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Next generation solution
for automated physchem
          measurement
SiriusT3 Assays
pKa assays:                                                                 Distribution of species
- Determine pKa values to the highest commercially
  available accuracy
- Generate distribution of species plots
- Determine buffer capacity

Understanding the ionisation state of a drug and how it varies with
pH provides key information about the proportion of species available
for absorption.


Running pKa determinations in different media reveals detailed
information about how the pKa changes due to solvent interactions,
partitioning, precipitation or binding.


logP assays:                                                                Lipophilicity profile
- Determine logP
- Determine logD vs. pH
- Study octanol/water & many other mixtures


Understanding the logP and logD reveal how the ionisation state of
the molecule influences its lipophilicity. This information can be used
to improve ADME predictions as well as evaluating how changes
to the molecule can increase/decrease the lipophilicity for a
desired application.


Solubility assays:                                                          pH vs. Solubility profile
- Determine intrinsic solubility
- Determine kinetic solubility
- Derive pH vs. solubility profile
- Determine supersaturation


Solubility is a complex and fundamental parameter affecting drug
absorption. Understanding the full kinetics of supersaturation,
precipitation, dissolution and the relationship between solubility
and pH is crucial to understanding the ADME behaviour of a
drug molecule.


Dissolution assays:                                                         Dissolution profile with variable pH
- Profile drugs for dissolution and precipitation rates
- Explore the effects of changing pH
- Run assays with excipients, additives and biorelevant media


Dissolution assays with pH control and in the presence of excipients
and biorelevant media (FaSSIF/FeSSIF) can be used to evaluate the
effects of different formulations on the dissolution and precipitation
kinetics. This infomation can aid the selection of appropriate
formulations for different routes of administration.



SiriusT3 automation reduces operator time and replaces the need for time consuming shake-flask style
experiments and reliance on multiple pH buffers.

Measuring physchem data at early stages of drug development reduces the risk of costly late stage failures.
SiriusT3 key features and benefits

                              ·   pKa, logP, logD, pH-Solubility         ·   Fully automated cosolvent assays
                                  profiling and dissolution integrated       included as standard.
                                  on a single system.
                                                                         ·   Measure under physiologically
                              ·   Full automation - no manual moving          relevant conditions.
                                  or cleaning of probes required.
                                                                         ·   Study effects of solvents, excipients,
                              ·   Minimal running costs - uses off the       additives, biorelevant media.
                                  shelf reagents with no special
                                  “kits” required.
                                                                         ·   pH range of 1.8 - 12.2, extendable
                                                                             to 0.5 - 13.5 with UV options.
                              ·   Built in ultra-sonic bath to aid
                                                                         ·   Powerful software can model
                                  measurements of insoluble                   effects of ionisation, partitioning,
                                  compounds.                                  precipitation and solvent shifts.
                              ·   1ml assay volume, less than 1mg
                                  of sample required for most
                                  experiments.                                              s
                              ·   Automatic calibration and cleaning
                                  protocols.
                                                                                    Detailed Data
                              ·   Built-in automatic turbidity
                                  detection - precise detection of                          s
                                  precipitation events.
                              ·   Computer controlled temperature
                                                                                Better Decisions
                                  management - no water circulator
                                  required.
                                                 s

                                     Time & Cost Savings
                                                 s

                                   Improved Efficiency




               The SiriusT3 allows
          physchem measurements to be
     performed on sub-milligram quantities
   of material. This revolution allows the best
  quality data to be obtained even on discovery
 compounds where sample quantity is a limiting
 factor. By obtaining high quality information at                                          Ordering Information:
      an earlier stage in the discovery and                                               Interested in SiriusT3?
development process, decisions about chemistry                                             Contact us to arrange
  changes and formulation routes can be made                                                 a demonstration or
   early, saving money, and potential problem                                              free of charge sample
    areas in other assays can be indentified                                                     evaluation
             and resolved with ease.
SiriusT3 Technical Specification

 pH electrode:                           Ag/AgCI, double junction reference

 Stirrer:                                Overhead, variable speed, computer controlled

