Multi-Active Oral Formulation With Immediate and Sustained Release

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Solution Overview

Problem

Existing pharmaceutical compositions fail to provide sustained therapeutic effects for expectorants, analgesics, and antitussives for at least twelve hours due to challenges in formulation, particularly with low-solubility analgesics like naproxen, leading to the need for frequent re-dosing.

Innovation Solution

A pharmaceutical composition comprising guaifenesin, naproxen, and dextromethorphan with specific ratios and a combination of immediate and sustained release portions, utilizing polymers and excipients to maintain therapeutic effects for up to 12 hours.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If conventional immediate release products are used, then rapid therapeutic effect is achieved, but frequent re-dosing is required every 4 to 6 hours

Engineering Contradiction:

Improveonset of therapeutic effectVSAvoidduration of therapeutic effect

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The patent divides the dosage form into multiple functional segments: immediate release portion for rapid onset and sustained release portion for extended duration. This segmentation allows different parts of the formulation to address different temporal requirements of therapeutic effect.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent combines immediate release and sustained release portions into a single unified dosage form. This merging integrates the advantages of both rapid onset and extended duration into one product, eliminating the need for separate dosing events.

Inventive Principle:

Principle #5Merging (Combining)

2Adaptability or versatility

If low solubility analgesics like naproxen are included in combination products, then multi-symptom relief is achieved, but dissolution and release control become difficult

Engineering Contradiction:

Improvemulti-symptom relief capabilityVSAvoiddissolution and release control

Core Design Contradiction:

Adaptability or versatilityVSEase of manufacture

Solution Approach 1:

The patent applies different release characteristics to different components within the same dosage form. The immediate release portion handles rapidly dissolving components, while the sustained release portion manages low solubility analgesics like naproxen, allowing each component to be optimized for its specific properties.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent uses excipients and formulation additives as intermediaries to facilitate the dissolution and release of low solubility analgesics. These intermediary substances help bridge the gap between the analgesic's low solubility and the requirement for effective dissolution in the gastrointestinal tract.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Duration of action of moving object

If sustained release polymers are used to extend duration of action, then therapeutic effect is maintained for up to 12 hours, but formulation complexity increases

Engineering Contradiction:

Improveduration of therapeutic effectVSAvoidformulation complexity

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The sustained release polymers serve multiple functions simultaneously: they provide extended duration of action, control release rates, and work synergistically with excipients to optimize dissolution. This multi-functionality reduces the need for additional separate mechanisms, thereby limiting the increase in overall formulation complexity.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS20250319050A1Pharmaceutical formulation

Publication Date: 2025.10.16 RB HEALTH US LLC

AI summary

A formulation for oral administration comprises an expectorant, an analgesic, and at least one additional active ingredient having a modified release providing a therapeutic effect for each of the active ingredients for up to 12 hours.