Glimepiride Stability via Premixing Binder

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current glimepiride-containing solid oral pharmaceutical compositions fail to meet stability requirements for drug approval, with high levels of impurities and degradation products posing risks to patients and complicating the approval process.

Innovation Solution

A process involving the production of a premix using glimepiride and a binder/wetting agent, such as povidone, followed by mixing with additional excipients and processing into a final dosage form, enhances the stability of glimepiride compositions by reducing impurities and degradation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If glimepiride is formulated in solid oral pharmaceutical compositions with common carriers and auxiliary substances, then the compositions can be manufactured and administered orally, but the compositions exhibit poor stability and generate high levels of impurities and degradation products

Engineering Contradiction:
ImprovestabilityVSAvoidimpurities and degradation products
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies preliminary action by pre-mixing glimepiride with a binder and wetting agent before incorporating other excipients. This preliminary mixing step ensures uniform distribution and protective coating of glimepiride particles, preventing degradation and impurity formation during subsequent manufacturing and storage processes.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses a binder and wetting agent as intermediary substances that mediate between glimepiride and other excipients. These intermediaries form protective matrices that isolate glimepiride from degrading conditions while maintaining tablet integrity and oral bioavailability.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of manufacture

If glimepiride is mixed with common carriers and auxiliary substances in conventional processes, then the manufacturing process is simple, but the stability of the composition deteriorates

Engineering Contradiction:
Improvemanufacturing process simplicityVSAvoidcomposition stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent segments the manufacturing process into distinct stages: first pre-mixing glimepiride with binder and wetting agent, then incorporating other excipients separately, and finally compressing into tablets. This segmentation allows each component to be optimized for its specific function while maintaining overall process feasibility.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies local quality by providing different functional properties to different components: glimepiride is protected by local coating with binder and wetting agent, while other excipients maintain their conventional roles. This localized functional differentiation improves stability without requiring complete process redesign.

Inventive Principle:
Principle #3Local quality

3Productivity

If conventional mixing processes are used without premixing, then the manufacturing process is faster and simpler, but impurity levels increase and stability decreases

Engineering Contradiction:
Improvemanufacturing speedVSAvoidpurity level
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

The patent performs preliminary mixing of glimepiride with binder and wetting agent before final tablet formation. This pre-action ensures uniform distribution and protective coating, preventing impurity formation during compression and storage while adding minimal time to the overall manufacturing process.

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 process significantly reduces impurities and degradation products, ensuring that glimepiride compositions meet stability standards, as demonstrated by lower impurity levels in stability studies, thereby improving drug approval prospects.

Implementation Method 1

producing a premix from the active ingredient and an excipient which is a binder and/or a wetting agent

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentEP1904033B1Method for producing pharmaceutical compositions containing glimepiride
Publication Date: 2009.09.09 ALFRED E TIEFENBACHER (GMBH & CO KG)

AI summary

The invention relates to a method for producing solid oral pharmaceutical compositions containing glimepiride. The compositions produced according to the inventive method are characterized by a high stability.