title: Dissolution evaluation in vitro and bioavailability in vivo of self-microemulsifying drug delivery systems for pH-sensitive drug loratadine.
abstract: The aim of this study was to improve the oral absorption of loratadine, a pH-sensitive drug, by self-microemulsifying drug delivery systems (SMEDDSs). The optimal SMEDDS was analysed and evaluated after emulsification in distilled water with diameter of 26.57 ± 0.71 nm and zeta potential of -30.5 ± 4.5 mV. Dissolution experiments in vitro were carried out in different released media of pH values and the SMEDDS formulations were able to release loratadine completely in different media while market tablets just performed similarly in the media of pH 1.2. Furthermore, the oral bioavailability and the pharmacokinetic behaviour of loratadine formulations in vivo were studied after a single dose of 1 mg/kg loratadine in beagle dogs. The SMEDDS formulations displayed higher Cmax and AUC, approximately 9 and 5 times increase than those of market tablets (p < 0.01) respectively. These results demonstrated that SMEDDS formulations had significantly increased the oral absorption of loratadine in beagle dogs.
authors.affiliation: Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences , Beijing , China.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Li
authors.forename: Yonggang
authors.initials: Y
authors.lastname: Tan
authors.forename: Lixia
authors.initials: L
authors.lastname: Yang
authors.forename: Lijun
authors.initials: L
authors.lastname: Gao
authors.forename: Tao
authors.initials: T
authors.lastname: Wang
authors.forename: Xi
authors.initials: X
authors.lastname: Yang
authors.forename: Dongqin
authors.initials: D
authors.lastname: Quan
mesh_terms: D000818:Animals; D018926:Anti-Allergic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004285:Dogs; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical; D065546:Drug Liberation; D004655:Emulsions; D006863:Hydrogen-Ion Concentration; D017336:Loratadine / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D065568:Oral Mucosal Absorption
chemical_list: D018926:Anti-Allergic Agents; D004655:Emulsions; D017336:Loratadine
keywords: Dissolution; loratadine; oral absorption; pharmacokinetics; self-microemulsifying drug delivery systems