Pellets Coated with Amphiphilic Copolymers for Stable Solubilization
Solution Overview
Problem
Existing methods for solubilizing poorly water-soluble substances in pharmaceutical and other applications face challenges due to instability of solid solutions, stickiness of solubilizers, and equipment-intensive processes like extrusion, which can cause temperature stresses.
Innovation Solution
Development of pellets coated with amphiphilic copolymers formed from N-vinyl lactam, vinyl acetate, and polyether, produced by radically initiated polymerization, where the active ingredients are embedded in a coating made by spraying a solution onto a fluidized bed of carrier particles, allowing for improved solubility and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If known polymeric solubilizers are used, then solubilization of poorly water-soluble substances is achieved, but stable solid solutions are not formed
Solution Approach 1:
The patent uses a composite polymer system comprising poly(N-vinyl lactam) as the primary solubilizing component combined with polyether as a secondary component. This composite structure leverages the strong solubilization capability of poly(N-vinyl lactam) while the polyether component enhances solid solution stability through its amphiphilic nature and ability to form stable molecular complexes with hydrophobic active ingredients.
2Ease of manufacture
If known solubilizers are used, then solubilization is achieved, but the solubilizers are sticky and do not represent sufficiently flowable powders
Solution Approach 1:
The patent modifies the physical parameters of the solubilizer by controlling the molecular weight, degree of polymerization, and compositional ratios of the poly(N-vinyl lactam) and polyether components. These parameter changes optimize the balance between solubilization effectiveness and powder flowability, reducing stickiness while maintaining solubilization capability.
3Ease of manufacture
If extrusion process is used, then mixing of active ingredients with solubilizer is achieved, but a lot of equipment is required and temperature stresses occur
Solution Approach 1:
The patent replaces the mechanical extrusion process with a spray-drying process. Instead of using complex extrusion equipment that requires high temperatures and mechanical mixing, the invention uses a spray system to atomize the active ingredient and solubilizer mixture, which then dries rapidly in a fluidized bed, achieving uniform distribution without extensive mechanical mixing or high-temperature stress.
4Ease of manufacture
If extrusion process is used, then mixing of active ingredients with solubilizer is achieved, but undesirable temperature stresses on the starting materials occur
Solution Approach 1:
The patent replaces the thermal-mechanical extrusion process with a spray-drying process that operates at significantly lower temperatures. The spray-drying method achieves mixing and encapsulation through rapid solvent evaporation rather than thermal processing, thereby eliminating undesirable temperature stresses on heat-sensitive active ingredients and solubilizer materials.
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 process enables the creation of stable, bioavailable solid solutions with high active ingredient loading, reducing the need for extensive equipment and minimizing temperature stresses, while ensuring effective solubilization and controlled release of active ingredients.
Implementation Method 1
spraying a solution containing one or more active ingredients and an amphiphilic copolymer onto a fluidized bed of carrier particles
Implementation Method 2
spraying a solution containing one or more active ingredients and an amphiphilic copolymer onto a fluidized bed of carrier particles
Implementation Method 3
amphiphilic copolymers are obtained by radically initiated polymerization of a mixture
Data Source
AI summary
The invention relates to preparations of active substances of low solubility in water, made of carrier particles having coatings containing active substances, wherein the active substances of low solubility are embedded in coatings made of amphiphilic copolymers.