Polymeric Microcapsule Coating for Taste Masking

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Solution Overview

Problem

Current microencapsulation techniques for pharmaceuticals are lengthy, involve undesirable solvents, and have limitations in controlling microcapsule size and release rates, leading to issues with taste masking and controlled release of active ingredients.

Innovation Solution

A composition comprising a core material coated with a polymeric coating that includes a cationic and anionic polymer mixture, with a crosslinking agent, providing a uniform thickness ranging from 1 μm to 20 μm, which effectively taste-masks the core material and modifies its release profile in the oral cavity and gastrointestinal tract.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If simple or complex coacervation microencapsulation techniques are used, then microcapsules can be formed, but the processes are lengthy and involve undesirable solvents

Engineering Contradiction:
Improvemicrocapsule formationVSAvoidprocess duration
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The invention changes the chemical parameters of the coating solution by using pH-adjusted aqueous solutions with specific ionic strengths and compositions. The coating is applied by controlling pH transitions that trigger polymer precipitation and encapsulation, eliminating the need for organic solvents and lengthy processing steps while maintaining reliable microcapsule formation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention extracts and eliminates undesirable solvents from the microencapsulation process. By using aqueous-based coating solutions and pH-controlled precipitation, the method removes toxic organic solvents traditionally required in coacervation techniques, achieving faster and safer processing

Inventive Principle:
Principle #2Taking out (Extraction)

2Reliability

If coacervation techniques are used, then microcapsules can be formed, but unwanted agglomeration occurs

Engineering Contradiction:
Improvemicrocapsule formationVSAvoidmicrocapsule size control
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The invention applies local quality control by adjusting the coating solution properties and pH conditions specifically at the microcapsule surface during the coating process. This localized control prevents agglomeration by ensuring uniform coating deposition without causing particle clumping, while maintaining precise size control throughout the batch

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The method incorporates feedback control through monitoring and adjusting pH, ionic strength, and coating solution composition during the encapsulation process. This real-time adjustment prevents agglomeration by maintaining optimal conditions for uniform coating formation and precise microcapsule size control

Inventive Principle:
Principle #23Feedback

3Object-affected harmful factors

If polymeric coating with cationic and anionic polymers is applied, then taste masking is achieved, but the coating thickness must be precisely controlled

Engineering Contradiction:
Improvetaste maskingVSAvoidcoating thickness uniformity
Core Design Contradiction:
Object-affected harmful factorsVSManufacturing precision

Solution Approach 1:

The invention performs preliminary action by pre-adjusting the pH and ionic strength of the coating solution before application. This pre-conditioning ensures that the coating deposits uniformly at the desired thickness from the first application, achieving consistent taste masking without requiring multiple coating cycles or precise thickness control during application

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The method uses composite polymeric materials combining cationic and anionic polymers in a single coating formulation. This composite approach provides effective taste masking while the synergistic interaction between oppositely charged polymers enables uniform coating deposition at controlled thicknesses, reducing manufacturing precision requirements

Inventive Principle:
Principle #40Composite materials

4Reliability

If conventional coating methods are used, then core material can be enclosed, but controlled release rates cannot be effectively achieved

Engineering Contradiction:
Improvecore material enclosureVSAvoidrelease rate control
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The invention achieves controlled release by changing the physical-chemical parameters of the polymeric coating through pH adjustment and ionic strength control. The coating's mesh size, porosity, and degradation rate are tuned by these parameters, enabling precise control over drug release kinetics while maintaining reliable core material enclosure

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The method creates a dynamic coating system where the polymeric structure responds to environmental pH changes and ionic conditions. This dynamic behavior allows the coating to maintain structural integrity for enclosure while enabling controlled release through pH-triggered swelling, shrinking, or degradation, achieving both reliable enclosure and tunable release rates

Inventive Principle:
Principle #15Dynamics

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 polymeric coating effectively masks the taste of active pharmaceutical ingredients like acetaminophen and ibuprofen, achieving a controlled release that is faster than uncoated forms, with up to 95% of the core material dissolving within predetermined times, enhancing bioavailability and patient compliance.

Implementation Method 1

Simple or complex coacervation microencapsulation techniques can be used to make microcapsules

Methodology Applied
Scientific EffectCoacervation: Coacervate

Implementation Method 2

the polymer coating further includes a crosslinking agent

Methodology Applied
Scientific EffectCrosslinking: Chemical Bonding

Implementation Method 3

The release rate of the core material and the diffusion of the core material through the capsule wall can be controlled

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentUS11723877B2Microencapsulation process and product
Publication Date: 2023.08.15 SPI PHARMACEUTICALS INC
  • US11723877B2 patent drawing
  • US11723877B2 patent drawing
  • US11723877B2 patent drawing

AI summary

A composition comprising a core material, having a taste value and a polymeric coating. The polymeric coating substantially surrounds the core material and comprises a cationic polymer and optionally an anionic polymer. The polymeric coating has a uniform thickness ranging from 2 μm to 20 μm. The composition provides release of a portion of the core material which is taste masked over a time period ranging from 0.5 minute to 2 minutes in the oral cavity and provides a modified-release of the remaining core material in a gastrointestinal tract.