Strategies to stabilize dalbavancin in aqueous solutions: Section 4—identification of heat degradation products in 2-hydroxypropyl-β-cyclodextrin and divalent metal ion solutions at pH 4.5 and 7.0

Abstract Heat stress studies have been conducted in support of developing a heat-stable liquid solution dalbavancin. The degradation products that form heat-stressed buffered dalbavancin solutions identified, including the known major product, mannosyl aglycone (MAG), and four previously uncharacterized compounds. Liquid chromatography-mass spectrometry/mass spectrometry (LC–MS/MS) was used to identify acetate- phosphate-buffered under thermal at 70 °C changes pattern presence 2HPβCD divalent metal ions. Although Ca 2+ , Mg Zn did not reduce acetate buffer, significantly reduced its overall degradation, particular, formation MAG. This protective effect enhanced by addition formulation. In phosphate MAG also 2HPβCD, although significant increases other were observed this case. while increasing somewhat. results strongly suggest forms complex with hydrophobic glycone tail dalbavancin, suppressing hydrolysis glycosidic bond.