LabAutomation 2006 - SLAS

TP47
Jun Qiu
Bristol-Myers Squibb
New Brunswick, New Jersey
jun.qiu@bms.com
Where Laboratory Technologies Emerge and Merge
Co-Author(s)
Erik Rubin
Edward Delaney
Impact of an Automated Solubility Workflow on Pharmaceutical Process Research and
Development at Bristol-Myers Squibb
Solubility is frequently a critical parameter in pharmaceutical process development, but for countless practical reasons, this important
measurement is often not adequately pursued by PR&D scientists. To fill this gap, Bristol-Myers Squibb (BMS) acquired a Symyx solubility
workflow and began offering a solubility determination service in late 2003. In two years, the solubility team has worked on dozens of
projects and provided thousands of solubility measurements. This automated workflow allowed a large number of solvents and conditions
to be screened, and led to unexpected observations in many cases. As a result, it has significantly affected how processes are developed
in PR&D, and its success inspired development of other services that will be deployed in the near future.
TP48
Catherine Quintero
Merck
Boston, Massachusetts
catherine_quintero@merck.com
Co-Author(s)
Craig Rosenstein
Richard E. Middleton
Ilona Kariv
Merck
Quantitative Evaluation and Comparison of Piezoelectric and Acoustic Nanoliter
Dispense Technologies
Nanoliter compound dispensing has become an essential part of miniaturized screens in high density plate formats. As random screening
progresses to the lead optimization stage, the ability to generate response curves with high accuracy and precision becomes even more
critical. Thus, novel liquid dispensers able to deliver nanoliter volumes of compounds in DMSO, allowing conservation of compound as
well as eliminating the need for intermediate compound dilutions steps to minimize DMSO concentrations, are becoming an integral part
of miniaturized assays. We have evaluated accuracy and precision of two different nanodispensers, Aurora PicoRapTR, which employs
piezo-dispensing technology, and the Labcyte Echo, which relies on acoustic wave dispensing, and compared these instruments
to traditional approaches. Among the challenges in evaluating the performance of nanodispensers is choosing between the different
standard methods available to find the most reliable strategy to measure dispense volumes. For this task the fluorophore, Alexa Fluor, was
used instead of the traditional Fluorescein due to Alexa Fluor’s resistance to photo-bleaching and higher quantum yield. We have tested
accuracy and precision under a variety of conditions and over a wide volume range to determine parameters to reproducibly and reliably
generate compound dose titrations using both instruments. The results of this study validate the use of nanoliter dispense technology for
the titration of compounds in high-throughput lead optimization strategies.
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