Agomelatine Crystalline Form V Atomization Process
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Solution Overview
Problem
Crystalline form V of agomelatine has a weak durability over time, typically lasting less than six months, which poses challenges for its pharmaceutical use and storage stability.
Innovation Solution
A new process involving the atomization of a solution of agomelatine dissolved in miscible solvents with a boiling temperature less than 120°C, using an atomizer with compressed air or inert gas, such as nitrogen, to produce crystalline form V with enhanced stability and reproducibility.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If crystalline form V is obtained by conventional methods (grinding or seeding), then it can be produced, but its durability over time is weak (less than 6 months)
Solution Approach 1:
The patent changes the physical-chemical parameters of the crystallization process by using atomization instead of conventional grinding or seeding methods. This parameter change in the production process results in crystalline form V with enhanced durability and storage stability, extending its reliability from less than 6 months to over 21 months under standard storage conditions.
Solution Approach 2:
The patent utilizes phase transition during the atomization process, where the solution transitions from liquid to solid crystalline form through rapid evaporation and cooling. This controlled phase transition enables the formation of crystalline form V with improved structural stability and durability compared to conventional preparation methods.
2Duration of action of stationary object
If atomization is used to obtain crystalline form V, then durability is increased, but the process complexity increases
Solution Approach 1:
The patent replaces the mechanical grinding system with an atomization system that uses fluid dynamics and thermal processes. Instead of mechanical force to create crystals, the process uses sprayed solution droplets that undergo phase transition in a controlled atmosphere, simplifying the mechanical complexity while achieving superior durability results.
3Area of stationary object
If conventional methods are used to obtain crystalline form V, then the process is simple, but the specific surface area is smaller
Solution Approach 1:
The atomization process segments the solution into numerous fine droplets that rapidly solidify into small crystalline particles. This segmentation creates a much larger total surface area compared to conventional methods that produce larger crystals, while the automated atomization process maintains ease of manufacture through continuous production capability.
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 atomization process effectively increases the durability of crystalline form V, allowing it to maintain its characteristics for extended periods, such as 21 months under standard storage conditions, making it suitable for pharmaceutical use.
Implementation Method 1
a solution of agomelatine dissolved in one or two miscible solvents in all proportions and of which the boiling temperature is less than 120°C, is atomized in an atomizer
Implementation Method 2
Atomization is a technique commonly used in the food and pharmaceutical industries to dry a solution sprayed through a hot gas
Implementation Method 3
in the present invention, atomization made it possible to obtain a well-defined crystalline form, form V
Data Source
AI summary
Process for preparing crystalline form of N-[2-(7-methoxy-naphthalen-1-yl)-ethyl]-acetamide (or agomelatine) comprises dissolving a solution of agomelatine in one or two solvents miscible in all proportions, where the boiling temperature is less than 120[deg] C, and the solution is atomized in an atomizer. ACTIVITY : Antidepressant; Hypnotic; Cardiovascular-Gen.; CNS-Gen.; Muscular-Gen.; Eating-Disorders-Gen.; Anorectic. MECHANISM OF ACTION : 5-Hydroxytryptamine 2C receptor antagonist.