betadex has been researched along with epalrestat* in 1 studies
1 other study(ies) available for betadex and epalrestat
| Article | Year |
|---|---|
Enhanced dissolution and skin permeation profiles of epalrestat with β-cyclodextrin derivatives using a cogrinding method.
Epalrestat (EPL) is a water-insoluble drug (14μM) that inhibits aldose reductase. This study investigated the interactions between β-cyclodextrin (CD) derivatives and EPL to determine the solubilizing effect on EPL from phase solubility diagrams. We improved the solubility of EPL in water by adding β-CD derivatives. Moreover, the solubility of EPL mixed with β-CD derivatives by cogrinding in a ball mill method was about 2-3 times higher than those of EPL with the same CD concentration (5mM) calculated from phase solubility diagrams. In addition, we investigated the effect of β-CD derivatives on in vitro percutaneous absorption of EPL through hairless mouse skin. Among the coground mixtures of EPL and β-CD derivatives, the mixture containing methyl (ME)-β-CD showed the strongest enhancement of EPL skin permeation. Furthermore, adding 10wt% urea as a skin permeation enhancer after cogrinding with ME-β-CD improved the flux of EPL 300 times compared to the flux of EPL alone. This result indicates the ME-β-CD ground mixture system with urea has potential as a new transdermal drug delivery system of EPL for diabetic neuropathy. Topics: Administration, Cutaneous; Aldehyde Reductase; Animals; beta-Cyclodextrins; Calorimetry, Differential Scanning; Chromatography, High Pressure Liquid; Drug Carriers; Drug Liberation; Male; Mice; Permeability; Rhodanine; Skin Absorption; Solubility; Surface Properties; Thiazolidines; X-Ray Diffraction | 2017 |