Empagliflozin Particle Size Control for Dissolution and Adhesion
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Solution Overview
Problem
Current pharmaceutical formulations of Empagliflozin often face issues with adhesion during manufacturing, poor dissolution profiles, content uniformity, and compressibility, particularly due to inappropriate particle sizes, which affect bioavailability and stability.
Innovation Solution
A pharmaceutical formulation with Empagliflozin or its pharmaceutically acceptable salt having a d(0.9) particle size between 1 µm and 5 µm, combined with suitable excipients like microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, and anhydrous colloidal silicon dioxide, to enhance dissolution properties, homogeneity, and compressibility, prepared through a simple and efficient manufacturing process.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If empagliflozin with larger particle size (D(0.9) > 180 μm) is used, then adhesion during manufacturing is reduced, but dissolution profile and bioavailability deteriorate
Solution Approach 1:
The patent changes the particle size parameter of empagliflozin from conventional large sizes (D(0.9) > 180 μm) to a specific fine range (D(0.9) between 1-5 μm). This parameter change simultaneously improves dissolution profile and bioavailability while maintaining acceptable manufacturing characteristics through optimized formulation
Solution Approach 2:
The patent performs preliminary particle size reduction and homogenization of empagliflozin before formulation. By pre-processing the active ingredient to achieve uniform fine particle size distribution, the formulation achieves both good manufacturability and superior dissolution characteristics
2Manufacturing precision
If empagliflozin with finer particle size is used, then dissolution profile and bioavailability are improved, but adhesion during manufacturing increases
Solution Approach 1:
The patent optimizes the particle size parameter to a specific range (D(0.9) between 1-5 μm) that balances dissolution performance with manufacturability. This precise parameter control prevents excessive adhesion while ensuring superior dissolution profile
Solution Approach 2:
The patent creates a composite formulation system where fine particle size empagliflozin is combined with specific excipients and manufacturing approaches. This composite approach enables the use of fine particles without suffering from adhesion problems, as the overall formulation system is designed to accommodate the fine particle characteristics
3Productivity
If empagliflozin particle size is not optimized, then content uniformity is poor, but manufacturing process is simpler
Solution Approach 1:
The patent performs preliminary particle size reduction and homogenization of empagliflozin before formulation. By pre-processing the active ingredient to achieve uniform fine particle size distribution, the formulation achieves both good manufacturability and superior dissolution characteristics
Solution Approach 2:
The patent changes the particle size parameter of empagliflozin from conventional large sizes (D(0.9) > 180 μm) to a specific fine range (D(0.9) between 1-5 μm). This parameter change simultaneously improves dissolution profile and bioavailability while maintaining acceptable manufacturing characteristics through optimized formulation
Data Source
AI summary
The present invention relates to a pharmaceutical formulation comprising Empagliflozin or a pharmaceutically acceptable salt thereof wherein Empagliflozin or pharmaceutically acceptable salt has a d (0.9) particle size between 1 and 5 µm. The present invention also relates to a simple, rapid, cost effective, time-saving and industrially convenient method of preparing the formulation.