Solid Formulation Mixing for Content Uniformity
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Solution Overview
Problem
Existing methods for producing tablets with low active ingredient content face challenges in achieving good content uniformity using the direct compression method, often requiring complex processes and risking active ingredient degradation with solvent use.
Innovation Solution
A manufacturing method involving mixing an active ingredient with an excipient having a median particle size 15 times or more than the active ingredient, followed by direct compression or dry granulation, to achieve a standard deviation of active ingredient content within 5% or less.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If the direct compression method is used to produce tablets with low active ingredient content, then the manufacturing process is simple, but the content uniformity is poor
Solution Approach 1:
The patent changes the particle size parameter of the excipient to solve the content uniformity problem. Specifically, it uses excipients with a median particle size of 15 times or more that of the active ingredient, which improves content uniformity while maintaining the simplicity of the direct compression method. This parameter change allows the active ingredient to be more evenly distributed in the formulation without requiring complex multi-step mixing processes.
2Manufacturing precision
If granulation with solvents is used to improve content uniformity, then the content uniformity is good, but the active ingredient may be degraded
Solution Approach 1:
The patent extracts and eliminates the harmful element (solvents) from the granulation process. By using solvent-free direct compression with specifically sized excipients, it achieves content uniformity without exposing the active ingredient to degradation risks from water or other solvents. This removes the harmful factor while preserving the beneficial outcome of content uniformity.
Solution Approach 2:
The patent replaces the traditional granulation process with a simpler, solvent-free direct compression approach. This substitutes a complex, potentially harmful process with a simpler, safer alternative that achieves the same or better results in terms of content uniformity without the risk of active ingredient degradation.
3Manufacturing precision
If multiple mixing steps are used to achieve good content uniformity, then the content uniformity is improved, but the manufacturing process becomes complicated
Solution Approach 1:
The patent changes the particle size parameter of the excipient to enable good content uniformity to be achieved in a single mixing step rather than requiring multiple steps. By using excipients with a median particle size of 15 times or more that of the active ingredient, the mixing process becomes more efficient and uniform distribution is achieved more easily, reducing process complexity.
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 ensures high content uniformity of active ingredients in solid formulations, preventing degradation and simplifying the manufacturing process, especially for unstable compounds and low-content active ingredients.
Implementation Method 1
mixing an active ingredient and an excipient with a median particle size of 15 times or more, preferably 20 times or more, relative to the median particle size of the active ingredient
Data Source
AI summary
The present invention offers the manufacturing method of the solid formulation wherein the standard deviation of the active ingredient content in the solid formulation becomes 5% or less by mixing the excipients which have a median particle size of 15 or more times, preferably 20 times or more to the median particle size of an active ingredient.