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In vitro and in vivo study in rats of rectal suppositories containing furosemide. 2002

Szilvia Berkó, and Géza Regdon, and Eszter Ducza, and George Falkay, and István Erós
Department of Pharmaceutical Technology, University of Szeged, Hungary.

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.

UI MeSH Term Description Entries
D008297 Male Males
D004058 Diffusion The tendency of a gas or solute to pass from a point of higher pressure or concentration to a point of lower pressure or concentration and to distribute itself throughout the available space. Diffusion, especially FACILITATED DIFFUSION, is a major mechanism of BIOLOGICAL TRANSPORT. Diffusions
D004231 Diuresis An increase in the excretion of URINE. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Diureses
D004232 Diuretics Agents that promote the excretion of urine through their effects on kidney function. Diuretic,Diuretic Effect,Diuretic Effects,Effect, Diuretic,Effects, Diuretic
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005665 Furosemide A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY. Frusemide,Fursemide,Errolon,Frusemid,Furanthril,Furantral,Furosemide Monohydrochloride,Furosemide Monosodium Salt,Fusid,Lasix
D000285 Administration, Rectal The insertion of drugs into the rectum, usually for confused or incompetent patients, like children, infants, and the very old or comatose. Anal Drug Administration,Drug Administration, Rectal,Instillation, Rectal,Rectal Drug Administration,Drug Administration, Anal,Rectal Administration,Administration, Anal Drug,Administration, Rectal Drug,Administrations, Anal Drug,Administrations, Rectal,Administrations, Rectal Drug,Anal Drug Administrations,Drug Administrations, Anal,Drug Administrations, Rectal,Instillations, Rectal,Rectal Administrations,Rectal Drug Administrations,Rectal Instillation,Rectal Instillations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013488 Suppositories Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature. Rectal Suppositories,Vaginal Suppositories,Vaginal Suppository,Suppositories, Rectal,Suppositories, Vaginal,Suppository, Vaginal
D013501 Surface-Active Agents Agents that modify interfacial tension of water; usually substances that have one lipophilic and one hydrophilic group in the molecule; includes soaps, detergents, emulsifiers, dispersing and wetting agents, and several groups of antiseptics. Surface Active Agent,Surface-Active Agent,Surfactant,Surfactants,Tenside,Amphiphilic Agents,Surface Active Agents,Tensides,Active Agent, Surface,Active Agents, Surface,Agent, Surface Active,Agent, Surface-Active,Agents, Amphiphilic,Agents, Surface Active,Agents, Surface-Active

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