Tamsulosin Solid Dosage Using Segmented Polyethylene Oxide

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Solution Overview

Problem

Current pharmaceutical compositions of tamsulosin face challenges in achieving stable drug content uniformity and satisfactory drug release profiles, often requiring expensive excipients and complex manufacturing processes, particularly with high molecular weight polyethylene oxide which can be difficult to handle due to sticky properties.

Innovation Solution

A solid pharmaceutical composition comprising granules with tamsulosin and a hydrogel-forming polymer like polyethylene oxide, combined with an extragranular phase of polyethylene oxide, which allows for improved gelling and drug release without the need for water-soluble hydrophilic bases, enabling a simple and quick manufacturing process.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If high molecular weight polyethylene oxide is used as hydrogel-forming polymer, then sustained drug release is achieved, but manufacturing difficulty increases due to sticky properties

Engineering Contradiction:
Improvesustained drug releaseVSAvoidhandling during pulverization and granulation
Core Design Contradiction:
Duration of action of moving objectVSEase of manufacture

Solution Approach 1:

The polyethylene oxide is divided into two distinct molecular weight fractions: a first fraction (average molecular weight 10,000 to 1,000,000) for granulation and a second fraction (average molecular weight 1,000,000 to 10,000,000) for sustained release. This segmentation allows each fraction to perform its specific function effectively without the handling difficulties of using only high molecular weight polymer.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention changes the molecular weight parameter of polyethylene oxide by using a mixture of different molecular weight fractions rather than a single uniform molecular weight. This parameter change enables the polymer to exhibit both good processability (from lower molecular weight fraction) and sustained release properties (from higher molecular weight fraction).

Inventive Principle:
Principle #35Parameter changes

2Duration of action of moving object

If polyethylene oxide is used as hydrogel-forming polymer, then controlled release is achieved, but tableting properties deteriorate due to stickiness

Engineering Contradiction:
Improvecontrolled releaseVSAvoidtableting properties
Core Design Contradiction:
Duration of action of moving objectVSEase of manufacture

Solution Approach 1:

The polyethylene oxide is segmented into two molecular weight fractions with distinct roles: the first fraction (lower molecular weight) provides good tableting properties and processability, while the second fraction (higher molecular weight) provides controlled release characteristics. This segmentation resolves the contradiction between tableting properties and controlled release.

Inventive Principle:
Principle #1Segmentation

3Duration of action of moving object

If water-soluble hydrophilic bases are used to improve gelling, then drug release is enhanced, but manufacturing complexity and cost increase

Engineering Contradiction:
Improvedrug releaseVSAvoidmanufacturing process complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The invention extracts and eliminates the need for water-soluble hydrophilic bases from the formulation. Instead, it uses a combination of two polyethylene oxide fractions with different molecular weights to achieve both gelling and drug release functions, thereby simplifying the manufacturing process and reducing costs while maintaining effective drug release.

Inventive Principle:
Principle #2Taking out (Extraction)

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 achieves good drug content uniformity and sustained drug release without the use of expensive excipients, with improved gelling properties and reduced manufacturing complexity, ensuring consistent drug delivery over prolonged periods.

Implementation Method 1

hydrogel-forming polymer, namely polyethylene oxide

Methodology Applied
Scientific EffectHydrogel formation: Hydrogel

Data Source

PatentEP2435029B1Pharmaceutical composition comprising tamsulosin
Publication Date: 2016.12.14 KRKA TOVARNA ZDRAVIL D D

AI summary

The present invention relates to a pharmaceutical composition comprising tamsulosin or a pharmaceutically acceptable salt or solvate thereof in a solid dosage form and to a process for preparing such a composition.