Abstract
A supercritical particle formation equipment, designed and constructed by our research group, was validated in this study using supercritical CO2 as an antisolvent. Ibuprofen sodium salt was successfully micronized by supercritical antisolvent (SAS) precipitation. Ethanol and CO2 was used as solvent and antisolvent, respectively, and the effect of the operating conditions on the precipitation yield, residual organic solvent content and particle morphology were evaluated using a split-plot experimental design and the analysis of variance (ANOVA) method. This study showed that when selecting appropriate process conditions, it is possible to produce a sheet-like morphology, which is the best for tableting purposes, with high precipitation yield (70%) and low residual solvent content (4.7 mg kg−1).
This is a preview of subscription content, log in via an institution.
Buying options
Tax calculation will be finalised at checkout
Purchases are for personal use only
Learn about institutional subscriptionsReferences
Z. Knez, E. Weidner, Particles formation and particle design using supercritical fluids. Curr. Opin. Solid State Mater. Sci. 7, 353–361 (2003)
S. Dalziel, G. Foggin, W. Ford, H. Gommeren, High pressure media milling system and process of forming particles, Patent US 20050258288 A1, Google Patents (2004)
P.J. Linstrom, W. Mallard, NIST Chemistry, National Institute of Standards and Technology. Gaithersburg (2003)
P. Gruber, M. Reher, Dosage form of sodium ibuprofen, Patent US 20040102522 A1, Google Patents (2004)
T.L. Rogers, K.P. Johnston, R.O. Williams 3rd, Solution-based particle formation of pharmaceutical powders by supercritical or compressed fluid CO2 and cryogenic spray-freezing technologies. Drug Dev. Ind. Pharm. 27, 1003–1015 (2001)
K.M. Sharif, M.M. Rahman, J. Azmir, A. Mohamed, M.H.A. Jahurul, F. Sahena, I.S.M. Zaidul, Experimental design of supercritical fluid extraction—A review. J. Food Eng. 124, 105–116 (2014)
G.E. Box, J.S. Hunter, W.G. Hunter, Statistics for experimenters: design, innovation, and discovery, 2nd edn. (Wiley, New York, 2005)
Á. Martín, K. Scholle, F. Mattea, D. Meterc, M.J. Cocero, Production of Polymorphs of Ibuprofen Sodium by Supercritical Antisolvent (SAS) Precipitation. Cryst. Growth Des. 9, 2504–2511 (2009)
C.J. Chang, K.-L. Chiu, C.-Y. Day, A new apparatus for the determination of P–x–y diagrams and Henry’s constants in high pressure alcohols with critical carbon dioxide. J. Supercrit. Fluids 12, 223–237 (1998)
C.S. Su, W.S. Lo, L.H. Lien, Micronization of fluticasone propionate using supercritical antisolvent (SAS) process. Chem. Eng. Technol. 34, 535–541 (2011)
A. Visentin, S. Rodríguez-Rojo, A. Navarrete, D. Maestri, M.J. Cocero, Precipitation and encapsulation of rosemary antioxidants by supercritical antisolvent process. J. Food Eng. 109, 9–15 (2012)
V. Majerik, G. Charbit, E. Badens, G. Horváth, L. Szokonya, N. Bosc, E. Teillaud, Bioavailability enhancement of an active substance by supercritical antisolvent precipitation. J. Supercrit. Fluids 40, 101–110 (2007)
X. Sui, W. Wei, L. Yang, Y. Zu, C. Zhao, L. Zhang, F. Yang, Z. Zhang, Preparation, characterization and in vivo assessment of the bioavailability of glycyrrhizic acid microparticles by supercritical anti-solvent process. Int. J. Pharm. 423, 471–479 (2012)
P. Imsanguan, S. Pongamphai, S. Douglas, W. Teppaitoon, P.L. Douglas, Supercritical antisolvent precipitation of andrographolide from Andrographis paniculata extracts: Effect of pressure, temperature and CO2 flow rate. Powder Technol. 200, 246–253 (2010)
ICH, International Conference on Harmonization (ICH) of Technical Requirements for the Registration of Pharmaceuticals for Human Use. Guideline for Residual Solvents Step 4 (1997)
R. Adami, E. Reverchon, E. Järvenpää, R. Huopalahti, Supercritical AntiSolvent micronization of nalmefene HCl on laboratory and pilot scale. Powder Technol. 182, 105–112 (2008)
M.-S. Kim, S. Lee, J.-S. Park, J.-S. Woo, S.-J. Hwang, Micronization of cilostazol using supercritical antisolvent (SAS) process: effect of process parameters. Powder Technol. 177, 64–70 (2007)
E. Reverchon, G. Caputo, I. De Marco, Role of phase behavior and atomization in the supercritical antisolvent precipitation. Ind. Eng. Chem. Res. 42, 6406–6414 (2003)
Y. Bakhbakhi, S. Alfadul, A. Ajbar, Precipitation of Ibuprofen Sodium using compressed carbon dioxide as antisolvent, European journal of pharmaceutical sciences: official journal of the European Federation for. Pharm. Sci. 48, 30–39 (2013)
E. Reverchon, Supercritical antisolvent precipitation of micro- and nano-particles. J. Supercrit. Fluids 15, 1–21 (1999)
P.J. Linstrom, W. Mallard, NIST chemistry webbook (National Institute of Standards and Technology Gaithersburg, MD, 2001)
P. Pathak, M.J. Meziani, T. Desai, Y.-P. Sun, Formation and stabilization of ibuprofen nanoparticles in supercritical fluid processing. J. Supercrit. Fluids 37, 279–286 (2006)
Y. Li, D.J. Yang, S.L. Chen, S.B. Chen, A.S.C. Chan, Comparative physicochemical characterization of phospholipids complex of puerarin formulated by conventional and supercritical methods. Pharm. Res. 25, 563–577 (2008)
D.H. Won, M.S. Kim, S. Lee, J.S. Park, S.J. Hwang, Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process. Int. J. Pharm. 301, 199–208 (2005)
R.E. Gordon, S.I. Amin, Crystallization of ibuprofen, Patent US 4476248 A, Google Patents (1984)
Acknowledgements
The authors are grateful to CNPq (470916/2012-5) and FAPESP (2012/10685-8) for their financial support. M. Thereza M. G. Rosa and Eric Keven Silva thanks CNPq (140641/2011-4 and 140275/2014-2) for the Ph.D. assistantship. Diego T. Santos thanks the FAPESP (10/16485-5; 12/19304-7) and CAPES for the postdoctoral fellowships. M. Angela A. Meireles thanks CNPq for a productivity grant (301301/2010-7). The authors also thank Moyses N. Moraes for his assistance with the statistical analyses.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
Copyright information
© 2019 The Author(s), under exclusive license to Springer Nature Switzerland AG
About this chapter
Cite this chapter
Santos, D.T. et al. (2019). Effect of Process Conditions on the Morphological Characteristics of Particles Obtained by Supercritical Antisolvent Precipitation. In: Supercritical Antisolvent Precipitation Process. SpringerBriefs in Applied Sciences and Technology. Springer, Cham. https://doi.org/10.1007/978-3-030-26998-2_2
Download citation
DOI: https://doi.org/10.1007/978-3-030-26998-2_2
Published:
Publisher Name: Springer, Cham
Print ISBN: 978-3-030-26997-5
Online ISBN: 978-3-030-26998-2
eBook Packages: Chemistry and Materials ScienceChemistry and Material Science (R0)