Biopharmaceutics of rectal administration of drugs in man I. Introduction of benzoic acid as a test drug

Autor: A.G.G. Stuurman-Bieze, Frits Moolenaar, Jan Visser, T. Huizinga
Rok vydání: 1978
Předmět:
Zdroj: International Journal of Pharmaceutics. 1:323-336
ISSN: 0378-5173
DOI: 10.1016/s0378-5173(78)80003-9
Popis: Summary In this report it will be shown that benzoic acid is a suitable test drug to study the biopharmaceutics of rectally administered dosage forms in man. After intravenous administration of sodium benzoate it can be seen from pharmacokinetic parameters that biotransformation to hippurate is extremely rapid. The clearance of hippurate occurs exclusively by renal excretion. At relatively low concentrations, as used in our rectal experiments, elimination of hippurate is not capacity limited and therefore linear pharmacokinetics is assumed, according to a multi-compartment model. After rectal administration the absorption of sodium benzoate is fast and complete. Bioavailability after 4 h has been found in the same range for both oral and rectal routes. There was an excellent correlation between plasma and urine levels of hippurate. It is concluded that, by measuring hippurate levels in plasma or urine, the influence on absorption rate and bioavailability of formulation factors using rectal dosage forms with sodium benzoate and benzoic acid can be determined.
Databáze: OpenAIRE