Lipid-Coated Pellets via Cold Extrusion for Taste Masking
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current methods for taste masking in pharmaceuticals, such as polymer coatings, often require additional process steps and use excipients with toxicity concerns, especially in pediatric formulations, and lack effective solvent-free cold extrusion techniques for controlled release and taste masking.
Innovation Solution
The development of spherical pellets with a lipid coating formed through cold solvent-free extrusion using a lipid binder composition comprising hard fat, glycerol trimyristate, and glycerol distearate, which creates a taste-masked, controlled release formulation without active ingredient release at room temperature and allows for delayed release at body temperature.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If polymer coating is used for taste masking, then taste masking effect is improved, but process complexity increases and toxicity concerns arise
Solution Approach 1:
The invention combines the granulation and coating steps into a single simultaneous process. The lipid binder composition is applied during granulation itself, forming a coating layer on the particle surfaces without requiring a separate coating step. This merging eliminates the additional process complexity while maintaining effective taste masking.
Solution Approach 2:
The granulation process itself provides the coating function through the lipid binder composition. The binder naturally forms a coating layer on the particle surfaces during granulation, making the system self-sufficient for both granulation and taste masking without external coating equipment or additional processing steps.
2Object-affected harmful factors
If polymer coating is used for taste masking, then taste masking effect is improved, but excipient toxicity increases
Solution Approach 1:
The invention changes the chemical nature of the coating material from synthetic polymers to natural lipids. The lipid binder composition uses physiologically compatible lipid materials that are naturally present in the body, fundamentally altering the toxicity parameter from potentially harmful synthetic excipients to biocompatible natural substances while maintaining coating functionality.
Solution Approach 2:
The invention uses simple, naturally occurring lipid materials instead of complex synthetic polymers. These lipids are physiologically compatible, naturally metabolizable, and eliminate the need for long-term persistence in the body, reducing toxicity concerns associated with synthetic excipient accumulation.
3Object-affected harmful factors
If additional coating step is added for taste masking, then taste masking effect is improved, but manufacturing time increases
Solution Approach 1:
The invention merges the granulation and coating operations into a single integrated process step. The lipid binder composition performs dual functions as both granulation binder and coating material, eliminating the sequential nature of traditional processes and reducing total manufacturing time.
Solution Approach 2:
The coating formation occurs continuously during the granulation process rather than as a separate subsequent step. The lipid binder is applied and forms the coating layer simultaneously with particle aggregation, maintaining continuous productive action without interruption or additional processing cycles.
4Ease of manufacture
If solvent-free cold extrusion is used, then process simplicity is improved, but coating completeness deteriorates
Solution Approach 1:
The invention changes the physical state and application method of the lipid binder. By using a liquid or semi-liquid lipid binder composition applied during granulation rather than solid extrusion, the coating can form more completely and uniformly on particle surfaces while maintaining the solvent-free and cold process advantages.
Solution Approach 2:
The invention uses a composite lipid binder composition containing multiple lipid components in specific ratios. This composite formulation optimizes both the coating formation characteristics and the taste masking effectiveness, achieving complete coverage while maintaining process simplicity through the synergistic interaction of lipid components.
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 provides an economical, one-step process for producing taste-masked pharmaceuticals with enhanced pediatric compliance, reducing toxicity concerns and enabling controlled release profiles without the need for additional coating steps or toxic excipients.
Implementation Method 1
a coating of a lipid binder composition obtainable by cold solvent-free extrusion... the coating is formed on the surface of said pellets or granules covering completely said pellets or granules during spheronisation
Implementation Method 2
cold extruding the mixture... cold solvent-free extrusion comprising the steps of a) mixing the active ingredient with said lipid binder composition... b) cold extruding the mixture
Implementation Method 3
spheronising the extrudate to obtain spherical pellets or granules... having spherical shape
Implementation Method 4
the coating does not substantially contain any active ingredients which are released at 24°C within 20 min... allowing the preparation of release-controlled pellets
Data Source
Figure 1a~1b
Figure 2a~2b
Figure 2c~3
AI summary
The present invention relates to pellets obtainable by a method for preparing solid pellets by cold solvent-free extrusion. Said pellets are characterized by having spherical shape and a lipid coating formed completely on the surface. Moreover, said pellets provide enhanced taste-masking of e.g. acitive ingredients present in said pellets. In another aspect, methods for obtaining said pellets are provided. In addition, the present application relates to lipid binder compositions for pellets allowing the preparation of release-controlled pellets having enhanced taste- masking.