Enhanced drug dissolution using evaporative precipitation into aqueous solution.
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.
Sarkari
Marazban
M
Department of Chemical Engineering, University of Texas at Austin, Austin, TX 78712-1062, USA.
Brown
Judith
J
Chen
Xiaoxia
X
Swinnea
Steve
S
Williams
Robert O
RO
Johnston
Keith P
KP
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
D000927:Anticonvulsants; D005079:Excipients; D019999:Pharmaceutical Solutions; D013501:Surface-Active Agents; D013535:Suspensions; D014867:Water; D002220:Carbamazepine