The binary eutectic of NSAIDS and two-phase liquid system for enhanced membrane permeation.
The eutectic properties of binary mixtures of some nonsteroidal anti-inflammatory drugs (NSAIDs) with ibuprofen were studied using differential scanning calorimetry (DSC) and phase equilibrium diagrams. The melting points of selected NSAIDs were significantly depressed due to binary eutectic formation with ibuprofen. Ketoprofen and ibuprofen were selected to study the effect of eutectic formation on membrane permeation using Franz diffusion cells and snake skin as the model membrane. The presence of aqueous isopropyl alcohol (IPA) was necessary to completely transform the solid drugs into an oily state at ambient temperature. As much as the 99.6% of ibuprofen and the 88.8% of ketoprofen added were found in the oily phase of the two-phase liquid system formed when aqueous IPA was added to the eutectic mixture. Due to the high drug concentration in the oily phase, and maximum thermodynamic activity, the two-phase liquid system showed enhanced membrane permeation rates of ibuprofen (37.5 microg/cm2/hr) and ketoprofen (33.4 microg/cm2/hr) compared to other reference preparations used.
Yuan
Xudong
X
Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, Georgia 30602, USA.
Capomacchia
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AC
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000032:analysis* / Q000493:pharmacokinetics*; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002463:Cell Membrane Permeability / Q000187:drug effects / Q000502:physiology; D002626:Chemistry, Pharmaceutical; D007660:Ketoprofen / Q000032:analysis / Q000493:pharmacokinetics; D010539:Permeability / Q000187:drug effects; D012867:Skin / Q000187:drug effects / Q000378:metabolism*; D012911:Snakes
D000894:Anti-Inflammatory Agents, Non-Steroidal; D007660:Ketoprofen