Co-crystallized Sweetener Composition for Rapid Dissolution

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Solution Overview

Problem

Existing sweet receptor modulators, such as Compound I, face challenges with poor solubility and demixing issues when used in food and beverage compositions, leading to unsightly clumps and slow dissolution rates in aqueous solutions.

Innovation Solution

A sugar co-crystallized composition of 3-(4-amino-2,2-dioxide-1H-benzo[c][1,2,6]thiadiazin-5-yloxy)-2′,2′-dimethyl-N-propylpropanamide (Compound I) is developed, where the compound is uniformly dispersed with sugar through a process involving the formation of a hot concentrated sucrose/water syrup, incorporation of Compound I, and subsequent cooling and sieving to create agglomerates that enhance solubility and prevent clumping.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Compound I is used as a sweetener in food and beverage compositions, then sweetness enhancement is achieved, but solubility is poor and dissolution rate is slow

Engineering Contradiction:
Improvesweetness enhancement effectivenessVSAvoidsolubility and dissolution rate
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent creates a composite material by co-crystallizing Compound I with sugar, forming a new crystalline structure where Compound I molecules are incorporated into the sugar crystal lattice. This composite approach combines the sweetness enhancement property of Compound I with the high solubility of sugar, resolving the contradiction between effectiveness and solubility.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent changes the physical and chemical parameters of Compound I by forming co-crystals with sugar. This alters the dissolution behavior and solubility characteristics of Compound I, transforming it from a poorly soluble substance to one that dissolves rapidly in aqueous solutions while maintaining its sweetness enhancement function.

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If Compound I is mixed with sugar in simple powder form, then uniform blend is attempted, but demixing occurs and unsightly flocks form

Engineering Contradiction:
Improveuniformity of blendVSAvoiddemixing and flock formation
Core Design Contradiction:
Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent merges Compound I and sugar at the molecular level through co-crystallization, creating a single integrated crystalline structure rather than a physical mixture. This prevents demixing and flock formation because the two substances are chemically associated within the crystal lattice, maintaining uniformity throughout the composition.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

By forming a co-crystallized composite material, the patent creates a stable, homogeneous structure where Compound I and sugar are uniformly distributed at the molecular level within the crystal. This composite structure eliminates the segregation and flocking problems that occur in simple powder mixes.

Inventive Principle:
Principle #40Composite materials

3Reliability

If Compound I is used to enhance sweetness, then sweetener effectiveness is improved, but dissolution time increases

Engineering Contradiction:
Improvesweetener effectivenessVSAvoiddissolution time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The co-crystallized composite of Compound I and sugar provides rapid dissolution because sugar's high solubility drives the quick dissolution of the entire crystal structure. This maintains sweetener effectiveness while reducing dissolution time from potentially minutes to seconds.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent changes the dissolution parameters of Compound I by incorporating it into sugar crystals. This transformation reduces the dissolution time significantly while preserving the sweetness enhancement property, as the sugar matrix facilitates rapid dissolution in aqueous environments.

Inventive Principle:
Principle #35Parameter changes

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 sugar co-crystallized composition significantly accelerates the dissolution of Compound I in water, achieving rapid and uniform dispersion, preventing clumping, and maintaining the sweetener's effectiveness in various food and beverage applications.

Implementation Method 1

the co-crystallization of 3-(4-amino-2,2-dioxide-1H-benzo[c][1,2,6]thiadiazin-5-yloxy)-2′,2′-dimethyl-N-propylpropanamide (Compound I) having the structure: or salts thereof with sugar in various ratios

Methodology Applied
Scientific EffectCrystallization: Crystallisation

Implementation Method 2

heating the resultant mixture to form a hot concentrated sucrose/water syrup

Methodology Applied
Scientific EffectHeating: Heating

Implementation Method 3

removing the mixture from the heat and allowing the mixture to cool with vigorous agitation

Methodology Applied
Scientific EffectCooling: Cooling

Data Source

PatentUS11993821B2Co-crystallized sweeteners
Publication Date: 2024.05.28 FIRMENICH SA
  • US11993821B2 patent drawing
  • US11993821B2 patent drawing
  • US11993821B2 patent drawing

AI summary

Sweeteners made from the co-crystallization of 3-(4-amino-2,2-dioxide-1H-benzo[c][1,2,6]thiadiazin-5-yloxy)-2′,2′-dimethyl-N-propylpropanamide (Compound I) having the structure:or salt thereof, with sugar in various ratios. The sugar co-crystallized sweeteners are very soluble in water and have no dusting problems.