Preparation of lorazepam-loaded microemulsions for intranasal delivery and its pharmacokinetics
会议名称：《2010年中国药学大会暨第十届中国药师周》
会议日期：2010年
学科分类：100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学]
关 键 词：lorazepam microemulsions intranasal delivery pharmacokinetics
摘 要：The purpose of this study was to develop a microemulsion system for intranasal delivery of lorazepam. The phase behavior and properties of microemulsions were characterized in a pseudo-ternary system composed of Cremophor EL 35 /Transcutol P/Lauroglycol FCC or Labrafil M 1944CS/water, and intranasal absorption of loazepam from microemulsions was investigated in rabbit. The microemulsions comprising of FCC, Cremophor EL 35 /Transcutol P （1.5:1） and water was optimal for intranasal delivery of lorazepam. These systems had a higher solubilization capacity with the particle size of 150 nm, and were stable at ambient conditions for at least six months. In vivo absorption studies showed that intranasal absorption of lorazepam from microemulsions at 0.38 mg/kg had the larger AUC0-t, the longer half-life and the prolonged circulation time with the mean bioavailability of 80.84% for ME2 and 63.48% for ME8 as compared to the intramuscular injection at 0.16mg/kg. These results indicate that the microemulsions may be a promising approach for the intranasal delivery of lorazepan.