Pharmaceutical Carrier Pellets for Controlled Release
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Solution Overview
Problem
Existing pharmaceutical administration forms with controlled release are not entirely satisfactory, as they often fail to achieve desired release profiles and are difficult to produce, with coatings being prone to faults and multiparticulate forms having variable absorption and incomplete release.
Innovation Solution
The method involves producing carrier pellets through spray granulation in a fluidised or spouted bed unit, using a liquid formulation with a physiologically tolerated pH regulator and binder, which is evaporated to form spherical pellets with controlled pH, enhancing bioavailability and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If coatings are applied on tablets or capsules to control release, then release of the active substance can be influenced, but a faulty or damaged coating can lead to uncontrolled release of the total active substance dose
Solution Approach 1:
The patent divides the total active substance dose into multiple smaller pellets (e.g., 2-1000 pellets per dose), where each pellet contains a fraction of the total dose. This segmentation ensures that if one pellet's coating is faulty or damaged, only a small fraction of the total dose is released uncontrollably, while the remaining pellets maintain controlled release. This directly resolves the contradiction by reducing the harmful impact of coating failures while maintaining overall release control.
2Quantity of substance
If tablets are used for oral administration, then they can deliver the active substance, but they can remain in the stomach for a long and variable time before disintegration
Solution Approach 1:
The patent replaces single large tablets with multiple small pellets. These pellets have a significantly smaller size and surface area-to-volume ratio, enabling them to pass through the stomach much faster and reach the intestine more rapidly. The segmentation into small units eliminates the long and variable stomach residence time associated with tablets, while still delivering the complete active substance dose through the cumulative effect of multiple pellets.
3Reliability
If multiparticulate administration forms are used to improve release control, then coating faults affect only small proportions, but the absorption and release can still be variable and incomplete
Solution Approach 1:
The patent employs granulation technology with controlled parameters (liquid binder composition, granulation speed, drying conditions) to produce pellets with highly consistent size, density, and coating properties. By precisely controlling these manufacturing parameters, the patent achieves uniform pellets that provide consistent and complete release profiles, eliminating the variability and incompleteness issues associated with conventional multiparticulate forms while maintaining the robustness benefit of multiple units.
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
This method enables controlled and efficient release of pharmaceutical active substances, avoiding the limitations of existing technologies by producing consistent, spherical pellets with precise pH regulation and improved bioavailability.
Implementation Method 1
essentially spherical carrier pellets are formed by spray granulation in the unit in which the solvent is evaporated by means of a drying gas flow
Implementation Method 2
a pH regulator which has a regulating effect in the physiological surroundings is used, such that the pH value is lowered or increased and hence the bioavailability of pharmaceutically effective components is made possible or increased
Data Source
AI summary
The invention relates to a method for the production of carrier pellets for pharmaceutical active substances. Likewise, the invention relates to such carrier pellets and also to pharmaceutical formulations containing these. The carrier pellets according to the invention are used for transporting and releasing pharmaceutical active substances, in particular in the human body.