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Volume 7
Pharmaceutical Regulatory Affairs: Open Access
ISSN: 2167-7689
Pharma Europe 2018
May 07-09, 2018
May 07-09, 2018 | Frankfurt, Germany
15
th
Annual European Pharma Congress
Solubility strategies in pharmaceutical research and development
Philippe Lienard
Sanofi, France
T
he ideal drug attributes allow easy formulation into common and already registered dosage forms. Solubility into
conventional oral (per os) and intravenous formulations as well as good absorption in the gastrointestinal tract always
facilitate achieving desired therapeutic goals as well as demonstrating acceptable pharmacokinetic profiles. However, during
drug discovery optimization phase, the low solubility of drug candidates has become one of themost frequent issues that prevent
these attributes from being fulfilled. Low solubility impacts the intravenous formulation feasibility and the oral bioavailability.
In parallel, safety and toxicity concerns have to be anticipated, thus challenging clinical development. This lecture describes
comprehensive strategies towards these ends, at the interface between research and development, to alleviate solubility deficit
in order to realize essential animal studies. The main enabling formulations to tackle solubility will be described through
several unpublished case studies. Some undisclosed formulations for low water soluble molecules will be presented. A focus on
nanotechnology, enabling formulation to deliver drug substance via an intravenous administration will be discussed, including
feedback from the FDA for incrementally modified drug (IMD) submission. However, to avoid labor intense and resource-
consuming pharmaceutical development, approaches to design solubilizing prodrugs or salts compatible with standard drug
formulation technologies will be considered. Finally, these approaches either based on enabling formulation or molecule
design will be compared to allow making strategic choices as early as possible in the discovery phase to ensure fast and smooth
pharmaceutical development.
Philippe.lienard@sanofi.comPharmaceut Reg Affairs 2018, Volume 7
DOI: 10.4172/2167-7689-C1-031