Multiparticulate Tapentadol Dosage Form for Rapid, Prolonged Release
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Solution Overview
Problem
Existing oral pharmaceutical formulations of Tapentadol do not adequately address the need for rapid onset of medicinal action while providing controlled release, and are susceptible to dose dumping when exposed to alcohol, leading to safety concerns and fluctuating plasma concentrations.
Innovation Solution
A multiparticulate oral dosage form comprising coated particles with a core containing Tapentadol, coated with a controlled release coating material comprising a lubricant component, particularly magnesium stearate, and a polymer component, such as ethylcellulose, which allows for controlled release and resistance to ethanol-induced dose dumping.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If controlled release formulation is used, then frequency of administration is reduced and plasma concentration fluctuations are minimized, but onset of medicinal action is delayed
Solution Approach 1:
The dosage form is divided into multiple coated particles, each containing a portion of the active ingredient. This segmentation allows different particles to release at different rates, with some providing rapid onset and others providing sustained release, thereby resolving the contradiction between fast onset and prolonged duration.
Solution Approach 2:
Different regions of the dosage form have different release characteristics. The coated particles vary in coating thickness, composition, or structure to create local differences in release rates, enabling simultaneous rapid onset and prolonged action through spatial variation in formulation properties.
2Stability of the object's composition
If controlled release coating material is applied, then plasma concentration fluctuations are reduced, but the formulation becomes susceptible to dose dumping in alcohol exposure
Solution Approach 1:
The controlled release coating is formulated as a composite material combining multiple components (e.g., polymer matrices, pore-forming agents, lubricants, and adhesion promoters) that work synergistically to provide both controlled release and resistance to alcohol-induced dose dumping, resolving the contradiction between concentration stability and alcohol resistance.
Solution Approach 2:
The coating material's physical and chemical parameters (such as polymer molecular weight, crystallinity, pore size, or composition ratios) are specifically adjusted to alter the coating's permeability and integrity, making it resistant to alcohol while maintaining controlled release properties and plasma concentration stability.
3Ease of operation
If multiparticulate dosage form is used, then ease of administration to specific patient populations is improved, but manufacturing complexity increases
Solution Approach 1:
The dosage form is segmented into multiple small coated particles that can be easily administered to pediatric or geriatric patients who have difficulty swallowing tablets. The segmentation is achieved through controlled particle formation techniques during manufacturing, balancing ease of administration with manageable manufacturing complexity.
Solution Approach 2:
The coated particles are formed by nesting the active ingredient within a core material, which is then coated with the controlled release coating. This nested structure allows for controlled release properties while maintaining simple manufacturing steps and appropriate particle sizes for easy administration to vulnerable patient populations.
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 formulation provides bioequivalent controlled release of Tapentadol, allowing for rapid onset of medicinal action and reduced frequency of administration, while maintaining stability and safety by minimizing dose dumping in alcohol exposure.
Implementation Method 1
the release kinetics of the pharmacologically active ingredients is an important factor. It is well known that depending on how a pharmacologically active ingredient is formulated into a dosage form its release pattern can be modified.
Implementation Method 2
Controlled release (e.g. delayed release, prolonged release, sustained release, extended release and the like) may be based upon various concepts such as coating the pharmaceutical dosage form with a controlled release membrane
Implementation Method 3
the controlled release coating material comprises a lubricant component and a polymer component
Data Source
AI summary
The invention relates to an oral pharmaceutical dosage form comprising a plurality of coated particles, wherein said coated particles comprise a core which comprises a Tapentadol component and which is coated with a controlled release coating material, wherein the controlled release coating material comprises a lubricant component and a polymer component, wherein the polymer component comprises one or more cellulose ethers and/or one or more acrylates, and wherein the pharmaceutical dosage form provides controlled release of the Tapentadol component.