Etoricoxib Dry Granulation Polymorphic Stability

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Solution Overview

Problem

The existing methods for preparing etoricoxib compositions, such as wet granulation, often lead to polymorphic conversion, reducing solubility and stability, whereas dry granulation maintains the original polymorphic form and solubility of etoricoxib.

Innovation Solution

A pharmaceutical composition of crystalline Form I of etoricoxib is prepared using a dry granulation process with solubility-enhancing surfactants like sodium lauryl sulfate and pharmaceutically acceptable excipients, avoiding polymorphic conversion and ensuring stability and solubility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If wet granulation is used to prepare etoricoxib composition, then the composition can be manufactured, but polymorphic conversion occurs reducing solubility and stability

Engineering Contradiction:

Improvemanufacturability of compositionVSAvoidstability and solubility of etoricoxib

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the granulation parameter from wet to dry process, eliminating water as a variable that triggers polymorphic conversion. This parameter change maintains manufacturability through dry granulation while preserving the stability and solubility of etoricoxib by preventing polymorphic conversion.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If dry granulation is used to prepare etoricoxib composition, then polymorphic form and solubility are maintained, but the manufacturing process must be specifically controlled

Engineering Contradiction:

Improvestability and solubility of etoricoxibVSAvoidprocess control requirements

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent extracts water from the granulation process, using dry granulation instead of wet granulation. This removal of water eliminates the trigger for polymorphic conversion, maintaining etoricoxib stability and solubility while simplifying process control by removing the need to manage water content and drying parameters.

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 dry granulation process stabilizes etoricoxib, maintaining its original polymorphic form and solubility, resulting in a stable and effective pharmaceutical composition.

Implementation Method 1

there exists a polymorphic conversion of etoricoxib in the composition, which may lead to decrease in solubility and/or stability of the final composition

Methodology Applied

Scientific EffectPolymorphic conversion: Crystallisation

Implementation Method 2

at least one solubility enhancing agent which is a surfactant selected from the group consisting of anionic surfactants, cationic surfactants, non-ionic surfactants and zwitterionic surfactants

Methodology Applied

Scientific EffectSurfactant action: Surfactant

Data Source

PatentEP2887924B1Pharmaceutical compositions of etoricoxib

Publication Date: 2017.03.29 ZYDUS LIFESCIENCES LTD

AI summary

The present invention discloses a pharmaceutical composition comprising etoricoxib or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients and the process of preparing the composition.