Granule Core Coating for Rapid Drug Dissolution

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Existing drug compositions, particularly enteric preparations, face challenges in achieving a stable and rapid release of active ingredients due to variations in gastric emptying time and pH levels in the digestive tract, leading to inconsistent blood concentrations and increased manufacturing costs.

Innovation Solution

A granule or fine particle formulation with a core particle coated with an active ingredient-containing A layer and a dusting powder-containing B layer, optionally coated with a release-controlling film, using a pH-dependent polymer, and incorporating a basic inorganic salt, to ensure rapid dissolution and controlled release of proton pump inhibitors like benzimidazole compounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If a large amount of active ingredient is blended with excipients to achieve effective dosage, then the drug efficacy is improved, but the size of the composition becomes larger and dosing becomes difficult

Engineering Contradiction:

Improveamount of active ingredientVSAvoiddosing difficulty

Core Design Contradiction:

Quantity of substanceVSEase of operation

Solution Approach 1:

The composition is divided into multiple granules or particles, each containing a concentrated amount of active ingredient. This segmentation allows the total effective dosage to be distributed across multiple smaller units that are easier to administer, while maintaining high active ingredient concentration in each unit.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The active ingredient is concentrated in specific regions or layers of the granule structure rather than being uniformly distributed. This creates local areas of high concentration that provide effective dosage while keeping the overall granule size manageable for dosing.

Inventive Principle:

Principle #3Local quality

2Speed

If the active ingredient is rapidly dissolved to achieve quick onset of action, then the drug efficacy is improved, but the variation in blood concentration increases due to gastric emptying time variations

Engineering Contradiction:

Improvedissolution rateVSAvoidblood concentration stability

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The composition is divided into multiple granules with controlled release properties. This segmentation creates a more uniform overall release profile by averaging out individual granule variations, reducing blood concentration fluctuations while maintaining rapid dissolution characteristics.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The release characteristics are modified by changing physical or chemical parameters of the granule structure, such as coating properties or matrix composition. This allows control over the dissolution rate to achieve both rapid onset and stable blood concentration levels.

Inventive Principle:

Principle #35Parameter changes

3Duration of action of moving object

If a release-controlling membrane or matrix is used to control the release rate, then the sustained release property is improved, but the manufacturing complexity and cost increase

Engineering Contradiction:

Improvesustained release durationVSAvoidmanufacturing complexity

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

Different regions of the granule structure have different release-controlling properties. This local differentiation allows sustained release functionality to be achieved through simple structural variations rather than complex manufacturing processes, reducing overall system complexity.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The granules are formed using composite materials that inherently provide controlled release properties through their composition rather than requiring additional release-controlling membranes. This approach achieves sustained release with simpler manufacturing by integrating the release control function into the material itself.

Inventive Principle:

Principle #40Composite materials

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 allows for a high concentration of active ingredients to be administered in a dosable size, improving compliance and reducing manufacturing costs by ensuring rapid and stable release, maintaining effective drug efficacy with reduced variation in blood concentration.

Implementation Method 1

using a pH-dependent polymer

Methodology Applied

Scientific EffectpH-dependent dissolution: Phase Change

Implementation Method 2

an active ingredient-containing A layer formed by spraying a solution or suspension containing an active ingredient and a binder, and an active ingredient-containing B layer formed by dispersing a dusting powder containing an active ingredient while spraying a solution containing a binder

Methodology Applied

Scientific EffectAdhesion: Adhesive

Data Source

PatentUS8449911B2Drug composition having active ingredient adhered at high concentration to spherical core

Publication Date: 2013.05.28 TAKEDA PHARMA CO LTD

AI summary

Granule, fine particle or tablet of excellent leaching property, comprising a drug active ingredient in high content realized by forming a layer containing drug active ingredient on core particles through a combination of a method of dispersing and adhering an active ingredient while spraying or adding a binder with a method of spraying or adding a solution or suspension wherein an active ingredient and a binder are contained so as to effect adhesion. Further, there are provided a drug composition containing such a granule, fine particle or tablet and a process for producing the same.