 Temperature probe:                      Thermocouple, Temperature measured with every datapoint

 Temperature control:                    Peltier, Range: 12°C to 70°C

 Turbidity detection:                    Pass-through light detection – percentage light detected reported to 0.1%

                                         Water, Acid, Base, partition solvent, CoSolvent (six-installed, via automated 6-way valve), minimum
 Precision dispensers:
                                         volume of 0.024m L

 MultiTip dispenser:                     Multi-tip capillary bundle

 Probe movement:                         Fully automated X-Y axis on titrator module

 Electrode storage/calibration:          Home position for electrode storage and pH7 buffer positions for calibration

 Washes:                                 Two static washes and flowing water wash station

 Autoloader:                             Holds up to 192 samples, automatic gripper arm for transfer to sample position

 Purge gas:                              Two internal flow meters, nitrogen or argon supply required

 Partition solvents:                     Supports 7 including Octanol, Dodecane, Toluene

 CoSolvents:                             Supports 10 including Methanol, Acetonitrile, DMSO and MDM

 System standardisation:                 Sirius Four-Plus™ procedure

 pH-range:                               1.8 - 12.2

 Assay volume:                           0.5 to 3.5mls

 Services required:                      One mains power inlet (110 or 240 V), 50-60Hz

 Connection to the PC:                   USB

                                         Intel compatible processor, 2GB Memory, 10GB Available disk space, one free USB port,
 Computer:
                                         CD/DVD-ROM-drive, 1280x1024 screen resolution. XP/Vista/Windows7 with IE6 or higher.

                                         For indoor use only
                                         Altitude ≤ 2000m
                                         Temp. 5°C to 40°C
 Environment:                            Max relative humidity 80% @ 31°C
                                         Mains voltage fluctuation +/- 10%
                                         Installation overvoltage Cat II
                                         Pollution degree 2

 Physical Dimensions                                  Weight                        Height              Width                   Depth
 Dispenser module                                 35kg/77.16lbs                    700mm               260mm                   460mm

 Titrator                                         23kg/50.71lbs                    490mm                215mm                  460mm

 Autoloader                                       27kg/59.52lbs                    490mm               350mm                   460mm

 Total                                           85kg/187.39lbs                    700mm               825mm                   460mm




                                                                        Distributed by:




Sirius Analytical, Inc
100 Cummings Center,
Suite 231c,
Beverly,
MA 01915-6126
Telephone:   978 338 5790
Fax:         866 410 7668
Email:       sales@sirius-ai.com
web:         www.sirius-analytical.com

