Fixed-Dose DPP-4 Inhibitor and Metformin Combinations

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for Type 2 diabetes often require complex regimens involving multiple oral antidiabetic drugs, which can be difficult for patients to manage, and there is a need for a combination therapy that simplifies medication administration while maintaining effective glycemic control.

Innovation Solution

Development of pharmaceutical compositions in the form of fixed-dose combinations of DPP-4 inhibitors, such as sitagliptin, vildagliptin, or saxagliptin, with metformin hydrochloride, prepared using dry or wet processing methods, resulting in immediate-release tablets that combine these active ingredients in a single dosage form.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If multiple oral antidiabetic drugs are co-prescribed, then glycemic control effectiveness is improved, but treatment regimen complexity increases

Engineering Contradiction:
Improveglycemic control effectivenessVSAvoidtreatment regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines multiple oral antidiabetic drugs (metformin and a second antidiabetic agent) into a single fixed-dose combination tablet. This merging of multiple medications into one dosage form directly reduces treatment regimen complexity while maintaining the therapeutic effectiveness of each component drug for glycemic control.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The single tablet formulation serves multiple functions simultaneously: it delivers metformin for its primary antidiabetic effect, includes a second antidiabetic agent for complementary glycemic control, and provides a simplified administration regimen. This multi-functionality in one dosage form addresses both effectiveness and complexity concerns.

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Reliability

If multiple oral antidiabetic drugs are co-prescribed, then glycemic control effectiveness is improved, but patient compliance deteriorates

Engineering Contradiction:
Improveglycemic control effectivenessVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

By merging multiple antidiabetic medications into a single fixed-dose combination tablet, the invention simplifies the patient's daily medication routine from taking multiple separate pills to taking one tablet, thereby improving compliance while preserving the therapeutic benefits of combination therapy.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If combination therapy is implemented, then treatment efficacy is improved, but regimen complexity increases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidregimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The fixed-dose combination tablet merges multiple antidiabetic agents into one unified dosage form, allowing combination therapy to be administered through a single tablet rather than multiple separate medications, thus maintaining treatment efficacy while reducing regimen complexity.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS8414921B2Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
Publication Date: 2013.04.09 MERCK SHARP & DOHME LLC
  • US8414921B2 patent drawing
  • US8414921B2 patent drawing
  • US8414921B2 patent drawing

AI summary

Disclosed are pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and metformin, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.