• Featured in Physics
  • Open Access

Amorphization of Molecular Liquids of Pharmaceutical Drugs by Acoustic Levitation

C. J. Benmore and J. K. R. Weber
Phys. Rev. X 1, 011004 – Published 8 August 2011
Physics logo See Synopsis: A floating apothecary

Abstract

It is demonstrated that acoustic levitation is able to produce amorphous forms from a variety of organic molecular compounds with different glass forming abilities. This can lead to enhanced solubility for pharmaceutical applications. High-energy x-ray experiments show that several viscous gels form from saturated pharmaceutical drug solutions after 10–20 min of levitation at room temperature, most of which can be frozen in solid form. Laser heating of ultrasonically levitated drugs can also result in the vitrification of molecular liquids, which is not attainable using conventional amorphization methods.

  • Figure
  • Figure
  • Figure
  • Figure
  • Figure
  • Received 22 February 2011

DOI:https://doi.org/10.1103/PhysRevX.1.011004

This article is available under the terms of the Creative Commons Attribution 3.0 License. Further distribution of this work must maintain attribution to the author(s) and the published article’s title, journal citation, and DOI.

Published by the American Physical Society

Synopsis

Key Image

A floating apothecary

Published 8 August 2011

Levitation technique provides a way to solidify pharmaceutical drugs in a highly soluble form.

See more in Physics

Authors & Affiliations

C. J. Benmore and J. K. R. Weber

  • X-ray Science Division, Advanced Photon Source, Argonne National Laboratory, Argonne, Illinois 60439, USA

Popular Summary

Making fast acting drugs is a goal of almost every pharmaceutical company. The route of delivering them in the forms of amorphous solids has long been recognized as a possible way to enhance dissolution rates and increase both solubility and bioavailability. The development in this direction is becoming increasingly important due to the emergence of many new drugs that are virtually insoluble in their crystalline forms. In this experimental paper, we exploit the technique of acoustic levitation of liquid droplets and present two new methods for forming amorphous solids from molecular liquids and solutions of a wide range of pharmaceutical drugs of varying chemical structures and different functions. One method combines acoustic levitation with solvent evaporation and produces amorphous gels of the drugs; the other integrates laser-heating induced melting and subsequent cooling with acoustic levitation and turns drugs that are usually obtained in crystalline, functionally less effective forms to more desirable amorphous forms (a process also known as vitrification in materials science and engineering). Proof-of-principle applications of the two containerless methods are demonstrated with in situ characterizations of the samples by use of high-energy x-ray diffraction at the Advanced Photon Source.

We anticipate that such containerless processing methods, combined with sophisticated, high-throughput droplet-forming or dispensing methods, may provide practical routes for scaled-up productions of amorphous drugs.

Key Image

Article Text

Click to Expand

References

Click to Expand
Issue

Vol. 1, Iss. 1 — August - September 2011

Subject Areas
Reuse & Permissions
Access Options
CHORUS

Article part of CHORUS

Author publication services for translation and copyediting assistance advertisement

Authorization Required


×
×

Images

×

Sign up to receive regular email alerts from Physical Review X

Reuse & Permissions

It is not necessary to obtain permission to reuse this article or its components as it is available under the terms of the Creative Commons Attribution 3.0 License. This license permits unrestricted use, distribution, and reproduction in any medium, provided attribution to the author(s) and the published article's title, journal citation, and DOI are maintained. Please note that some figures may have been included with permission from other third parties. It is your responsibility to obtain the proper permission from the rights holder directly for these figures.

×

Log In

Cancel
×

Search


Article Lookup

Paste a citation or DOI

Enter a citation
×