High-Throughput Experimentation (HTE) – Robotic Sample Preparation

High throughput experimentation or screening (HTE or HTS) is used in the pharmaceutical industry in the development of newly discovered compounds or in the early preclinical development of drug candidates. The rational exploration of thousands of molecules finishes when a single new molecular entity (NME) reaches commercialization: Only 1 in 10000 potential candidates will make it to the market. This dynamic shift from a high to a low number of compounds needs an efficient screening process. Once an NME is found, its molecular properties and synthesis conditions are optimized before undergoing preclinical and clinical testing. This work is usually carried out by the Chemistry, Manufacturing and Controls (CMC) department of a pharmaceutical company. Since there are usually many parameters and factors that can be varied when synthesizing a molecule, this process results in an enormous amount of testing.

To achieve the required throughput, researchers often use parallel reaction screening. This method allows multiple reactions to be run simultaneously in a reactor system, with each vial being slightly modified. In such parallel testing, miniaturization and automation are powerful ways to accelerate processes and increase productivity.
 

Why weighing automation is important?

Sample preparation is one of the first steps in a high-throughput experimentation workflow and it typically involves weighing multiple powders to prepare a single formulation. Especially with a large number of formulations to be tested, manual weighing soon becomes tedious, time-consuming and prone to error. Automate and let a Robotic Powder Dispensing System accurately prepare your reaction samples!
 

The unique CHRONECT XPR Robotic Powder Dispensing platform represents the latest development in robotic powder dispensing, designed to prepare powder formulations for reaction screening. Find out how it enables unattended weighing and preparation of powder samples for high-throughput screening of up to 288 samples in one single run.

The key principle of high-throughput experimentation is parallelization. Experiments are no longer carried out on a typical serial basis but are conducted simultaneously.

High-throughput experimentation (HTE) has revolutionized pharmaceutical research, by enabling rapid reaction optimization and screening of compound libraries against therapeutic targets. Prior to the introduction of HTE, manual procedures limited a laboratory’s capacity for screening tests to 20-50 compounds per week. A compound library of, for example, 3000 compounds would have required a testing time of 1-2 years. Automation technology has accelerated such screening experiments exponentially. With HTE, a very large number of experimental samples can be tested simultaneously under specified conditions - quickly and relentlessly. It is not uncommon to perform 800-1000 screening reactions per week. Screening the hypothetical library of 3000 compounds can then be reduced to a testing time of 3-4 weeks. Sample volumes can be further reduced from 1 ml to 100 μl for significant savings in reagents.

HTE and combinatorial approaches generate a large amount of data. Managing the data, processes, standards, contextualization, metadata, integration and DoE is challenging. The importance of an appropriate software and informatics infrastructure to fully capture all data cannot be overstated.

Do you need to prepare powder samples for high-throughput screening? Would you like to weigh solid substances automatically and avoid repetitive, time-consuming manual steps? Or perhaps you want to take advantage of the lower minimum weights offered by automated solutions and use less of an expensive substance? Do you want to improve user safety by reducing the risk of exposure? Would you like to automate such sample preparation processes and free your time for other important tasks?

Interested to see the CHRONECT XPR Robotic Powder Dispensing platform in action? Contact us today to request a free online demonstration.

Most challenges in HTE are due to the large number of samples to be processed and the required miniaturization.

• Manual preparation of hundreds of reaction samples is tedious and time-consuming
• Accurate weighing of statically charged powders into small diameter vials or vessels can be difficult and slow
• Handling of hazardous materials and spilling during manual preparation of samples can result in safety risks to the user
• Manual data logging and transfer is error prone

In a fully automatic process, the CHRONECT XPR Robotic Powder Dispensing platform enables you to prepare up to 288 samples / formulations, each consisting of up to 32 powders in a single run.

This unique system combines the advanced weighing and dispensing technology of the XPR Automatic Balance with a state-of-the-art 6-axis robotic arm and the easy-to-use CHRONOS software. It offers unprecedented accuracy, repeatability, efficiency, and flexibility. CHRONECT XPR dispenses from 1 mg up to several grams of fine, flaky, statically charged, compacted, granular or heterogeneous powder substances.

The compact footprint of the platform allows the system to be used on any lab bench as well as in cabinets and glove boxes.

Boost efficiency

Thanks to the 6-axis robotic arm, highly accurate multi-component formulations and calibration standards can be prepared fully automatically, freeing up time to work on other tasks.

Maximize sample yield

The XPR automated dispensing technology enables samples as small as 1 mg to be dispensed with the highest precision. Automated dispensing minimizes spillage and maximizes the yield of your valuable samples.

Dispense with flexibility

CHRONECT XPR can accommodate 3 different vial plates, each holding from 15 up to 96 vials of 1–20 mL volume. With space for up to 32 different powders you have the ultimate flexibility for formulations.

Maintain full control

CHRONOS software enables you to schedule multiple multi-component formulations. The dispensing process can be monitored directly in CHRONOS. Results can be analyzed and exported if desired.

Automated powder dispensing with CHRONECT XPR is easy, accurate and safe, in all lab locations, even at the lowest target weights, with no expert user required.

Check out our infographic and learn how laboratory automation can reduce process errors by 50% and increase productivity by up to 75%. Discover the many advantages of automated weighing with the CHRONECT XPR Robotic Powder Dispensing platform in facts and figures and find out how you can eliminate bottlenecks in the preparation of high-throughput experiments (HTE).

For applications where only a few samples need to be prepared for screening, we recommend the XPR Automatic Balance as a standalone solution or equipped with a sample changer. The automated dispensing with the XPR Automatic Balance offers a level of accuracy and user safety that cannot be achieved with a manual process.

Need to dispense a single solid substance into a large number of tare vessels? Increase your productivity and throughput by using the XPR Automatic Balance together with a sample changer. This allows you to prepare batches of up to 30 samples with the same powdered solid in one fully automated run.

With LabX^TM laboratory software it is possible to use step-by-step guided workflows to prepare formulations. In addition, LabX provides an electronic record of the exact amount dispensed for audit trail purposes, supporting compliance with 21 CFR part 11.