Mirabegron Extended-Release Composition Using Hydrophobic Excipients
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Solution Overview
Problem
Existing Mirabegron formulations, such as those using the Oral Controlled Absorption System (OCAS), do not effectively utilize specific non-polymeric hydrophobic excipients to achieve an optimal extended release profile for treating overactive bladder symptoms, lacking clarity on how these excipients interact with Mirabegron.
Innovation Solution
The formulation employs non-polymeric hydrophobic excipients like glyceryl behenate, carnauba wax, cetyl alcohol, hydrogenated vegetable oil, and stearic acid to control the release of Mirabegron, providing a stable and similar in vitro release profile to commercial products without relying on OCAS systems.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If non-polymeric hydrophobic excipients are used in Mirabegron formulation, then extended release profile is achieved, but clarity on excipient-drug interaction is lacking
Solution Approach 1:
The patent uses non-polymeric hydrophobic excipients as intermediary substances to control drug release. Specifically, excipients like glyceryl behenate, carnauba wax, cetyl alcohol, hydrogenated vegetable oil, and stearic acid act as mediators between the drug and the release environment, providing a controlled release profile while maintaining stability. The patent identifies glyceryl behenate as the most effective excipient among these intermediaries.
2Duration of action of moving object
If OCAS system is used for Mirabegron extended release, then controlled absorption is achieved, but formulation complexity increases
Solution Approach 1:
The patent extracts and eliminates the OCAS (Oral Controlled Absorption System) polymeric matrix from the formulation, replacing it with simpler non-polymeric hydrophobic excipients. This extraction of the complex polymeric system while retaining the controlled release functionality simplifies the formulation. The patent specifically removes the need for complex polymeric matrices like those in OCAS tablets, using instead straightforward hydrophobic excipients that achieve similar release profiles with fewer components.
Solution Approach 2:
The patent changes the fundamental parameter of the release-controlling substance from polymeric (OCAS) to non-polymeric hydrophobic excipients. This parameter change transforms the formulation from a complex polymeric matrix system to a simpler hydrophobic excipient-based system, maintaining controlled release functionality while reducing formulation complexity. The shift from polymeric to non-polymeric materials represents a fundamental parameter change in the release mechanism.
3Duration of action of moving object
If multiple polymeric excipients are used in extended release tablet, then release control is achieved, but manufacturing stability decreases
Solution Approach 1:
The patent extracts multiple polymeric excipients from the formulation and replaces them with a single or limited number of non-polymeric hydrophobic excipients. This extraction of multiple polymeric components (such as polyethylene oxide, polyethylene glycol, hydroxypropyl cellulose, hypromellose) simplifies the formulation and improves manufacturing stability by reducing the number of variables and potential incompatibilities among multiple polymers.
Solution Approach 2:
The patent uses composite materials approach by combining Mirabegron with non-polymeric hydrophobic excipients to create a stable extended release formulation. The composite of drug and hydrophobic excipient provides both release control and manufacturing stability, eliminating the need for complex polymeric composites. The hydrophobic excipients form a stable composite matrix that controls release without the stability issues associated with multiple polymeric excipients.
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 extended release composition ensures patient compliance by maintaining consistent drug release, addressing symptoms of overactive bladder like urge urinary incontinence and urinary frequency, with a dissolution profile comparable to existing products.
Implementation Method 1
non-polymeric hydrophobic excipients like glyceryl behenate, carnauba wax, cetyl alcohol, hydrogenated vegetable oil, and stearic acid to control the release of Mirabegron
Data Source
AI summary
The present invention relates to extended release composition of Mirabegron and process of manufacture thereof. The extended release composition of mirabegron comprising non-polymeric hydrophobic excipient as release controlling agent along with one or more pharmaceutically acceptable excipient is used in the treatment of symptoms associated with overactive bladder.