The bioavailability of seven commercially available rectal aminophylline suppositories
- 26 Downloads
The bioavailability and thein vitro parameters of seven aminophylline 360 mg suppositories were compared with an oral hydroalcoholic solution of aminophylline as reference, using cross-over designs in groups of four subjects in single dose experiments. Plasma concentrations were followed for eight hours after drug administration. Four products gave extents of bioavailability of less than 80% of the reference solution. A dissolution test gave results which did not correlate well with the bioavailability results. It was concluded that no satisfactory plasma levels can be reached with the examined dose of aminophylline after single administration of one suppository.
Calculation of the steady-state concentration was performed as well as a graphic simulation of the plasma concentration-time curves, after repeated administration; it was demonstrated that with most of the suppositories no sufficiently high level could be obtained after three doses per day.
KeywordsTheophylline Aminophylline Theobromine Melting Time Graphic Simulation
Unable to display preview. Download preview PDF.
- Blaey, C.J. De, andA.G. De Boer (1976)Pharm. Weekblad 111, 1216–1221.Google Scholar
- Blaey, C.J. De, andJ.J. Rutten-Kingma (1976)Pharm. Act. Helv. 51, 186–192;Ibidem (1977) 52, 11–14.Google Scholar
- Breimer, D.D. (1976)Pharm. Weekblad 111, 1221–1236.Google Scholar
- British Pharmacopoeia (1980) University Press, Cambridge, England.Google Scholar
- Dutch Pharmacopoeia (1978) ed. VIII. Staatsuitgeverij, The Hague, The Netherlands.Google Scholar
- European Pharmacopoeia (1975) ed. 1, Vol. III Maisonneuve S.A., Sainte Ruffine, France.Google Scholar
- Krówczynski, L. (1959)Dissertationes Pharm. 269.Google Scholar
- Mcgilveray, I.J., K.K. Midha andJ.K. Cooper (1978b)Can. J. Pharm. Sci. 13, 33–39.Google Scholar
- Mcgilveray, I.J., K.K. Midha andJ.K. Cooper (1978b)Can. J. Pharm. Sci. 13, 9–11.Google Scholar
- Riegelman, S., andR.A. Upton (1979) In:Drug Absorption (Prescott, L.F., andW.S. Nimmo, Eds.).Adis Press, Sidney, 297.Google Scholar
- Stuurman-Bieze, A.G.G., A.J.M. Schoonen, A. Fens, V.D. Heuy, L.M. Peeters-Udding andT. Huizinga (1980)Pharm. Weekblad Sci. Ed. 2, 172–179.Google Scholar
- Sved, S., andD.L. Wilson (1977)Res. Comm. Chem. Pathol. Pharmacol. 17, 319–331.Google Scholar
- Tukker, J.J., andC.J. De Blaey (1981) In preparation.Google Scholar
- Zuidema, J. (1978) Ph.D. Thesis, Amsterdam, The Netherlands.Google Scholar