Stable Multi-Component Atherosclerosis Drug Composition

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Solution Overview

Problem

Current multi-component pharmaceutical compositions for managing atherosclerosis face challenges such as drug-drug interactions, stability issues, and poor patient compliance due to the complexity of combining multiple active ingredients, leading to altered pharmacokinetic and pharmacodynamic profiles and increased adverse events.

Innovation Solution

A stable solid oral pharmaceutical composition comprising a β-adrenergic receptor blocking agent, a HMG Co-enzyme-A reductase inhibitor, an ACE inhibitor, and a diuretic, with each active ingredient separated and granulated using an alcoholic binder solution, and without organic acids as excipients, to maintain individual pharmacokinetic and pharmacodynamic profiles and minimize side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If multiple active ingredients are combined in a single pharmaceutical composition, then patient compliance and adherence are improved, but drug-drug interactions and stability issues occur

Engineering Contradiction:
Improvepatient complianceVSAvoidstability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent divides the single multi-component composition into multiple separate pharmaceutical compositions, each containing one or more active ingredients. This segmentation prevents drug-drug interactions and stability issues while maintaining patient compliance through coordinated administration of the separate compositions.

Inventive Principle:
Principle #1Segmentation

2Device complexity

If multiple active ingredients are combined in a single pharmaceutical composition, then therapy complexity is reduced, but adverse events and altered pharmacokinetic profiles increase

Engineering Contradiction:
Improvetherapy complexityVSAvoidadverse events
Core Design Contradiction:
Device complexityVSObject-generated harmful factors

Solution Approach 1:

By separating active ingredients into distinct pharmaceutical compositions, the patent eliminates drug-drug interactions that cause adverse events and altered pharmacokinetic profiles, while still simplifying therapy through coordinated administration of the segmented compositions.

Inventive Principle:
Principle #1Segmentation

3Quantity of substance

If active ingredients are combined in a single dosage form, then pill burden is reduced, but drug activity and pharmacokinetic profile are altered

Engineering Contradiction:
Improvepill burdenVSAvoiddrug activity
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent segments the combination therapy into multiple separate dosage forms, each preserving the individual drug activity and pharmacokinetic profile of its active ingredient, while collectively reducing overall pill burden through optimized dosing regimens.

Inventive Principle:
Principle #1Segmentation

4Reliability

If multiple drugs are used to manage atherosclerosis, then therapeutic efficacy is improved, but adherence to dosing schedule decreases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidadherence
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent combines multiple separate pharmaceutical compositions into a coordinated dosing regimen that maintains therapeutic efficacy of all active ingredients while improving adherence through simplified administration schedules and reduced pill burden.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP2395838B1Stable pharmaceutical composition for atherosclerosis
Publication Date: 2018.07.25 CADILA PHARMA LTD
  • EP2395838B1 patent drawingFigure 1
  • EP2395838B1 patent drawingFigure 2
  • EP2395838B1 patent drawingFigure 3

AI summary

The present invention relates to a stable solid oral pharmaceutical multi-component composition comprising combination of blood pressure lowering drugs with lipid lowering agent/s and optionally a platelet aggregation inhibitor in a single dosage form. The blood pressure lowering agents are selected from ß-adrenergic receptor blocking agent, ACE inhibitor and diuretic. The lipid lowering agent is selected from HMG Co-enzyme-A reductase inhibitor. The pharmaceutical composition made as per present invention a) overcomes any drug-drug interactions, b) exhibits pharmacokinetic and pharmacodynamic profile of individual therapeutic agent, c) has minimal side effects. The invention provides multi-component composition (MCC) to increase adherences to therapy. The MCC as per present invention provides compositions that maintain activity of all active ingredients without significant increase in adverse event profile. The present invention further relates to a method of preparing the said pharmaceutical composition.