Synthesis and evaluation of PEG414, a novel formulating agent that avoids analytical problems associated with polydisperse vehicles such as PEG400.
Polyethylene glycol (PEG) 400 is widely used as a formulating agent for both intravenous and oral studies during drug discovery. It is a polydisperse material containing more than 16 oligomers, which can cause significant problems for high-performance liquid chromatography-mass spectrometry analysis due to ion suppression and isobaric interference. To overcome these difficulties, we have synthesized the single oligomer PEG414. The material has been characterized with a range of diverse drug compounds and shown to be comparable to PEG400 and superior to propylene glycol in terms of its solubilization power. The toxicological and metabolic properties of PEG414 should be similar to PEG400. It suffers none of the analytical problems associated with polydisperse agents and we expect it to be a useful alternative for the formulation of test compounds for intravenous and oral dosing during drug discovery.
Temesi
David
D
Discovery DMPK, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
Law
Brian
B
Howe
Nicholas
N
D002626:Chemistry, Pharmaceutical; D004353:Drug Evaluation, Preclinical / Q000379:methods; D014677:Pharmaceutical Vehicles; D011092:Polyethylene Glycols / Q000032:analysis* / Q000138:chemical synthesis* / Q000737:chemistry
D014677:Pharmaceutical Vehicles; D011092:Polyethylene Glycols