ADHD Drug Delivery with Delayed Release Coating

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Solution Overview

Problem

Current treatments for ADHD and other CNS stimulant-responsive conditions face challenges in maintaining effective drug concentrations throughout the day, particularly in morning and afternoon periods, due to rapid release formulations that lead to compliance issues and variable absorption profiles.

Innovation Solution

Development of novel pharmaceutical compositions with a core comprising a CNS stimulant coated with a sustained release layer and a delayed release layer, allowing for a controlled release of the drug over 4 to 12 hours, ensuring therapeutic levels are maintained during active periods without the need for multiple doses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate release formulations are used for ADHD treatment, then the drug is quickly absorbed and reaches therapeutic levels, but compliance becomes problematic due to twice daily administration requirements

Engineering Contradiction:

Improvedrug absorption speedVSAvoidpatient compliance

Core Design Contradiction:

SpeedVSEase of operation

Solution Approach 1:

The patent divides the drug delivery system into multiple functional layers: an immediate release layer for rapid initial absorption, a sustained release layer for extended therapeutic levels, and an enteric coating layer for delayed gastric release. This segmentation allows the single dosage form to provide both quick onset and prolonged effect, eliminating the need for twice-daily administration and improving patient compliance.

Inventive Principle:

Principle #1Segmentation

2Ease of operation

If long-acting formulations are developed to reduce administration frequency, then compliance improves, but the drug must be taken 4-12 hours before the active period begins

Engineering Contradiction:

Improvepatient complianceVSAvoidtime lag before therapeutic effect

Core Design Contradiction:

Ease of operationVSLoss of time

Solution Approach 1:

The enteric coating layer is designed to remain intact during gastric passage and only dissolve in the alkaline environment of the small intestine. This preliminary protective action delays drug release until the formulation reaches the intestine, where it then provides sustained release during the active daytime period. The coating acts in advance to time the release appropriately.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The multi-layer formulation creates a periodic release pattern: the enteric coating prevents release during gastric transit, then the sustained release layer provides extended drug delivery during intestinal passage and subsequent absorption. This periodic action ensures therapeutic levels are maintained during school or work hours without requiring early morning administration.

Inventive Principle:

Principle #19Periodic action

3Ease of operation

If a single delayed release dosage form is used to provide morning therapeutic levels, then compliance improves and administration is convenient, but the drug must remain intact during gastric passage for extended periods

Engineering Contradiction:

Improveonce-daily administration convenienceVSAvoidgastric residence time requirement

Core Design Contradiction:

Ease of operationVSDuration of action of moving object

Solution Approach 1:

The enteric coating serves as an intermediary barrier between the drug formulation and the gastric environment. This coating layer protects the sustained release mechanism during gastric passage by remaining insoluble in acidic conditions, then dissolves in the alkaline environment of the small intestine to allow drug release. This intermediary structure enables the formulation to withstand extended gastric residence without premature release.

Inventive Principle:

Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compositions provide a convenient once-daily administration option, ensuring a therapeutic effect from waking until the active portion of the day, with a controlled release profile that minimizes side effects and improves compliance by maintaining consistent drug levels.

Implementation Method 1

an outer enteric coating layer designed to delay release of the CNS stimulant during passage through the stomach and dissolve in the alkaline environment of the small intestine

Methodology Applied

Scientific EffectpH-dependent dissolution:

Implementation Method 2

a sustained release layer providing controlled release of the CNS stimulant over an extended period

Methodology Applied

Scientific EffectSustained release:

Data Source

PatentUS9603809B2Methods of treatment of attention deficit hyperactivity disorder

Publication Date: 2017.03.28 IRONSHORE PHARMA & DEV

AI summary

Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 5 to 7 hours or longer, followed by an ascending release rate. When administered at night the composition provides early morning improvement in symptoms of ADHD and sustained improvement over a period of at least 12 hours.