Fulvestrant Solid-Particle Composition for Pain-Reduced Sustained Release
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Solution Overview
Problem
Current fulvestrant formulations suffer from non-ideal sustained release, inconvenient administration, and high injection pain, necessitating a need for long-acting, pain-reducing, and easily administered dosage forms.
Innovation Solution
A fulvestrant pharmaceutical composition with specific particle size distributions and optional additives, formulated into various vehicles, is prepared using zirconium beads grinding to enhance sustained release and bioavailability, reducing injection pain.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If fulvestrant is dissolved with viscous oil-based vehicle to improve solubility, then solubility is improved, but injection pain degree increases and administration becomes inconvenient
Solution Approach 1:
The patent changes the physical state of fulvestrant from dissolved state in viscous oil to suspended state as solid particles in aqueous vehicle. This parameter change in formulation state allows the drug to be administered without requiring viscous co-solvents, thereby reducing injection pain while maintaining adequate solubility through particle suspension.
Solution Approach 2:
The patent introduces solid particles as an intermediary form between completely dissolved and undissolved states. These solid particles with specific size distribution (Dv(10) 0.400-6.000 μm, Dv(50) 0.700-6000 μm, Dv(90) 1.000-6.000 μm) serve as a mediator that provides sustained release while avoiding the need for painful oil-based vehicles.
2Object-affected harmful factors
If fulvestrant is formulated as oil-based suspension to reduce injection pain, then injection pain is reduced, but sustained release effect becomes non-ideal
Solution Approach 1:
The patent optimizes multiple parameters simultaneously: particle size distribution (Dv(10) 0.400-6.000 μm, Dv(50) 0.700-6000 μm, Dv(90) 1.000-6.000 μm), vehicle composition (aqueous-based with specific excipients), and formulation pH. These parameter changes enable the formulation to achieve both reduced injection pain and ideal sustained release effect through controlled dissolution and release of solid particles.
3Device complexity
If fulvestrant is administered as large particle size to simplify formulation, then formulation complexity is reduced, but bioavailability decreases
Solution Approach 1:
The patent specifies an optimal particle size range (Dv(10) 0.400-6.000 μm, Dv(50) 0.700-6000 μm, Dv(90) 1.000-6.000 μm) that balances formulation simplicity with bioavailability. This parameter optimization ensures particles are small enough for adequate absorption but large enough to maintain suspension stability and controlled release, achieving both formulation simplicity and high bioavailability.
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 composition achieves long-acting sustained release, high bioavailability, and significantly reduces injection pain while being convenient to administer, offering a promising marketing prospect.
Implementation Method 1
The fulvestrant solid particles are prepared by grinding with zirconium beads
Data Source
AI summary
A fulvestrant pharmaceutical composition, a preparation method therefor, and an application thereof are provided. The fulvestrant pharmaceutical composition contains fulvestrant solid particles. The particle size of the fulvestrant solid particles satisfies that Dv(10) is selected from 0.400 micrometers to 6.000 micrometers, Dv(50) is selected from 0.700 micrometers to 6.000 micrometers, and Dv(90) is selected from 1.000 micrometers to 6.000 micrometers, provided that Dv(10) is not 0.400 micrometers, Dv(50) is not 0.700 micrometers, and Dv(90) is not 1.000 micrometers. The fulvestrant pharmaceutical composition has a long-acting sustained release.