Multilayered Miniparticles for Dual Oral Release and Lower GI Irritation
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Solution Overview
Problem
Existing pharmaceutical formulations for oral administration face challenges such as large volume, difficulty in swallowing, uneven release profiles, high concentration in specific gastrointestinal locations leading to local irritations, and poor bioavailability, especially for multiple active substances requiring different release times or amounts.
Innovation Solution
Development of multilayered miniparticles with a size range of 200 µm to 850 µm, comprising a core of active substance, an inner protective film layer for modified release, and an outer film layer for faster release, allowing dual release profiles of active substances like thioctic acid, iron salts, vitamin C, or folic acid, spread uniformly throughout the gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If a single dosage unit contains both fast release and slow release formulations of active ingredients, then the requirement for multiple daily intakes is met, but the dosage unit becomes voluminous and difficult to swallow
Solution Approach 1:
The patent divides the dosage unit into multiple mini-particles, each containing a single active ingredient in either fast-release or slow-release form. These mini-particles are then combined in a single capsule, allowing dual release capability while maintaining a compact, swallowable size. This segmentation resolves the contradiction by distributing multiple active ingredients across multiple small units rather than combining them in one large unit.
Solution Approach 2:
The patent employs a nested structure where mini-particles (containing active ingredients) are enclosed within a capsule (outer layer). Each mini-particle itself has a nested structure with a core active ingredient surrounded by a release-modifying membrane. This nesting allows multiple functional components to be contained within a compact overall form, achieving dual release capability without increasing the external volume of the dosage unit.
2Quantity of substance
If high concentration of active ingredients is used in a single dosage unit, then the dosage strength is sufficient, but local irritations in the gastrointestinal tract occur
Solution Approach 1:
The patent segments the total dose of active ingredients into multiple mini-particles dispersed throughout the gastrointestinal tract. Instead of one concentrated dose localized at a single site, the active ingredients are distributed across many small particles that travel through and release at different locations, reducing peak local concentration and minimizing irritation while maintaining sufficient total quantity for therapeutic effect.
3Duration of action of moving object
If multiple excipients are added to achieve fast and slow release in a single tablet, then the release profiles are achieved, but the tablet becomes voluminous and requires division for administration
Solution Approach 1:
The patent assigns different release-modifying membranes to different mini-particles based on their intended release profile (fast or slow). Instead of adding multiple excipients to a single homogeneous tablet, each mini-particle is individually coated with the appropriate membrane type, allowing diverse release profiles while maintaining small, swallowable particle sizes that do not require division for administration.
4Volume of moving object
If the entire dose is located in one point of the gastrointestinal tract, then the dosage unit is compact, but the concentration of released active principle is very high causing local irritations
Solution Approach 1:
The patent maintains dosage unit compactness by enclosing multiple mini-particles within a single capsule, while simultaneously preventing high local concentration by ensuring these mini-particles are dispersed throughout the gastrointestinal tract rather than remaining clustered at one location. The segmented structure allows the compact outer form to contain distributed internal components that release active ingredients at multiple sites.
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 multilayered miniparticles ensure controlled and uniform release, reduce the risk of local irritations, enhance bioavailability, and allow higher dosages in a smaller volume, improving patient compliance and reducing administration frequency.
Implementation Method 1
an inner film layer which is protective or for the modified release and an outer film layer which more rapidly releases compared to the inner film layer
Implementation Method 2
The miniparticles can be used as such or for the preparation of other forms of administration... controlled and reproducible bioavailability... spreading the active ingredients uniformly throughout the gastrointestinal tract
Data Source
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AI summary
The present invention relates to a multilayered miniparticle for oral use comprising, from the inside to outside: A) a core of an active substance; B) an inner film layer which is protective or for the modified release; C) a layer of at least an active substance which is equal to or different from the one in the core A); D) an outer film layer which more rapidly releases compared to the inner film layer which is protective or for the modified release B). The invention relates to a method for a multilayered miniparticle preparation too and formulations for oral use comprising multilayered miniparticles according to the present invention.