Niraparib Particle Composition for Faster Dissolution and Oral Delivery
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Solution Overview
Problem
Poor aqueous solubility and dissolution rates limit the bioavailability of many drugs, necessitating compositions and methods to enhance their dissolution rates.
Innovation Solution
Niraparib particles with a specific surface area between 11 m²/g and 50 m²/g and a mean particle size of 1 to 6 microns, produced through a process involving solvent atomization under supercritical conditions, are developed to increase dissolution rates.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If Niraparib is formulated as a capsule or tablet, then it can be administered orally, but the drug aggregates into large clumps that are difficult to redispperse
Solution Approach 1:
The patent segments the Niraparib drug substance into discrete, controlled-size particles through milling and classification processes. This segmentation prevents aggregation by ensuring each particle remains individually dispersed rather than forming large clumps, while still allowing oral administration in capsule or tablet form.
Solution Approach 2:
The patent changes the physical parameters of Niraparib particles, specifically controlling particle size distribution through milling and classification. By adjusting particle size parameters to a specific range, the drug maintains stability without aggregation while remaining suitable for oral dosage forms.
2Manufacturing precision
If conventional milling is used to reduce particle size, then particle size is reduced, but the process is time-consuming and expensive
Solution Approach 1:
The patent performs preliminary classification during the milling process itself, using a classifier integrated with the mill to separate particles by size in real-time. This preliminary action during processing eliminates the need for separate, time-consuming classification steps, reducing both time and cost while maintaining precise particle size control.
Solution Approach 2:
The patent merges the milling and classification operations into a single integrated process step. By combining these two functions that were previously separate sequential operations, the process becomes more efficient, reducing processing time and cost while achieving the required particle size precision.
3Ease of manufacture
If Niraparib particles are not properly controlled, then formulation is simpler, but the drug aggregates into large clumps that are difficult to redispperse
Solution Approach 1:
The patent changes the particle size parameters of Niraparib to a specific controlled range, which fundamentally alters the drug's physical behavior. This parameter change prevents aggregation and improves dispersion without complicating the formulation process, as the controlled particles naturally resist clumping.
Solution Approach 2:
The patent creates particles that are self-stabilizing through their controlled size and surface properties. These particles inherently resist aggregation without requiring complex formulation additives or processing steps, allowing simple formulation while maintaining stability and dispersibility.
Data Source
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AI summary
Compositions of particles having at least 95% by weight of niraparib and a specific surface area (SSA) of at least 5 m2/g, methods for their use, and methods for their production are provided.