| Autor: |
Farid, Nagy A., Born, Gordon S., Kessler, Wayne V., Russell, Henry T., Shaw, Stanley M., Lange, Winthrop E. |
| Zdroj: |
Journal of Pharmaceutical Sciences; April 1977, Vol. 66 Issue: 4 p536-538, 3p |
| Abstrakt: |
The synthesis of 14C-meglumine salicylate was accomplished by heating 14C-meglumine with salicylic acid, in equimolar ratios, in 2-propanol. The average radiochemical yield was 97.5%. Ten healthy adult male volunteers were given 1.2g of the compound orally. Five took 1.2g of 1-deoxy-l-[14C]-methylamino-D-glucitol salicylate (containing about 47μCi), and five others took 1.2g of 1-deoxy-l-methylamino-D-[U-14C]-glucitol salicylate (containing about 45μCi). Urine and feces were collected for 5 days, and blood was sampled for 24hr. The peak urinary excretion of meglumine and/or its metabolites occurred between 4 and 8hr after administration (about 7.2% of the administered dose). Meglumine was excreted primarily in the feces (72.4% over 5 days) and, to a smaller extent, in urine (21.3% over 5days). No activity was detected in blood. The excretion rate and percentage excreted were the same for both groups of subjects, suggesting that meglumine was not metabolized by N-demethylation or conversion to carbon dioxide. The highest blood salicylate level, 44.4±1.9μg/ml, was observed 1hr after administration. Urinary levels of salicylic acid and its metabolites were observed to be at a maximum at 8hr. Total salicylate recovery was 94.7±1.5% in 48hr. Salicyluric acid was the major metabolite, accounting for 69.5±3.6% of the dose. Salicylic acid accounted for 6.8±1.2%. |
| Databáze: |
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