Ibuprofen Codeine Tablet Coating for Stability

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Solution Overview

Problem

Pharmaceutical formulations containing ibuprofen and codeine face challenges with stability during storage, deformation during compression due to low fusion point, and adherence issues with punches, leading to deformed tablets and instability.

Innovation Solution

A single-phase formulation using ibuprofen and codeine with sodium stearyl fumarate as a lubricant, along with a diluent and disintegrant, which simplifies the production process, enhances stability, and prevents adherence, maintaining the physical and pharmacological properties of the formulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If ibuprofen is compressed during tablet manufacturing, then tablets are produced, but ibuprofen melts and sticks to punches due to low fusion point (70°C), causing deformed tablets

Engineering Contradiction:
Improvetablet production rateVSAvoidtablet appearance quality
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

A coating composition comprising a film-forming polymer, plasticizing agent, and opacifying agent is applied as an intermediary layer between the ibuprofen-containing tablet core and the external environment. This coating prevents direct exposure to heat and moisture during compression, eliminating the melting and sticking problems while maintaining production efficiency and tablet appearance quality

Inventive Principle:
Principle #24Intermediary (Mediator)

2Duration of action of stationary object

If tablets are stored for extended periods, then distribution and usage are enabled, but tablets discolour and disintegrate, losing stability

Engineering Contradiction:
Improvestorage durationVSAvoidtablet colour and structural stability
Core Design Contradiction:
Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

The coating composition creates a protective barrier that isolates the ibuprofen and codeine from environmental factors such as oxygen, moisture, and light during storage. This inert environment prevents oxidation, hydrolysis, and photodegradation, maintaining tablet colour and structural integrity over extended storage periods while enabling long-term distribution and usage

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

3Reliability

If ibuprofen and codeine are combined for enhanced analgesic effect, then therapeutic efficacy is improved, but formulation stability and compatibility become more complex

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines ibuprofen and codeine in a single-phase tablet formulation with a unified coating system, merging multiple functions (analgesic, anti-inflammatory, and stability protection) into one integrated dosage form. This approach maintains enhanced therapeutic efficacy while simplifying the formulation structure and manufacturing process compared to separate formulations or complex multi-layer systems

Inventive Principle:
Principle #5Merging (Combining)

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 achieves improved stability, faster dissolution, and better compaction, maintaining therapeutic efficacy while avoiding the use of incompatible excipients, ensuring safer and more potent drug delivery.

Implementation Method 1

sodium stearyl fumarate as a lubricant, along with a diluent and disintegrant, which simplifies the production process, enhances stability, and prevents adherence

Methodology Applied
Scientific EffectLubrication: Lubrication

Implementation Method 2

better compaction, maintaining therapeutic efficacy while avoiding the use of incompatible excipients

Methodology Applied
Scientific EffectCompression: Compression

Implementation Method 3

along with a diluent and disintegrant, which simplifies the production process, enhances stability, and prevents adherence

Methodology Applied
Scientific EffectDisintegration:

Data Source

PatentEP2554164B1Pharmaceutical formulation based on ibuprofen and codeine having having improved stability
Publication Date: 2020.04.15 FARMASIERRA MFG
  • EP2554164B1 patent drawingFigure 1~2
  • EP2554164B1 patent drawingFigure 3
  • EP2554164B1 patent drawingFigure 4

AI summary

Pharmaceutical formulation based on ibuprofen and codeine having improved stability. The invention consists of a novel pharmaceutical formulation having the form of tablets or similar comprising a core composed of an association of ibuprofen and codeine as active ingredients, together with an excipient including at least a diluent, a disintegrating agent, a fluidizing agent and a lubricant which is sodium stearyl fumarate. Said core is coated with a composition based on one or several polymers of diverse modified cellulose ethers and polymers derived from acrylic and methacrylic acids, a plasticiser and, an opacifier or colouring agent and any of the mixtures thereof. These characteristics render the tablets of the invention more efficacious and safe having the form of more stable preparations, without this fact implying greater technological complexity.