Extensive experience in supporting early phase API development
Concept Life Sciences have extensive experience in supporting early phase API development, from solid form optimization through pre-formulation to pre-clinical formulation characterisation.
Clients have direct access to our multi-disciplinary project team allowing for clear communication of project needs, progress updates and rapid idea generation. Our approach has an early emphasis on defining critical to quality (CtQ) and critical to processing (CtP) attributes. We work with our clients to ensure a solid understanding of the key project milestones and we pride ourselves in providing the high quality analysis required to allow prompt and scientifically sound decisions.
Salt and polymorph screening
It is well understood that early optimization and understanding of your candidate can pay dividends later in the project. A robust understanding of polymorphism will ensure that you are working with the most appropriate form, balancing reliable crystallization with stability and efficacy. Similarly, a stage-appropriate salt screen can transform a potential candidate with poor thermal stability and solubility into a high potential lead candidate.
It also offers maximum intellectual property protection to your valuable candidate, and minimizes the risk of having to repeat expensive and time consuming development phases.
We begin all of our studies by offering a comprehensive physico-chemical assessment of your candidate molecule including predicted pKa, LogP/D. We design a screening program in collaboration with our clients to stress the molecule or promote salt formation.
We are able to quickly identify novel forms using the high throughput analysis compatibility of our Empyrean S3 X-Ray diffractometer, combining the automated XRPD analysis of multi-well plates with the data processing power of HighScore Plus.
Any hits are then evaluated utilizing the same wide range of analytical techniques used to characterize the starting molecule, facilitating side by side comparison of physical/chemical property enhancements. Promising candidates are accelerated to synthesis optimization and further characterization, as needed.
Pre-formulation and formulation
We offer a wide-ranging service for formulation development and GMP batch production, up to kg scale, for pre-clinical trial materials.
We generate reference batches and develop and validate the required methodologies to provide release specifications.
We offer additional formulation services to maximize in-vivo exposure of an NCE for toxicity assessing and de-risking programs, including but not limiting to amorphous solid dispersion, solubility enhancing via excipient screening (using our proprietary solubility screen), particle size reduction via milling to generate suspensions of nano-sized API in a suitable dosing vehicle (nanosuspension).
We have available a wide range of characterization tools for formulation development, encompassing parenteral, oral and inhalation products.
Additional API post-processing services such as micronizing or blending to prepare samples for further development can be undertaken in-house; these services are supported by a full suite of physical and chemical characterization techniques.
Capabilities and key techniques
- Pre-formulation / Pre-nomination support
- Screens: Salt/Polymorph/Co-crystal
- pKa, LogP/D outputs, Drug absorption modeling
- Extensive API and product characterization including key technologies to support IVBE studies.
- Solubility in aqueous, organic, biorelevant media
- Scale-up in GMP for pre-clinical administration supported by a comprehensive analytical package including stability studies where necessary
- Tablets, capsules, liquids, suspensions, pulmonary (pMDI / DPI)
- Powder blending and release for toxicology trials
- Particle size modification through micronizing
- PXRD – Empyrean S3
- Thermal characterization DSC, TGA
- H1 NMR
- BET Specific Surface Area
- Morphologi 4