突破預配方瓶頸，加速成藥決策

Unchained Labs Big Kahuna and Junior automated platforms deliver comprehensive high-throughput solutions for small molecule preformulation, enabling pharmaceutical scientists to systematically explore the physicochemical property space of drug candidates and identify optimal solid forms with enhanced druggability characteristics.

As poorly soluble drug candidates increasingly enter development pipelines, the importance of early-stage systematic solid form screening has become critical for drug development success. The Big Kahuna and Junior systems address this challenge by providing automated, end-to-end workflows for solubility screening, polymorph screening, cocrystal screening, salt selection, chiral resolution, and reaction optimization.

The platforms feature innovative hardware technologies that set them apart from traditional manual methods. The Universal Substrate technology enables direct crystallization in an 8x12 array format, allowing crystals to be analyzed by birefringence imaging, X-ray powder diffraction (XRPD), and Raman spectroscopy without manual manipulation or sample transfer. This non-destructive approach preserves crystal integrity and enables sequential characterization experiments on the same samples.

Powdernium solid dispensing technology employs an adaptive learning algorithm that dynamically adjusts dispensing parameters to accommodate powders with different densities, particle sizes, particle shapes, and static charges. The system remembers optimal settings for reproducible dosing with RSD of 1-5%, even at quantities as low as 0.5 mg with the Storage Vial (SV) dispenser.

Temperature-controlled liquid handling capabilities include heated 4-tip liquid dispensers with septum-piercing tips operating up to 120 degrees Celsius, preventing API precipitation during solution transfer. The heated filter block with 96 isolated sample wells eliminates well-to-well cross-contamination while maintaining precise temperature control throughout filtration processes.

The heating/cooling/stirring stations provide temperature control from -20 to 180 degrees Celsius with magnetic tumble stirring up to 750 rpm, enabling parallel slurry, precipitation, cooling, and evaporation crystallization experiments on a single platform. This flexibility allows comprehensive exploration of crystallization conditions within a single experimental run.

The Laboratory Execution and Analysis (LEA) software suite provides a complete digital pathway from experimental design to data analysis and reporting. Library Studio offers a recipe-oriented approach with built-in combination generators for designing complex high-throughput experiments in array-based formats. Automation Studio controls instrument execution while automatically storing process and analytical data in the LEA database. PolyView and Spectra Studio enable integrated review and reporting of experimental design, execution, and analytics, with statistical grouping of XRPD and Raman spectra based on Pearson correlation for automated identification of potential new crystal forms.

Validated applications include high-throughput polymorph screening where a single scientist explored 384 different crystallization conditions using approximately one gram of API in just five days. The 96-well cocrystal screening workflow developed by Amgen scientists using solvent mediated sonic blending successfully identified known cocrystals and discovered new cocrystal forms with hydration stability exceeding two weeks at 98% relative humidity. The chiral resolution application demonstrated by the Medicines for Malaria Venture achieved breakthrough results, solving in two weeks a challenging intermediate separation that had stalled development for over a year, with final scale-up yielding 85% recovery and 99.3% enantiomeric excess.

Big Kahuna represents the full-featured high-throughput configuration with vial/plate gripper and capping/de-capping capabilities, while Junior offers a compact, efficient platform for laboratories with space constraints or moderate throughput requirements. Both systems share identical core specifications for crystallization capacity, temperature-controlled liquid handling, solid dispensing, and third-party instrument integration including XRD, birefringence microscopy, Raman spectroscopy, and HPLC.

These automated preformulation platforms enable pharmaceutical development teams to explore broader experimental design spaces with minimal API consumption, accelerate solid form selection decisions, reduce late-stage development risks from unexpected polymorph appearance, and ensure comprehensive intellectual property coverage through systematic crystallization condition exploration.