Bi-layer Tablet for Diabetes Co-therapy via Segmentation

Solution Overview

Problem

Current treatments for glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X are inadequate in effectively managing elevated glucose levels and preventing the progression of these conditions.

Innovation Solution

A pharmaceutical composition comprising an extended release layer of metformin hydrochloride with a controlled release excipient mixture of carbomers and an immediate release layer of a crystalline hemihydrate form of a compound inhibiting sodium-dependent glucose transporter SGLT2, formulated as a bi-layer tablet for sustained and rapid glucose control.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a single-release formulation is used, then the device complexity is reduced, but the glucose control effectiveness deteriorates due to inability to provide both immediate and sustained release

Engineering Contradiction:

Improveglucose control effectivenessVSAvoidtablet structure complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The tablet is divided into two distinct layers: an immediate release layer containing SGLT2 inhibitor and an extended release layer containing metformin. This segmentation allows each layer to perform its specific function independently, providing both rapid glucose control and sustained glucose management without requiring complex release mechanisms in a single layer.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention transitions from a single-layer to a multi-layer (bi-layer) tablet structure, adding the dimension of layering to the dosage form. This dimensional change enables simultaneous inclusion of both immediate and extended release functionalities within a single oral dosage unit, resolving the contradiction between simplicity and effectiveness.

Inventive Principle:

Principle #17Another dimension (Dimensionality change)

2Duration of action of moving object

If extended release formulation is used, then the duration of action is improved, but the immediate glucose control effectiveness deteriorates

Engineering Contradiction:

Improveduration of glucose controlVSAvoidonset of glucose control

Core Design Contradiction:

Duration of action of moving objectVSSpeed

Solution Approach 1:

The tablet is divided into two distinct layers: an immediate release layer containing SGLT2 inhibitor and an extended release layer containing metformin. This segmentation allows each layer to perform its specific function independently, providing both rapid glucose control and sustained glucose management without requiring complex release mechanisms in a single layer.

Inventive Principle:

Principle #1Segmentation

3Speed

If immediate release formulation is used, then the onset of action is improved, but the duration of action deteriorates

Engineering Contradiction:

Improveonset of glucose controlVSAvoidduration of glucose control

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The tablet is divided into two distinct layers: an immediate release layer containing SGLT2 inhibitor and an extended release layer containing metformin. This segmentation allows each layer to perform its specific function independently, providing both rapid glucose control and sustained glucose management without requiring complex release mechanisms in a single layer.

Inventive Principle:

Principle #1Segmentation

4Reliability

If multiple separate medications are used, then the therapeutic effectiveness is improved, but the ease of operation deteriorates due to multiple dosing

Engineering Contradiction:

Improveco-therapy effectivenessVSAvoiddosing convenience

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The invention merges two separate medications (SGLT2 inhibitor and metformin) into a single bi-layer tablet dosage form. This combination allows patients to receive both immediate and extended release therapies in one pill, eliminating the need for multiple separate dosing events and improving compliance while maintaining the therapeutic effectiveness of co-therapy.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The single tablet dosage form serves multiple functions: it provides both immediate and extended release glucose control, combines two different mechanisms of action (SGLT2 inhibition and metformin), and simplifies the dosing regimen. This multi-functionality resolves the contradiction between maintaining co-therapy effectiveness and improving ease of operation.

Inventive Principle:

Principle #6Universality (Multi-functionality)

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 provides effective glucose regulation, delaying the progression of Type 2 diabetes mellitus and Syndrome X by maintaining near-normal blood glucose levels and improving insulin sensitivity, thereby preventing complications associated with these disorders.

Implementation Method 1

an extended release layer comprising metformin hydrochloride and a controlled release excipient comprising a mixture of two carbomers

Methodology Applied

Scientific EffectControlled release:

Implementation Method 2

an immediate release layer comprising a crystalline hemihydrate form of a compound of formula (I-X) or pharmaceutically acceptable salt thereof

Methodology Applied

Scientific EffectSGLT2 inhibition:

Data Source

PatentEP2590631B1Formulation for co-therapy treatment of diabetes

Publication Date: 2016.10.26 JANSSEN PHARMA NV

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AI summary

The present invention is directed a pharmaceutical compositions for co- therapy treatment and prevention of glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X.