Gastric Resistant Capsule Shell Using Integrated Pectin Gelatin Matrix

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Solution Overview

Problem

Existing enteric dosage forms face issues such as 'orange peel' surface formation, coat integrity failure, and uneven coating distribution, particularly with gelatin or polysaccharide capsules, which are sensitive to heat and require a subcoating step for proper coating, and synthetic polymers are not always preferred.

Innovation Solution

A gastric resistant film-forming composition containing 2-4% gastric resistant natural polymer, 25-40% film-forming natural polymer, 8-30% plasticizers, and less than 1% gelling agent, such as pectin and gelatin, is used to create a gastric resistant capsule shell through a rotary die encapsulation process, preventing gastric reflux and esophageal irritation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a film coating process is used to apply enteric polymer coating, then gastric protection is achieved, but surface roughness and coat integrity failure occur

Engineering Contradiction:
Improvegastric protectionVSAvoidsurface roughness
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The invention extracts the enteric coating function from a separate film coating process and integrates it into the capsule shell formulation itself. By incorporating acid-insoluble polymers directly into the gelatin or polysaccharide shell matrix, the coating is eliminated and the shell itself provides gastric resistance, thereby avoiding all coating-related surface defects.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention merges the structural function of the capsule shell with the protective function of the enteric coating. The acid-insoluble polymer is combined with gelatin or polysaccharide to create a unified shell structure that simultaneously provides mechanical integrity and gastric protection, eliminating the need for separate coating layers.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If film coating process is used, then enteric protection is achieved, but coating integrity failure such as cracking or flaking occurs

Engineering Contradiction:
Improveenteric protectionVSAvoidcoating integrity
Core Design Contradiction:
ReliabilityVSStrength

Solution Approach 1:

The invention removes the separate film coating layer that is prone to cracking and flaking. By integrating the enteric function directly into the shell formulation, the weak interface between coating and shell is eliminated, and the unified structure prevents coating integrity failures.

Inventive Principle:
Principle #2Taking out (Extraction)

3Reliability

If enteric coating is applied to gelatin capsules, then gastric resistance is achieved, but the shiny and clear appearance is lost

Engineering Contradiction:
Improvegastric resistanceVSAvoidappearance clarity
Core Design Contradiction:
ReliabilityVSIllumination intensity

Solution Approach 1:

The invention combines the aesthetic properties of gelatin capsules with the gastric resistance function in a single integrated shell. By incorporating acid-insoluble polymers into the gelatin shell formulation, the shell maintains the natural shine and clarity of gelatin while simultaneously providing enteric protection, eliminating the need for opaque coating layers.

Inventive Principle:
Principle #5Merging (Combining)

4Reliability

If conventional enteric coating is used, then gastric protection is achieved, but uneven coating distribution occurs

Engineering Contradiction:
Improvegastric protectionVSAvoidcoating uniformity
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The invention merges the enteric polymer with the shell-forming polymer in a homogeneous mixture before shell formation. This ensures uniform distribution of the acid-insoluble polymer throughout the entire shell structure, eliminating the uneven coating distribution that occurs with conventional film coating processes.

Inventive Principle:
Principle #5Merging (Combining)

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 composition provides a stable, gastric resistant capsule shell that effectively encapsulates liquid, semi-solid, or solid fills, preventing gastric reflux and esophageal irritation, while maintaining the clarity and shine of gelatin capsules, and can be used for drug delivery with active agents and excipients.

Implementation Method 1

a gastric resistant film-forming composition which contains a gastric resistant film-forming composition

Methodology Applied
Scientific EffectGelling: Gel

Data Source

PatentEP2923696B1Gastric reflux resistant dosage forms
Publication Date: 2018.07.11 PATHEON SOFTGELS INC

AI summary

Gastric resistant film-forming compositions are described herein. The composition contains a gastric resistant natural polymer, a film-forming natural polymer, and optionally a gelling agent. Suitable gastric resistant natural polymers include polysaccharides such as pectin and pectin-like polymers. The film-forming composition can be used to prepare soft or hard shell gelatin capsules which can encapsulate a liquid or semi-solid fill material or a solid tablet (SOFTLET®) containing an active agent and one or more pharmaceutically acceptable excipients. Alternatively, the composition can be administered as a liquid with an active agent dissolved or dispersed in the composition. The compositions are not only gastric resistant but may also prevent gastric reflux associated with odor causing liquids, such as fish oil or garlic oil, encapsulated in a unit dosage form and esophageal irritation due to the reflux of irritant drugs delivered orally.