title: Physicochemical and pharmacokinetic characterization of a spray-dried malotilate emulsion.
abstract: Malotilate (MT) is a hepatoprotective drug administered orally. However, MT was found to be a poorly water-soluble drug with low oral bioavailability. In the present investigation, a novel spray-dried emulsion (SDE) loaded with MT was prepared, and its physicochemical properties were characterized by rheological evaluation, particle size measurement, in vitro release, and surface morphology. The pharmacokinetic study of SDE, in comparison to MT suspension with the pure MT powder homogeneously dispersed in 0.5% CMC-Na solution, was also performed in rats after a single oral dose. It was found that SDE exhibited a 2.9-fold higher peak plasma concentration (C(max)) and 2.3-fold higher area under the curve (AUC) than MT suspension.
authors.affiliation: School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Jianjun
authors.initials: J
authors.lastname: Zhang
authors.forename: Yuan
authors.initials: Y
authors.lastname: Gao
authors.forename: Shuai
authors.initials: S
authors.lastname: Qian
authors.forename: Xin
authors.initials: X
authors.lastname: Liu
authors.forename: Hui
authors.initials: H
authors.lastname: Zu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004655:Emulsions; D005079:Excipients; D008107:Liver Diseases / Q000378:metabolism; D008297:Male; D008314:Malonates / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D010316:Particle Size; D011208:Powders; D020011:Protective Agents / Q000032:analysis* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D051381:Rats; D012995:Solubility
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D008314:Malonates; D011208:Powders; D020011:Protective Agents; C024808:diisopropyl 1,3-dithiol-2-ylidenemalonate