Solubility Parameters for Prediction of Drug/Polymer Miscibility in Hot-Melt Extruded Formulations

Hot-Melt Extrusion: Pharmaceutical Applications

Volumn , Issue , 2012, Pages 71-92

  Gryczke, Andreas ^a  

^a NONE   (Germany)

Author keywords

Drug dispersion in polymer, and appropriate polymers; Drug, monomer miscibility estimation; Flory Huggins and solubility parameter models; Models, estimating drug monomer, drug polymer miscibility; Particle size reduction of drugs, and milling; Solid dispersions and melt extrusion process; Solubility parameter, miscibility of a drug with excipients; System integrated software, for drug polymer systems

Indexed keywords

DISPERSIONS; MELT SPINNING; MONOMERS; PARTICLE SIZE; POLYMERS; SOLUBILITY;

DRUG-POLYMER MISCIBILITY; MELT EXTRUSION PROCESS; PARTICLE SIZE REDUCTION; POLYMER SYSTEMS; SOLUBILITY PARAMETERS;

DRUG DELIVERY;

EID: 84886136919     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1002/9780470711415.ch4     Document Type: Chapter

References (36)

1. Hansen, C.M. (2007) Hansen Solubility Parameters: A User's Handbook. CRC Press.
2. Atkins, P.W. (1996). Physikalische Chemie: Auflage v. 2 (p. 226). Wiley-VCH Verlag GmbH.
3. Lin, S.L., Menig, J. and Lachman, L. (1968) Interdependence of physiological surfactant and drug particle size on the dissolution behavior of water insoluble drugs. Journal of Pharmaceutical Sciences, 57, 2143-2146.
4. Chiou,W.L. and Riegelman, S. (1970) Pharmaceutical applications of solid dispersion systems. Journal of Pharmaceutical Sciences, 59, 937-942.
5. Chiou,W.L., and Riegelman, S. (1971) Pharmaceutical applications of solid dispersion systems. Journal of Pharmaceutical Sciences, 60(9), 1281-1302.
6. Qi, S., Gryczke, A., Belton, P. and Craig, D.Q.M. (2008) Characterisation of solid dispersions of paracetamol and EUDRAGIT E prepared by hot-melt extrusion using thermal, microthermal and spectroscopic analysis. International Journal of Pharmaceutics, 354(1-2), 158-167.
7. Van Krevelen, D.W. and Hoftyzer, P. (1976) Properties of Polymers. Their Estimation and Correlation with Chemical Structure, 2nd ed. Elsevier, Amsterdam.
8. Van Krevelen D.W. (1997) Properties of Polymers: Their Correlation with Chemical Structure, Third Edition. Elsevier, Amsterdam.
9. Hancock, B.C., York, P. and Rowe, R.C. (1997) The use of solubility parameters in pharmaceutical dosage form design. International Journal of Pharmaceutics, 148, 1-21.
10. Leuner, C. and Dressman, J. (2000) Improving drug solubility for oral delivery using solid dispersions. European Journal of Pharmaceutics & Biopharmaceutics, 50(1), 47-60.
11. Qi, S., Belton, P., Nollenberger, K., Clayden, N., Reading, M. and Craig, D.Q.M. (2010) Characterisation and prediction of phase separation in hot-melt extruded solid dispersions: a thermal, microscopic and NMR relaxometry study. Pharmaceutical Research, 27(9), 1869-1883.
12. Radebaugh, G.W. (1992) Film coatings and film forming materials: Evaluation. In Swarbrick, J. and Boylan, J.C. (eds) Encyclopedia of Pharmaceutical Technology, Vol. 6. Marcel Dekker, New York and Basel, pp 1-28.
13. Brabander, C.D., Mooter, G.V.D.,Vervaet, C. and Remon, J.P. (2002) Characterization of ibuprofen as a nontraditional plasticizer of ethyl cellulose. Journal of Pharmaceutical Sciences, 91, 1678-1685.
14. Vollmert, B. (1988) Grundriss der Makromolekularen Chemie Band IV Makromolekulare Aggregatzustaende. E. Vollmert-Verlag, Karlsruhe.
