Discovery Solutions

SMALL-SCALE FORMULATIONS FOR PRE-CLINICAL TESTING

Ascendia develops and evaluates a variety of formulations for preclinical non-GLP and GLP  studies.  We understand the needs of companies with an exciting compound in the discovery pipeline, but with limited amounts of drug substance.  We have developed methods for carrying out formulation screening studies with as little as several mg of drug substance. These methodologies can be used to formulate new drugs for initial in vivo experiments when only low milligram quantities of the drug have been synthesized and/or purified.

After screening, our formulation development includes feasibility studies to assist compatibility studies of excipients, active ingredients and delivery components; and formulation selection and optimization.  We provide statistical experimental design, short-term and accelerated stability studies, and method development and validation. Using our expertise in modeling and simulation (e.g., GastroPlus and WinNolin), we can predict the animal PK profile and propose an efficient formulation strategy for preclinical studies accordingly.  Often these small-scale formulations are provided in oral, liquid form.

Solutions

Depending on the drug candidate’s solubility properties, surfactants, complexation agents and co-solvents can be added to increase solubility, and hence enhance bioavailability for initial animal testing.
 

Suspensions

Particle size is frequently a critical parameter impacting the dissolution rate. Micronization of the drug substance, or wet milling in a suspending vehicle, can therefore be important to obtain good bioavailability of a poorly water soluble drug substance.
 

Nano-suspensions

Nanonization of a poorly water soluble drug substance further increases the dissolution rate (by increasing the crystal surface area). A nano-suspension of a poorly water soluble drug substances shows a faster dissolution and a higher bioavailability when compared to a micronized suspension.
 

Emulsions

If dictated by solubility data (in oily vehicles, co-surfactants and solvents), an emulsion – a fine dispersion of droplets – can be formulated to improve the initial probability of success.  The drug may be dissolved or suspended in either the oily liquid, or aqueous liquid phase.
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