Preparation and central action of propofol/hydroxypropyl-beta-cyclodextrin complexes in rabbits.
Inclusion complexes of propofol (CAS 2078-54-8) and hydroxypropyl-beta-cyclodextrin (HP-beta-CD) were examined in aqueous solution and in the solid state by phase solubility technique, IR-spectroscopy and differential scanning calorimetry. Solid complexes obtained by kneading method were dissolved in artificial plasma leading to a colloidal solution which was suitable for intravenous administration. In the in vivo studies propofol (15 mg/kg) was given intravenously to rabbits in equimolar doses as cyclodextrin complexes and as Diprivan. The central action of the drug was verified by recording the bioelectrical activity of the precentral cortex. The statistical evaluation of the results do not indicate differences in onset, duration and maximum of action between the two dosage forms.
Viernstein
H
H
Institute of Pharmaceutical Technology, University of Vienna, Austria.
Stumpf
C
C
Spiegl
P
P
Reiter
S
S
D000818:Animals; D002152:Calorimetry, Differential Scanning; D002490:Central Nervous System / Q000187:drug effects*; D002855:Chromatography, Thin Layer; D003505:Cyclodextrins / Q000138:chemical synthesis / Q000494:pharmacology*; D004355:Drug Stability; D004569:Electroencephalography / Q000187:drug effects; D005260:Female; D008297:Male; D015742:Propofol / Q000138:chemical synthesis / Q000494:pharmacology*; D011817:Rabbits; D012995:Solubility; D013055:Spectrophotometry, Infrared; D047392:beta-Cyclodextrins
D003505:Cyclodextrins; D047392:beta-Cyclodextrins; C083507:propofol hydroxypropyl-beta-cyclodextrin; D015742:Propofol