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Improve your solvent evaporation process in small molecule drug development with EXALT

Traditionally, small molecule drugs dominated the treatment of human diseases, due to their adaptable nature, size, and typical physiochemical properties. All of which help support highly effective enzyme inhibitor and allosteric modifier, plus the ability to target extracellular proteins, nuclei, and central nervous systems; small molecules, therefore, remain the major component of an ever-expanding therapeutic toolbox.

With a growing emphasis by industry and academia alike to patent specific crystal structures, the capability to carry out techniques like polymorph screening and identification of stable forms as efficiently as possible is becoming increasingly sought after, crystalline structures allow the drug to be soluble to the desired requirements of the purpose. This comes with several different challenges when trying to develop key crystalline structure in small molecule drug development.

EXALT is a specialised piece of technology that works alongside the Genevac EZ-2 4.0 range of centrifugal solvent evaporators, allowing operators the opportunity to retrieve a better level of evaporation rate control, leading to much improved results in their crystalline structure and information.

Crystalline formation within small molecule drug development

Polymorph screening is one of the key stages for drug development, as it allows the user to understand the crystal structure and formulation, which leads to future development and scale-up for manufacturing.

 

The importance of the technique is unrivalled; however, some users find crystallisation studies for polymorph screening to take a long time, and in some cases, difficult to conduct. This can come down to a few different reasons, one significant factor is the evaporation of different solvents within the drug development. Secondly, small molecule drug development can use highly sensitive materials, for example specific enzymes or proteins etc. Despite these factors, small molecules remain one of the main focuses in drug development; the use of EXALT technology as part of a development helps increase productivity, crystalline structure and better-informed decisions.

What is EXALT and how does it work?

EXALT was developed by Genevac’s experts in collaboration pharmaceutical companies from around the world, specifically to facilitate a wide range of solvents to be evaporated at the same time, and all at the same slow rate and is used for polymorph screening and stable form identification. For example, the EXALT can have DCM and Toluene placed in the same system and evaporated such that both samples dry at the same time.

By incorporating EXALT into your drug development process, you’ll benefit from the following features:

  • Up to 3ml of solvent can be processed within the boiling point range of 40ºC to 165ºC – DCM to DMAc.
  • Evaporation time can be controlled to range from 6 hours to 72 hours, or more, as required for solvent being used.
  • The system can deliver polymorphs of a drug at the same time, in a controlled and reproducible way.
  • EXALT uses a special holder for vials which allows a selection of baffles to be placed on top of the vial to slow the evaporation rate of the volatile solvents.

 

In some cases, no baffle is required. The holder is then placed in a Genevac evaporator which cycles the samples at atmosphere and at a slightly reduced pressure for the duration of the process.

 

The graph above demonstrates how evaporation is improved as EXALT controls solvent evaporation over time, with the special holders allowing the process of solvent evaporation to be under more control, whilst at same evaporation rate. This, in turn,

  • Reduces time
  • Reduces processing cost
  • Allows faster identification of crystalline structure.

The EXALT is being used by many of the world’s largest pharmaceutical companies. Why? It offers the user the security and ability to increase the production capabilities of drug development in the most efficient way, whilst employing a non-destructive technique meaning no waste of product in the process.

In conclusion, Genevac solvent evaporators already provide a trusted safety net and ongoing innovation in solvent evaporation technologies that help to speed up and improve up drug development processes. With EXALT technology, the process of crystalised formation can be fine-tuned to work every time. It will help revolutionise the overall R&D process and futureproof development through to production with a high success rate (c. 75%) resulting in crystals suitable for ongoing and advanced research, especially with small molecules for the therapeutics fields.

Learn more about the EXALT and the EZ-2 4.0, click here. Speak with our product specialists .