Experimental design; Plackett-Burman; central composite design; supercritical carbon dioxide; solid dispersion; Particles from Gas Saturated Solutions
Abstract :
[en] The Particle from Gas Saturated Solutions process was successfully used to micronize solid
dispersions containing hydrophilic carriers and a new chemical entity, YNS3107. By means
of experimental design, the effects of several experimental parameters on micronization were
investigated. Within the chosen experimental conditions, the results showed that the autoclave
temperature, autoclave pressure, drug loading, flow rate of carbon dioxide and air pressure
were significant parameters. During the optimization step, the most relevant parameters of the
screening were optimized using a central composite design meanwhile other factors were kept
constant. Optimal conditions were used to produce microparticles with a volume weighted
mean diameter of 30.4 µm. The closeness between the measured and predicted response,
evaluated at 28.1 µm, demonstrated the validity of the statistical analyses. Finally, an
enhancement of the rate of dissolution of YNS3107 in the solid dispersion microparticles was
measured using USP II dissolution test apparatus.
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Brion, Michaël ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique et magistrale
Jaspart, Séverine ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Perrone, Leonardo
Piel, Géraldine ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique et magistrale
Evrard, Brigitte ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Language :
English
Title :
The supercritical micronization of solid dispersions by Particles from Gas Saturated Solutions using experimental design
Goddeeris C., Willems T., Houthoofd K., Martens J.A., and Van den Mooter G. Dissolution enhancement of the anti-HIV drug UC 781 by formulation in a ternary solid dispersion with TPGS 1000 and Eudragit E100. European Journal of Pharmaceutics and Biopharmaceutics 70 (2008) 861-868
Konno H., Handa T., Alonzo D.E., and Taylor L.S. Effect of polymer type on the dissolution profile of amorphous solid dispersions containing félodipine. European Journal of Pharmaceutics and Biopharmaceutics 70 (2008) 493-499
Xie Y., Xie P., Song X., Tang X., and Song H. Preparation of esomeprazole zinc solid dispersion and study on its pharmacokinetics. International Journal of Pharmaceutics 360 (2008) 53-57
Varshosaz J., Hassanzadeh F., Mahmoudzadeh M., and Sadeghi A. Preparation of cefuroxime axetil nanoparticles by rapid expansion of supercritical fluid technology. Powder Technology 189 (2009) 97-102
Vemavarapu C., Mollan M.J., and Needham T.E. Coprecipitation of pharmaceutical actives and their structurally related additives by the RESS process. Powder Technology 189 (2009) 444-453
Tenorio A., Gordillo M.D., Pereyra C.M., and de la Ossa E.J.M. Screening design of experiment applied to supercritical antisolvent precipitation of amoxicillin. Journal of Supercritical Fluids 44 (2008) 230-237
Cardoso M.A.T., Monteiro G.A., Cardoso J.P., Prazeres T.J.V., Figueiredo J.M.F., Martinho J.M.G., Cabral J.M.S., and Palavra A.M.F. Supercritical antisolvent micronization of minocycline hydrochloride. Journal of Supercritical Fluids 44 (2008) 238-244
de Sousa A.R.S., Silva R., Tay F.H., Simplício A.L., Kazarian S.G., and Duarte C.M.M. Solubility enhancement of trans-chalcone using lipid carriers and supercritical CO2 processing. Journal of Supercritical Fluids 48 (2009) 120-125
Mandzuka Z., and Knez Z. Influence of temperature and pressure during PGSS™ micronization and storage time on degree of crystallinity and crystal forms of monostearate and tristearate. Journal of Supercritical Fluids 45 (2008) 102-111
Fages J., Lochard H., Letourneau J.-J., Sauceau M., and Rodier E. Particle generation for pharmaceutical applications using supercritical fluid technology. Powder Technology 141 (2004) 219-226
Li J., Matos H.A., and de Azevedo E.G. Two-phase homogeneous model for particle formation from gas-saturated solution processes. Journal of Supercritical fluids 32 (2004) 275-286
A. Semenzato, S. Salmaso, N. Elvassore, A. Bertucco, P. Calicetti, Preparation and characterization of solid lipid nanoparticules using PGSS for cosmetic applications, in: 15th International Symposium on Microencapsulation, Parma, Italy, September 2005, pp. 18-21.
Yeo S.-D., and Kiran E. Formation of polymer particles with supercritical fluids: a review. Journal of Supercritical Fluids 34 (2005) 287-308
Nalawade S.P., Picchioni F., and Jnassen L.P.B.M. Batch production of micron size particles from poly(ethylene glycol) using supercritical CO2 as a processing solvent. Chemical Engineering Science 62 (2007) 1712-1720
Kikic I. Polymer-supercritical fluid interactions. Journal of Supercritical Fluids 47 (2009) 458-465
Lundstedt T., Seifert E., Abramo L., Thelin B., Nystrom A., Pettersen J., and Bergman R. Experimental design and optimization. Chemometrics and Intelligent Laboratory Systems 42 (1998) 3-40
Guillaume B., Boshini F., Garcia-Cano I., Rulmont A., Cloots R., and Ausloos M. BaZrO3 sintering process optimization with a precise control of the initial powder size distribution: a factorial design statistical analysis. Journal of the European Ceramic Society 25 (2005) 3593-3604
Vatanara A., Najafabadi A.R., Gilani K., Asgharian R., Darabi M., and Rafiee-Tehrani M. A Plackett-Burman design for screening of the operation variables in the formation of salbutamol sulphate particles by supercritical antisolvent. Journal of Supercritical Fluids 40 (2007) 111-116
Gelmeza N., Ki{dotless}ncala N.S., and Yenerb M.E. Optimization of supercritical carbon dioxide extraction of antioxidants from roasted wheat germ based on yield, total phenolic and tocopherol contents, and antioxidant activities of the extracts. Journal of Supercritical Fluids 48 (2009) 217-224
Nelder J.A., and Mead R. A simplex method for function minimization. Computer Journal 7 (1965) 308-313
US Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, Guidance for Industry: Dissolution Testing of Immediate Release Solid Oral Dosage Forms, August 1997.
Adams E., De Maesschalck R., De Spiegeleer B., Vader Heyden Y., Smeyers-Verbeke J., and Massart D.L. Evaluation of dissolution profiles using principal component analysis. International Journal of Pharmaceutics 212 (2001) 41-53
Arifin D.Y., Lee L.Y., and Wang C.-H. Mathematical modelling and simulation of drug release from microspheres: implications to drug delivery systems. Advanced Drug Delivery Reviews 58 (2006) 1274-1325
Hubert Ph., Nguyen-Huu J.-J., Boulanger B., Chapuzet E., Cohen N., Compagnon P.-A., Dew' W., Feinberg M., Laurentie M., Mercier N., Muzard G., Valat L., and Rozet E. Harmonization of strategies for the validation of quantitative analytical procedures: a SFSTP proposal. Part III. Journal of Pharmaceutical and Biomedical Analysis 45 (2007) 82-96
Hubert Ph., Nguyen-Huu J.-J., Boulanger B., Chapuzet E., Cohen N., Compagnon P.-A., Dew' W., Feinberg M., Laurentie M., Mercier N., Muzard G., Valat L., and Rozet E. Harmonization of strategies for the validation of quantitative analytical procedures: a SFSTP proposal. Part IV. Journal of Pharmaceutical and Biomedical Analysis 36 (2004) 579-586
Strumendo M., Bertucco A., and Elvassore N. Modeling of particle formation processes using gas saturated solution atomization. Journal of Supercritical Fluids 41 (2007) 115-125
