Reverse-Enteric Capsule Coatings for Timed Gastric Unfolding
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Solution Overview
Problem
Existing gastric residence systems face challenges in controlling their unfolding within the gastrointestinal tract, potentially leading to premature deployment in the esophagus, delayed deployment in the intestine, or failure to deploy at all, thereby compromising the delivery of therapeutic agents to the stomach.
Innovation Solution
The use of capsules and capsule coatings, including a sleeve or band to maintain a folded configuration and a reverse-enteric coating to ensure gastric residence systems unfold at the desired location and time within the stomach, utilizing polymers, anti-tacking agents, and plasticizers to control deployment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the gastric residence system is designed to remain folded for transit, then it can pass through the esophagus and stomach without obstruction, but it may fail to unfold timely in the stomach or unfold too early causing obstruction
Solution Approach 1:
The capsule is designed with a reverse-enteric coating that is already prepared to dissolve at a specific pH level (stomach acid environment). This preliminary preparation ensures that the capsule will automatically dissolve at the correct location and time without requiring active control mechanisms, thereby achieving reliable controlled deployment while preventing premature or delayed unfolding.
Solution Approach 2:
The reverse-enteric coating utilizes pH-dependent dissolution characteristics to control capsule deployment. The coating is designed to remain intact in neutral or basic environments (esophagus, intestine) but dissolves rapidly in the acidic stomach environment. This parameter change (pH) serves as the trigger for controlled deployment, ensuring the gastric residence system unfolds only in the stomach after successful transit.
2Reliability
If the capsule dissolves rapidly in the stomach, then the gastric residence system can unfold timely, but it may dissolve too early in the esophagus causing obstruction
Solution Approach 1:
The reverse-enteric coating is applied specifically to the capsule surface to provide localized pH-dependent dissolution control. This local modification allows the capsule to remain stable in neutral environments while dissolving rapidly in the acidic stomach environment, ensuring timely deployment without premature dissolution in the esophagus.
Solution Approach 2:
The reverse-enteric coating acts as an intermediary layer between the capsule and the gastrointestinal environment. It mediates the dissolution process by selectively responding to pH changes, allowing the capsule to withstand neutral environments during transit while triggering rapid dissolution only in the acidic stomach, thus preventing premature deployment.
3Reliability
If the capsule is coated with reverse-enteric coating, then deployment is controlled to the stomach, but the coating process adds complexity to manufacturing
Solution Approach 1:
The reverse-enteric coating utilizes pH-dependent dissolution characteristics to control capsule deployment. The coating is designed to remain intact in neutral environments (esophagus, intestine) but dissolves rapidly in the acidic stomach environment. This parameter change (pH) serves as the trigger for controlled deployment, ensuring the gastric residence system unfolds only in the stomach after successful transit.
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
Ensures controlled deployment of gastric residence systems in the stomach, minimizing the risk of esophageal or intestinal obstructions and ensuring timely delivery of therapeutic agents.
Implementation Method 1
a coating on the capsule, wherein the gastric residence dosage form is configured to release the folded gastric residence system in a stomach of a patient
Data Source
AI summary
Disclosed herein are coatings for an encapsulated gastric residence system. The coating includes 50-95 wt. % reverse-enteric polymer; 3-25 wt. % anti-tacking agent; and 1-20 wt. % plasticizer.