Ropinirole Matrix Tablet Dissolution Control

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Solution Overview

Problem

Existing pharmaceutical compositions of ropinirole for sustained-release formulations are complex and time-consuming to produce, requiring specialized equipment and multiple layers that complicate the dissolution rate control.

Innovation Solution

A simple pharmaceutical composition in the form of a matrix tablet that can be manufactured through direct compression or granulation, using a hydrophilic matrix former like hydroxypropylmethyl cellulose and release rate modifiers like carbomer, without separate layers, allowing for prolonged release of ropinirole suitable for once-a-day application.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If multi-layer tablet structures are used to control dissolution rate, then the dissolution control is improved, but the manufacturing complexity increases significantly

Engineering Contradiction:
Improvedissolution rate controlVSAvoidmanufacturing process complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent combines multiple functions (dissolution control, drug release, structural integrity) into a single-layer matrix tablet containing ropinirole hydrochloride and hydrophilic polymeric substances, eliminating the need for multiple separate layers while maintaining controlled release capabilities

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The hydrophilic polymeric matrix serves multiple functions simultaneously: it acts as the tablet structure, controls dissolution rate, regulates drug release kinetics, and provides mechanical strength, replacing what would traditionally require separate layers

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

2Reliability

If specialized equipment like rotary double layer press is used, then the controlled release performance is improved, but the production time and cost increase

Engineering Contradiction:
Improvecontrolled release performanceVSAvoidproduction efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines controlled release functionality with a standard single-layer tablet structure, allowing production using conventional tablet press equipment rather than specialized rotary double layer presses, thereby improving production efficiency

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent achieves controlled release by changing the chemical composition parameters of the matrix (using hydrophilic polymeric substances with specific properties) rather than changing the physical structure to multiple layers, enabling use of standard equipment

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If multiple pharmaceutical excipients are used in multi-layer tablets, then the dissolution rate control is improved, but the number of processing steps increases

Engineering Contradiction:
Improvedissolution rate controlVSAvoidprocessing time
Core Design Contradiction:
Manufacturing precisionVSLoss of time

Solution Approach 1:

The patent merges all necessary excipients and functional components into a single homogeneous matrix layer, eliminating the need for separate processing of multiple layers and reducing the number of processing steps while maintaining dissolution control

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent performs preliminary mixing of ropinirole hydrochloride with hydrophilic polymeric substances and other excipients to form a homogeneous blend before compression, ensuring proper dissolution control without requiring subsequent layering operations

Inventive Principle:
Principle #10Preliminary action

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 matrix tablet composition simplifies the manufacturing process, eliminates the need for specialized equipment, and achieves a controlled release of ropinirole, ensuring prolonged drug release with improved production efficiency and patient convenience.

Implementation Method 1

a hydrophilic matrix former, in particular hydroxypropylmethyl cellulose

Methodology Applied
Scientific EffectHydrophilic swelling: Absorption (physical)

Implementation Method 2

hydrophilic matrix former

Methodology Applied
Scientific EffectGel formation: Gel

Implementation Method 3

at least one release rate modifier, in particular carbomer

Methodology Applied
Scientific EffectPolymer chain interaction:

Data Source

PatentEP2323634B1Ropinirole composition
Publication Date: 2017.11.15 KRKA TOVARNA ZDRAVIL D D
  • EP2323634B1 patent drawing

AI summary

The present invention relates to novel pharmaceutical composition comprising ropinirole or its salt, hydrophilic matrix former, hydrophilic release rate modifier and optionally other excipients.