Ticagrelor Oral Dosage Form with Semi-Permeable Membrane
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Solution Overview
Problem
Current formulations of ticagrelor require patients to take a tablet every 12 hours due to its absorption profile, leading to inconvenience and potential noncompliance in treating or preventing conditions like stroke and heart attack.
Innovation Solution
A controlled-release oral dosage form of ticagrelor with a core and semi-permeable membrane coating, including a first drug layer and a push layer with a swelling agent and osmogen, allowing for once-daily administration by releasing ticagrelor over 24 hours, with optional additional drug layers for enhanced delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If ticagrelor is administered using current formulation design, then the drug can be delivered to patients, but patients must take a tablet every 12 hours which causes inconvenience and potential noncompliance
Solution Approach 1:
The tablet is segmented into two distinct layers: a first drug layer containing ticagrelor and a second push layer containing swelling and osmotic agents. This segmentation enables controlled release kinetics where the drug layer releases medication over 24 hours while the push layer provides mechanical force to maintain release pressure, solving the contradiction between extended duration and patient compliance.
Solution Approach 2:
The invention changes the release parameter from immediate release to controlled sustained release over 24 hours. By modifying the tablet structure to include a semi-permeable membrane and controlled-release matrix, the drug delivery parameter is transformed from frequent dosing to once-daily dosing, thereby improving patient compliance while maintaining therapeutic effect.
2Reliability
If ticagrelor is administered every 12 hours to maintain effective concentration, then therapeutic effect is maintained, but patient convenience is reduced and noncompliance increases
Solution Approach 1:
The controlled-release formulation provides continuous drug release over 24 hours through the semi-permeable membrane and osmotic push mechanism. This continuous action maintains stable plasma concentrations of ticagrelor throughout the day, ensuring reliable therapeutic effect while reducing dosing frequency from twice daily to once daily, thereby minimizing time loss and improving compliance.
3Ease of operation
If a controlled-release formulation is designed to extend drug release to 24 hours, then dosing frequency is reduced, but formulation complexity increases
Solution Approach 1:
The invention employs a semi-permeable membrane with controlled porosity to regulate drug release. The membrane's pore structure allows selective passage of water and dissolved ticagrelor while maintaining structural integrity. This porous material approach achieves 24-hour controlled release with a relatively simple tablet structure, balancing extended dosing interval against formulation complexity.
Solution Approach 2:
The tablet uses composite material structure combining a drug-containing layer with a push layer containing swelling polymers and osmotic agents. This composite design integrates multiple functional materials to achieve controlled release kinetics, enabling once-daily dosing while managing formulation complexity through synergistic material combinations.
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 a sustained release of ticagrelor for up to 24 hours with reduced variation in release rate, improving patient compliance and maintaining effective drug concentration for extended periods.
Implementation Method 1
The semi-permeable membrane is provided with at least one passageway, which is formed through the semi-permeable membrane. The at least one passageway is positionally configured to face the first drug layer, but not to face the push layer, of the core, and is functionally configured to allow the ticagrelor in the first drug layer to release out of the core therethrough
Implementation Method 2
the push layer comprises a swelling agent and an osmogen agent
Data Source
AI summary
An oral dosage form of ticagrelor includes a core and a semi-permeable membrane coating the core. The core comprises a first drug layer and a push layer. The first drug layer contains ticagrelor that is sufficient to deliver an effective amount of the drug over an intended delivery time. The push layer comprises a swelling agent and an osmogen agent. The semi-permeable membrane has at least one passageway formed therethrough, positionally configured to face the first drug layer, but not to face the push layer, of the core, and functionally configured to allow the ticagrelor to realize an extended release out of the core upon contacting an aqueous environment. The dosage form optionally further includes a second ticagrelor-containing drug layer coating the semi-permeable membrane, thereby providing a starting effective dose upon administration. The dosage form can realize once-a-day administration of ticagrelor of patients in need thereof.