omation mbers - Society for Laboratory Automation and Screening
omation mbers - Society for Laboratory Automation and Screening
omation mbers - Society for Laboratory Automation and Screening
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WP068<br />
Anny Tangkilisan<br />
Symyx Technologies<br />
Life Sciences<br />
3100 Central Expressway<br />
Santa Clara, Cali<strong>for</strong>nia 95051<br />
atangkilisan@symyx.com<br />
Application of High Throughput <strong>Screening</strong> <strong>for</strong> Pre-<strong>for</strong>mulations Using the Symyx<br />
Technologies Workflow<br />
A high throughput crystallization system has been developed at Symyx Technologies with applications in pre<strong>for</strong>mulations.<br />
Capability of running over 384 different crystallizations/day with four different independently<br />
controlled heating/cooling environments <strong>and</strong> rapid serial screening will be described. Crystallizations are pre<strong>for</strong>med<br />
on the Symyx Technologies developed crystallization unit <strong>and</strong> screened using birefringence, Raman, XRD <strong>and</strong> a<br />
Symyx parallel melting point apparatus. All the screening data is stored into a database <strong>and</strong> sorted by using a<br />
proprietary software package developed at Symyx Technologies. Examples of a salt selection of ephedrine <strong>and</strong> a<br />
polymorph study of phenylbutazone using this system will also be presented.<br />
WP069<br />
Kerstin Thurow<br />
University of Rostock<br />
Institute <strong>for</strong> Aut<strong>omation</strong><br />
R.-Wagner-Strasse 31<br />
Rostock18119 Germany<br />
Kerstin.Thurow@uni-rostock.de<br />
Automated <strong>Screening</strong> of Cytotoxic Compounds<br />
225<br />
Co-Author(s)<br />
Kristin Entzian<br />
Toxicology <strong>and</strong> pharmacological activity of cytotoxic drugs where tested in a robotic high throughput screening<br />
cell assay (HTS), which allows prediction <strong>for</strong> the efficacy <strong>and</strong> <strong>for</strong> toxic effects of the drug. A robotic HTS system<br />
was assembled <strong>and</strong> programmed to seed cells in 96 well plates. The cell lines are incubated with a serial dilution<br />
of the test substance. After incubation <strong>for</strong> 2 to 3 days are metabolic indicator dye added. The remaining metabolic<br />
rate is measured after an additional incubation <strong>for</strong> several hours in a plate reader. The accumulation of dye in the<br />
remaining vital cells is plotted against the dilution of the test substance. The concentration of test substance where<br />
the absorbance is half of the maximum is considered the pharmacological activity or the toxic limit respectively.<br />
The activity is calibrated against the activity of substances with known cytotoxic activity <strong>and</strong> toxicity. The activity<br />
of Busulfan, Piposulfan <strong>and</strong> of several commonly used <strong>for</strong>mulation components such as Cremophor EL, PEG<br />
400, DMSO, Acetone, Ethanol <strong>and</strong> Cyclodextrin were tested against several carcinoma <strong>and</strong> non-carcinoma cell<br />
lines.The assay is reproducible <strong>and</strong> is able to rank cytotoxic compounds according to relative cytotoxicity. This<br />
assay is suitable <strong>for</strong> screening of cytotoxic compounds <strong>for</strong> cytotoxic activity as well as <strong>for</strong> general toxicity. The<br />
assay is also indicative of cytotoxic effects of excipients.<br />
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