Taxane Particles with High Surface Area for Dissolution
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Poor aqueous solubility and in vivo dissolution rates limit the bioavailability of many drugs, necessitating methods and compositions to enhance drug absorption.
Innovation Solution
Compositions comprising particles with at least 95% by weight of a taxane, characterized by a mean bulk density between 0.050 g/cm3 and 0.15 g/cm3 and/or a specific surface area of at least 18 m2/g, which significantly increase the dissolution rate of poorly soluble drugs.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If conventional taxane formulations are used, then the drug can be administered, but the dissolution rate remains poor due to low aqueous solubility
Solution Approach 1:
The taxane drug is divided into fine particles with mean size of 0.5-2.0 μm, increasing the total surface area available for dissolution. This segmentation transforms the bulk drug into numerous small particles that dissolve more rapidly, directly addressing the poor dissolution rate problem while maintaining the drug's therapeutic properties.
Solution Approach 2:
The patent changes physical parameters of the taxane by controlling particle size distribution and bulk density (0.05-0.15 g/cm³). By adjusting these parameters through specific formulation techniques, the drug achieves enhanced dissolution characteristics without altering its chemical structure or therapeutic activity.
2Productivity
If particle size is reduced to increase surface area, then dissolution rate improves, but manufacturing complexity increases
Solution Approach 1:
The patent establishes specific parameter ranges for particle size (0.5-2.0 μm mean size) and bulk density (0.05-0.15 g/cm³) that can be achieved through conventional pharmaceutical manufacturing techniques. By defining these target parameters, the invention balances dissolution enhancement with manufacturing feasibility, avoiding excessive complexity while achieving the desired dissolution rate improvement.
Data Source
AI summary
Compositions are provided that include having at least 95% by weight of a taxane, or a pharmaceutically acceptable salt thereof, where the particles have a mean bulk density between about 0.050 g/cm3 and about 0.15 g/cm3, and/or a specific surface area (SSA) of at least 18 m2/g, 20 m2m/g, 25 m2/g, 30 m2/g, 32 m2/g, 34 m2/g, or 35 m2/g. Methods for making and using such compositions are also provided.