In vitro and in vivo study in rats of rectal suppositories containing furosemide.
The aim of our experimental work was to formulate furosemide-containing rectal suppositories, to study drug release with in vitro membrane diffusion examinations and to increase drug liberation with the use of non-ionic surfactants (Solutol HS 15, Cremophor RH 60, Montanox 60 DF), which were incorporated in the suppository base in various concentrations. Suppocire AS2X proved to be the best suppository base (diffused drug: 69.78%). The use of 1% Cremophor RH 60 additive with the Witepsol H 15 base increased the quantity of the diffused drug from 62 to 75%. The membrane diffusion examinations were followed by studying the influence of suppository bases and additives exerted on the actual diuretic effect in Sprague-Dawley male rats. Once again the Suppocire AS2X suppository base gave the best results compared to the control; the quantity of the animals' urine showed a fourfold increase. Used with the Witepsol H 15 base, even 1% of all the three additives resulted in a considerable increase of diuretic effect, so their use proved to be advantageous. The comparison of the membrane diffusion examinations with the in vivo diuretic effect reveals that in vitro drug release and the pharmacological effect usually showed the same tendency, that is a greater extent of in vitro furosemide release was associated with a greater quantity of rat urine.
Berkó
Szilvia
S
Department of Pharmaceutical Technology, University of Szeged, Hungary.
Regdon
Géza
G
Ducza
Eszter
E
Falkay
George
G
Erós
István
I
D000285:Administration, Rectal; D000818:Animals; D004058:Diffusion; D004231:Diuresis / Q000187:drug effects; D004232:Diuretics / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D005665:Furosemide / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D014677:Pharmaceutical Vehicles; D051381:Rats; D017207:Rats, Sprague-Dawley; D013488:Suppositories; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology
D004232:Diuretics; D014677:Pharmaceutical Vehicles; D013488:Suppositories; D013501:Surface-Active Agents; D005665:Furosemide