Crystalline Solid Dispersion for Rapid Dissolution
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Solution Overview
Problem
Existing delivery systems for poorly water-soluble solid active ingredients, such as Compound I, fail to enhance the dissolution rate effectively, and methods like spray drying and melt spinning can produce amorphous or glassy solids that are disadvantageous for certain applications.
Innovation Solution
A delivery system comprising a crystalline matrix material, preferably erythritol, with the active ingredient dispersed throughout, formed by melting the carrier material, incorporating the active ingredient, and cooling to create discrete particles, which are then optionally ground to enhance dissolution kinetics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If spray drying or melt spinning is used to prepare solid dispersions, then the active ingredient dissolution rate is improved, but the resulting amorphous or glassy solids are disadvantageous for certain applications
Solution Approach 1:
The invention changes the physical state parameter of the carrier material from amorphous/glassy to crystalline. This is achieved by selecting specific crystalline carrier materials (such as sugars, sugar alcohols, or amino acids) and controlling the processing conditions to maintain crystalline structure while still achieving rapid dissolution of the active ingredient through the crystalline matrix effect.
Solution Approach 2:
The invention creates a composite material system consisting of crystalline carrier material particles with active ingredient dispersed within the crystalline matrix. This composite structure combines the stability of crystalline materials with the dissolution-enhancing properties of solid dispersions, where the active ingredient is intimately mixed within the crystalline carrier particles.
2Speed
If the active ingredient is dispersed in a crystalline matrix, then the dissolution rate is significantly improved, but the process complexity increases compared to simple mixing
Solution Approach 1:
The invention utilizes phase transition of the carrier material between solid and liquid states to achieve intimate mixing and uniform dispersion of the active ingredient. The carrier is melted to form a liquid matrix where active ingredient disperses uniformly, then cooled to solidify into a crystalline structure, creating homogeneous solid dispersion particles without complex equipment.
3Speed
If the active ingredient has slow dissolution rate like Compound I, then the sweetening effect cannot be achieved at desired speed, but increasing the amount of active ingredient is not feasible
Solution Approach 1:
The invention applies local quality enhancement by creating intimate contact between the active ingredient and aqueous environment through the crystalline matrix structure. The active ingredient is dispersed at molecular or micromolecular level within the crystalline carrier particles, creating numerous local dissolution sites that dramatically increase the effective dissolution rate without increasing the total amount of active ingredient needed.
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 crystalline delivery system significantly improves the dissolution rate of the active ingredient, preventing raft formation and ensuring uniform distribution, leading to enhanced wetting and faster dissolution in aqueous environments.
Implementation Method 1
leading to enhanced wetting and faster dissolution in aqueous environments
Implementation Method 2
cooling the discrete particles
Implementation Method 3
ensuring uniform distribution
Data Source
AI summary
A delivery system in the form of a solid dispersion comprises (i) a carrier material consisting essentially of a crystalline matrix material, such as erythritol or mannitol and (ii) a solid active ingredient having the structure: (Compound I) or salts thereof wherein the solid active ingredient (ii) is dispersed throughout a matrix of the carrier material (i).