By the time a promising new drug reaches formulation development, significant investments have been made for the success of that molecule. At such a critical point in the path to the first clinical studies, the Formulation Development scientists at deCODE chemistry can help clients to attain the benefits of time and cost efficiency.
New drug molecules must be formulated into a delivery system that is suitable for administration in pre-clinical and clinical studies. An optimal formulation (or a lack thereof) can significantly impact the results of these studies. Our Formulation Development scientists work in tandem with our Process and Analytical Chemistry teams to perform a thorough pre-formulation analysis to assess the unique characteristics of your molecule. After a carefully coordinated assessment of pre-formulation results with the Drug Safety & Metabolism research team, our Formulation Development scientists work to provide an optimized pre-clinical formulation to meet the dosage range and preferred route of delivery indicated by our client. This is followed by development of a formulation suitable for Phase I clinical studies. Information developed during this process can also be used to support the drug product CMC section of the sponsor's IND.
Pre-formulation Screening (ParaSol™) ParaSol™ is a Parallel Solubility screen developed at deCODE to assess solubility in a high-throughput manner. The foundation of ParaSol™ lies in its innovative utilization of proprietary research tools and methods that were originally developed by deCODE biostructures for protein crystallization. The process capitalizes on laboratory automation controlled through a sophisticated database approach to yield results quickly and cost-efficiently. Using as little as 10 mg of compound, our researchers screen API against our exclusive 96i™ pre-formulation screening set (patent-pending), which represents a wide variety of liquid-based formulation excipients. The resulting data drives the direction of our Formulation Development group to produce suitable formulations for pre-clinical development and early-phase clinical trials.
Physicochemical Characterization In parallel to the ParaSol™ screen, our Formulation Development scientists coordinate and perform a thorough pre-formulation evaluation to assess key properties of the new drug molecule in order to understand the best way to develop a formulation. Studies can include, but are not limited to, pKa, log P, log D, crystallinity, aqueous and non-aqueous solubility, solid state and solution stability, polymorph screening, and preparation of a salt form (if needed) to enhance solubility and chemical stability, while minimizing hygroscopicity.
Formulation Development The Formulation Development scientists at deCODE chemistry are dedicated to developing formulations that will lead to successful completion of IND-directed safety pharmacology and toxicology studies, and entry into Phase I human clinical trials. Our team is experienced in developing liquid-based formulations (typically desirable for pre-clinical development), as well as liquid-based capsule oral dosage forms. Information obtained from the ParaSol™ screen and physicochemical characterization set the stage for pre-clinical and clinical formulation development. This data along with the specified dosage range and preferred route of administration, are evaluated in order to understand the best options for fast and economical development of pre-clinical and clinical formulations. We then develop the formulations needed for these studies using a minimal amount of API. Development of solid dosage forms includes assessment of a dissolution profile using either USP I or USP II methods. We evaluate formulation stability with an appropriate analytical method developed in a coordinated effort with our Analytical Chemistry department. The resulting formulations are suitable for pre-clinical studies and entry into First-in-Human studies.
