Floating Gastro-Retentive DAPTZ Formulations for Stomach Release
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Solution Overview
Problem
Existing formulations of 3,7-diaminophenothiazines (DAPTZ) suffer from absorption limitations in the gut, leading to undesirable side effects and reduced efficacy in treating neurodegenerative diseases, as they are not optimized for rapid release in the stomach and can cause sensitization of the distal gut and antimicrobial effects.
Innovation Solution
Development of gastro-retentive formulations that float in the stomach, allowing rapid release of DAPTZ compounds in an acidic environment, minimizing side effects and optimizing absorption in the upper gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If DAPTZ compounds are administered in conventional formulations, then they can be delivered to the gastrointestinal tract, but they cause sensitization of the distal gut and antimicrobial effects leading to diarrhea
Solution Approach 1:
The patent segments the gastrointestinal tract into two zones: the stomach (upper GI) as the target site for drug release, and the distal gut (lower GI) as the site to avoid. By using gastro-retentive floating formulations, the drug is confined to release only in the stomach, preventing contact with the distal gut and eliminating the harmful sensitization and antimicrobial effects while maintaining deliverability.
Solution Approach 2:
The patent introduces gastro-retentive floating formulations as an intermediary vehicle that mediates between the DAPTZ compound and the gastrointestinal tract. This formulation acts as a controlled release system that releases the drug exclusively in the stomach environment, preventing the compound from reaching the distal gut where it would cause harmful effects.
2Reliability
If DAPTZ compounds are released in the distal gut, then absorption can occur, but efficacy is reduced due to side effects and poor bioavailability
Solution Approach 1:
The patent employs preliminary action by designing formulations that release DAPTZ compounds in the stomach before they reach the distal gut. The gastro-retentive floating formulations ensure that absorption occurs in the stomach environment, optimizing bioavailability and therapeutic efficacy while avoiding the harmful effects associated with distal gut release.
Solution Approach 2:
The patent utilizes parameter changes by exploiting the pH difference between the stomach (acidic environment) and the distal gut. The formulations are designed to release DAPTZ compounds specifically in the acidic stomach environment, where the compounds exhibit optimal solubility and absorption characteristics, thereby maximizing bioavailability and efficacy.
3Productivity
If conventional formulations are used, then dosing frequency can be maintained, but patient compliance deteriorates due to frequent dosing requirements
Solution Approach 1:
The patent applies partial or excessive action by using gastro-retentive floating formulations that provide sustained release of DAPTZ compounds over an extended period in the stomach. This prolonged release mechanism allows for less frequent dosing (e.g., once daily or once weekly), thereby improving patient compliance while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent ensures continuity of useful action through gastro-retentive floating formulations that maintain a sustained concentration of DAPTZ compounds in the stomach over time. This continuous release pattern eliminates the need for frequent dosing, thereby improving patient compliance while ensuring consistent therapeutic action.
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 gastro-retentive formulations enhance bioavailability and reduce side effects by ensuring DAPTZ compounds are absorbed in the stomach, thereby improving therapeutic efficacy and compliance through less frequent dosing.
Implementation Method 1
gastro-retentive formulations that float in the stomach
Implementation Method 2
rapid release of DAPTZ compounds in an acidic environment
Data Source
AI summary
The invention provides different types of floating composition of diaminophenothiazine (DAPTZ) compounds such as methylene blue, which provide rapid-release in the stomach, or are gastro-retained. They further provide methods of making and using the same in the treatment and/or prevention of diseases. In one embodiment the invention provides an oral pharmaceutical composition which is a film-coated solid tablet comprising a DAPTZ compound as active ingredient in a gastro-retentive platform. In another embodiment the invention provides an oral pharmaceutical composition comprising an elongate hollow cylindrical capsule containing a weighting agent which is retained at one end, the capsule being buoyant and self-orientating, wherein the capsule is coated with an inner sustained release layer comprising a DAPTZ compound as active ingredient, and a further protective outer layer.