Enhanced dissolution of oxcarbazepine microcrystals using a static mixer process.
The purpose of this study was to form micronized powders of Oxcarbazepine (OXC), a poorly water-soluble drug, using a static mixer technique to enhance the dissolution rate. Controlled precipitation was achieved injecting the organic OXC solution rapidly into an aqueous methylcellulose (MC) protective solution by means of a static mixer thus providing turbulent and homogeneous mixing. Furthermore, a factorial design was implemented for data analysis. The physicochemical properties of the freeze-dried dispersions were evaluated by differential scanning calorimetry (DSC), infrared spectroscopy (FTIR) and X-ray diffraction (XRD). Drug microcrystals showed a narrow size distribution with approximately 2 microm mean particle size and high drug loading. DSC and FTIR studies revealed that the drug remained in crystalline state and no drug-polymer interaction occurred. The dissolution studies showed enhanced dissolution of OXC microcrystals compared to the pure drug. The static mixer technique was proved capable for micro-sized polymeric particles. This is an inexpensive, less time consuming and fully scalable process for development of poorly soluble drugs.
Douroumis
D
D
Department of Pharmaceutical Technology, Friedrich-Schiller University of Jena, Lessing Strasse 8, D-07743 Jena, Germany. dionysios.douroumis@phoqus.com
Fahr
A
A
D002152:Calorimetry, Differential Scanning / Q000295:instrumentation / Q000379:methods; D002220:Carbamazepine / Q000031:analogs & derivatives* / Q000737:chemistry; D011232:Chemical Precipitation; D003460:Crystallization; D000078330:Oxcarbazepine; D010316:Particle Size; D011208:Powders; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
D011208:Powders; D002220:Carbamazepine; D000078330:Oxcarbazepine