Solid dispersion of acetaminophen and poly(ethylene oxide) prepared by hot-melt mixing

International Journal of Pharmaceutics

Volumn 395, Issue 1-2, 2010, Pages 53-61

  Yang, Min ^a   Wang, Peng ^a   Huang, Chien Yueh ^c   Ku, M Sherry ^c   Liu, Huiju ^a   Gogos, Costas ^a,b  

^a NEW JERSEY INSTITUTE OF TECHNOLOGY   (United States)

^b Polymer Processing Institute   (United States)

^c WYETH RESEARCH   (United States)

Author keywords

Acetaminophen paracetamol; Clay; Hot melt Mixing; PEO; Recrystallization; Solid Dispersion

Indexed keywords

CLOISITE; MACROGOL; NANOCLAY; NANOPARTICLE; PARACETAMOL; UNCLASSIFIED DRUG; ALUMINUM SILICATE; ANALGESIC AGENT; CLAY; DELAYED RELEASE FORMULATION; EXCIPIENT; MACROGOL DERIVATIVE;

ARTICLE; CLAY; CONTACT ANGLE; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG STABILITY; HOT MELT EXTRUSION; PELLET EXTRUSION; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPY; THERMOGRAVIMETRY; WETTABILITY; X RAY DIFFRACTION; CHEMICAL MODEL; CHEMISTRY; DELAYED RELEASE FORMULATION; DIFFUSION; DRUG FORMULATION; HEAT; KINETICS; MEDICINAL CHEMISTRY; PHARMACEUTICS; POLARIZATION MICROSCOPY; POWDER DIFFRACTION; PROCEDURES; SOLUBILITY; SURFACE PROPERTY; X RAY CRYSTALLOGRAPHY;

ACETAMINOPHEN; ALUMINUM SILICATES; ANALGESICS, NON-NARCOTIC; CALORIMETRY, DIFFERENTIAL SCANNING; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; CRYSTALLOGRAPHY, X-RAY; DELAYED-ACTION PREPARATIONS; DIFFUSION; DRUG COMPOUNDING; EXCIPIENTS; HOT TEMPERATURE; KINETICS; MICROSCOPY, ELECTRON, SCANNING; MICROSCOPY, POLARIZATION; MODELS, CHEMICAL; POLYETHYLENE GLYCOLS; POWDER DIFFRACTION; SOLUBILITY; SURFACE PROPERTIES; TECHNOLOGY, PHARMACEUTICAL; THERMOGRAVIMETRY; WETTABILITY;

EID: 77954310058     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2010.04.033     Document Type: Article

References (35)

