Disposition of thiazinamium in humans after administration as an ion pair
In this study we have investigated to what extent the concept of ‘ion pair’ absorption is valid after administering the quaternary ammonium ion thiazinamium rectally to humans. Salicylate has been selected as counter ion. The bioavailability was estimated by determining the amount of unchanged drug excreted in urine over a period of 24 hours. The ion pair was administered either alone or in the presence of an excess of counter ions.
The results were compared with those obtained after giving the drug as the completely ionized salt thiazinamium methylsulphate. In addition, ‘in vivo’ ion pair formation was studied. Both the ion pair and the salt were administered in two suppository bases, namely a lipophilic (Witepsolh15) and a hydrophilic one (a polyethylene glycol mixture). Absorption after rectal administration of the ion pair was found to be of the same order of magnitude as that found with the salt. So, administration in suppositories of thiazinamium as salicylate ion pair would offer only slight advantages over administration of the salt.
KeywordsSalicylate Systemic Availability Rectal Administration Pharmaceutisch Weekblad Scientific Edition Suppository Base
Unable to display preview. Download preview PDF.
- Bevernage, K. B. M., andJ. Polderman (1973)Pharm. Weekblad 108, 429–438.Google Scholar
- Jonkman, J. H. G. (1977)Thiazinamium methylsulphate, bioanalysis and pharmacokinetics. Ph. D. Thesis. University of Groningen, The Netherlands.Google Scholar
- Jonkman, J. H. G., L. E. Van Bork, J. Wijsbeek, A. S. Bolhuis-De Vries, R. A. De Zeeuw, J. E. Greving andN. G. M. Orie (1979a)Pharm. Weekblad Sci. Ed. 1, 121–124.Google Scholar
- Jonkman, J. H. G., L. E. Van Bork, J. Wusbeek, A. S. Bolhuis-De Vries, R. A. De Zeeuw, N. G. M. Orie andH. L. M. Cox (1979b)Int. J. of Pharmaceutics, in press.Google Scholar
- Ritschel, W. A. (1973)Angewandte Biopharmazie. Wissenschaftliche Verlagsgesellschaft, Stuttgart, p. 465–487.Google Scholar