In Vitro Hepatobiotransformation of Sulphadimethoxine in Laying Hens

Abstract

The biotransformation of sulphadimethoxine (SDM) was estimated in liver post-mitochondrial supernatants (S-9) from laying hens. The pathway and activity for hen S-9 were compared with those for cow and pig S-9. The formation of the hydroxylation of SDM, 6-hydroxy SDM (6-OH-SDM), was found only with hen S-9. The N4-acetylating activity of SDM in hen S-9 was lower than in cow and pig S-9. All S-9 from the three species de-acetylated N4-acetyl SDM (N4-AcSDM). With respect to the hydroxylation and N4-acetylation rates in hen S-9, the values incubated at 41 degrees C were higher than those at 37 degrees C (P < 0.01).

Characterization and estimation of sulfaquinoxaline metabolites in animal tissues using liquid chromatography coupled to tandem mass spectrometry

“…18 Moreover, acetylated metabolites of sulfonamides have no bacterial activity, a lower solubility in physiological pH, which may lead to kidney precipitation, de-acetylation of the parent drug both in vivo and in vitro and higher plasma protein binding than the parent drug. [19][20][21][22][23][24] Considering the differences found among animal species in sulfonamide metabolization, especially for liver mediated biotransformation, further knowledge of these processes can be considered relevant not only for pharmacological studies, but also for the analysis of sulfonamide residues in food. 25 Like other sulfonamides, SQX has a maximum residue limit (MRL) established for several food matrices.…”

Photodegradation of sulphadimethoxine in water by medium pressure UV lamp

“…The primary metabolite AcSa is lost in the urine; however, a small fraction is metabolised to sulphonamide hydroxylamine which exerts an immunosuppressive effect and may risk certain subpopulations in humans (Sisson et al 1997). The metabolites (N acetylation and 6-hydroxylation) have also been found in SMT biotransformation from in vitro experiments on laying hens (Furusawa 2001). In another study, a photo-catalytic process with near-UV light and titanium dioxide used to simulate environmental phototransformation also showed the formation of 6-hydroxy sulphadimethoxine (among other metabolites) (Calza et al 2004).…”

“…The first intermediate detected, (a) (a1 is more favourite),consisted of 326 mass units and can be attributed to zOH radical attack on the aromatic ring related to the aniline group(Calza et al 2004), forming a hydroxylated structure. As mentioned earlier, 6-hydroxysulphadimethoxine was found from in vitro experiments on laying hens(Furusawa 2001). In humans, a small fraction of SMT is metabolised to sulphonamide hydroxylamine, which exerts an immunosuppressive effect and may risk certain subpopulations in humans(Sisson et al 1997).…”

Development and validation of analytical method for sulfonamide residues in eggs by liquid chromatography Tandem Mass Spectrometry based on the Comission Decision 2002/657/EC

“…3, 2011 technique of analysis. There are methods that use high performance liquid chromatography (HPLC) with fluorescence detector, [2][3][4][5][6] or with ultra-violet (UV) detector, [7][8][9][10] or else with diode array detector (DAD), [11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26][27] but mass spectrometer (MS) detectors are the most appropriate because they give enough information for molecular identification.…”