Prediction of drug-polymer miscibility through the use of solubility parameter based flory-huggins interaction parameter and the experimental validation: PEG as model polymer

Journal of Pharmaceutical Sciences

Volumn 102, Issue 7, 2013, Pages 2254-2263

  Thakral, Seema ^a,b   Thakral, Naveen K ^a  

^a UNIVERSITY OF MINNESOTA   (United States)

^b GVM College of Pharmacy   (India)

Author keywords

Formulation; Physical stability; Solid dispersion; Thermal analysis; Thermodynamics

Indexed keywords

ACETOPHENONE; ACETYLSALICYLIC ACID; CARBAMAZEPINE; CHLORAMPHENICOL; DIAZEPAM; ETODOLAC; FENOFIBRATE; GRISEOFULVIN; IBUPROFEN; INDOMETACIN; ITRACONAZOLE; KETOCONAZOLE; KETOPROFEN; MACROGOL 6000; MEBENDAZOLE; MEFENAMIC ACID; NAPROXEN; NIFEDIPINE; NITROFURANTOIN; OFLOXACIN; PARACETAMOL; PHENACETIN; PHENOBARBITAL; PHENYLBUTAZONE; PHENYTOIN; PIROXICAM; PREDNISONE; SULFATHIAZOLE; TOLBUTAMIDE; UNINDEXED DRUG;

ARTICLE; DRUG SOLUBILITY; ENTHALPY; ENTROPY; FLORY HUGGINS INTERACTION PARAMETER; MISCIBILITY; PRODUCT PARAMETERS; VALIDATION PROCESS;

EID: 84879009609     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23583     Document Type: Article

References (26)

1. Qian F, Huang J, Hussain MA. 2010. Drug-polymer solubility and miscibility: Stability consideration and practical challenges in amorphous solid dispersion development. J Pharm Sci 99:2941-2947.
2. Olabisi O, Robeson LM, Shaw MT. 1979. Polymer-polymer miscibility. New York: Academic Press.
3. Freed K, Clarke N. 2005. Phase behaviour of polymer blends. Berlin: Springer.
4. Hiemenz PC, Lodge TP. 2007. Polymer chemistry. Boca Raton: CRC Press.
5. Flory PJ. 1941. Thermodynamics of polymer solutions. J Chem Phys 9:660-661.
6. Huggins ML. 1942. Thermodynamic properties of solutions of long chain compounds. Ann N Y Acad Sci 43:1-32.
7. Arrighi V, Cabral J, Cowie JMG. 2010. Encyclopaedia of polymer science and technology. Miscibilty. New York: John Wiley and Sons.
8. Paudel A, Humbeeck JV, Van den Mooter G. 2010. Theoretical and experimental investigation on the solid solubility and miscibility of naproxen in poly(vinylpyrrolidine). Mol Pharm 7:1133-48.
9. Qian F, Wang J, Hartley R, Tao J, Haddadin Mathias N, Hussain MA. 2012. Solution behaviour of PVP-VA and HPMC-AS-based amorphous solid dispersions and their bioavailability implications. Pharm Res 2012:2766-2776.
10. Tian Y, Jones DS, Li S, Andrews GP. 2013. Construction of drug-polymer thermodynamic phase diagrams using Flory-Huggins Interaction theory: Identifying the relevance of temperature and drug weight fraction to phase separation within solid dispersion. Mol Pharm 10:236-248.
11. Zhao Y, Inbar P, Chokshi HP, Malick AW, Chio DS. 2011. Prediction of the thermal phase diagram of amorphous dispersions by Flory-Huggins theory. J Pharm Sci 100:3196-3207.
12. Paluja K, Taskinen M, Lehto V-P, Ketolainen J, Korhonen O. 2010. Predicting the formation and stability of amorphous small molecules binary mixtures from computationally determined Flory-Huggins interaction parameter and phase diagram. Mol Pharm 7:795-804.
13. Lin D, Huang Y. 2010. A thermal analysis method to predict the complete phase diagram of drug-polymer solid dispersion. Int J Pharm 399:109-115.
14. Ruinstein M, Colby RH. 2003. Polymer physics. New York: Oxford University.
15. Sinko PJ. 2011. Martin's physical pharmacy and pharmaceutical sciences. Philedelphia: Lippincot William and Willkins.
16. Van Krevelen DW, te Nijenhuis K. 2009. Properties of polymers: 4th ed. Their correlation with chemical structure: Their numerical estimation and prediction from additive group contributions. Chapter 7, Cohesive properties and solubility. Amsterdam, Boston: Elsevier.
17. Hansen CM. 2000. Hansen solubility parameters: A user's handbook. Boca Raton, Florida: CRC Press.
18. Barton ATM. 1991. Handbook of solubility parameters and other cohesion parameters. 2nd ed. Boca Raton, Florida: CRC Press.
19. Martin SC. 2000. Phase transitions. Chem Rev 100:3403-3453.
20. Gupta J, Nunes C, Vyas S, Jonnalagadda 2011. Prediction of solubility parameters and miscibility of pharmaceutical compounds by molecular simulations. J Phys Chem B 115:2014-2023.
21. Bruno J, Cole JC, Edgington PR, Kessler M, Macrae CF, McCabe P, Pearson J, Taylor R. 2002. New software for searching the Cambridge Structural Database and visualizing crystal structures. Acta Crystallogr Sect B Struct Sci 58:389-397.
22. Coleman MM, Serman CJ, Bhagwager DE, Painter PC. 1990. Polymer reviews: A practical guide to polymer miscibility. Polymer 31:1187-1203.
23. Bagley EB, Nelson TP, Scigliano JM. 1971. Three-dimensional solubility parameters and their relationship to internal pressure measurements in polar and hydrogen bonding solvents. J Paint Technol 43:35.
24. Marsac PJ, Shamblin SL, Taylor LS. 2006. Theoretical and practical approaches for the prediction of drug-polymer miscibility and solubility. Pharm Res 23:2417-2426.
25. Nishi T, Wang TT. 1975. Melting point depression and kinetic effect of cooling on crystallization in poly (vinylidene fluoride)-poly (methyl methacrylate) mixtures. Macromolecules 8:909-915.
26. Khan S, Batchelor H, Hanson P, Perrie Y, Mohammed AR. 2011. Physicochemical characterization, drug-polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000. J Pharm Sci 100:4281-4294.