Effect of various vehicles on ketoprofen permeation across excised hairless mouse skin. 1993

S Goto, and T Uchida, and C K Lee, and T Yasutake, and J B Zhang
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.

The effects of glycerides, short-chain alcohols, and their binary vehicles as donor components on the permeation of ketoprofen (KP) across the excised hairless mouse skin were evaluated with the modified LOVEDAY-type diffusion cell. Among single vehicles, Panasate 800 as tricaprylin appeared to be the most favorable lipophilic vehicle, with no toxicity and with a short lag time (0.9 h), and methanol (MeOH) or ethanol (EtOH) as hydrophilic single vehicles showed the highest KP permeation flux (244.1 and 134.1 micrograms/cm2/h, respectively). Furthermore, KP permeation was enhanced remarkably by the combination of EtOH and Panasate 800 compared with each single vehicle as reflected in the decreased lag time and increased flux. The greatest enhancement was observed in the EtOH/Panasate 800 (40/60) binary vehicle (permeation ratio at 24 h, 40.0%; steady-state flux, 314.0 micrograms/cm2/h; lag time, 3.7 h). Further investigations involving stripping studies and KP accumulation within the skin were performed to explain the mechanism of enhancement caused by the above binary vehicle. It was suggested that the mutual enhancement effect of EtOH/Panasate 800 (40/60) binary vehicle is due to decreasing the barrier ability of the stratum corneum by EtOH and the viable skin by Panasate 800.

UI MeSH Term Description Entries
D007660 Ketoprofen An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis. Benzoylhydratropic Acid,19,583 RP,2-(3-Benzoylphenyl)propionic Acid,Alrheumat,Alrheumum,Orudis,Profenid,RP-19583,RP 19583,RP, 19,583,RP19583
D008812 Mice, Hairless Mutant strains of mice that produce little or no hair. Hairless Mice,Mice, Inbred HRS,Mice, hr,Hairless Mouse,Mice, HRS,Mouse, HRS,Mouse, Inbred HRS,HRS Mice,HRS Mice, Inbred,HRS Mouse,HRS Mouse, Inbred,Inbred HRS Mice,Inbred HRS Mouse,Mouse, Hairless
D005989 Glycerides GLYCEROL esterified with FATTY ACIDS. Acylglycerol,Acylglycerols
D000431 Ethanol A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in ALCOHOLIC BEVERAGES. Alcohol, Ethyl,Absolute Alcohol,Grain Alcohol,Alcohol, Absolute,Alcohol, Grain,Ethyl Alcohol
D000438 Alcohols Alkyl compounds containing a hydroxyl group. They are classified according to relation of the carbon atom: primary alcohols, R-CH2OH; secondary alcohols, R2-CHOH; tertiary alcohols, R3-COH. (From Grant & Hackh's Chemical Dictionary, 5th ed)
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
D012869 Skin Absorption Uptake of substances through the SKIN. Absorption, Skin,Intracutaneous Absorption,Intradermal Absorption,Percutaneous Absorption,Transcutaneous Absorption,Transdermal Absorption,Absorption, Intracutaneous,Absorption, Intradermal,Absorption, Percutaneous,Absorption, Transcutaneous,Absorption, Transdermal,Absorptions, Intracutaneous,Absorptions, Intradermal,Absorptions, Percutaneous,Absorptions, Skin,Absorptions, Transcutaneous,Absorptions, Transdermal,Intracutaneous Absorptions,Intradermal Absorptions,Percutaneous Absorptions,Skin Absorptions,Transcutaneous Absorptions,Transdermal Absorptions
D014677 Pharmaceutical Vehicles A carrier or inert medium used as a solvent (or diluent) in which the medicinally active agent is formulated and or administered. (Dictionary of Pharmacy, 1986) Pharmaceutical Vehicle,Vehicle, Pharmaceutical,Vehicles, Pharmaceutical
D015194 Diffusion Chambers, Culture Devices used in a technique by which cells or tissues are grown in vitro or, by implantation, in vivo within chambers permeable to diffusion of solutes across the chamber walls. The chambers are used for studies of drug effects, osmotic responses, cytogenic and immunologic phenomena, metabolism, etc., and include tissue cages. Culture Diffusion Chambers,Semi-Permeable Chambers,Tissue Cages,Semipermeable Chambers,Cage, Tissue,Cages, Tissue,Chamber, Culture Diffusion,Chamber, Semi-Permeable,Chamber, Semipermeable,Chambers, Culture Diffusion,Chambers, Semi-Permeable,Chambers, Semipermeable,Culture Diffusion Chamber,Diffusion Chamber, Culture,Semi Permeable Chambers,Semi-Permeable Chamber,Semipermeable Chamber,Tissue Cage
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

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