Lactose Cellulose Granules for Direct Tabletting
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Solution Overview
Problem
Direct tabletting of pharmaceutical formulations is challenging due to difficulties in achieving sufficient plastic deformability, good flow properties, and preventing segregation of components, especially with high cellulose derivative content, which limits the production of tablets with improved hardness and abrasion resistance.
Innovation Solution
A method involving suspending and/or partially dissolving lactose in a liquid, followed by atomizing the solution into an environment with controlled temperature and pressure, where cellulose derivatives are present, to produce granules with enhanced flow properties and compressibility, allowing for increased cellulose derivative content without compromising flowability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Strength
If high cellulose derivative content is used in tablet formulation, then tablet hardness and abrasion resistance are improved, but flow properties deteriorate
Solution Approach 1:
The patent changes the physical-chemical parameters of cellulose derivatives by converting them into low-viscosity derivatives (such as hydroxypropyl cellulose with specific viscosity ranges) and controlling their particle size distribution. This allows high cellulose content formulations to maintain both improved tablet hardness and adequate flow properties, resolving the contradiction between strength and ease of operation.
Solution Approach 2:
The patent creates composite tablet formulations combining cellulose derivatives with specific proportions of fillers (lactose, calcium phosphate), disintegrants, and lubricants. This composite approach allows the formulation to achieve both high tablet hardness from cellulose and good flow properties from the synergistic combination of multiple excipients, resolving the contradiction between strength and ease of operation.
2Ease of manufacture
If direct tabletting is used, then production cost and complexity are reduced, but achieving sufficient plastic deformability and preventing segregation becomes difficult
Solution Approach 1:
The patent modifies the particle size distribution of excipients and the viscosity characteristics of cellulose derivatives to optimize plastic deformability for direct compression. By controlling these parameters, the formulation achieves sufficient deformability for direct tabletting while maintaining cost-effectiveness and eliminating the need for granulation processes, thus resolving the contradiction between ease of manufacture and reliability.
3Stability of the object's composition
If different particle size distributions are used, then segregation of components is minimized, but manufacturing complexity increases
Solution Approach 1:
The patent specifies particular particle size ranges and distributions for different excipients (cellulose derivatives, fillers, disintegrants, lubricants) to minimize segregation during tablet manufacturing. By establishing these controlled particle size parameters, the formulation achieves compositional stability without requiring complex manufacturing equipment or processes, resolving the contradiction between segregation prevention and manufacturing 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
The method produces granules that enable direct tabletting with improved tablet hardness and abrasion resistance, allowing for increased cellulose derivative content without affecting flowability, and allows for controlled release profiles, making them suitable for sustained-release formulations.
Implementation Method 1
suspending and/or at least partially dissolving lactose in a liquid
Implementation Method 2
atomizing the solution or suspension obtained in i) into an environment with a temperature of 30-250 °C
Implementation Method 3
atomizing the solution or suspension obtained in i) into an environment with a temperature of 30-250 °C on cellulose derivatives
Implementation Method 4
the liquid being at least partially removed
Data Source
AI summary
The present invention relates to a method for producing a lactose and cellulose (derivative)-based granulate, to a granulate obtained by way of the method, and to the use thereof as a tableting aid.