Enhanced controlled release of loratadine from the ethylene-vinyl acetate matrix containing plasticizer.
An ethylene-vinyl acetate (EVA) matrix containing plasticizer was prepared as a potential controlled release system for loratadine. The EVA matrix containing loratadine was prepared as the transdermal device using casting methods. The solubility of loratadine according to the volume fraction of PEG 400 was determined. The effects of the drug concentration, temperature, and plasticizers on the release of the drug were determined at 37 degrees C using 40% PEG 400 solution as the receptor medium using the modified Keshary-Chien cell. Some types of plasticizers. such as citrates and phthalates, were used to prepare the pores and increase the flexibility of the EVA matrix. The solubility test according to the PEG 400 volume fraction revealed the highest solubility in the 40% PEG 400 solution. The rate of drug released from the EVA matrix increased with increasing temperature and drug loading. There was a linear relationship between the release rate and the square root of the loading dose. The activation energy for drug release from the EVA matrix with a loading dose of 1%, 2%, 3%, 4%, and 5% was estimated to be 6.83, 6.80, 6.77, 6.71, and 6.65 kcal/mol, respectively Among the plasticizers used, diethyl phthalate showed the highest level of loratadine release. In conclusion, an EVA matrix containing plasticizer could be used to enhance the controlled release of loratadine.
Cho
Cheong-Weon
CW
College of Pharmacy, Chungnam National University, Daejeon, South Korea.
Kim
Seong-Jin
SJ
Yang
Kyu-Ho
KH
Song
Jae-Haeng
JH
Jeong
Hyun-Jon
HJ
Shin
Sang-Chul
SC
D000279:Administration, Cutaneous; D002851:Chromatography, High Pressure Liquid; D002951:Citrates / Q000737:chemistry; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D005079:Excipients / Q000737:chemistry*; D039563:Histamine H1 Antagonists, Non-Sedating / Q000737:chemistry*; D007700:Kinetics; D017336:Loratadine / Q000737:chemistry*; D008567:Membranes, Artificial; D010539:Permeability; D010795:Phthalic Acids / Q000737:chemistry; D010968:Plasticizers / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry*; D012995:Solubility; D013696:Temperature
D002951:Citrates; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D039563:Histamine H1 Antagonists, Non-Sedating; D008567:Membranes, Artificial; D010795:Phthalic Acids; D010968:Plasticizers; D011145:Polyvinyls; C016438:ethylenevinylacetate copolymer; D011092:Polyethylene Glycols; D017336:Loratadine; C007379:diethyl phthalate