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ANALYSIS OF THE METABOLITES OF 4-METHYL 2-SULFANILAMIDO-OXAZOLE (SULFAMETHOXAXOLE) EXCRETED IN THE URINE OF RUMINANTS

Beg, Muhammad Iqbal (1995) ANALYSIS OF THE METABOLITES OF 4-METHYL 2-SULFANILAMIDO-OXAZOLE (SULFAMETHOXAXOLE) EXCRETED IN THE URINE OF RUMINANTS. PhD thesis, University of the Punjab, Lahore.

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Abstract

Extensive use of assorted chemicals for varied intentions seems a willful attempt to jeopardize the global environments. Amongst chemicals, therapeutic agents constitute a major group of which sulfonamides are still in use either in combination or as a single agent, 4-methyl 2-sulfanilamido-oxazole (Sulfamethoxazole) is frequently employed sulfonamide for susceptible infections of common agricultural animal species including dairy buffaloes, cows, goat’s and sheep. Studies on the metabolism of exogenous or endogenous chemical molecules ± xenobiotics ± yield valuable knowledge for the rational use of these agents. The present study, therefore, was undertaken to investigate the urinary excretion and metabolism of sulfamethoxazole each in 8 in-milk buffaloes, cows, goats and sheep. As a single intravenous dose the drug was given 50 mg/kg bw following which urine samples were collected at different time intervals. The samples were analyzed by spectrophotometric, thin layer chromatographic (TLC) and high performance liquid chromatographic (HPLC) methods to find out the extent and nature of metabolite of the drug. The findings are summarized: 6.1 BUFFALOES Spectrophotometric analysis revealed the mean ± SE values for the cumulative percentage of intravenous dose of sulfamethoxazole excreted in urine at 24 hours as total amine was 40.8 ± 4.0 percent, free amine 27.1 ± 3.0 percent and acetyl amine was 13.7 ± 1.2 percent. The thin layer chromatographic analysis of 24 hours urine sample revealed total drug 37.1 ± 2.2 percent of which 24.2 ± 1.7 percent as unchanged drug, 5.6 ± 0.4 percent acetyl derivative, and 2.6 ± 0.2 percent as hydroxy derivative while 4.3 ± 0.7 percent was conjugated metabolite. The high performance liquid chromatographic analysis of 24 hours urine sample revealed that mean ± SE values for total dose was 40.0 ± 4.1 percent of which unchanged drug was 13.7 ± 1.2 percent, 4 methyl, 2-sulfanilamido 5-hydroxy-oxazole 5.2 ± 0.6 percent, N4 acetyl 4 methyl 2-sulfanilamido-oxazole 12.1 ± 1.4 percent and the conjugated metabolite 9.0 ± 1.3 percent. 6.2 COWS Spectrophotometric analysis revealed the mean ± SE values for the cumulative percentage of intravenous dose of sulfamethoxazole excreted in urine at 24 hours as total amine was 62.5 ± 4.3 percent, free amine 52.1 ± 3.8 percent and acetyl amine was 10.4 ± 1.1 percent. The thin layer chromatographic analysis of 24 hours urine samples revealed total drug 61.2 ± 3.5 percent of which 37.3 ± 2.2 percent as unchanged drug, 11.4 ± 0.9 percent acetyl derivative, 5.1 ± 0.3 percent as 5-hydroxy derivative while 7.4 ± 0.6 percent was conjugated metabolite. The high performance liquid chromatographic analysis of 24 hours urine samples revealed that mean ± SE values for total dose was 58.7 ± 4.3 percent of which unchanged drug was 20.7 ± 1.7 percent, 4-mathyl 2-sulfanilamido 5-hydroxy-oxazole 9.1 ± 1.1 percent, N4 acetyl 4-methyl 2-sulfanilamido-oxazole 15.8 ± 1.3 percent and the conjugated metabolite was 13.1 ± 1.7 percent. 6.3 GOATS Spectrophotometric analysis revealed the mean ± SE values for the cumulative percentage of intravenous dose of sulfamethoxazole excreted in urine at 24 hours as total amine was 61.0 ± 5.2 percent, free amine 43.2 ± 4.6 percent and acetyl amine was 17.8 ± 1.2 percent. The thin layer chromatographic analysis of 24 hours urine samples revealed total drug 59.8 ± 5.3 percent of which 25.4 ± 2.1 percent as unchanged drug, 9.4 ± 1.1 percent as acetyl derivative and 11.0 ± 1.1 percent as hydroxy derivative while 14.0 ± 1.6 percent was conjugated metabolites. The high performance liquid chromatographic analysis of 24 hours urine samples revealed that the mean ± SE values for total dose was 60.5 ± 5.1 percent of which unchanged drug was 24.1 ± 2.0 percent 4 methyl 2-sulfanilamido 5-hydroxy-oxazole 9.4 ± 1.1 percent, N4- acetyl 4-methyl 2-sulfanilamido 5-hydroxy-oxazole 14.8 ± 1.9 percent and the conjugated metabolite 12.2 ± 2.4 percent. 6.4 SHEEP Spectrophotometric analysis revealed the mean ± SE values for the cumulative percentage of intravenous dose of sulfamethoxazole excreted in urine at 24 hours as total amine was 42.9 ± 4.7 percent, free amine 30.7 ± 3.2 percent and acetyl amine was 12.2 ± 2.0 percent. The thin layer chromatographic analysis of 24 hours urine samples revealed total drug 43.3 ± 4.5 percent of which 19.9 ± 2.4 percent as unchanged drug, 7.1 ± 0.7 percent as acetyl derivative and 6.8 ± 0.8 percent as hydroxy derivative, while 9.5 ± 1.0 percent was conjugated metabolite. The high performance liquid chromatographic analysis of 24 hours urine samples revealed that the mean ± SE values for total dose was 41.6 ± 4.7 percent of which unchanged drug was 14.4 ± 2.0 percent, 4-methyl 2-sulfanilamido 5-hydroxy-oxazole 6.3 ± 0.8 percent, N4- acetyl 4-methyl 2-sulfanilamido-oxazole 11.0 ± 1.3 percent and the conjugated metabolite 9.9 ± 1.8 percent. These measurements clearly indicate that the percentage of the dose excreted in the urine of buffaloes 40 percent is almost two third against 62 percent of the dose excreted in the urine of cows. While these values for goats and sheep clearly indicate that the percentage of dose excreted in the urine of sheep is almost two third (43 percent against 63 percent) of the dose excreted in the urine of goats.

Item Type:Thesis (PhD)
Uncontrolled Keywords:4-Methyl 2-Sulfanilamido-Oxazole (Sulfamethoxaxole), Non Conjugation Reaction, Conjugation Reaction, Sulphonamides, Thin Layer Chromatographic Analysis, High Performance Liquid Chromatography
Subjects:Physical Sciences (f) > Chemistry(f2)
ID Code:344
Deposited By:Mr Ghulam Murtaza
Deposited On:27 Jun 2006
Last Modified:04 Oct 2007 21:00

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