Delayed-Release Mesalamine Capsule With Enteric Layered Delivery
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Solution Overview
Problem
Current oral mesalamine formulations for treating inflammatory bowel disease suffer from suboptimal drug release profiles and bioavailability, leading to poor patient compliance and limited therapeutic efficacy, particularly due to issues with size and frequency of administration.
Innovation Solution
A delayed-release capsule formulation comprising a multi-layered structure with an inert core, mesalamine layer, hyaluronan layer, and enteric coating layer, designed to release mesalamine primarily in the intestinal tract, enhancing bioavailability and patient compliance.
Engineering Contradictions & Design Principles
Engineering 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
Solution Approach 1:
The capsule is segmented into multiple compartments, each containing particles with specific coating formulations. This segmentation allows different regions of the capsule to release drug at different locations along the digestive tract, with enteric-coated particles specifically designed to resist gastric acid and release mesalamine in the colon or rectum, preventing premature absorption
Solution Approach 2:
An enteric coating layer acts as an intermediary barrier between the mesalamine drug and the gastric environment. This coating prevents the drug from being absorbed in the stomach and small intestine, allowing it to reach the colon or rectum intact where it is needed for therapeutic effect
2Reliability
If rectal administration (suppositories or enemas) is used to deliver mesalamine to the colon or rectum, then the drug reaches the target area, but the method is less convenient and less acceptable to patients
Solution Approach 1:
The oral capsule formulation combines multiple functions in a single convenient dosage form: it provides systemic absorption protection through enteric coating, enables targeted delivery to both colon and rectum through multi-compartment design, and maintains the ease of oral administration that patients prefer over rectal routes
3Reliability
If suppositories are used for rectal administration, then the drug reaches the rectum, but it only reaches the rectum and not the right and transverse side of the colon
Solution Approach 1:
The capsule is divided into multiple compartments containing particles with different coating formulations. Some particles are designed with coatings that dissolve at specific pH levels or under specific conditions, enabling the drug to be released at different locations along the colon, including the right side, transverse side, and rectum, providing comprehensive coverage
4Reliability
If enemas are used for rectal administration, then the drug covers the left side of the colon, but it does not effectively treat the right and transverse side of the colon
Solution Approach 1:
The multi-compartment capsule contains particles with different enteric coating formulations that respond to different physiological conditions along the digestive tract. This segmentation enables the drug to be released at multiple locations including the right side, transverse side, and left side of the colon, providing comprehensive coverage that enemas cannot achieve
5Reliability
If delayed-release products are administered three times per day with a total dose of at least 2 grams, then the drug provides therapeutic effect, but patient compliance is poor
Solution Approach 1:
The capsule is designed to provide continuous drug release along the digestive tract as it passes through different regions. The multi-compartment design with particles having different release characteristics ensures sustained therapeutic action throughout the day, potentially reducing the frequency of administration and improving patient compliance
6Quantity of substance
If large capsule sizes (25.3 and 23.4 millimeters) are used, then the capsule can contain sufficient drug dose, but it is difficult for pediatric patients or those with swallowing difficulties to swallow
Solution Approach 1:
The capsule employs a nested structure where multiple smaller compartments containing drug particles are housed within a single capsule shell. This nesting approach allows the total drug dose to be distributed across multiple smaller units, reducing the overall capsule size and improving swallowability while maintaining the required dosage
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 peak plasma concentrations and sustained drug absorption, minimizing gastric irritation and maximizing therapeutic effect in inflamed colon areas, thus improving treatment efficacy and compliance.
Implementation Method 1
designed to release mesalamine primarily in the intestinal tract
Implementation Method 2
a delayed-release capsule formulation... designed to release mesalamine primarily in the intestinal tract
Data Source
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 capsule formulation containing a mesalamine layer, a hyaluronan layer, and at least one coating layer.