Quantitative determination of Sulfisoxazole (cas 127-69-5) and its three N-acetylated metabolites using HPLC–MS/MS, and the saturable pharmacokinetics of Sulfisoxazole (cas 127-69-5) in mice

Add time:09/26/2019    Source:sciencedirect.com

Sulfisoxazole (cas 127-69-5) (SFX) is still used in combination with trimethoprim in cattle despite adverse drug reactions (e.g., urolithiasis). Recently, SFX is known to be a promising repositioned drug candidate for pulmonary hypertension and cancer. We developed a simultaneous determination method of SFX and its N-acetylated metabolites (N1-acetyl SFX, N1AS; N4-acetyl SFX, N4AS; diacetyl SFX, DAS) using HPLC–MS/MS for the first time, and examined the pharmacokinetics of SFX in mice. N1AS and DAS were converted rapidly to SFX and N4AS, respectively, in mouse plasma. The time courses of plasma SFX and N4AS concentrations were well-characterised following the oral administration of SFX to mice. The absorption, metabolism, and/or excretion of SFX given at >700 mg/kg may be saturable, and in contrast to humans and rats, the extent of systemic exposure of mice to N4AS was much greater than that of SFX. Interestingly, the acetyl groups at both N1- and N4-positions were degraded during the ionisation required to generate precursor ions. In additional experiments the carboxyl group of N-acetyl-5-aminosalicylic acid (NA5AS) was lost instead of the acetyl group during the ionisation, and acetaminophen (AAP) appeared. As the acetyl and carboxyl groups of some substances can be degraded during ionisation in the mass spectrometer, caution is appropriate when it is sought to simultaneously quantify similar structures containing these moieties; chromatographic separation is essential.

We also recommend Trading Suppliers and Manufacturers of Sulfisoxazole (cas 127-69-5). Pls Click Website Link as below: cas 127-69-5 suppliers

Prev:Insight into the mechanisms for hexavalent chromium reduction and Sulfisoxazole (cas 127-69-5) degradation catalyzed by graphitic carbon nitride: The Yin and Yang in the photo-assisted processes
Next:Electro-catalytic degradation of Sulfisoxazole (cas 127-69-5) by using graphene anode)