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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 determine compatibility of excipients, active ingredients and delivery components, formulation selection, and optimization. We provide statistical experimental design, short-term and accelerated stability studies, and analytical 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 liquid form, developed for various routes of administration (oral, iv, ip, sc, etc.).
Depending on the drug candidate’s solubility properties, lipids, surfactants, complexation agents, and co-solvents can be added to increase solubility, and hence enhance solubility and bioavailability for initial animal testing.
Particle size and selection of a suspending vehicle are frequently critical factors impacting the stability and dissolution rate. Micronization of the drug substance by jet milling, or wet milling in a suspending vehicle, can therefore be important to obtain good bioavailability of a poorly water soluble drug substance.
Preparation of nano-suspensions of a poorly water soluble drug substance further increases the dissolution rate (by increasing the surface area). A nano-suspension of a poorly water soluble drug substances may show a faster dissolution rate and a higher solubility/bioavailability when compared to a micronized suspension.
If dictated by solubility data (in oily vehicles, co-surfactants and solvents), an emulsion – a fine dispersion of oil droplets – can be formulated to improve the initial probability of success. The drug may be dissolved or suspended in either the oily liquid, formulated as an emulsion, and/or then further incorporated into solid matrix or aqueous liquid phase.
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