Controlled release of triprolidine using ethylene-vinyl acetate membrane and matrix systems.

摘要

The studies on the permeability of triprolidine through ethylene-vinyl acetate (EVA) copolymer membrane using two-chamber diffusion cell was carried out to develop the controlled delivery system. To evaluate the effect of drug concentration in reservoir, polyethylene glycol (PEG) 400 was added to saline solution as a solubilizer and a sink condition was maintained in the receptor solution. The permeation rate of drug through EVA membrane was proportional to PEG 400 volume fraction. A linear relationship existed between the permeation rate and the reciprocal of the membrane thickness. Triprolidine-containing matrix was fabricated with EVA copolymer to control the release of the drug. The plasticizers was added for preparing the pore structure of EVA membranes to increase the drug release. The effects of PEG 400, vinyl acetate (VA) contents of EVA, membrane thickness, drug concentration, temperature, and plasticizers, on drug release were studied. The release rate of drug from the EVA matrix increased with PEG 400 volume fraction, increased temperature and drug loading doses. An increased vinyl acetate comonomer content in EVA membrane increased the drug release rate and permeability coefficient. Among the plasticizers used such as alkyl citrates and phthalates, tetra ethyl citrate showed the best enhancing effects showing the enhancement factor of 1.88. The release of triprolidine from the EVA matrix follows a diffusion controlled model, where the quantity released per unit area is proportional to the square root of time. The controlled release of triprolidine could be achieved using the EVA polymer including the plasticizer.