Tasquinimod Particle Size Distribution for Faster Oral Dissolution
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Solution Overview
Problem
Tasquinimod, despite its high solubility and permeability, exhibits unexpectedly low dissolution rates, which can reduce bioavailability and hinder efficient oral administration.
Innovation Solution
Formulating tasquinimod particles with a specific particle size distribution, characterized by D(v,0.9) of at most 30 μm and D(v,0.5) of at most 15 μm, to enhance dissolution rates and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If tasquinimod is formulated with conventional particle sizes, then manufacturing is simpler, but dissolution rate is low and bioavailability is reduced
Solution Approach 1:
The patent applies parameter changes by optimizing the particle size distribution of tasquinimod, specifically controlling D(v,0.9) to at most 30 μm and D(v,0.5) to at most 15 μm. This physical parameter modification directly addresses the contradiction by enhancing dissolution rate while establishing precise manufacturing specifications for particle size control.
2Reliability
If tasquinimod particles are reduced to increase dissolution rate, then bioavailability improves, but manufacturing complexity increases
Solution Approach 1:
The patent applies segmentation by dividing tasquinimod into particles with specific size distributions (D(v,0.9) ≤ 30 μm, D(v,0.5) ≤ 15 μm). This segmentation approach improves bioavailability through enhanced dissolution while the defined parameters provide clear manufacturing guidance, balancing reliability improvement with manageable process complexity.
3Ease of manufacture
If conventional formulation methods are used, then manufacturing is easier, but dissolution rate remains low
Solution Approach 1:
The patent modifies the physical parameter of particle size distribution (D(v,0.9) ≤ 30 μm, D(v,0.5) ≤ 15 μm) to enhance dissolution efficiency. This parameter change maintains ease of manufacture through standard micronization and classification techniques while dramatically improving dissolution rate and overall productivity.
Data Source
AI summary
A plurality of particles of tasquinimod in free base form or as a pharmaceutically acceptable salt, the particles having a D(v,0.9) of at most 30 μm and a D(v,0.5) of at most 15 μm. A pharmaceutical composition comprising the particles and preferably one or more pharmaceutically acceptable excipients. A pharmaceutical dosage unit. The particles, composition and dosage unit are useful in the treatment of cancer.