Wax-Based Pellet Sustained Release Formulations
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Solution Overview
Problem
Conventional sustained release formulations, such as tablets and capsules, face challenges in delivering high doses or maintaining therapeutic levels for extended periods, especially for drugs with short half-lives or requiring specific release kinetics, due to size constraints and patient compliance issues, particularly in animals and individuals with swallowing difficulties.
Innovation Solution
Development of pharmaceutical compositions in the form of pellets comprising an active ingredient, a wax-like agent, and a spheronizing agent, which provide sustained release without the need for a sustained release barrier coating, allowing for flexible dosing and easier administration, with options for spherical or non-spherical shapes and various coatings for enhanced bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If tablet or capsule dosage forms are used for high-dose sustained release, then therapeutic levels can be maintained for extended periods, but the size becomes too large to swallow
Solution Approach 1:
The patent divides the high-dose sustained release formulation into multiple small spherical pellets instead of using a single large tablet or capsule. Each pellet contains a portion of the active ingredient dispersed in a wax-like matrix, allowing the total therapeutic dose to be delivered in many small units that can be easily administered and swallowed.
2Manufacturing precision
If barrier coatings are applied to achieve sustained release, then release kinetics can be controlled, but manufacturing complexity and cost increase
Solution Approach 1:
The patent removes the barrier coating layer entirely from the sustained release mechanism. Instead of coating the pellets with polymers or waxes to control release, the active ingredient is directly dispersed within a wax-like matrix during pellet formation, achieving sustained release through the matrix structure itself without requiring additional coating steps.
3Duration of action of moving object
If multiple daily dosing is used for short half-life drugs, then therapeutic activity can be maintained, but patient compliance decreases
Solution Approach 1:
The patent creates a sustained release formulation that continuously releases the active ingredient over an extended period (24 hours or longer) through the wax-like matrix erosion mechanism. This continuous release maintains therapeutic blood plasma levels without requiring multiple daily doses, thereby improving patient compliance while keeping the dosage form small and easy to administer.
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 pellet compositions achieve sustained release profiles that maintain therapeutic levels for extended periods, reducing the need for frequent dosing and improving patient compliance, especially for high-dose or short-half-life drugs, while eliminating the complexity and cost associated with barrier coatings.
Implementation Method 1
a wax-like agent, and a spheronizing agent, (b) is in the form of pellets, and (c) provides sustained release of the active ingredient
Implementation Method 2
provides sustained release of the active ingredient without the need for a sustained release barrier coating
Data Source
AI summary
Sustained release spherical or non-spherical pellets comprising (a) an active ingredient (b) a wax-like agent, and (c) a spheronizing agent are provided. Oral dosage forms comprising said pellets and methods for preparing and using such pellets and dosage forms are also provided.