1. Andrews G.P., Jones D.S., Diak O.A., Mccoy C.P., Watts A.B., Mcginity J.W. The manufacture and characterisation of hot-melt extruded enteric tablets. Eur. J. Pharm. Biopharm. 2008, 69:264-273.
2. Breitkreutz J. Prediction of intestinal drug absorption properties by three-dimensional solubility parameters. Pharm. Res. 1998, 15:1370-1375.
3. Campbell K., Craig D.Q.M., Mcnally T. Poly(ethylene glycol) layered silicate nanocomposites for retarded drug release prepared by hot-melt extrusion. Int. J. Pharm. 2008, 363:126-131.
4. Coppens K.A., Hall M.J., Mitchell S.A., Read M.D. Hypromellose, ethylcellulose, and polyethylene oxide use in hot melt extrusion (cover story). Pharm. Technol. 2006, 30:62-70.
5. Crank J. The Mathematics of Diffusion 1975, Clarendon Press, Oxford. 2nd ed.
6. De Brabander C., Vervaet C., Remon J.P. Development and evaluation of sustained release mini-matrices prepared via hot melt extrusion. J. Control. Release 2003, 89:235-247.
7. De Wet F.N., Gerber J.J., Lotter A.P., Van Der Watt J.G., Dekker T.G. A study of the changes during heating of paracetamol. Drug Dev. Ind. Pharm. 1998, 24:447-453.
8. Fornes T.D., Paul D.R. Crystallization behavior of nylon 6 nanocomposites. Polymer 2003, 44:3945-3961.
9. Ghebremeskel A., Vemavarapu C., Lodaya M. Use of surfactants as plasticizers in preparing solid dispersions of poorly soluble API: stability testing of selected solid dispersions. Pharm. Res. 2006, 23:1928-1936.
10. Ghebremeskel A.N., Vemavarapu C., Lodaya M. Use of surfactants as plasticizers in preparing solid dispersions of poorly soluble API: selection of polymer-surfactant combinations using solubility parameters and testing the processability. Int. J. Pharm. 2007, 328:119-129.
11. Granberg R.A., Rasmuson A.C. Solubility of paracetamol in pure solvents. J. Chem. Eng. Data 1999, 44:1391-1395.
12. Greenhalgh D.J., Williams A.C., Timmins P., York P. Solubility parameters as predictors of miscibility in solid dispersions. J. Pharm. Sci. 1999, 88:1182-1190.
13. Homminga D., Goderis B., Dolbnya I., Reynaers H., Groeninckx G. Crystallization behavior of polymer/montmorillonite nanocomposites. Part I. Intercalated poly(ethylene oxide)/montmorillonite nanocomposites. Polymer 2005, 46:11359-11365.
14. Hopfenberg H.B., Hsu K.C. Swelling-controlled, constant rate delivery systems. Polym. Eng. Sci. 1978, 18:1186-1191.
15. Hülsmann S., Backensfeld T., Keitel S., Bodmeier R. Melt extrusion-an alternative method for enhancing the dissolution rate of 17β-estradiol hemihydrate. Eur. J. Pharm. Biopharm. 2000, 49:237-242.
16. Lang M., Grzesiak A.L., Matzger A.J. The use of polymer heteronuclei for crystalline polymorph selection. J. Am. Chem. Soc. 2002, 124:14834-14835.
17. Langer R., Peppas N.A. Chemical and physical structure of polymers as carriers for controlled release of bioactive agents: a review. Rev. Macromol. Chem. Phys. 1983, 23:61-126.
18. Li L., Abubaker O., Shao Z. Characterization of poly(ethylene oxide) as a drug carrier in hot-melt extrusion. Drug Dev. Ind. Pharm. 2006, 32:991-1002.
19. ® E PO solid dispersions. Int. J. Pharm. 2010, 383:161-169.
20. Liu X., Wu Q. Non-isothermal crystallization behaviors of polyamide 6/clay nanocomposites. Eur. Polym. J. 2002, 38:1383-1389.
21. Lloyd G.R., Craig D.Q.M., Smith A. An investigation into the production of paracetamol solid dispersions in PEG 4000 using hot stage differential interference contrast microscopy. Int. J. Pharm. 1997, 158:39-46.
22. Loyens W., Jannasch P., Maurer F.H.J. Effect of clay modifier and matrix molar mass on the structure and properties of poly(ethylene oxide)/cloisite nanocomposites via melt-compounding. Polymer 2005, 46:903-914.
23. Maiti P., Nam P.H., Okamoto M., Hasegawa N., Usuki A. Influence of crystallization on intercalation, morphology, and mechanical properties of polypropylene/clay nanocomposites. Macromolecules 2002, 35:2042-2049.
24. Mididoddi P.K., Repka M.A. Characterization of hot-melt extruded drug delivery systems for onychomycosis. Eur. J. Pharm. Biopharm. 2007, 66:95-105.
25. ® SR mini-matrices prepared by hot-melt extrusion. Eur. J. Pharm. Biopharm. 2009, 73:140-145.
26. Peppas N.A., Korsmeyer R.W. Dynamically swelling hydrogels in controlled release applications. Hydrogels Med. Pharm. 1986, vol. 3:109-136. CRC Press, Boca Raton.
27. Peppas N.A., Sahlin J.J. A simple equation for the description of solute release. III. Coupling of diffusion and relaxation. Int. J. Pharm. 1989, 57:169-172.
28. Prodduturi S., Manek R.V., Kolling W.M., Stodghill S.P., Repka M.A. Solid-state stability and characterization of hot-melt extruded poly(ethylene oxide) films. J. Pharm. Sci. 2005, 94:2232-2245.
29. Repka M.A., Prodduturi S., Stodghill S.P. Production and characterization of hot-melt extruded films containing clotrimazole. Drug Dev. Ind. Pharm. 2003, 29:757-765.
30. Ritger P., Peppas N. A simple equation for description of solute release II. Fickian and anomalous release from swellable devices. J. Control. Release 1987, 5:37-42.
31. Schilling S.U., Shah N.H., Waseem Malick A., Mcginity J.W. Properties of melt extruded enteric matrix pellets. Eur. J. Pharm. Biopharm. 2010, 74:352-361.
32. Siepmann J., Peppas N.A. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv. Drug Deliv. Rev. 2001, 48:139-157.
33. Verhoeven E., De Beer T.R.M., Schacht E., Van Den Mooter G., Remon J.P., Vervaet C. Influence of polyethylene glycol/polyethylene oxide on the release characteristics of sustained-release ethylcellulose mini-matrices produced by hot-melt extrusion: in vitro and in vivo evaluations. Eur. J. Pharm. Biopharm. 2009, 72:463-470.
34. Yang R., Wang Y., Zheng X., Meng J., Tang X., Zhang X. Preparation and evaluation of ketoprofen hot-melt extruded enteric and sustained-release tablets. Drug Dev. Ind. Pharm. 2008, 34:83-89.
35. Zhang F., Mcginity J. Properties of sustained-release tablets prepared by hot-melt extrusion. Pharm. Dev. Tech. 1999, 4:241-250.