Membrane penetration enhancement of ibuprofen using supersaturation.
Permeation enhancement of ibuprofen from supersaturated solutions formed using the cosolvent technique was investigated using silicone as a model membrane. Hydroxpropyl methyl cellulose and hydroxpropyl-beta-cyclodextrin were used to stabilise the supersaturated states. Physical stability studies showed best results for low drug concentrations in a 40:60 propylene glycol/water cosolvent system. Variations in flux across model silicone membranes from saturated solutions were observed as the PG content was increased. The flux of IBU increased with the degree of saturation for solutions prepared in a 40:60 PG/water cosolvent mixture. HPMC and CD were found to be effective in enhancing the stability of supersaturated solutions of IBU. The mechanisms of action are different for the two additives and are discussed.
Iervolino
M
M
Dipartimento di Chimica Farmaceutica e Tossicologica, Universitá di Napoli 'Federico II', Via D. Montesano 49, Napoli, Italy.
Raghavan
S L
SL
Hadgraft
J
J
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage*; D003505:Cyclodextrins; D004058:Diffusion; D004355:Drug Stability; D007052:Ibuprofen / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D007785:Lactose / Q000031:analogs & derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives; D010078:Oxazines; D010539:Permeability; D012995:Solubility; D047392:beta-Cyclodextrins
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003505:Cyclodextrins; D010078:Oxazines; D047392:beta-Cyclodextrins; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose; C031215:betadex; D007052:Ibuprofen