of particles. Methods of weight management for a subject, comprising administering the pharmaceutical preparation to a subject in need thereof.