Polmacoxib Pregabalin Double-Layered Tablet Pain Management

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Solution Overview

Problem

Current pain management treatments for acute and chronic pain, particularly those involving inflammation and neuropathy, often require multiple medications and have stability issues due to external factors, leading to suboptimal efficacy and convenience.

Innovation Solution

A pharmaceutical composition combining polmacoxib and pregabalin in a single dosage form, with varying weight ratios and formulations such as tablets or suspensions, including a double-layered or multi-layered structure for sustained and immediate release, using pharmaceutically acceptable excipients and carriers to enhance stability and bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If multiple medications are used for pain management, then treatment coverage is improved, but treatment complexity and patient burden increase

Engineering Contradiction:
Improvetreatment coverageVSAvoidtreatment complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent combines two distinct analgesic mechanisms (COX-2 inhibition by polmacoxib and calcium channel modulation by pregabalin) into a single fixed-dose tablet formulation. This merging approach maintains comprehensive treatment coverage for inflammatory and neuropathic pain components while reducing pill burden and simplifying the treatment regimen for patients

Inventive Principle:
Principle #5Merging (Combining)

2Ease of operation

If medications are combined in a single dosage form, then convenience is improved, but drug stability and interaction control become more difficult

Engineering Contradiction:
ImproveconvenienceVSAvoiddrug stability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The tablet is divided into two distinct layers: an upper immediate-release layer containing polmacoxib and a lower sustained-release layer containing pregabalin. This segmentation physically separates the two drugs within the single dosage form, preventing direct chemical interactions while maintaining convenient single-pill administration. The layer structure also allows independent optimization of stability conditions for each drug component

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs specific excipients and coating materials as intermediaries between the two drug substances. These intermediary materials act as barriers that prevent direct contact between polmacoxib and pregabalin, thereby avoiding potential drug-drug interactions while still allowing both drugs to be delivered through a single formulation

Inventive Principle:
Principle #24Intermediary (Mediator)

3Duration of action of moving object

If sustained-release formulation is used, then duration of action is improved, but manufacturing complexity increases

Engineering Contradiction:
Improveduration of actionVSAvoidmanufacturing complexity
Core Design Contradiction:
Duration of action of moving objectVSEase of manufacture

Solution Approach 1:

The sustained-release mechanism is achieved through segmentation into two functional layers with different release profiles. The lower layer uses sustained-release excipients and a specific matrix structure to extend pregabalin release, while the upper layer provides immediate polmacoxib release. This segmented approach allows each layer to be optimized independently for its release characteristics

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The tablet utilizes composite material structures with different excipients tailored to each drug's release requirements. The sustained-release layer incorporates polymers and matrix materials specifically selected to control pregabalin release kinetics, while the immediate-release layer uses excipients optimized for rapid polmacoxib dissolution. This composite material strategy enables differentiated release profiles within a single manufactured dosage form

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS11602517B2Pharmaceutical composition, comprising polmacoxib and pregabalin, for treatment of pain
Publication Date: 2023.03.14 CRYSTAL GENOMICS INC
  • US11602517B2 patent drawing
  • US11602517B2 patent drawing
  • US11602517B2 patent drawing

AI summary

The present invention relates to a composite agent comprising polmacoxib and pregabalin. The present invention relates to a pharmaceutical composition and a drug or pain reliever, which each comprise the two active ingredients of polmacoxib and pregabalin and, more particularly, to a drug or pain reliever for treatment of moderately severe, acute, chronic, or neuropathic pain attributed to inflammation and various factors, an effect thereof, and a use thereof.