Hypertonic Suspension Base for Extended Release Coated Cores
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Solution Overview
Problem
Extended release solid compositions face challenges such as difficulty in swallowing, poor patient compliance, and inaccurate dosing due to their large size and tendency to be divided, especially in pediatric and geriatric patients, and existing liquid compositions struggle with maintaining consistent drug release during storage.
Innovation Solution
The development of extended release suspension compositions with multiple coated cores of metformin or guanfacine in a hypertonic suspension base, which maintains a consistent in-vitro dissolution release profile for at least seven days, preventing significant leaching of the active ingredient and allowing for flexible dosing and improved bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If extended release solid compositions are used, then the duration of action is extended, but the ease of operation deteriorates due to difficulty in swallowing and poor patient compliance
Solution Approach 1:
The patent transitions from solid dosage forms to liquid suspension formulations, utilizing the fluid state to improve ease of administration. The liquid suspension can be easily swallowed by pediatric and geriatric patients who have difficulty swallowing tablets or capsules, while maintaining extended release properties through coated cores suspended in the liquid medium.
Solution Approach 2:
The patent changes the physical state parameter from solid to liquid suspension, transforming the dosage form to improve patient compliance. The extended release mechanism is preserved through the use of coated cores that control drug release kinetics, while the liquid form eliminates swallowing difficulties.
2Ease of operation
If extended release liquid compositions are formulated, then the ease of operation improves, but the stability deteriorates due to leaching of active ingredient during storage
Solution Approach 1:
The patent introduces coated cores as an intermediary structure between the active ingredient and the liquid suspension medium. The coating layers act as a barrier that prevents direct contact and leaching of the active ingredient into the suspension base during storage, while allowing controlled release when the composition reaches the gastrointestinal tract.
Solution Approach 2:
The patent employs thin film coating layers on the cores that provide a protective barrier. These flexible coating films maintain their integrity during storage in the liquid suspension, preventing leaching, and are designed to dissolve or become permeable under gastrointestinal conditions to enable drug release.
3Duration of action of moving object
If high doses of active ingredient are used, then the duration of action is extended, but the volume increases leading to difficulty in swallowing
Solution Approach 1:
The patent divides the total dose into multiple coated cores, each containing a portion of the active ingredient. This segmentation allows high doses to be delivered through multiple small particles rather than a single large composition, maintaining ease of swallowing while achieving the required total dose and extended duration of 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 hypertonic suspension base ensures stable and consistent release of the active ingredient, enhancing patient compliance and bioavailability, while allowing for flexible dosing and reduced frequency, particularly beneficial for pediatric and geriatric patients, with minimal fluctuations in plasma concentration.
Implementation Method 1
the suspension base generates a hypertonic condition such that there is no substantial change in the in-vitro dissolution release profile of the extended release suspension compositions upon storage
Data Source
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AI summary
The present invention relates to extended release suspension compositions of an active ingredient. Said extended release suspension compositions comprise multiple coated cores of the active ingredient and a suspension base, wherein the suspension base generates a hypertonic condition such that there is no substantial change in the in-vitro dissolution release profile of the extended release suspension compositions upon storage for at least seven days. The invention also relates to processes for the preparation of said extended release suspension compositions.