Expandable Coating for Gastric Retention via Segmentation

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Solution Overview

Problem

Existing gastric retention systems face challenges in maintaining prolonged gastric retention and controlled drug release due to variability in gastrointestinal conditions, with prior solutions often requiring optimization of multiple components to achieve buoyancy, swelling, and integrity, which can be difficult to achieve simultaneously.

Innovation Solution

A gastric retention system comprising a tablet or capsule coated with an expandable coating formed by a film-forming polymer and expandable components, allowing rapid floatation and swelling while maintaining physical integrity, and capable of controlling the release of therapeutically active agents in both immediate and modified release forms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If systems containing swellable polymers and gas-generating agents are used to increase gastric retention, then the system attains large size and floatation capability, but the system becomes difficult to manufacture with consistent performance

Engineering Contradiction:
Improvegastric retention timeVSAvoidmanufacturing consistency
Core Design Contradiction:
Duration of action of stationary objectVSEase of manufacture

Solution Approach 1:

The system is divided into two separate functional components: an inner core containing the drug and swellable polymer, and an outer coating layer containing the gas-generating agent. This segmentation allows each component to be optimized and manufactured separately, improving manufacturing consistency while maintaining the combined effect of swelling and floatation for prolonged gastric retention.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The system uses a composite structure with an inner core of swellable polymer matrix and an outer coating of gas-generating composition. This composite material approach enables independent optimization of each layer's properties, allowing consistent control of swelling rate, gas generation, and floatation behavior, thereby resolving the manufacturing difficulty while achieving prolonged gastric retention.

Inventive Principle:
Principle #40Composite materials

2Duration of action of stationary object

If the system is made large in size to prevent passage through the pyloric sphincter, then gastric retention is improved, but the system becomes difficult to administer and may cause patient discomfort

Engineering Contradiction:
Improvegastric retention timeVSAvoidadministration convenience
Core Design Contradiction:
Duration of action of stationary objectVSEase of operation

Solution Approach 1:

The system transitions from a small, swallowable size to a large, retained size through dynamic expansion in the stomach. The inner core swells and the outer coating generates gas to create floatation, allowing the system to be administered easily in a compact form and then expand to a size that prevents pyloric passage, thus resolving the contradiction between administration convenience and gastric retention.

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The system utilizes phase transitions of the swellable polymer and gas-generating agents upon contact with gastric fluids. The polymer absorbs water and swells, while the gas-generating agents produce carbon dioxide bubbles, causing the system to expand from a small swallowable size to a large retained size, enabling easy administration followed by effective gastric retention.

Inventive Principle:
Principle #36Phase transitions

3Reliability

If multiple components are optimized to achieve simultaneous buoyancy, swelling, and integrity, then gastric retention performance is improved, but the device complexity increases

Engineering Contradiction:
Improvegastric retention performanceVSAvoidsystem structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The system is segmented into two distinct functional layers: an inner core containing the drug and swellable polymer, and an outer coating containing gas-generating agents. This segmentation simplifies the overall structure by assigning specific functions to each layer, making the system easier to design and manufacture while maintaining reliable performance for buoyancy, swelling, and integrity control.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The outer coating layer serves multiple functions: it protects the inner core, generates gas for floatation, and controls the release of the gas-generating agents. This multi-functionality reduces the need for additional separate components, simplifying the overall device structure while ensuring reliable gastric retention performance through coordinated swelling and buoyancy.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 system achieves prolonged gastric retention and controlled drug release by ensuring rapid floatation and swelling, maintaining physical integrity, and providing consistent delivery of therapeutically active agents, addressing the limitations of prior systems.

Implementation Method 1

an expandable coating comprising a film-forming polymer and an expandable component

Methodology Applied
Scientific EffectSwelling: Hydrogel

Implementation Method 2

a composition containing highly swellable polymers in admixture with a gas-generating agent to form systems that are large in size as well as capable of floating on gastric fluids

Methodology Applied
Scientific EffectGas generation:

Implementation Method 3

systems that are large in size as well as capable of floating on gastric fluids

Methodology Applied
Scientific EffectBuoyancy: Archimedes' Principle (Buoyancy)

Data Source

PatentUS9439851B2Gastric retention system
Publication Date: 2016.09.13 SUN PHARMA ADVANCED RESEARCH CO LTD

AI summary

The present invention provides a novel gastric retention system in the form of a tablet or a capsule coated with an expandable coating, more particularly, with an expandable coating comprising a film-forming polymer and an expandable component.