Enhancement of permeability of ethyl cellulose films for drug penetration.
Permeability constants of salicylic acid, caffeine and benzoic acid have been measured at 37 degrees for heterogeneous films of ethyl cellulose containing up to 50% PEG 4000, the latter component undergoing leaching out. For the first two compounds, steady state constants were independent of film thickness and solute concentration but increased linearly and sharply with PEG content and were reproducible. The films were impermeable to NaOH and permeation rates were independent of receiver compartment pH. Solubility coefficients and diffusion coefficients of the substances in the films were measured using sorption and/or time lag methods and were low as compared with polyethylene films. High solubility seemed to be associated with the presence of a free activated hydrogen, shown by sorption studies on other substances. From the evidence, it appeared that mass transfer was controlled by the solubility diffusion process in the ethyl cellulose of the membranes with all three substances. Enhancement of permeability by PEG thus seemed due to increased porosity, equivalent to reduction in the effective thickness of the matrix, which nevertheless retained its barrier properties. Enhancement coefficients calculated from the slopes of PEG concentration plots may be useful for predicting the increased mass transfer of drugs through such membranes and could enable the porosity and thickness factors to be balanced against each other for formulation of coated products.
D000042:Absorption; D002110:Caffeine; D002482:Cellulose; D055598:Chemical Phenomena; D002621:Chemistry; D004058:Diffusion; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008567:Membranes, Artificial; D010539:Permeability; D004364:Pharmaceutical Preparations; D011092:Polyethylene Glycols; D012459:Salicylates; D012995:Solubility; D013696:Temperature
D008567:Membranes, Artificial; D004364:Pharmaceutical Preparations; D012459:Salicylates; D002110:Caffeine; D011092:Polyethylene Glycols; D002482:Cellulose