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SiriusT3 Brochure

  • 1. Next generation solution for automated physchem measurement
  • 2. SiriusT3 Assays pKa assays: Distribution of species - Determine pKa values to the highest commercially available accuracy - Generate distribution of species plots - Determine buffer capacity Understanding the ionisation state of a drug and how it varies with pH provides key information about the proportion of species available for absorption. Running pKa determinations in different media reveals detailed information about how the pKa changes due to solvent interactions, partitioning, precipitation or binding. logP assays: Lipophilicity profile - Determine logP - Determine logD vs. pH - Study octanol/water & many other mixtures Understanding the logP and logD reveal how the ionisation state of the molecule influences its lipophilicity. This information can be used to improve ADME predictions as well as evaluating how changes to the molecule can increase/decrease the lipophilicity for a desired application. Solubility assays: pH vs. Solubility profile - Determine intrinsic solubility - Determine kinetic solubility - Derive pH vs. solubility profile - Determine supersaturation Solubility is a complex and fundamental parameter affecting drug absorption. Understanding the full kinetics of supersaturation, precipitation, dissolution and the relationship between solubility and pH is crucial to understanding the ADME behaviour of a drug molecule. Dissolution assays: Dissolution profile with variable pH - Profile drugs for dissolution and precipitation rates - Explore the effects of changing pH - Run assays with excipients, additives and biorelevant media Dissolution assays with pH control and in the presence of excipients and biorelevant media (FaSSIF/FeSSIF) can be used to evaluate the effects of different formulations on the dissolution and precipitation kinetics. This infomation can aid the selection of appropriate formulations for different routes of administration. SiriusT3 automation reduces operator time and replaces the need for time consuming shake-flask style experiments and reliance on multiple pH buffers. Measuring physchem data at early stages of drug development reduces the risk of costly late stage failures.
  • 3. SiriusT3 key features and benefits · pKa, logP, logD, pH-Solubility · Fully automated cosolvent assays profiling and dissolution integrated included as standard. on a single system. · Measure under physiologically · Full automation - no manual moving relevant conditions. or cleaning of probes required. · Study effects of solvents, excipients, · Minimal running costs - uses off the additives, biorelevant media. shelf reagents with no special “kits” required. · pH range of 1.8 - 12.2, extendable to 0.5 - 13.5 with UV options. · Built in ultra-sonic bath to aid · Powerful software can model measurements of insoluble effects of ionisation, partitioning, compounds. precipitation and solvent shifts. · 1ml assay volume, less than 1mg of sample required for most experiments. s · Automatic calibration and cleaning protocols. Detailed Data · Built-in automatic turbidity detection - precise detection of s precipitation events. · Computer controlled temperature Better Decisions management - no water circulator required. s Time & Cost Savings s Improved Efficiency The SiriusT3 allows physchem measurements to be performed on sub-milligram quantities of material. This revolution allows the best quality data to be obtained even on discovery compounds where sample quantity is a limiting factor. By obtaining high quality information at Ordering Information: an earlier stage in the discovery and Interested in SiriusT3? development process, decisions about chemistry Contact us to arrange changes and formulation routes can be made a demonstration or early, saving money, and potential problem free of charge sample areas in other assays can be indentified evaluation and resolved with ease.
  • 4. SiriusT3 Technical Specification pH electrode: Ag/AgCI, double junction reference Stirrer: Overhead, variable speed, computer controlled Temperature probe: Thermocouple, Temperature measured with every datapoint Temperature control: Peltier, Range: 12°C to 70°C Turbidity detection: Pass-through light detection – percentage light detected reported to 0.1% Water, Acid, Base, partition solvent, CoSolvent (six-installed, via automated 6-way valve), minimum Precision dispensers: volume of 0.024m L MultiTip dispenser: Multi-tip capillary bundle Probe movement: Fully automated X-Y axis on titrator module Electrode storage/calibration: Home position for electrode storage and pH7 buffer positions for calibration Washes: Two static washes and flowing water wash station Autoloader: Holds up to 192 samples, automatic gripper arm for transfer to sample position Purge gas: Two internal flow meters, nitrogen or argon supply required Partition solvents: Supports 7 including Octanol, Dodecane, Toluene CoSolvents: Supports 10 including Methanol, Acetonitrile, DMSO and MDM System standardisation: Sirius Four-Plus™ procedure pH-range: 1.8 - 12.2 Assay volume: 0.5 to 3.5mls Services required: One mains power inlet (110 or 240 V), 50-60Hz Connection to the PC: USB Intel compatible processor, 2GB Memory, 10GB Available disk space, one free USB port, Computer: CD/DVD-ROM-drive, 1280x1024 screen resolution. XP/Vista/Windows7 with IE6 or higher. For indoor use only Altitude ≤ 2000m Temp. 5°C to 40°C Environment: Max relative humidity 80% @ 31°C Mains voltage fluctuation +/- 10% Installation overvoltage Cat II Pollution degree 2 Physical Dimensions Weight Height Width Depth Dispenser module 35kg/77.16lbs 700mm 260mm 460mm Titrator 23kg/50.71lbs 490mm 215mm 460mm Autoloader 27kg/59.52lbs 490mm 350mm 460mm Total 85kg/187.39lbs 700mm 825mm 460mm Distributed by: Sirius Analytical, Inc 100 Cummings Center, Suite 231c, Beverly, MA 01915-6126 Telephone: 978 338 5790 Fax: 866 410 7668 Email: sales@sirius-ai.com web: www.sirius-analytical.com