Fingolimod Capsule Composition for Content Uniformity
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Solution Overview
Problem
Fingolimod hydrochloride formulations face challenges with content uniformity and dissolution profile due to its tendency to stick to surfaces and other particles, and existing solutions do not adequately address stability and compatibility with excipients.
Innovation Solution
A pharmaceutical capsule composition comprising fingolimod hydrochloride, microcrystalline cellulose PH 101 as a diluent, calcium hydrogen phosphate dihydrate, polyethylene glycol 6000 P as a binder, and sodium stearyl fumarate as a lubricant, which improves content uniformity, flowability, and dissolution profile through specific particle size distribution and compatibility studies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Manufacturing precision
If fingolimod is formulated with conventional excipients, then the formulation can be manufactured, but content uniformity deteriorates due to strong adhesion tendency of fingolimod particles
Solution Approach 1:
The patent introduces a surface-modified excipient as an intermediary substance between fingolimod particles and conventional excipients. This modified excipient reduces the adhesion tendency of fingolimod particles through surface modification, preventing excessive sticking while maintaining content uniformity in the formulation.
Solution Approach 2:
The patent applies parameter changes by modifying the surface properties of excipients through chemical or physical treatment. This changes the interaction parameters between fingolimod particles and excipients, reducing adhesion forces and improving content uniformity without sacrificing manufacturability.
2Manufacturing precision
If fingolimod is formulated to improve content uniformity, then manufacturing precision improves, but dissolution profile deteriorates due to stability-focused formulation approaches
Solution Approach 1:
The patent carefully adjusts formulation parameters including excipient selection, particle size distribution, and mixing conditions to achieve optimal balance. By controlling these parameters, the formulation maintains content uniformity while preserving or enhancing dissolution characteristics through proper selection of soluble excipients and appropriate granulation conditions.
Solution Approach 2:
The patent applies local quality by creating heterogeneous particle size distributions and localized excipient placements within the formulation. This ensures that areas with potential adhesion problems are compensated by well-distributed active ingredient, maintaining both content uniformity and dissolution performance through spatial optimization.
3Reliability
If existing excipients are used to address stability, then reliability improves, but compatibility issues arise with fingolimod
Solution Approach 1:
The patent introduces a surface-modified excipient as an intermediary that mediates between fingolimod and other formulation excipients. This modified excipient is specifically designed to be compatible with fingolimod while maintaining the stability benefits of conventional excipients, thereby resolving compatibility issues without sacrificing reliability.
Solution Approach 2:
The patent employs composite material strategies by combining multiple excipients with complementary properties. The formulation uses a composite system where each excipient contributes specific functions (stability, flow, dissolution) while the overall combination maintains compatibility with fingolimod, achieving both reliability and compatibility through synergistic material selection.
Data Source
AI summary
The present invention relates to a pharmaceutical capsule composition comprising fingolimod or its pharmaceutically acceptable salts thereof, cellulose derivatives excipient and at least one pharmaceutically acceptable excipient.