Application of TPX polymer membranes for the controlled release of triprolidine.

摘要

Oral administration of triprolidine, antihistamines, may cause many adverse effects such as dry mouth, sedation, dizziness and transdermal drug delivery was considered. Poly(4-methyl-1-pentene) (TPX) membrane, which has good mechanical strength was fabricated by the casting method. TPX membranes was a little brittle and the plasticizers was added for preparing the membranes. The present study was carried out to evaluate the possibility of using the polymer TPX membrane as a controlling membrane and further develop a TPX matrix system for transdermal delivery of triprolidine. The effects of molecular weights of TPX, plasticizers, polyethylene glycol (PEG) 400, drug concentration, and temperature on drug release were studied. The solubility of triprolidine increased exponentially as the increased volume fraction of PEG 400 in saline, and the rate of permeation through TPX membrane was proportional to PEG 400 volume fraction. The release rate of drug from the TPX matrix increased with increased temperature and drug concentration. Among the plasticizers used such as alkyl citrates, phthalates and sebacate, tetra ethyl citrate (TEC) showed the best enhancing effects. Enhancement factor of TEC was 3.76 from TPX matrix at 37 degrees C. The transdermal controlled release of triprolidine system could be developed using the TPX polymer including the plasticizer.