Water-Dispersible Deferasirox Tablets for Solubility and Flow
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Solution Overview
Problem
Existing water-dispersible tablet formulations of deferasirox face challenges such as poor solubility, adherence of particles, and low flow properties due to electrostatic characteristics, leading to difficulties in production and administration, especially for large tablet sizes.
Innovation Solution
A formulation comprising deferasirox with specific amounts of crospovidone as a disintegrant, sodium lauryl sulfate as a surfactant, and copovidone as a binder, along with other excipients, enhances solubility and dissolution, ensuring adequate hardness and mechanical strength for effective processing and packaging.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If deferasirox is formulated as oral tablets, then the dosage form is suitable for administration, but the tablet size becomes too large for patients with difficulty swallowing
Solution Approach 1:
The patent divides the large tablet into smaller individual tablets or granules that can be easily swallowed. Each small unit contains a portion of the total deferasirox dose, allowing patients to take multiple smaller units instead of one large tablet, thereby improving swallowability while maintaining the required dosage.
Solution Approach 2:
The patent transitions from solid tablets to water-dispersible formulations that can be administered as suspensions or solutions. This dimensional change from solid to liquid-like form eliminates the swallowing difficulty associated with large tablets while delivering the same therapeutic dose.
2Reliability
If deferasirox is made water-dispersible, then solubility and dissolution are improved, but particles adhere to each other due to electrostatic characteristics
Solution Approach 1:
The patent introduces surfactants as intermediary substances that coat the deferasirox particles and reduce electrostatic attraction between them. These surfactants act as mediators that prevent particle adhesion while maintaining water dispersibility, allowing the formulation to achieve both good solubility and particle separation.
Solution Approach 2:
The patent modifies the surface properties of deferasirox particles by changing parameters such as surface charge, hydrophobicity, or steric stabilization through coating with polymers or surfactants. These parameter changes reduce electrostatic interactions and prevent particle adhesion while preserving water dispersibility.
3Device complexity
If deferasirox particles are used directly, then the formulation is simple, but particles have low flow properties and are prone to adherence
Solution Approach 1:
The patent creates composite granules or tablets by combining deferasirox particles with excipients such as flow promoters, binders, and lubricants. This composite approach improves flow properties and manufacturing characteristics while maintaining the active pharmaceutical ingredient's efficacy, resolving the conflict between formulation simplicity and ease of manufacture.
4Quantity of substance
If large tablet size is used to achieve adequate dose, then the dosage requirement is met, but patient compliance decreases due to difficulty swallowing
Solution Approach 1:
The patent segments the total dosage into multiple smaller tablets or granules, each containing a fraction of the total deferasirox dose. Patients can swallow these smaller units more easily, improving compliance while the cumulative dose across all units meets the therapeutic requirement.
Solution Approach 2:
The patent transforms the dosage form from large solid tablets to water-dispersible small units or suspensions that can be easily administered. This dimensional change improves patient compliance by eliminating swallowing difficulties while maintaining the required dosage through proper formulation concentration.
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 formulation achieves high solubility, rapid dissolution, and improved patient compliance by using optimized ratios of crospovidone to sodium lauryl sulfate, resulting in tablets that disintegrate easily in water.
Implementation Method 1
crospovidone as a disintegrant, wherein crospovidone is in an amount of between 37.00 and 38.00% by weight of the total formulation
Implementation Method 2
sodium lauryl sulfate as a surfactant
Implementation Method 3
copovidone as a binder
Data Source
AI summary
The present invention relates to formulations comprising deferasirox or a pharmaceutically acceptable salt thereof. More particularly, the present invention relates to water-dispersible tablet formulations of deferasirox.