15. Marsac, P.J., Li, T. and Taylor, L.S. (2009) Estimation of drug-polymer miscibility and solubility in amorphous solid dispersions using experimentally determined interaction parameters. Pharmaceutical Research, 26(1), 139-151.
16. David, D., Rotstein, N. and Sincock, T. (1994) The application of miscibility parameter to the measurement of polymer-plasticizer compatibility. Polymer Bulletin, 33(6), 725-732.
17. Patterson, D. (1982) Polymer compatibility with and without a solvent. Polymer Engineering & Science, 22, 64-72.
18. Patterson, D. and Robard, A. (1978) Thermodynamics of polymer compatibility. Macromolecules, 11, 690-695.
19. Flory, P.J. (1941) Thermodynamic of high polymer solution. Journal of Chemical Physics, 9, 660-661.
20. Huggins, M.L. (1941) Solution of long chain compound. Journal of Chemical Physics, 9, 440.
21. Flory, P.J. (1953) Principles of Polymer Chemistry. Cornell University Press.
22. Hildebrand, J.H. and Scott, R.L. (1950) The Solubility of Nonelectrolytes. Reinhold.
23. Fedors, R. (1974) A method for estimating both the solubility parameters and molar volumes of liquids. Polymer Engineering & Science, 14, 147-154.
24. Stefanis, E. and Panayiotou, C. (2008) Prediction of Hansen solubility parameters with a new group-contribution method. International Journal of Thermophysics, 29(2), 568-585.
25. Bagley, E.B., Nelson, T.P. and Scigliano, J.M. (1971) Three-dimensional solubility parameters and their relationship to internal pressure measurements in polar and hydrogen bonding solvents. Journal of Paint Technology, 43, 35-42.
26. Greenhalgh, D.J., Williams, A.C., Timmins, P. and York, P. (1999) Solubility parameters as predictors of miscibility in solid dispersions. Journal of Pharmaceutical Sciences, 88, 1182-1190.
27. Forster, A., Hempenstall, J., Tucker, I. and Rades, T. (2001) Selection of excipients for melt extrusion with two poorlywater-soluble drugs by solubility parameter calculation and thermal analysis. International Journal of Pharmaceutics, 226(1-2), 147-161.
28. Schroeder, L.W. (1993-1995) SOLPE: A program designed to predict Hansen Solubility Parameters and Flory's Chi Parameter From Molecular Composition. DYNACOMP, Inc.
29. Gancia, E., Montana, J.G. and Manallack, D.T. (2001) Theoretical hydrogen bonding parameters for drug design. Journal of Molecular Graphics Modeling, 19(3-4), 349-362.
30. Gardon, J.L. (1966) The influence of polarity upon the solubility parameter concept. Journal of Paint Technology, 38, 43-55.
31. Hildebrand, J.H. and Scott, R. L. (1962) Regular Solutions (Prentice Hall International Series in Chemistry). Prentice Hall.
32. Hildebrand, J.H. and Scott, R.L. (1964) The Solubility of Nonelectrolytes. Dover Publications.
33. Scatchard, G. (1931) Equilibria in non-electrolyte solutions in relation to the vapor pressures and densities of the components. Chemical Reviews, 8, 321-333.
34. Six, K., Daems, T., Hoon, J. de, Hecken, A.V., Depre, M., Bouche, M.-P., Prinsen, P., Verreck, G., Peeters, J., Brewster, M.E. and Mooter, G.V.d. (2005) Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion. European Journal of Pharmaceutical Sciences, 24(2-3), 179-186.
35. Janssens, S.,De Zeure, A., Paudel, A., Humbeek, J.V., Rombaut, P. and Mooter, G.V.d. (2010) Influence of preparation methods on solid state supersaturation of amorphous solid dispersions: a case study with itraconazole and Eudragit E100. Pharmaceutical Research, 27(5), 775-785.
36. Kolter, K., Karl, M., Nalawade, S. and Rottmann, N. (2010) Hot-melt Extrusion with BASF Pharma Polymers Extrusion Compendium. Book brochure by BASF SE.