Spray Drying Sustained-Release Formulations

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Solution Overview

Problem

The manufacture of sustained-release formulations is hindered by the decomposition of active ingredients due to stringent conditions in kneading and drying processes, leading to performance decline and stability issues.

Innovation Solution

A method involving spray drying with controlled exit temperature to minimize solvent content and prevent active ingredient decomposition, using a composition of active ingredient, resin, and release control agents, specifically with styrene-maleic anhydride copolymer and hydrophobic silica, to produce a stable and efficient sustained-release formulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If kneading and granulation are conducted to formulate the active ingredient with resin and release control agents, then uniform matrix formation is achieved, but decomposition of the active ingredient occurs due to pressure, shear force, and thermal history

Engineering Contradiction:
Improveuniformity of matrixVSAvoidstability of active ingredient
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent replaces the mechanical kneading and granulation process with a spray drying process. Instead of using mechanical force to mix and form the matrix, the formulation is applied as a liquid composition that is sprayed into a drying chamber, allowing the matrix to form through evaporation rather than mechanical action. This eliminates the harmful mechanical stresses that cause active ingredient decomposition.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent changes the physical state and processing parameters from solid-state mechanical processing to liquid-state spray drying. By formulating as a liquid composition and using spray drying with controlled temperature and airflow parameters, the process achieves uniform matrix formation without the high pressure, shear force, and thermal history associated with conventional kneading and granulation.

Inventive Principle:
Principle #35Parameter changes

2Loss of substance

If conventional drying processes are used to remove solvents, then solvent removal is achieved, but thermal history causes decomposition of the active ingredient

Engineering Contradiction:
Improvesolvent contentVSAvoidstability of active ingredient
Core Design Contradiction:
Loss of substanceVSReliability

Solution Approach 1:

The patent replaces conventional thermal drying with spray drying, which uses a combination of atomization and rapid evaporation in a controlled airflow environment. This substitution allows for much faster solvent removal with significantly reduced thermal exposure, preventing active ingredient decomposition while achieving the same solvent removal objective.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The spray drying process rapidly evaporates solvents in a short residence time, essentially 'skipping through' the drying phase before thermal decomposition can occur. The liquid composition is sprayed into fine droplets that quickly evaporate in the drying chamber, removing solvents before prolonged thermal exposure could harm the active ingredient.

Inventive Principle:
Principle #21Skipping (Rushing through)

3Loss of substance

If spray drying is used to remove solvents rapidly, then solvent content is reduced, but decomposition may occur if exit temperature is not controlled

Engineering Contradiction:
Improvesolvent contentVSAvoidstability of active ingredient
Core Design Contradiction:
Loss of substanceVSReliability

Solution Approach 1:

The patent implements temperature control in the spray drying process, specifically controlling the exit temperature to prevent active ingredient decomposition. By monitoring and controlling the temperature parameters throughout the spray drying process, the system achieves rapid solvent removal while maintaining conditions that protect the active ingredient from thermal degradation.

Inventive Principle:
Principle #23Feedback

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

This method effectively prevents active ingredient decomposition and reduces solvent content, enabling the stable and efficient production of sustained-release formulations with controlled release properties.

Implementation Method 1

a step of spray drying a liquid composition using a spray dryer, characterized in that exit temperature in the spray drying is controlled

Methodology Applied
Scientific EffectEvaporation: Evaporation

Implementation Method 2

exit temperature in the spray drying is controlled; solvent content in the composition after spray drying is 5 mass % or less

Methodology Applied
Scientific EffectHeating: Heating

Data Source

PatentEP2305029B1Method for producing extended-release preparation composition
Publication Date: 2018.06.13 NIPPON SODA CO LTD

AI summary

The present invention offers a method of manufacture of sustained-release formulation composition which includes a step of spray drying a composition that contains (1) an active ingredient, (2) a resin ingredient, and (3) a solvent, using a spray dryer and controlling the exit temperature of the spray dryer, wherein solvent content in the composition after spray drying is 5 mass % or less, and the composition after the aforementioned spray drying does not substantially contain decomposed matter of the aforementioned active ingredient.