High-SSA Cisplatin Particles for Faster Dissolution
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Solution Overview
Problem
Poor aqueous solubility and dissolution rates hinder the in vivo bioavailability of many drugs, necessitating methods to enhance dissolution rates for improved drug absorption.
Innovation Solution
The development of cisplatin particles with a specific surface area of at least 3.5 m2/g and a mean particle size of 0.7 μm to 8 μm, produced through a process involving solvent atomization under supercritical conditions, results in enhanced dissolution rates.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If conventional dissolution methods are used, then manufacturing simplicity is maintained, but dissolution rate remains poor
Solution Approach 1:
The patent changes physical parameters of the cisplatin particles, specifically increasing the specific surface area to at least 3.5 m2/g and controlling particle size distribution (Dv50 between 1.0-12 microns), which directly enhances dissolution rate without requiring complex processing equipment
Solution Approach 2:
The patent segments cisplatin into fine particles with controlled size distribution to increase total surface area. This segmentation approach breaks down the drug into smaller units that dissolve faster, resolving the contradiction between maintaining simple manufacturing and improving dissolution rate
2Productivity
If particle size is reduced to increase surface area, then dissolution rate improves, but particle handling and aerosolization become more difficult
Solution Approach 1:
The patent optimizes particle size parameters to achieve Dv50 between 1.0-12 microns and SSA of at least 3.5 m2/g. This parameter optimization ensures particles are small enough for rapid dissolution but large enough to maintain ease of handling and suitable aerosolization characteristics
Solution Approach 2:
The patent creates a dynamic balance in particle size - not too small to lose handleability, not too large to slow dissolution. The controlled size distribution allows particles to be manipulated practically while maintaining high surface area for rapid dissolution
3Productivity
If high surface area particles are produced, then bioavailability improves, but manufacturing precision requirements increase
Solution Approach 1:
The patent defines specific parameter ranges for particle size (Dv50: 1.0-12 microns) and surface area (SSA: at least 3.5 m2/g) that balance bioavailability improvement with achievable manufacturing precision. These parameters are set to be sufficiently strict to ensure efficacy but attainable with standard pharmaceutical manufacturing capabilities
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 increased surface area and controlled particle size lead to faster dissolution and improved bioavailability of cisplatin, reducing systemic side effects and enhancing tumor treatment efficacy.
Implementation Method 1
contacting the atomized droplets with the compressed fluid, to cause depletion of the solvent from the atomized droplets, to produce cisplatin particles comprising at least 95% cisplatin, wherein the cisplatin particles have a specific surface area (SSA) of at 3.5 m2/g and have a mean particle size of between about 0.7 μm and about 8 μm, wherein steps (a), (b), and (c) are carried out under supercritical temperature and pressure for the compressed fluid
Implementation Method 2
passing the solution out of a nozzle orifice and into the pressurizable chamber to produce an output stream of atomized droplets
Data Source
AI summary
Compositions of particles having at least 95% by weight of cisplatin and a specific surface area (SSA) of at least 3.5 m2/g. methods for their use. and methods for their production are provided.