Co-processed Excipient Composition with Lactose Coating
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Solution Overview
Problem
In the pharmaceutical industry, the use of lubricants in tablet production can negatively affect binding and disintegration properties, leading to the belief that they must be added just before compression and sprayed onto granules to minimize contact with other components, but this process is not optimized for producing ready-to-use co-processed excipient compositions.
Innovation Solution
Incorporating the lubricant into the granulation process with filler-binders and disintegrants, and coating the granules with lactose, which enhances binding and flowability, eliminating the need for glidants and allowing for a simplified tablet formulation without the lubricant being directly on the outside, thus avoiding the formation of a non-adhering lubricant film.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Force
If lubricant is added just before compression and sprayed onto granules, then tablet ejection is improved, but binding and disintegration properties deteriorate due to lubricant coating excipient components
Solution Approach 1:
The lubricant is incorporated into the granulation process beforehand, during which it is evenly distributed throughout the granule matrix rather than being sprayed onto the surface just before compression. This preliminary incorporation ensures the lubricant is present for ejection while minimizing its ability to form surface coatings that would interfere with binding and disintegration
Solution Approach 2:
The lubricant is distributed heterogeneously within the granules, with higher concentrations in the interior and lower concentrations at the surface. This local quality variation ensures adequate lubrication for ejection while maintaining surface properties necessary for binding and disintegration
2Reliability
If lubricant is added just before compression, then contact time with other components is minimized, but the process complexity increases and ready-to-use co-processed excipient composition cannot be achieved
Solution Approach 1:
The lubricant incorporation step is merged with the granulation process, allowing all excipient components including the lubricant to be processed together in a single operation. This creates a ready-to-use co-processed excipient composition that eliminates subsequent separate lubricant addition steps while maintaining reliable disintegration properties
3Ease of manufacture
If lubricant is incorporated into granulation process, then ready-to-use co-processed excipient composition is achieved and process is simplified, but lubricant may form non-adhering film on granule surface
Solution Approach 1:
The granulation parameters (liquid binder composition, granulation time, drying conditions) are optimized to control the distribution and state of the lubricant within the granules. These parameter changes ensure the lubricant remains incorporated in the granule matrix rather than migrating to the surface where it would form non-adhering films
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 results in tablets with improved disintegration and compactability, reduced sensitivity to mixing time, and maintains excellent ejection forces, providing a ready-to-use co-processed excipient composition that simplifies the tablet formulation process.
Implementation Method 1
coating the granules with lactose, which enhances binding and flowability
Data Source
AI summary
The invention pertains to a co-processed excipient composition suitable for tableting, said composition comprising at least one filler-binder, at least one disintegrant, and at least one lubricant which have been subjected to granulation together, and said composition partially or completely coated with lactose, preferably in crystalline form. The inventors have overcome the prejudice against the use of lubricants in tableting excipient compositions early in the tableting process. It was found that the alleged detrimental affects of the lubricant in terms of binding and disintegration could readily be controlled in a excipient composition wherein the lubricant is co-processed in the matrix, and the composition is provided with a lactose coat.