Stabilizing Amine Actives in Oral Films via Segmented Mixing
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Solution Overview
Problem
The existing methods for preparing oral film dosage forms often result in undesirable gel-like masses when combining amine-containing actives with sweeteners, leading to difficulties in achieving uniform dispersion and processing, which hinders the formation of uniform and acceptable dosage forms.
Innovation Solution
A method involving a multi-step mixing process is employed, where a slurry comprising an amine-containing active, an electrolyte, and a sweetener is formed separately and then combined with a polymeric matrix, followed by controlled drying to prevent gelation and ensure uniform distribution, using a combination of polymers and polar solvents to maintain component uniformity throughout the film.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Manufacturing precision
If a multi-step mixing process is used to achieve uniform dispersion of components, then uniformity of content is improved, but the process complexity increases and gel-like mass formation may occur
Solution Approach 1:
The mixing process is divided into distinct segments: first mixing the polymer with solvent to form a polymer solution, then separately preparing a slurry of amine-containing active with electrolyte and sweetener, and finally combining these two separate mixtures. This segmentation prevents gel-like mass formation while achieving uniform dispersion of all components throughout the film matrix.
Solution Approach 2:
The polymer solution and active slurry are prepared in advance as separate homogeneous mixtures before being combined. This preliminary preparation ensures that each component is properly dispersed in its respective medium before final combination, preventing gelation and ensuring uniform content distribution in the final film.
2Manufacturing precision
If components are mixed together to achieve uniform dispersion, then content uniformity is improved, but gel-like mass formation occurs making processing difficult
Solution Approach 1:
The electrolyte serves as an intermediary component that mediates between the amine-containing active and the polymer matrix. By first mixing the active with the electrolyte to form a stable slurry, and then adding this slurry to the polymer solution, the electrolyte prevents direct interaction that would cause gel-like mass formation while ensuring uniform dispersion of the active throughout the final film.
3Reliability
If amine-containing actives are combined with sweeteners to achieve desired formulation, then therapeutic effectiveness is improved, but gel-like mass formation occurs
Solution Approach 1:
The problematic direct combination of amine-containing active with sweetener is avoided by extracting the sweetener into a separate mixing stage. The active is first mixed with electrolyte to form a stable slurry, then this slurry is combined with the polymer solution containing the sweetener. This separation prevents gel-like mass formation while maintaining the therapeutic effectiveness of the amine-containing active in the final film composition.
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 approach prevents gel-like mass formation, allowing for the production of uniformly distributed and processable edible film dosage compositions, ensuring consistent and effective delivery of pharmaceutical actives.
Implementation Method 1
the combination of certain actives and sweeteners has a tendency to result in an undesirable gel-like mass... it has been surprisingly discovered that the combination of certain actives and sweeteners has a tendency to result in an undesirable gel-like mass
Implementation Method 2
using a combination of polymers and polar solvents to maintain component uniformity throughout the film
Implementation Method 3
drying said wet matrix to form an edible film dosage composition from said wet film matrix
Data Source
AI summary
The present invention relates to compositions relating to films containing active pharmaceutical agents. In particular, the present invention relates to methods and systems useful for stabilizing amine-containing actives for dispersion in a film product.