title: Enhanced drug dissolution using evaporative precipitation into aqueous solution.
abstract: A new process, evaporative precipitation into aqueous solution (EPAS) has been developed to coat poorly water soluble drugs, in this case carbamazepine, with hydrophilic stabilizers to enhance dissolution rates. A heated organic solution of the drug in dichloromethane is sprayed though a fine nozzle into a heated aqueous solution. The rapid evaporation of the organic solvent produces high supersaturation and rapid precipitation of the drug in the form of a colloidal suspension that is stabilized by a variety of low molecular weight and polymeric surfactants. The stabilizer adsorbs to the drug surface and prevents particle growth and crystallization during the spray process. The suspensions are dried by spray drying or ultra-rapid freezing. The high dissolution rates are a consequence of the following advantages of the EPAS process: a small primary particle size, a hydrophilic coating on the particles that enhances wetting, and low crystallinity.
authors.affiliation: Department of Chemical Engineering, University of Texas at Austin, Austin, TX 78712-1062, USA.
authors.forename: Marazban
authors.initials: M
authors.lastname: Sarkari
authors.forename: Judith
authors.initials: J
authors.lastname: Brown
authors.forename: Xiaoxia
authors.initials: X
authors.lastname: Chen
authors.forename: Steve
authors.initials: S
authors.lastname: Swinnea
authors.forename: Robert O
authors.initials: RO
authors.lastname: Williams
authors.forename: Keith P
authors.initials: KP
authors.lastname: Johnston
mesh_terms: D000927:Anticonvulsants / Q000737:chemistry*; D002220:Carbamazepine / Q000737:chemistry*; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical; D005079:Excipients; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D019999:Pharmaceutical Solutions; D012995:Solubility; D013501:Surface-Active Agents; D013535:Suspensions; D014867:Water; D014961:X-Ray Diffraction
chemical_list: D000927:Anticonvulsants; D005079:Excipients; D019999:Pharmaceutical Solutions; D013501:Surface-Active Agents; D013535:Suspensions; D014867:Water; D002220:Carbamazepine