Enteric Coated Psychostimulant for Sustained Release
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Solution Overview
Problem
Current methylphenidate treatments for ADHD and related disorders require frequent administration due to short half-life, leading to poor compliance and potential abuse, with existing sustained release formulations either providing inadequate therapeutic effects or causing patient tolerance.
Innovation Solution
A pharmaceutical composition with an initial immediate release dosage followed by a sustained release of psychostimulant, achieved through an enteric coating comprising (co-)polymers of (meth)acrylic acid and/or (meth)acrylate containing carboxyl groups, which modifies the release pattern to provide a high initial peak followed by a lower secondary peak, optimizing plasma concentrations and treatment duration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If immediate release methylphenidate preparations are used, then rapid onset of therapeutic effect is achieved, but frequent administration is required due to short half-life
Solution Approach 1:
The pharmaceutical composition is segmented into two distinct components: an immediate release dosage form that dissolves rapidly in gastric acid to provide quick onset, and an enteric coated dosage form that resists gastric acid and releases the psychostimulant in the alkaline environment of the intestine to provide prolonged therapeutic effect. This segmentation allows both rapid onset and extended duration to be achieved simultaneously.
Solution Approach 2:
The invention utilizes parameter changes in the gastrointestinal environment, specifically the pH transition from acidic conditions in the stomach to alkaline conditions in the intestine. The enteric coating is designed to remain intact in acidic pH (resisting dissolution) and dissolve in alkaline pH (releasing the psychostimulant), thereby extending the duration of action without compromising the rapid onset provided by the immediate release component.
2Reliability
If frequent administration of methylphenidate is required, then adequate treatment coverage is maintained, but patient compliance deteriorates
Solution Approach 1:
By segmenting the dosage form into immediate release and enteric coated components, the invention achieves both rapid onset and prolonged duration of action within a single daily administration. This eliminates the need for frequent dosing while maintaining adequate treatment coverage throughout the day, thereby improving patient compliance.
Solution Approach 2:
The enteric coated component provides continuous release of the psychostimulant in the intestine, maintaining therapeutic levels throughout the day. This continuous action ensures adequate treatment coverage without requiring multiple administrations, thus improving ease of operation and patient compliance.
3Duration of action of moving object
If enteric coating is applied to sustain release, then treatment duration is extended, but initial peak plasma concentration is reduced
Solution Approach 1:
The invention segments the total psychostimulant dose into two components: one in immediate release form that provides a high initial peak plasma concentration, and another in enteric coated form that extends treatment duration. This segmentation allows both objectives to be achieved simultaneously without compromising either the initial peak or the duration.
Solution Approach 2:
The invention merges two different release mechanisms (immediate release and enteric-coated sustained release) into a single pharmaceutical composition. The immediate release component ensures high initial peak plasma concentration, while the enteric coated component extends treatment duration, achieving both goals through combination.
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 composition achieves a prolonged therapeutic effect with a single daily administration, maintaining high plasma concentrations over a longer period, thereby improving treatment compliance and minimizing potential abuse while maintaining therapeutic efficacy.
Implementation Method 1
an enteric coating comprising (co-)polymers of (meth)acrylic acid and/or (meth)acrylate containing carboxyl groups, which modifies the release pattern
Data Source
AI summary
The present invention is directed to a psychostimulant containing pharmaceutical composition comprising an enteric coating and showing a sustained release of said psychostimulant in vivo. The invention is further directed to the use of said pharmaceutical composition in the treatment of the Attention Deficit Hyperactivity Disorder (ADHD) and comorbidities, narcolepsy, fatigue and/or cognitive decline associated with systemic diseases such as acquired immunodeficiency syndrome or oncological diseases. Additionally, the present invention provides a method for the manufacture of said pharmaceutical composition.