Methylphenidate Controlled Release Carrier System

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Solution Overview

Problem

Current oral pharmaceutical dosage forms, particularly controlled release formulations of methylphenidate, face challenges in maintaining a steady drug delivery over eight hours due to mechanical and chemical stresses in the gastrointestinal tract, and are susceptible to abuse through crushing, inhalation, or injection.

Innovation Solution

Development of a controlled release oral dosage form with a carrier system that provides an initial increasing rate of methylphenidate release for rapid onset and a subsequent non-ascending phase for sustained release, incorporating a high viscosity liquid carrier material and network former, which is abuse-resistant and resistant to extraction by solvents, ensuring a single Tmax of 5.5 to 7.5 hours and prolonged therapeutic effect.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If a tablet is formulated with a coating or slow disintegration to achieve sustained release, then the duration of action is improved, but the reliability of controlled release deteriorates due to mechanical and chemical stresses in the gastrointestinal tract causing tablet breakdown

Engineering Contradiction:
Improveduration of drug releaseVSAvoidcontrolled release stability
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent employs a composite matrix system combining hydrophilic polymers (such as hydroxypropyl methylcellulose, carbopol, or sodium carboxymethylcellulose) with methylphenidate. This composite structure creates a gel-forming matrix that maintains structural integrity under gastrointestinal stresses while enabling controlled drug diffusion. The hydrophilic polymer network provides mechanical strength to prevent tablet disintegration, yet allows sustained drug release through gel layer formation and diffusion mechanisms.

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If an oral dosage form is designed for controlled release over eight hours, then the duration of action is improved, but the object-generated harmful factors worsen due to increased susceptibility to abuse through extraction, grinding, and injection

Engineering Contradiction:
Improveduration of drug releaseVSAvoidabuse potential
Core Design Contradiction:
Duration of action of moving objectVSObject-generated harmful factors

Solution Approach 1:

The patent fundamentally changes the physical state parameter of the drug carrier system by using a high viscosity liquid or gel matrix instead of traditional solid tablet formulations. This parameter change makes the formulation resistant to common abuse methods: the gel structure prevents easy grinding into powder for inhalation, the high viscosity resists solvent extraction, and the formulation maintains its integrity under mechanical stress. The abuse-deterrent properties are inherently built into the physical characteristics of the gel system rather than added as separate features.

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If a coating is applied to delay drug release, then the controlled release properties are improved, but the device complexity increases due to additional manufacturing steps and coating materials

Engineering Contradiction:
Improvecontrolled release profileVSAvoidformulation complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent merges the drug delivery function and the structural matrix function into a single integrated gel system. Rather than using separate components (tablet core plus coating layer), the invention combines methylphenidate with hydrophilic polymers to form a unified gel matrix that simultaneously provides structural integrity and controlled release functionality. This consolidation eliminates the need for separate coating operations and reduces manufacturing complexity while maintaining precise control over drug release kinetics through the gel's physical properties.

Inventive Principle:
Principle #5Merging (Combining)

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 dosage form achieves enhanced delivery kinetics and safety features, providing a prolonged therapeutic effect with reduced risk of abuse by maintaining a stable drug release profile and resisting common forms of misuse, such as crushing and solvent extraction.

Implementation Method 1

a controlled release carrier system that provides an initial increasing rate of release of methylphenidate

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 2

incorporating a high viscosity liquid carrier material and network former

Methodology Applied
Scientific EffectGel formation: Gel

Implementation Method 3

resistant to extraction by solvents

Methodology Applied
Scientific EffectGel structure resistance: Gel

Data Source

PatentUS10328068B2Oral pharmaceutical dosage forms
Publication Date: 2019.06.25 ORIENT PHARMA
  • US10328068B2 patent drawing
  • US10328068B2 patent drawing
  • US10328068B2 patent drawing

AI summary

Controlled release oral dosage forms suitable for administration of methylphenidate are provided. Abuse-resistant controlled release oral dosage forms suitable for administration of methylphenidate are also provided. Methods of treating ADD and ADHD using the oral dosage forms are also provided.