Intra-Extra Granular Formulation for Colonic Evacuation

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Solution Overview

Problem

Current bowel cleansing protocols for colonoscopy and colonic surgery lack a simplified and effective method to achieve clean colonic mucosa for detecting small lesions or abnormalities, requiring improved evacuation techniques.

Innovation Solution

A solid dosage formulation comprising an intra-granular fraction with osmotic evacuant agents, antacids, and pharmaceutically acceptable excipients, combined with an extra-granular fraction including organic acids and non-metallic lubricants, administered orally in a specific regimen to achieve effective colonic evacuation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional bowel cleansing protocols are used, then colonic evacuation can be achieved, but the protocols are complex and require large volumes of fluid

Engineering Contradiction:

Improvesimplicity of bowel cleansing protocolVSAvoidfluid volume required

Core Design Contradiction:

Ease of operationVSQuantity of substance

Solution Approach 1:

The formulation is divided into intra-granular and extra-granular fractions, allowing separate control of osmotic evacuant release and fluid absorption. This segmentation enables the system to achieve colonic evacuation with minimal fluid intake by decoupling the evacuation mechanism from fluid requirement

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent modifies the physical and chemical parameters of the formulation including granule size distribution, osmotic pressure characteristics, and release kinetics. These parameter changes enable effective colonic evacuation with reduced fluid volume by optimizing the osmotic gradient and water mobility within the formulation

Inventive Principle:

Principle #35Parameter changes

2Reliability

If high doses of evacuant agents are used to ensure effective colonic evacuation, then evacuation efficacy is improved, but side effects and fluid shifts increase

Engineering Contradiction:

Improveevacuation efficacyVSAvoidside effects and fluid shifts

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The formulation introduces water-mobility modifying agents and fluid absorption components as intermediaries between the osmotic evacuant agents and the colonic contents. These intermediaries modulate the osmotic effect to achieve reliable evacuation while minimizing harmful fluid shifts and side effects

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite formulation combining osmotic evacuant agents, fluid absorption components, water-mobility modifying agents, and excipients in specific ratios. This composite structure balances evacuation efficacy with reduced side effects by integrating multiple functional components that work synergistically

Inventive Principle:

Principle #40Composite materials

3Reliability

If the formulation includes multiple active ingredients for comprehensive bowel cleansing, then evacuation effectiveness is improved, but manufacturing complexity increases

Engineering Contradiction:

Improvebowel cleansing effectivenessVSAvoidformulation manufacturing complexity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The formulation is segmented into intra-granular and extra-granular fractions with distinct manufacturing processes. This segmentation allows each fraction to be manufactured separately with optimized parameters, then combined, reducing overall manufacturing complexity while maintaining comprehensive bowel cleansing effectiveness

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

Different regions of the formulation (intra-granular vs. extra-granular) have different quality attributes and manufacturing requirements. By assigning specific ingredients and functions to different regions, the patent enables localized manufacturing optimization that simplifies production of multi-ingredient formulations

Inventive Principle:

Principle #3Local quality

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 formulation provides optimal drug release, stability, and minimal fluid requirement, ensuring adequate shelf life and effective colonic evacuation while reducing side effects, making it suitable for detecting gastrointestinal conditions and infections.

Implementation Method 1

the intra-granular fraction includes granules comprising at least one osmotic evacuant agent

Methodology Applied

Scientific EffectOsmosis: Osmosis

Implementation Method 2

the extra-granular fraction includes one or more organic acids

Methodology Applied

Scientific EffectAcidification:

Data Source

PatentUS11058671B2Formulations and methods of manufacturing formulations for use in colonic evacuation

Publication Date: 2021.07.13 REDHILL BIOPHARMA LTD

AI summary

Formulations and methods of manufacturing formulations for use in colonic evacuation are disclosed herein, in an embodiment, a solid dosage formulation includes an intra-granular fraction intermingled with an extra-granular fraction, wherein the intra-granular fraction includes granules comprising at least one osmotic evacuant agent, at least one antacid, and a first pharmaceutically acceptable excipient component, and wherein the extra-granular fraction includes one or more organic acids, a non-metallic lubricating element, and a second pharmaceutically acceptable excipient component.