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Next generation solution for
automated physchem measurement
The SiriusT3 is the next generation physchem
measurement system from Sirius Analytical.
It replaces our world renowned and market leading
GLpKa system, which over the last decade has
been established as the industry standard for pKa,
logP/D and solubility determinations.




 SiriusT3 Assays
 pKa assays:                            Understanding the ionisation state of a drug and how it varies with pH provides
 - Provides pKa values to the highest   key information about the proportion of species available for absorption.
   commercially available accuracy
 - Distribution of species plots        Running pKa determinations in different media reveals detailed information about
 - Determine Buffer Capacity            how the pKa changes due to solvent interactions, partitioning, precipitation or
                                        binding.


 logP assays:                           Understanding the logP and logD reveal how the ionisation state of the molecule
 - Determine logP                       influences its lipophilicity. This information can be used to improve ADME
 - Determine logD vs. pH                predictions as well as evaluating how changes to the molecule can
 - Study Octanol/Water & many           increase/decrease the lipophilicity for a desired application.
   other mixtures


 Solubility assays:                     Solubility is a complex and fundamental parameter affecting drug absorption.
 - Determine Intrinsic solubility       Understanding the full kinetics of supersaturation, precipitation, dissolution and
 - Determine Kinetic solubility         the relationship between solubility and pH is crucial to understanding the ADME
 - Derive pH vs. Solubility profile     behaviour of a drug molecule.
 - Determine supersaturation


 Dissolution assays:                    Dissolution assays with pH control and in the presence of excipients and
 - Profile drugs for dissolution and    biorelevant media (FaSSIF/FeSSIF) can be used to evaluate the effects of different
   precipitation rates                  formulations on the dissolution and precipitation kinetics. This infomation can aid
 - Explore the effects of changing pH   the selection of appropriate formulations for different routes of administration.
 - Run assays with excipients,
   additives and biorelevant media


 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,
                        ·   Minimal running costs - uses off the            excipients, additives, biorelevant
                            shelf reagents with no special                  media.
                            “kits” required.
                                                                        ·   pH range of 1.8 - 12.2, extendable
                        ·   Built in ultra-sonic bath to aid                to 0.5 - 13.5 with UV options.
                            measurements of insoluble
                            compounds.
                                                                        ·   Powerful software can model
                                                                            effects of ionisation, partitioning,
                        ·   1ml assay volume, less than 1mg of              precipitation and solvent shifts.
                            sample required for most
                            experiments.                                                    L
                        ·   Automatic calibration and cleaning
                            protocols.
                                                                                   Detailed Data
                        ·   Built-in automatic turbidity
                            detection - precise detection of                                L
                            precipitation events.
                        ·   Computer controlled temperature
                                                                                Better Decisions
                            management - no water circulator
                            required.
                                           L

                               Time & Cost Savings
                                           L

                             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 an earlier
 stage in the discovery and development process,
                                                                   Ordering Information:
      decisions about chemistry changes and
                                                                    Visit our website for
   formulation routes can be made early, saving
                                                                    detailed information
   money, and potential problem areas in other
                                                                      on how to obtain
           assays can be indentified and
                                                                           SiriusT3
                 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
                                Pass-through light detection – percentage light detected
 Turbidity detection:
                                reported to 0.1%


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

 MultiTip dispenser:            Multi-tip capillary bundle
 Probe movement:                Fully automated X-Y axis on titrator module
 Electrode storage/             Home position for electrode storage and pH7 buffer positions
 calibration:                   for calibration
 Washes:                        Two static washes and flowing water wash station
                                Holds up to 192 samples, automatic gripper arm for transfer
 Autoloader:
                                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

                                Pentium compatible processor, 1GB Memory, 1GB Available
                                disk space, one free USB port, CDROM-drive, 1280x1024
 Computer:
                                screen resolution. Win2000(SP4)/XP Pro(SP2)/Vista (SP1)
                                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 Ltd.
Riverside, Unit 12, Forest Row Business Park,
Forest Row, East Sussex,
RH18 5DW, UK

