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Synthesizing Amorphous Pharmaceuticals Using Containerless Processing

Argonne National Laboratory

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(a) Acoustic levitator simultaneously levitates several samples (shown as white spheres). Illustrations on either side of the levitator show two methods used in this study to create amorphous forms of pharmaceutical drugs. (b) Melted in the levitator, pure cinnarizine forms a yellow amorphous product; in the laser hearth, it forms a white crystalline product.
(a) Acoustic levitator simultaneously levitates several samples (shown as white spheres). Illustrations on either side of the levitator show two methods used in this study to create amorphous forms of pharmaceutical drugs. (b) Melted in the levitator, pure cinnarizine forms a yellow amorphous product; in the laser hearth, it forms a white crystalline product.

Technology Marketing Summary

Scientists at Argonne National Laboratory have created a process by which amorphous and nanophase pharmaceutical compounds can be synthesized without the use of a container, thus avoiding potential contamination. The process involves acoustic levitation—that is, a technique in which an object is suspended through pressure created by intense sound waves—to form molecular gels and amorphous solids. The method is expected to help pharmaceutical manufacturers create drugs that dissolve more quickly on delivery.

Description

The containerless method involves the use of a levitator, a chamber in which objects can be suspended through sound-wave pressure. Argonne scientists developed two protocols using this technique on several over-the-counter and prescription medicines. In the first method, the team dissolved such drugs as ibuprofen and the antibiotic clofoctol in ethanol, and then allowed droplets of the solution to evaporate while suspended in the levitator. In the second method, researchers used a laser to melt the antihistamine cinnarizine into droplets and suspend them as they cooled. 

Benefits

A significant benefit offered by this process is that it does not use a container, since one cause of crystallinity in the manufacture of glassy drugs is heterogeneous nucleation caused by the interaction of the liquid with its container. Once perfected, this process is expected to advance the development of bulk amorphous drug forms, which are becoming increasingly important due to the emergence of new drugs that are virtually insoluble in their crystalline form.

Applications and Industries

?   Pharmaceutical industry

More Information

The proof-of-principle was established using high energy X-ray diffraction to characterize the amorphous nature of the drugs.  The process was successfully demonstrated on several reluctant glass forming drug molecules using both the evaporation and laser melting technique. In most cases, the shelf life of these drugs was found to be several months. Reference: C. J. Benmore and J. K. R. Weber, “Amorphization of Molecular Liquids of Pharmaceutical Drugs by Acoustic Levitation,” Phys. Rev. X 1, 011004 (2011), http://prx.aps.org/abstract/PRX/v1/i1/e011004.

Patents and Patent Applications
ID Number
Title and Abstract
Primary Lab
Date
Application 20120197005
Application
20120197005
CONTAINERLESS SYNTHESIS OF AMORPHOUS AND NANOPHASE ORGANIC MATERIALS
The invention provides a method for producing a mixture of amorphous compounds, the method comprising supplying a solution containing the compounds; and allowing at least a portion of the solvent of the solution to evaporate while preventing the solute of the solution from contacting a nucleation point. Also provided is a method for transforming solids to amorphous material, the method comprising heating the solids in an environment to form a melt, wherein the environment contains no nucleation points; and cooling the melt in the environment.
01/30/2012
Filed
Technology Status
Technology IDDevelopment StageAvailabilityPublishedLast Updated
ANL-10-011PrototypeAvailable02/11/201302/11/2013

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