Sugar-Coated Solid Forms Mannitol Stearic Acid Stability

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Solution Overview

Problem

Conventional sugar-coating methods face challenges in achieving stability and humidity resistance for hygroscopic solid forms, particularly due to the low solubility of mannitol and the need for high dry material content, which limits the use of thermolabile ingredients and requires high temperatures.

Innovation Solution

A method using a combination of mannitol and fatty acids, specifically stearic acid, for sugar-coating solid forms, which involves spraying a sugar-coating liquid onto moving cores in a perforated rotary drum chamber with concomitant drying, eliminating the need for high dry material content and synthetic film-forming polymers like PVA.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If mannitol is used as crystallizable material for sugar-coating, then humidity resistance is improved, but solubility in water is insufficient to form adequate coating layers

Engineering Contradiction:
Improvehumidity resistanceVSAvoiddry material content
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent combines mannitol with hydrocolloid binders (guar gum, xanthan gum, locust bean gum, or starch) to create a composite coating composition. This composite approach allows the coating to achieve adequate adhesion and film formation at lower dry material contents (5-50% w/w) while maintaining the humidity resistance properties of mannitol, resolving the contradiction between humidity protection and coating formation capability.

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If high dry material content is used in sugar-coating syrup, then coating stability is improved, but thermolabile ingredients cannot be used due to high processing temperatures

Engineering Contradiction:
Improvecoating stabilityVSAvoidprocessing temperature
Core Design Contradiction:
Stability of the object's compositionVSTemperature

Solution Approach 1:

The patent changes the concentration parameter of dry material content in the coating syrup to a lower range (5-50% w/w) and combines it with hydrocolloid binders that provide adequate film formation at these lower concentrations. This parameter change allows the coating to be applied and dried at lower temperatures that do not degrade thermolabile active ingredients, while still achieving stable and adherent coating layers.

Inventive Principle:
Principle #35Parameter changes

3Shape

If conventional sugar-coating methods are used, then crystallized coating is achieved, but erosion and sticking of cores occur during processing

Engineering Contradiction:
Improvecrystallized coatingVSAvoidprocessing reliability
Core Design Contradiction:
ShapeVSReliability

Solution Approach 1:

The patent introduces hydrocolloid binders (guar gum, xanthan gum, locust bean gum, or starch) as intermediary substances that mediate between the crystallizable material (mannitol) and the core surface. These binders form a adhesive matrix that prevents core sticking during coating and reduces erosion, while still allowing crystallization of mannitol to occur and provide the desired coating structure and humidity resistance.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Illumination intensity

If titanium dioxide is added to maintain white color, then appearance is improved, but complexity of formulation increases

Engineering Contradiction:
Improvewhite color appearanceVSAvoidformulation complexity
Core Design Contradiction:
Illumination intensityVSDevice complexity

Solution Approach 1:

The patent replaces the permanent, complex formulation requirement of titanium dioxide with a temporary aesthetic solution: inherent white pigmentation from the core material itself or from the hydrocolloid binders used in the coating. This eliminates the need for additional pigment additives and simplifies the formulation while maintaining acceptable appearance during the product's shelf life, applying the principle of using simpler, shorter-lived aesthetic solutions when permanent solutions are unnecessarily complex.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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 method provides enhanced humidity resistance and stability, allowing for the use of low dry material content and lower temperatures, preventing erosion and sticking, and maintaining the white color of coated forms without the need for titanium dioxide.

Implementation Method 1

The hard and crystalline coating is obtained by applying this liquid and evaporating the water provided by it.

Methodology Applied
Scientific EffectEvaporation: Evaporation

Implementation Method 2

mannitol coating compositions...exhibiting a certain stability...provide an excellent humidity barrier

Methodology Applied
Scientific EffectHumidity barrier:

Implementation Method 3

The coating is characterized in that it uses a combination of mannitol and fatty acids, in particular stearic acid

Methodology Applied
Scientific EffectCrystallization: Crystallisation

Data Source

PatentUS20220008344A1Sugar-coated solid forms having improved stability
Publication Date: 2022.01.13 ROQUETTE FRERES SA
  • US20220008344A1 patent drawing
  • US20220008344A1 patent drawing
  • US20220008344A1 patent drawing

AI summary

The present invention relates to novel sugar-coated solid forms having improved stability, in particular a superior humidity resistance, and to a sugar-coating method which is particularly useful for the preparation of same.