Quantitative structure — pharmacokinetic relationship of a series of sulfonamides in the rat
| Autor: | S. Kaul, W. A. Ritschel |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
Pharmacology
Volume of distribution Sulfonamides Time Factors Chromatography Series (mathematics) Chemistry Quantitative structure Blood Proteins Rats Rats Zucker Partition coefficient Structure-Activity Relationship Linear relationship Pharmacokinetics Injections Intravenous Animals Colorimetry Female Pharmacology (medical) Quantitative analysis (chemistry) Protein Binding Antibacterial agent |
| Zdroj: | European Journal of Drug Metabolism and Pharmacokinetics. 15:211-217 |
| ISSN: | 2107-0180 0378-7966 |
| Popis: | The pharmacokinetics of a series of sulfonamides were investigated after intravenous administration of a 7 mg/kg dose of individual sulfonamides to cannulated female lean Zucker rats. The concentrations of the sulfonamides in blood were determined by colorimetry. The blood concentration-time curves were fitted to a biexponential equation. The partition coefficient, log P, and pKa values of the sulfonamides were taken from the literature, log P and pKa values differed markedly across the series. The extent of protein binding varied enormously, increasing with partition coefficient. There was no significant relationship between the volume of distribution and partition coefficient. However, when the influence of protein binding on volume of distribution was eliminated, a significant linear relationship emerged. Total clearance formed a relatively complex nonlinear relationship with partition coefficient. The relationship of elimination half-life and partition coefficient was inverse of that between clearance and partition coefficient because of a lack of significant relationship between volume of distribution and partition coefficient. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink