Physicochemical characterization of solid dispersions of three antiepileptic drugs prepared by solvent evaporation method

Journal of Pharmacy and Pharmacology

Volumn 59, Issue 5, 2007, Pages 645-653

  Douroumis, Dionysios ^a   Bouropoulos, Nikolaos ^b   Fahr, Alfred ^c  

^a Phoqus Pharmaceutical Ltd   (United Kingdom)

^b Department of Material Science ^*  (Greece)

^c FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

AMIDE; CARBAMAZEPINE; HYDROXYL GROUP; HYDROXYPROPYLMETHYLCELLULOSE; OXCARBAZEPINE; POLYMER; RUFINAMIDE;

AQUEOUS SOLUTION; ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DISSOLUTION; DRUG STRUCTURE; INFRARED SPECTROSCOPY; PHYSICAL CHEMISTRY; SCANNING ELECTRON MICROSCOPE; X RAY DIFFRACTION;

ANTICONVULSANTS; CALORIMETRY, DIFFERENTIAL SCANNING; CARBAMAZEPINE; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; DRUG CARRIERS; HYDROGEN BONDING; METHYLCELLULOSE; MICROSCOPY, ELECTRON, SCANNING; SOLUBILITY; SOLVENTS; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; TRIAZOLES; WETTABILITY; X-RAY DIFFRACTION;

EID: 34447334239     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/jpp.59.5.0004     Document Type: Article

References (48)

1. Amidon, G. L., Lunnernas, H., Shah, V. P., Crison, J. R. (1995) A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 12: 413-420
2. Behme, R. J., Brooke, D. (1991) Heat of fusion measurement of a low melting polymorph of carbamazepine that undergoes multiple-phase changes during differential scanning calorimetry analysis. J. Pharm. Sci. 80: 986-990
3. Breitenbach, J., Schrof, W., Neumann, J. (1999) Confocal Raman-spectroscopy: analytical approach to solid dispersions and mapping of drugs. Pharm. Res. 16: 1109-1113
4. Chang, S. A., Gray, D. G. (1978) The surface tension of aqueous hydroxypropyl cellulose solutions. J. Colloid Interface Sci. 67: 255-265
5. Chiou, W. L., Riegelman, S. (1971) Pharmaceutical applications of solid dispersion systems. J. Pharm. Sci. 60: 1281-1301
6. Corrigan, O. I. (1985) Mechanisms of dissolution of fast release solid dispersions. Drug Dev. Ind. Pharm. 11: 697-724
7. Craig, D. Q. M. (1990) Polyethylene glycols and drug release. Drug Dev. Ind. Pharm. 16: 2501-2526
8. Doherty, C., York, P. (1987) Mechanisms of dissolution of frusemide-PVP solid dispersions. Int. J. Pharm. 34: 197-205
9. El-Bana, H. M., El-Gholmy, A. Z., Hammuda, Y. (1980) Phase diagram and dissolution rate studies on hydrochlorothiazide-urea solid dispersions. Pharm. Acta Helv. 55: 244-248
10. Ford, J. L. (1986) The current status of solid dispersions. Pharm. Acta Helv. 61: 69-88
11. Higuchi, T. (1961) Rate of release of medicaments from ointment bases containing drugs in suspensions. J. Pharm. Sci. 50: 874-875
12. Higuchi, T. (1963) Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J. Pharm. Sci. 52: 1145-1149
13. Hixson, A. W., Crowell, J. H. (1931) Dependence of reaction velocity upon surface and agitation. I. Theoretical consideration. Ind. Eng. Chem. 23: 923-931
14. Hoag, S. W., Nair, R., Gonen, S. (2002) Influence of polyethylene glycol and povidone on the polymorphic transformation and solubility of carbamazepine. Int. J. Pharm. 240: 11-22
15. Hrachovy, R. A., Frost, Jr J. D. (1989) Infantile spasms. Pediatr. Clin. North Am. 36: 311-330
16. Jun, S. W., Kim, M. S., Jo, G. H., Lee, S., Woo, J. S., Park, J. S, Hwang, S. J. (2005) Cefuroxime axetil solid dispersions prepared using solution enhanced dispersion by supercritical fluids. J. Pharm. Pharmacol. 57: 1529-1537
17. Karavas, E., Ktistis, G., Xenakis, A., Georgarakis, E. (2005) Miscibility behavior and formation mechanism of stabilized felodipine-polyvinylpyrrolidone amorphous solid dispersions. Drug Dev Ind Pharm 31: 473-489
18. Krahn, F. U., Mielck, J. B. (1987) Relations between several polymorphic forms and the dihydrate of carbamazepine. Pharm. Acta Helv. 62: 247
19. Leuner, G., Dressman, J. (2000) Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm. 50: 47-60
20. Liang, C. Y., Marchessault, R. H. (1959). Infrared spectra of crystalline polysaccharides. J Polymer Sci. 39: 269-278
21. Löbenberg, R., Amidon, G. L. (2000) Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur. J. Pharm. Biopharm. 50: 3-12
22. Lowes, M. M. J., Caira, M. R., Lotter, A. P., Van Der Watt, J. G. (1987) Physicochemical properties and X-ray structural studies of the trigonal polymorph of carbamazepine. J. Pharm. Sci. 76: 744-752
23. Martinez, M., Augsburger, L., Johnston, T., Jones, W. W. (2002) Applying the biopharmaceutics classification system to veterinary pharmaceutical products. Part I. Biopharmaceutics and formulation considerations. Adv. Drug Deliv. Rev. 54: 805-824
24. Meshali, M. M., Gabr, K. E. (1992) Physical properties of fast-release nonreverting hydrochlorothiazide solid dispersions. Pharm. Res. 9: 960-962
25. Moneghini, M., Kikic, I., Voinovich, D., Perissutti, B., Filipovic-Grcic, J. (2001) Processing of carbamazepine-PEG 4000 solid dispersions with supercritical carbon dioxide: preparation, characterization, and in vitro dissolution. Int. J. Pharm. 222: 129-138
26. Nakamichi, K., Nakano, T., Yasuura, H., Izumi, S., Kawashima, Y. (2002) The role of the kneading paddle and the effects of screw revolution speed and water content on the preparation of solid dispersions using a twin-screw extruder. Int. J. Pharm. 241: 203-211
27. Niebergall, P. J., Milosovich, G., Goyan, J. E., (1963) Dissolution rate studies. II. Dissolution of particles under conditions of rapid agitation. J. Pharm. Sci. 52: 236-241
28. Ohara, T., Kitamura, S., Kitagawa, T., Terada, K. (2005) Dissolution mechanism of poorly water-soluble drug from extended release solid dispersion system with ethylcellulose and hydroxypropyl-methylcellulose. Int. J. Pharm. 302: 95-102
29. Ohtahara, S. (1988) Lennox-Gastaut syndrome: considerations in its concept and categorization. Jpn J. Psychiatry Neurol. 42: 535-542
30. Rasenack, N., Müller, B. W., Hartenhauer, H. (2003) Microcrystals for dissolution rate enhancement of poorly water-soluble drugs, Int. J. Pharm. 254: 137-145
31. Remon, J. P., De Brabander, C., Van Den Mooter, G., Vervaet, C. (2002) Characterization of ibuprofen as a nontraditional plasticizer of ethyl cellulose. J. Pharm. Sci. 911: 678-685
32. Rustichelli, C., Gamberini, G., Ferioli, V., Gamberini, M. C., Ficarra, R., Tommasini S. (2000) Solid-state study of polymorphic drugs: carbamazepine. J. Pharm. Biomed. Anal. 23: 41-54
33. Sekikawa, H., Nakano, M., Arita, T. (1979) Dissolution mechanisms of drug-polyvinylpyrrolidone coprecipitates in aqueous solution. Chem. Pharm. Bull. 27: 1223-1230
34. Serajuddin, A. T. M. (1999) Solid dispersion of poorly water soluble drugs: early promises, subsequent problems, and recent breakthroughs. J. Pharm. Sci. 88: 1058-1066
35. Sethia, S., Squillante, E. (2002) Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method. J. Pharm. Sci. 91: 1948-1957
36. Sethia, S., Squillante, E. (2004a) In vitro-in vivo evaluation of supercritical processed solid dispersions: permeability and viability assessment in Caco-2 cells. J. Pharm. Sci. 93: 2985-2993
37. Sethia, S., Squillante, E. (2004b) Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods. Int. J. Pharm. 272: 1-10
38. Siepmann, J., Peppas, N. A. (2001) Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv. Drug Deliv. Rev. 48: 139-157
39. Simonelli, A. P., Mehta, S. C., Higuchi, W. I. (1976) Dissolution rates of high energy sulfathiazole-povidone coprecipitates. II: characterization of form of drug controlling its dissolution rate via solubility studies. J. Pharm. Sci. 65: 355-361
40. Stahl, P. H. (1972) Novartis -Pharmaceutische Entwicklung.
41. Van den Mooter, G., Verheyen, S., Blaton, N., Kinget, R. (2002) Mechanism of increased dissolution of diazepam and temazepam from polyethylene glycol 6000 solid dispersions. Int. J. Pharm. 249: 45-58
42. Van den Mooter, G., Six, K., Berghmans, H., Leuner, C., Dressman, J., Van Werde, K., Mullens, J., Benoist, L., Meublat, M. L., Verreck, G., Peeters, J., Brewster, M. (2003) Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion, Part II. Pharm. Res. 20: 1047-1054
43. Varelas, C. G., Dixon, D. G, Steiner, C. (1995) Zero-order release from biphasic polymer hydrogels. J. Control. Release 34: 185-192
44. Verreck, G., Decorte, A., Heymans, K, Adriaensen, J, Cleeren, D., Jacobs, A., Liu, D., Tomasko, D, Arien, A., Peeters, J., Rombaut, P., Van den Mooter, G., Brewster, M. E. (2005) The effect of pressurized carbon dioxide as a temporary plasticizer and foaming agent on the hot stage extrusion process and extrudate properties of solid dispersions of itraconazole with PVP-VA 64. Eur. J. Pharm. Sci. 26: 349-358
45. Wagner, J. G., (1969) Interpretation of percent dissolved-time plots derived form in vitro testing of conventional tablets and capsules. J. Pharm. Sci. 58: 1253-1257
46. Wagner, J. G., (1971) Biopharmaceutics and relevant pharmacokinetics. Drug Intelligence Publications, Hamilton, IL USA, pp 120
47. Won, D. H., Kim, M. S., Lee, S., Park, J. S., Hwang, S. J. (2005) Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process. Int. J. Pharm. 301: 199-208
48. Yuskel, N., Kanik, A. E., Baykara, T. (2000) Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and -independent methods. Int. J. Pharm. 209: 56-67