Telephone:   +44 (0) 1342 820720
Fax:         +44 (0) 1342 820725
Email:       sirius@sirius-analytical.com
web:         www.sirius-analytical.com

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SiriusT3 Brochure

  • 1. Next generation solution for automated physchem measurement
  • 2. The SiriusT3 is the next generation physchem measurement system from Sirius Analytical. It replaces our world renowned and market leading GLpKa system, which over the last decade has been established as the industry standard for pKa, logP/D and solubility determinations. SiriusT3 Assays pKa assays: Understanding the ionisation state of a drug and how it varies with pH provides - Provides pKa values to the highest key information about the proportion of species available for absorption. commercially available accuracy - Distribution of species plots Running pKa determinations in different media reveals detailed information about - Determine Buffer Capacity how the pKa changes due to solvent interactions, partitioning, precipitation or binding. logP assays: Understanding the logP and logD reveal how the ionisation state of the molecule - Determine logP influences its lipophilicity. This information can be used to improve ADME - Determine logD vs. pH predictions as well as evaluating how changes to the molecule can - Study Octanol/Water & many increase/decrease the lipophilicity for a desired application. other mixtures Solubility assays: Solubility is a complex and fundamental parameter affecting drug absorption. - Determine Intrinsic solubility Understanding the full kinetics of supersaturation, precipitation, dissolution and - Determine Kinetic solubility the relationship between solubility and pH is crucial to understanding the ADME - Derive pH vs. Solubility profile behaviour of a drug molecule. - Determine supersaturation Dissolution assays: Dissolution assays with pH control and in the presence of excipients and - Profile drugs for dissolution and biorelevant media (FaSSIF/FeSSIF) can be used to evaluate the effects of different precipitation rates formulations on the dissolution and precipitation kinetics. This infomation can aid - Explore the effects of changing pH the selection of appropriate formulations for different routes of administration. - Run assays with excipients, additives and biorelevant media 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, · Minimal running costs - uses off the excipients, additives, biorelevant shelf reagents with no special media. “kits” required. · pH range of 1.8 - 12.2, extendable · Built in ultra-sonic bath to aid to 0.5 - 13.5 with UV options. measurements of insoluble compounds. · Powerful software can model effects of ionisation, partitioning, · 1ml assay volume, less than 1mg of precipitation and solvent shifts. sample required for most experiments. L · Automatic calibration and cleaning protocols. Detailed Data · Built-in automatic turbidity detection - precise detection of L precipitation events. · Computer controlled temperature Better Decisions management - no water circulator required. L Time & Cost Savings L 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 an earlier stage in the discovery and development process, Ordering Information: decisions about chemistry changes and Visit our website for formulation routes can be made early, saving detailed information money, and potential problem areas in other on how to obtain assays can be indentified and SiriusT3 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 Pass-through light detection – percentage light detected Turbidity detection: reported to 0.1% via automated 6-way valve), minimum volume of 0.024µ L Water, Acid, Base, partition solvent, CoSolvent (six-installed, Precision dispensers: MultiTip dispenser: Multi-tip capillary bundle Probe movement: Fully automated X-Y axis on titrator module Electrode storage/ Home position for electrode storage and pH7 buffer positions calibration: for calibration Washes: Two static washes and flowing water wash station Holds up to 192 samples, automatic gripper arm for transfer Autoloader: 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 Pentium compatible processor, 1GB Memory, 1GB Available disk space, one free USB port, CDROM-drive, 1280x1024 Computer: screen resolution. Win2000(SP4)/XP Pro(SP2)/Vista (SP1) 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 Ltd. Riverside, Unit 12, Forest Row Business Park, Forest Row, East Sussex, RH18 5DW, UK Telephone: +44 (0) 1342 820720 Fax: +44 (0) 1342 820725 Email: sirius@sirius-analytical.com web: www.sirius-analytical.com