Segmented Metformin Sitagliptin Tablet Coating

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Existing tablet formulations of metformin and sitagliptin face challenges such as incompatibility and stability issues due to interactions between the active agents, leading to undesirable dissolution profiles and patient compliance problems.

Innovation Solution

A tablet formulation comprising a core tablet with metformin and microcrystalline cellulose, along with at least one matrix agent, coated with a solution containing sitagliptin, antioxidants, and coating agents, and further coated with a film coating to enhance stability and dissolution.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If metformin and sitagliptin are combined in a single tablet formulation, then therapeutic efficacy is improved through complementary mechanisms of action, but incompatibility and stability issues arise due to interactions between the active agents

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidformulation stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The tablet is divided into two distinct compartments: a core tablet containing metformin extended-release formulation and a coating layer containing sitagliptin immediate-release formulation. This segmentation physically separates the two active agents, preventing direct interactions while maintaining their complementary therapeutic effects. The core tablet provides sustained metformin release, while the coating provides rapid sitagliptin release, achieving both stability and efficacy.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

A coating layer acts as an intermediary barrier between metformin and sitagliptin. This coating contains sitagliptin in an immediate-release formulation and serves as a physical separator that prevents direct contact and potential incompatibility reactions between the two active agents, while still allowing both drugs to be delivered from the same tablet.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If extended-release formulation is used for metformin, then patient compliance is improved by reducing administration frequency, but dissolution profile control becomes more challenging

Engineering Contradiction:

Improvepatient complianceVSAvoiddissolution profile control

Core Design Contradiction:

Ease of operationVSManufacturing precision

Solution Approach 1:

The core tablet uses a composite formulation combining metformin with multiple excipients including hydroxypropyl methylcellulose (HPMC) as a matrix former, microcrystalline cellulose for disintegration, and other additives. This composite material system provides controlled extended-release of metformin over time, maintaining stable plasma concentrations and improving compliance while achieving reliable dissolution profiles through the synergistic interaction of formulation components.

Inventive Principle:

Principle #40Composite materials

3Speed

If sitagliptin is formulated with immediate-release characteristics, then rapid onset of action is achieved, but compatibility issues arise when combined with metformin in the same tablet

Engineering Contradiction:

Improveonset of actionVSAvoidcompatibility

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

Sitagliptin is segregated into a separate coating layer that provides immediate-release characteristics, while metformin remains in the core tablet with extended-release properties. This segmentation allows sitagliptin to act rapidly upon tablet ingestion without direct interaction with metformin, maintaining both the speed of onset and chemical compatibility.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The coating layer serves as an intermediary vehicle that delivers sitagliptin immediately upon contact with gastrointestinal fluids, while the coating structure itself prevents direct interaction between sitagliptin and metformin, resolving the compatibility issue while preserving the rapid onset of action.

Inventive Principle:

Principle #24Intermediary (Mediator)

4Stability of the object's composition

If a coating layer is applied to the core tablet, then stability and dissolution profile are improved, but device complexity increases

Engineering Contradiction:

Improveformulation stabilityVSAvoidtablet structure

Core Design Contradiction:

Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The coating layer performs multiple functions simultaneously: it serves as a protective barrier improving formulation stability, acts as a delivery vehicle for sitagliptin providing immediate-release action, and functions as a physical separator preventing incompatibility between metformin and sitagliptin. This multi-functionality justifies the increased structural complexity by delivering multiple benefits from a single design element.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentEP4566593A1A tablet comprising an extended-release formulation for metformin and immediate release formulation comprising sitagliptin

Publication Date: 2025.06.11 SANOVEL ILAC SANAYI & TICARET ANONIM SIRKETI

AI summary

The present invention relates to a tablet formulation comprising a core tablet having metformin and microcrystalline cellulose, at least one matrix agent and a coating solution having sitagliptin surrounding the core tablet and a film coating wherein the coating solution further comprises at least one antioxidant and at least one coating agent. Further, the present invention provides a method for the preparation of said composition.