Diphenhydramine Dosage Form with Controlled Release

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Solution Overview

Problem

Current pharmaceutical dosage forms of diphenhydramine fail to maintain therapeutic plasma concentrations for extended periods, as they often provide relief for different durations compared to other medications, leading to suboptimal treatment of combined symptoms such as allergic reactions, respiratory issues, and pain.

Innovation Solution

A pharmaceutical dosage form combining diphenhydramine with additional active ingredients like decongestants, antitussives, expectorants, and analgesics, designed to provide plasma concentrations within therapeutic ranges for both components over similar periods, using bi-layered or multi-layered tablets and liquid formulations with controlled release mechanisms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If diphenhydramine is administered alone, then it provides therapeutic effect for 4-6 hours, but it fails to maintain therapeutic plasma concentration for extended periods compared to other drugs

Engineering Contradiction:
Improveduration of therapeutic effectVSAvoidconsistency of therapeutic coverage
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent combines diphenhydramine with one or more additional active ingredients (such as analgesics, antitussives, decongestants, or expectorants) into a single dosage form. This merging of multiple drugs with different duration profiles creates a combination product that maintains therapeutic plasma concentrations for extended periods, resolving the contradiction between diphenhydramine's limited duration and the need for consistent therapeutic coverage.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention employs controlled-release or extended-release mechanisms to dynamically manage the release of diphenhydramine and co-administered drugs. By controlling the release rate and timing, the dosage form maintains therapeutic plasma concentrations over extended periods, transforming the static short-duration effect into a dynamic extended-duration therapeutic profile.

Inventive Principle:
Principle #15Dynamics

2Adaptability or versatility

If multiple separate drugs are administered to treat combined symptoms, then comprehensive symptom relief is achieved, but multiple doses and medications increase treatment complexity

Engineering Contradiction:
Improvecomprehensive symptom coverageVSAvoidnumber of medications and dosing regimens
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent merges multiple active ingredients that treat different symptoms (allergic reactions, respiratory issues, pain, cough, congestion) into a single dosage form. This combination approach provides comprehensive symptom coverage while reducing the number of separate medications and dosing regimens, directly resolving the contradiction between versatility and complexity.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a multi-functional dosage form that simultaneously addresses multiple symptom types through a single administration. The dosage form is designed to provide therapeutic effects for allergic reactions, respiratory conditions, pain, and other symptoms, making a single product universal for treating multiple conditions that would otherwise require separate medications.

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

3Speed

If diphenhydramine is released quickly, then rapid therapeutic effect is achieved, but plasma concentration cannot be maintained over extended periods

Engineering Contradiction:
Improverate of therapeutic onsetVSAvoidduration of plasma concentration maintenance
Core Design Contradiction:
SpeedVSDuration of action of moving object

Solution Approach 1:

The patent employs dynamic release mechanisms including controlled-release, extended-release, and sustained-release formulations. These mechanisms initially release the drug quickly to achieve rapid therapeutic onset, then continue releasing the drug at a controlled rate to maintain plasma concentrations over extended periods, resolving the contradiction between speed of onset and duration of maintenance.

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The invention uses preliminary controlled-release mechanisms that are pre-designed into the dosage form to first provide rapid release for quick therapeutic effect, then transition to sustained release for extended plasma concentration maintenance. This preliminary structuring of release patterns resolves the contradiction between fast onset and long duration.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS9592197B2Dosage form containing diphenhydramine and another drug
Publication Date: 2017.03.14 SOVEREIGN PHARMACEUTICALS LLC

AI summary

A pharmaceutical dosage form which comprises diphenhydramine and/or a pharmaceutically acceptable salt thereof and at least one second drug. The dosage form provides a plasma concentration within the therapeutic range of the at least one second drug over a period which is coextensive with a substantial part of the period over which the dosage form provides a plasma concentration within the therapeutic range of diphenhydramine or salt thereof. This Abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.