A comparative bioavailability study was performed using two commercially available types of carbamazepine tablets, by statistical analysis of serum levels and other bioavailability parameters. After single oral dose the extent of absorption from the two preparations was similar, although a statistically significant difference in absorption rates was observed. In a multiple-dose study no significant difference in serum carbamazepine levels was found, so the tablets could be considered as bioequivalent drug products.
Serum salicylate levels were determined fluorimetrically in 12 neurosurgical patients after rectal and oral administration of 1.0 g aspirin. There was no significant difference in the AUC-value between the two routes of administration, but a slower rate of absorption with no clear peak effect was found after rectal administration. Rectal aspirin is useful in clinical situations in which mediation is difficult by the oral route, e.g. after neurosurgical and open-heart surgical interventions.
41 children with juvenile rheumatoid arthritis (JRA) and 6 with postinfectious arthropathies, aged 3--15 years, were treated with acetylsalicylic acid for 14 days during which time the patients were hospitalized. Three different acetylsalicylic acid preparations were used: a microencapsulated form, an enteric-coated form and standard acetylsalicylic acid tablets. Serum salicylate concentrations were measured by Trinder's photometric method. With doses of 90--120 mg/kg/day symptoms of salicylism appeared in about 50% of the cases. Daily doses of 2 g/m2 (not exceeding 70 mg/kg) proved relatively safe in this study, whereas symptoms and signs of intoxication appeared at doses exceeding 3 g/m2/day. In this respect there were no significant differences between the three acetylsalicylic acid preparations used. The results of this study also suggest that the serum salicylate concentrations should not exceed 2000 mumol/l (about 27 mg/100 ml). The symptoms of salicylism correlated closely with serum salicylate levels, which, in turn, correlated well with the dosage in g/m2. Elevation of serum aspartate aminotransferase was noted in 1/3 of the cases. All of these had a dose exceeding 2 g/m2, and the frequency of elevated enzyme activities increased with increasing dosage. In the group receiving enteric coated form of acetylsalicylic acid, there were fewer positive benzidine tests (12%) than in the two other groups (22--28%).
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