Delayed-Release Mesalamine Coating for Targeted Colon Delivery

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current oral mesalamine formulations for treating ulcerative colitis suffer from suboptimal drug release profiles and bioavailability, leading to poor patient compliance due to large capsule sizes and frequent dosing requirements, with existing products being difficult for some patients to swallow and ineffective in reaching the right and transverse colon.

Innovation Solution

A delayed-release formulation comprising a multi-layered structure with an inert core, mesalamine layer, hyaluronan layer, and enteric coating, designed to release mesalamine primarily in the intestinal tract, enhancing bioavailability and absorption.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional oral mesalamine formulations are used, then the medication can be administered orally, but the drug is absorbed in the digestive tract before reaching the colon or rectum, reducing therapeutic efficacy

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidpremature drug absorption

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The formulation is divided into multiple particles, each consisting of a core and a coating layer. The coating layer is segmented into an inner enteric coating and an outer hydrophilic polymer coating, creating distinct functional zones that control drug release at different stages of gastrointestinal transit.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The enteric coating acts as an intermediary barrier that prevents premature drug release in the acidic stomach environment. The hydrophilic polymer coating serves as a secondary intermediary that controls the rate of drug release in the intestinal tract, ensuring the drug reaches the colon intact.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If existing delayed-release mesalamine capsules are used, then the drug can be delivered to the colon, but the capsule size is large (23.4-25.3 mm), making it difficult for some patients to swallow

Engineering Contradiction:

Improvedrug delivery to colonVSAvoidswallowability

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The total mesalamine dose is divided into multiple smaller particles that can be encapsulated in a smaller capsule. Each particle contains a controlled amount of drug (e.g., 40-80 mg), allowing the total dose to be delivered in a compact form factor that is easier to swallow while maintaining colonic delivery efficacy.

Inventive Principle:

Principle #1Segmentation

3Reliability

If conventional mesalamine formulations are used, then the drug can be administered, but the dosing frequency is at least three times per day, resulting in poor patient compliance

Engineering Contradiction:

Improvedrug availabilityVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The hydrophilic polymer coating provides sustained release of mesalamine throughout the intestinal transit time, maintaining therapeutic drug levels continuously as the particles move through the gastrointestinal tract. This eliminates the need for multiple daily doses and improves patient compliance.

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The formulation utilizes the dynamic pH environment and transit time of the gastrointestinal tract to control drug release. The enteric coating dissolves at intestinal pH, and the hydrophilic polymer provides time-dependent release as particles move through the digestive system, achieving continuous therapeutic action.

Inventive Principle:

Principle #15Dynamics

4Duration of action of moving object

If extended-release mesalamine formulations are used, then the medication is released throughout the colon and rectum, but the drug release profile and bioavailability remain suboptimal

Engineering Contradiction:

Improveduration of drug releaseVSAvoidbioavailability

Core Design Contradiction:

Duration of action of moving objectVSReliability

Solution Approach 1:

The formulation provides different release characteristics at different locations: the enteric coating ensures no release in the stomach, while the hydrophilic polymer coating provides controlled release in the intestinal tract. This localized control of drug release properties optimizes bioavailability at the target site.

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 achieves higher and more sustained mesalamine concentrations in the bloodstream, minimizing gastric irritation and maximizing therapeutic action in inflamed colon areas, improving treatment efficacy and compliance by maintaining effective drug concentrations over a longer period.

Implementation Method 1

an inner enteric coating layer... an outer hydrophilic polymer coating layer

Methodology Applied

Scientific EffectpH-dependent solubility:

Implementation Method 2

an outer hydrophilic polymer coating layer... comprising hydroxypropyl methylcellulose phthalate

Methodology Applied

Scientific EffectHydrophilic polymer hydration:

Implementation Method 3

controlled-rate release of mesalamine in the intestinal tract

Methodology Applied

Scientific EffectDiffusion: Diffusion

Data Source

PatentUS20260090996A1Delayed release oral pharmaceutical composition

Publication Date: 2026.04.02 AIHOL CORP

AI summary

Disclosed herein are compositions and methods for the treatment of inflammatory bowel disease. According to some embodiments, the compositions and methods involve the use of a delayed-release formulation containing a mesalamine layer, a hyaluronan layer, and at least one coating layer.