Paper on Fast Pharmaceuticals by APS Authors Featured in New Journal

AUGUST 11, 2011

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A paper authored by two Advanced Photon Source scientists, on “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,” is one of the first five papers published in volume 1, issue 1 of Physical Review X (PRX) a new, open-access journal. The publishers of PRX note that, “these papers, together with others that are to be published in the coming weeks into September, will constitute the first issue of the journal. Under PRX's open access publishing model, they are free for read and use.”

According to the authors of the paper, C.J. Benmore and J.K.R. Weber of the Argonne National Laboratory X-ray Science Division (XSD), “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, increase 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.”

The research was carried out at XSD x-ray beamline 11-ID-C at the U.S. Department of Energy Office of Science’s Advanced Photon Source at Argonne. Also participating in this research are Purdue University professors Steve Byrn and Lynne Taylor, and two graduate students, Ziyang Su and Xin Chen, also from Purdue University; Jeff Yager, Arizona State University; and Amit Tailor, a chemist with the Argonne X-ray Science Division.

See: C.J. Benmore and J.K.R. Weber, “Amorphization of Molecular Liquids of Pharmaceutical Drugs by Acoustic Levitation,” Phys. Rev. X 1, 011004 (Published August 8, 2011). DOI: 10.1103/PhysRevX.1.011004. URL: http://link.aps.org/doi/10.1103/PhysRevX.1.011004

See also: “A floating apothecary,” by Jessica Thomas, in APS Physics. “In an effort to make medicinal drugs that dissolve more quickly on delivery, scientists at Argonne National Laboratory in Illinois are using the technique of acoustic levitation to prepare molecular gels and amorphous solids. The technique could prove important for preparing several drugs that are known to be insoluble in crystalline form.” MORE >>

Use of the Advanced Photon Source at Argonne National Laboratory was supported by the DOE’s Office of Science under Contract No. DE-AC02-06CH11357.

The Advanced Photon Source at Argonne National Laboratory is one of five national synchrotron radiation light sources supported by the U.S. Department of Energy’s Office of Science to carry out applied and basic research to understand, predict, and ultimately control matter and energy at the electronic, atomic, and molecular levels, provide the foundations for new energy technologies, and support DOE missions in energy, environment, and national security. To learn more about the Office of Science x-ray user facilities, visit http://science.energy.gov/user-facilities/basic-energy-sciences/.

Argonne National Laboratory seeks solutions to pressing national problems in science and technology. The nation's first national laboratory, Argonne conducts leading-edge basic and applied scientific research in virtually every scientific discipline. Argonne researchers work closely with researchers from hundreds of companies, universities, and federal, state and municipal agencies to help them solve their specific problems, advance America's scientific leadership and prepare the nation for a better future. With employees from more than 60 nations, Argonne is managed by UChicago Argonne, LLC for the U.S. Department of Energy's Office of Science.