Controlled Release Pellets for High Dosage Swallowability
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Solution Overview
Problem
Existing controlled release formulations for oral administration, such as pellets and tablets, face challenges in delivering high dosages and are unsuitable for geriatric or pediatric use due to size limitations, leading to impractical multiple dosing or swallowing difficulties, and lack adaptations for single dose sachets that can mask unpleasant tastes and odors effectively.
Innovation Solution
Development of small-sized pellets with a controlled release membrane and the use of sweetening and flavoring agents in solid form or dissolved in a solvent to ensure smooth flow and exact dosage, combined with gelifying excipients for continuous release in the gastrointestinal tract, avoiding temperature extremes that could alter active ingredients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If conventional pellets are used for controlled release administration, then the active substance is released in a controlled manner, but the pellets are too large to be swallowed easily by geriatric or pediatric patients and require multiple capsules for high dosages
Solution Approach 1:
The invention divides the dosage into multiple small minipellets (each containing a fraction of the total dose) that can be easily swallowed, while collectively delivering the required high dosage. The pellets are spread homogeneously in many minidoses on a wide length of the gastro-intestinal tract, solving both the swallowability and dosage capacity contradiction.
Solution Approach 2:
The invention transitions from administering the entire dose in one or few large pellets to distributing the same total dose across many small pellets that occupy a wider spatial distribution in the gastro-intestinal tract, effectively using the dimensional space to resolve the contradiction between size and dosage capacity.
2Quantity of substance
If the number of pellets is increased to deliver high dosages, then the total dosage capacity increases, but the pellets become too small to maintain adequate titre and require larger capsules
Solution Approach 1:
The invention segments the total dosage into many small minipellets that can be contained in a single swallowable capsule. Each minipellet is small enough to be easily swallowed, but the collective ensemble of many minipellets delivers the required high total dosage without requiring an oversized capsule.
Solution Approach 2:
The invention changes the particle size parameter of the pellets to a specific range (under 710 μm) that optimizes both the number of pellets needed for high dosage and the swallowability of the final formulation, resolving the contradiction between total dosage and capsule size requirements.
3Ease of operation
If pellets are made smaller to improve swallowability, then ease of swallowing increases, but the pellet titre becomes too low requiring larger capsules
Solution Approach 1:
The invention accepts the lower titre of individual minipellets as a necessary compromise for swallowability, but compensates by increasing the number of minipellets in the ensemble. The total active substance content is maintained by having many small pellets rather than fewer large ones, resolving the contradiction between individual pellet titre and overall swallowability.
4Quantity of substance
If multiple capsules are used to achieve high dosages, then the required dosage can be met, but the administration becomes impractical and commercially unacceptable
Solution Approach 1:
The invention merges multiple small minipellets into a single unified oral administration unit (one sachet or one capsule containing many pellets) that delivers the complete high dosage in one go. This eliminates the need for patients to take multiple separate capsules, making the administration practical and commercially acceptable while still meeting the dosage requirement.
5Reliability
If conventional tablet or capsule formulations are used, then controlled release can be achieved, but unpleasant tastes and odors of active substances cannot be effectively masked
Solution Approach 1:
The invention introduces flavoring and sweetening agents as intermediary substances that mask the unpleasant taste and odor of the active substance. These masking agents are incorporated into the pellet coating or the surrounding matrix, allowing the controlled release function to be maintained while the harmful sensory effects are effectively concealed.
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
Enables the creation of single dose sachets with controlled release pellets that maintain release characteristics and mask unpleasant tastes and odors, allowing for effective administration of high dosages without swallowing issues, while protecting sensitive ingredients from thermal degradation.
Implementation Method 1
the active substance is released to the organism in a controlled, gradual, sustained or retarded way
Implementation Method 2
an outer membrane causing the controlled and/or delayed release
Implementation Method 3
gelifying excipients for continuous release in the gastrointestinal tract
Implementation Method 4
proper masking of unpleasant odor and/or taste
Data Source
AI summary
A formulation of controlled release solid products for oral administration is disclosed, adapted for administration of drugs, food supplements and the like in single dose sachets, when the active substance should be administered at a greater dosage than the quantity that can be contained in a tablet or capsule of a size suitable for being swallowed. The relevant method of preparation is also disclosed.