R. Tarantino, E. Bishop, F. C. Chen
Sep 1, 1994
Citations
0
Influential Citations
30
Citations
Journal
Journal of pharmaceutical sciences
Abstract
N-Methyl-2-pyrrolidone (methylpyrrolidone), a cosolvent which has been used in veterinary medicine and in transdermal delivery devices, was investigated as a cosolvent for model drug compounds of widely varying polarity. These compounds were digoxin, sulfamethoxazole, hydrocortisone acetate, theophylline, phenytoin, and reserpine. Methylpyrrolidone was found to be an extremely efficient cosolvent for low solubility polar drugs such as digoxin or drugs containing multiple proton-donating groups such as phenytoin. The increase in solubility observed in aqueous solutions of digoxin and phenytoin to which 0.2 volume fraction of methylpyrrolidone was added was 500x and 65x, respectively. Significant deviations from log-linear solubilization were observed with digoxin, sulfamethoxazole, phenytoin, and reserpine, indicating significant water-solute-cosolvent interactions.