Extended Release Suspension Cores Preventing Leaching
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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 large size and tendency to be divided, while existing liquid compositions struggle with maintaining stable release profiles and preventing leaching of active ingredients during storage.
Innovation Solution
A stable extended release suspension composition is developed using a suspension base with specific viscosity and osmolality ranges, incorporating multiple coated cores of active ingredients, which prevents leaching and ensures consistent in-vitro dissolution profiles for at least seven days, 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 active ingredient release is controlled, but difficulty in swallowing and poor patient compliance occur
Solution Approach 1:
The patent applies by transitioning from solid dosage forms to liquid suspension formulations. The liquid suspension allows the active ingredient to be dispersed in a liquid medium, making it easier to administer to patients who have difficulty swallowing tablets or capsules, thereby improving patient compliance while maintaining controlled release characteristics
Solution Approach 2:
The patent changes the physical state parameter of the dosage form from solid to liquid. By formulating the active ingredient as a liquid suspension rather than a solid tablet or capsule, the formulation becomes easier to swallow and administer, addressing the patient compliance issue while the controlled release properties are maintained through appropriate formulation design
2Quantity of substance
If high doses of active ingredient are used in extended release solid compositions, then the therapeutic effect is enhanced, but the composition size increases and aggravates swallowing difficulty
Solution Approach 1:
The patent uses liquid suspension formulation to accommodate high doses of active ingredient. The liquid medium allows for better distribution and dispersion of the active ingredient, enabling high doses to be delivered in a smaller, more manageable volume compared to solid formulations, thereby reducing swallowing difficulty
3Ease of operation
If extended release solid compositions are divided into small pieces, then administration is facilitated, but inaccurate dosing and dose dumping occur
Solution Approach 1:
The patent employs liquid suspension formulation which can be easily divided or measured in flexible portions without compromising the integrity of the controlled release mechanism. Unlike solid tablets that may cause dose dumping when broken, the liquid suspension maintains dosing accuracy when divided, allowing flexible administration while preventing dose dumping
4Reliability
If multiple coating systems are applied to prevent leaching, then the active ingredient release is controlled, but the process becomes time-consuming and complicated
Solution Approach 1:
The patent uses liquid suspension formulation which inherently prevents leaching of active ingredient through the suspension matrix design rather than requiring multiple complex coating layers. The liquid medium allows for controlled release while simplifying the manufacturing process by eliminating or reducing the need for multiple coating operations
5Speed
If aqueous phase saturated with active ingredient is used, then immediate dose is provided, but physical instability occurs due to temperature, pH, and ionic concentration variations
Solution Approach 1:
The patent adjusts the composition parameters of the suspension base, specifically the osmolality, to prevent precipitation and maintain physical stability. By optimizing the osmolality of the suspension base, the formulation remains stable across variations in temperature, pH, and ionic concentration while still providing the desired release profile of the active ingredient
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 solution provides enhanced patient compliance, stable and reproducible bioavailability, and consistent plasma concentration with reduced dosing frequency, while accommodating active ingredients with low solubility and varying release profiles, including those requiring immediate or prolonged release.
Implementation Method 1
The suspension base has an osmolality of at least about 1 osmol/kg
Implementation Method 2
a viscosity in a range of about 500 cps to about 15,000 cps
Data Source
AI summary
The present invention relates to a method for preparing a stable extended release suspension composition comprising multiple coated cores of an active ingredient by using a suspension base, wherein the suspension base ensures substantially similar in-vitro dissolution release profile of the active ingredient upon storage of the suspension compositions for at least seven days.