Abstract
A novel UPLC-MS/MS assay was developed for rapid quantification of delafloxacin (a novel fluoroquinolone antibiotic in plasma samples by one step sample cleanup procedure. Delafloxacin (DFX) and internal standard (losartan) were separated on a UPLC BEH C18 column (50 × 2.1 mm; 1.7 μm) by using gradient programing of a mobile phase containing 0.1% formic acid in acetonitrile and 0.1% formic acid in water. The quantification was performed by a using triple-quadrupole mass detector at an electrospray ionization interface in positive mode. The precursor to the product ion transition of 441.1 → 379.1 for the qualifier and 441.1 → 423.1 for the quantifier was used for DFX monitoring, whereas 423.1 → 207.1 was used for the internal standard. The validation was performed as per guidelines of bioanalytical method validation, and the evaluated parameters were within the acceptable range. The greenness assessment of the method was evaluated by using AGREE software covering all 12 principles of green analytical chemistry. The final score obtained was 0.78, suggesting excellent greenness of the method. Moreover, Deming regression analysis showed an excellent linear relationship between this method and our previously reported method, and it is suitable for high-throughput analysis for routine application. The proposed method was effectively applied in a pharmacokinetic study of novel formulation (self-nanoemulsifying drug delivery systems) of DFX in rats.
Highlights
Acute skin and skin structure infections (ASSSI) and community-acquired pneumonia (CAP) are the most common bacterial infection diseases across the globe
Patients infected by ASSSI and CAP are related with high morbidity, mortality or long term stays in clinics, in this manner forcing a critical burden from a societal and health-payer perspective [1,2,3]
The presence of a hetero-aromatic ring at the N1 position produces its antibacterial activity; a weak polar group at the C8 position enhances its potency against quinolone-resistant Gram-positive bacteria; and the absence of basic group at the C7 position makes it weakly acidic, thereby causing increased intracellular penetration in bacteria in acidic environments (Figure S1) [8,9,10]
Summary
Acute skin and skin structure infections (ASSSI) and community-acquired pneumonia (CAP) are the most common bacterial infection diseases across the globe. DFX is an anionic FQ and has broad spectrum activity against Gram-positive, Gram-negative and atypical activity, including activity against FQ non-susceptible methicillin-resistant staphylococcus aureus (MRSA) isolates [3,5,6]. Unlike other FQ, DFX possesses distinct chemical characteristics by three unique modifications in their quinolone ring, which increase its antimicrobial activity as well as its pharmacokinetic and toxicity profile [7]. The presence of a hetero-aromatic ring at the N1 position produces its antibacterial activity; a weak polar group at the C8 position enhances its potency against quinolone-resistant Gram-positive bacteria; and the absence of basic group at the C7 position makes it weakly acidic, thereby causing increased intracellular penetration in bacteria in acidic environments (Figure S1) [8,9,10]
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