Selexipag Tablet Formulation with Binder Particle Size Control
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current tablet formulations of selexipag suffer from low solubility and dissolution issues, leading to poor bioavailability and stability, and lack effective methods for achieving uniform content and physicochemical properties.
Innovation Solution
A tablet formulation comprising selexipag or its crystalline polymorph combined with a binder having a specific particle size range (15 µm to 250 µm) and excipients like hydroxypropyl cellulose, D-mannitol, and magnesium stearate, processed through wet granulation and film coating, to enhance dissolution, stability, and content uniformity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If selexipag is formulated in conventional tablet forms, then the tablet can be manufactured, but the solubility and dissolution rate are poor
Solution Approach 1:
The patent changes the particle size parameter of the binder from conventional ranges to a specific d(0.9) range of 15-250 µm. This parameter change fundamentally alters the dissolution behavior of the tablet, enabling selexipag to dissolve effectively while maintaining manufacturability. The specific binder particle size range creates optimal conditions for both production and dissolution performance.
Solution Approach 2:
The patent creates a composite tablet formulation by combining selexipag with a binder of specific particle size (15-250 µm) and other excipients in optimized proportions. This composite structure leverages the complementary properties of each component: the controlled particle size of the binder provides dissolution enhancement while the excipient mixture ensures proper flowability and compressibility for manufacturing.
2Adaptability or versatility
If selexipag is used in low amounts, then the dosage can be adjusted, but content uniformity becomes difficult to achieve
Solution Approach 1:
The patent changes the particle size parameter of the binder to a specific range (d(0.9) 15-250 µm) that enables effective mixing and uniform distribution even when selexipag is present in low amounts. This parameter change ensures that the active ingredient is properly dispersed throughout the tablet matrix, achieving content uniformity across multiple dosage strengths without requiring excessive amounts of active material.
3Ease of manufacture
If conventional binders are used, then the tablet can be formed, but flowability and compressibility are insufficient
Solution Approach 1:
The patent changes the particle size parameter of the binder from conventional specifications to a specific d(0.9) range of 15-250 µm. This parameter change simultaneously improves both flowability and compressibility by creating optimal particle morphology and size distribution. The specific particle size range allows for effective packing during compression while maintaining good flow characteristics during handling and dosing.
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 improved solubility, bioavailability, stability, and physicochemical properties such as flowability and compressibility, ensuring consistent drug delivery and long-term shelf life.
Implementation Method 1
binder has a d (0.9) particle size between 15 μm to 250 μm
Implementation Method 2
improved solubility and dissolution
Implementation Method 3
processed through wet granulation
Implementation Method 4
wet granulation
Implementation Method 5
film coating
Implementation Method 6
film coating
Data Source
AI summary
The present invention relates to a tablet formulation comprising selexipag or crystalline polymorph thereof and at least one binder, wherein binder has a d (0.9) particle size between 15 µm to 250 µm. Furthermore, the tablet is obtained using an effective process.