Enteric Soft Capsule Shell Formulation with Alkaline Agents

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Existing enteric soft capsule manufacturing processes face challenges with brittle and viscous gel masses, requiring additional plasticizers and volatile alkaline agents, which complicate the manufacturing process and pose safety concerns.

Innovation Solution

The development of enteric soft capsules with gastric-resistant polymer compositions that include film-forming polymers like gelatin and acid-insoluble polymers, such as acrylic and methacrylate acid copolymers, which reduce the need for plasticizers and eliminate the use of volatile alkaline agents, enhancing manufacturing efficiency and safety.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If integrated enteric polymers are used in capsule shell formulation, then enteric properties and surface homogeneity are improved, but gel mass becomes brittle and viscous requiring additional plasticizers

Engineering Contradiction:
Improveenteric propertiesVSAvoidmanufacturing process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent changes the chemical parameters of the gel mass formulation by incorporating alkaline agents (ammonium hydroxide, sodium hydroxide, or potassium hydroxide) at controlled concentrations (0.1-10% w/w). This parameter change modifies the gel mass properties to achieve optimal balance between enteric resistance, elasticity, and manufacturability, resolving the contradiction between improved enteric properties and manufacturing complexity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite gel mass formulation combining film-forming polymers (gelatin, HPMC, or carrageenan), enteric polymers (acrylic/methacrylate copolymers), plasticizers, and alkaline agents. This composite approach integrates multiple functional components that work synergistically to provide both enteric properties and manufacturing flexibility without requiring excessive plasticizers

Inventive Principle:
Principle #40Composite materials

2Manufacturing precision

If integrated enteric polymers are used to eliminate coating defects, then surface homogeneity is improved, but volatile alkaline agents are required posing safety concerns

Engineering Contradiction:
Improvesurface homogeneityVSAvoidsafety concerns
Core Design Contradiction:
Manufacturing precisionVSObject-affected harmful factors

Solution Approach 1:

The patent carefully controls the concentration parameters of alkaline agents within specific ranges (0.1-10% w/w in gel mass, 1-20% w/w of enteric polymer weight) to achieve the necessary pH modification for polymer dissolution without excessive volatility. This parameter optimization reduces safety hazards while maintaining enteric functionality and surface homogeneity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces alkaline agents as intermediary substances that facilitate the dissolution of enteric polymers at intestinal pH without requiring volatile alkaline compounds. The alkaline agents act as mediators between the enteric polymer matrix and the intestinal environment, enabling controlled drug release while improving manufacturing safety

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of manufacture

If additional plasticizers are used to reduce gel mass viscosity, then ease of manufacturing is improved, but device complexity increases

Engineering Contradiction:
Improvegel mass processabilityVSAvoidformulation complexity
Core Design Contradiction:
Ease of manufactureVSDevice complexity

Solution Approach 1:

The patent optimizes the plasticizer concentration parameter within specific ranges (5-50% w/w of gel mass) and combines it with controlled alkaline agent addition to achieve optimal gel mass viscosity and elasticity. This balanced parameter approach improves processability while minimizing the need for excessive plasticizers and reducing formulation complexity

Inventive Principle:
Principle #35Parameter changes

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 new compositions result in enteric soft capsules with improved elasticity and enteric properties, increased compatibility with alkali-labile active substances, and simplified manufacturing, while maintaining enhanced stability and controlled release profiles.

Implementation Method 1

at least one or more acid-insoluble polymers

Methodology Applied
Scientific EffectAcid-insoluble polymer resistance:

Implementation Method 2

formed from a gel mass composition comprising: (a) at least one or more film-forming polymers

Methodology Applied
Scientific EffectGel formation: Gel

Implementation Method 3

at least one or more plasticizers

Methodology Applied
Scientific EffectPlasticization:

Data Source

PatentUS10226432B2Enteric soft capsule compositions
Publication Date: 2019.03.12 PATHEON SOFTGELS INC

AI summary

Described herein are enteric soft capsules comprising gastric resistant polymers and gelatin and methods for manufacturing the same. The enteric soft capsules described herein have enhanced enteric and elastic properties and are simpler to manufacture and produce.