Intraorally fast-dissolving particles of a poorly soluble drug: Preparation and in vitro characterization

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 71, Issue 2, 2009, Pages 271-281

  Laitinen, Riikka ^a   Suihko, Eero ^a   Toukola, Kaisa ^a   Björkqvist, Mikko ^b   Riikonen, Joakim ^b   Lehto, Vesa Pekka ^b   Järvinen, Kristiina ^a   Ketolainen, Jarkko ^a  

^a UNIVERSITY OF EASTERN FINLAND   (Finland)

^b UNIVERSITY OF TURKU   (Finland)

Author keywords

Amorphous; Dissolution enhancement; PEG; PVP; Solid dispersion; Solid solution

Indexed keywords

MACROGOL 8000; PERPHENAZINE; POVIDONE;

ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DRUG FORMULATION; DRUG SOLUBILITY; FREEZE DRYING; HYDROGEN BOND; IN VITRO STUDY; INFRARED SPECTROSCOPY; X RAY CRYSTALLOGRAPHY; X RAY POWDER DIFFRACTION;

ADMINISTRATION, ORAL; ANTIPSYCHOTIC AGENTS; CALORIMETRY, DIFFERENTIAL SCANNING; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; FREEZE DRYING; HYDROGEN BONDING; HYDROGEN-ION CONCENTRATION; PERPHENAZINE; POLYETHYLENE GLYCOLS; POVIDONE; SCATTERING, SMALL ANGLE; SOLUBILITY; X-RAY DIFFRACTION;

EID: 59649094986     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2008.09.001     Document Type: Article

References (52)

1. Kellaway I.W., Ponchel G., and Duchene D. Oral mucosal drug delivery. In: Rathbone M. (Ed). Modified-release Drug Delivery Technology (2002), Marcel Dekker, Inc, New York, USA 349-364
2. Dobetti L. Fast-melting tablets: developments and technologies. Phar. Tech. Feb. 2 (2001) 44-50
3. Bredenberg S., Duberg M., Lennernäs B., Lennernäs H., Pettersson A., Westerberg M., and Nyström C. In vitro and in vivo evaluation of a new sublingual tablet system for rapid oromucosal absorption using fentanyl citrate as the active substance. Eur. J. Pharm. Sci. 20 (2003) 327-334
4. Jain A.C., Aungst B.J., and Adeyeye M.C. Development and in vivo evaluation of buccal tablets prepared using danazol-sulfobutylether 7 β-cyclodextrin (SBE 7) complexes. J. Pharm. Sci. 91 (2002) 1659-1668
5. Leuner C., and Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm. 50 (2000) 47-60
6. Sethia S., and Squillante E. Solid dispersions: revival with greater possibilities and applications in oral drug delivery. Crit. Rev. Therap. Drug. Carrier Syst. 20 (2003) 215-247
7. Chiou W.L., and Riegelman S. Pharmaceutical applications of solid dispersion systems. J. Pharm. Sci. 60 (1971) 1281-1302
8. Forster A., Hempenstall J., Tucker I., and Rades T. Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis. Int. J. Pharm. 226 (2001) 147-161
9. Karavas E., Ktistis G., Xenakis A., and Georgarakis E. Effect of hydrogen bonding interactions on the release of felodipine from nanodispersions with polyvinylpyrrolidone. Eur. J. Pharm. Sci. 63 (2006) 103-114
10. Dordunoo S.K., Ford J.L., and Rubinstein M.H. Physical stability of solid dispersions containing triamterene or temazepam in polyethylene glycols. J. Pharm. Pharmacol. 49 (1997) 390-396
11. Verheyen S., Blaton N., Kinget R., and Van den Mooter G. Mechanism of increased dissolution of diazepam and temazepam from polyethylene glycol 600 solid dispersions. Int. J. Pharm. 249 (2002) 45-58
12. Karavas E., Georgarakis M., Docoslis A., and Bikiaris D. Combining SEM, TEM and micro-Raman techniques to differentiate between the amorphous molecular level dispersions and nanodispersions of a poorly water-soluble drug within a polymer matrix. Int. J. Pharm. 340 (2007) 76-83
13. In: Guozhong C. (Ed). Characterization and properties of nanomaterials. Nanostructures and Nanomaterials (2004), World Scientific Publishing Company Inc., Singapore 333-336
14. Konno H., and Taylor L.S. Influence of different polymers on the crystallization tendency of molecularly dispersed amorphous felodipine. J. Pharm. Sci. 95 (2006) 2692-2705
15. Law D., Krill S.L., Schmitt E.A., Fort J.J., Qiu Y., Wang W., and Porter W.R. Physicochemical considerations in the preparation of amorphous ritonavir-poly(ethylene glycol) 8000 Solid dispersions. J. Pharm. Sci. 90 (2001) 1015-1025
16. Taylor L.S., and Zografi G. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm. Res. 14 (1997) 1691-1698
17. Anguiano-Igea S., Otero-Espinar F.J., Vila-Jato J.L., and Blanco-Mendez J. The properties of solid dispersions of clofibate in polyethylene glycols. Pharm. Acta Helv. 70 (1995) 57-66
18. Urbanetz N.A., and Lippold B.C. Solid dispersions of nimodipine, polyethylene glycol 2000 Dissolution properties and physico-chemical characterization. Eur. J. Pharm. Biopharm. 59 (2005) 107-118
19. Weuts I., Kempen D., Verreck G., Decorte A., Heymans K., Peeters J., Brewster M., and Van den Mooter G. Study of the physicochemical properties, stability of solid dispersions of loperamide, PEG 6000 Prepared by spray drying. Eur. J. Pharm. Biopharm. 59 (2005) 119-126
20. In: Moffat A.C., Osselton M.D., and Widdop B. (Eds). Clarke's Analysis of Drugs and Poisons (2006), Pharmaceutical Press, London, Great Britain
21. In: David D.J., and Misra A. (Eds). Cohesive properties and solubility parameter concepts. Relating Materials Properties to Structure. Handbook and Software for Polymer Calculations and Materials Properties (1999), Lancaster Technomic Publishing Co. Inc., USA 287-304
22. Greenhalg D.J., Williams A.C., Timmins P., and York P. Solubility parameters as predictors of miscibility in solid dispersions. J. Pharm. Sci. 88 (1999) 1182-1190
23. Marsac P.J., Shamblin S.L., and Taylor L.S. Theoretical and practical approaches for prediction of drug-polymer miscibility and solubility. Pharm. Res. 23 (2006) 2417-2426
24. Hancock B., York P., and Rowe R. The use of solubility parameters in pharmaceutical dosage form design. Int. J. Pharm. 148 (1997) 1-21
25. In: Van Krevelen D.W. (Ed). Cohesive properties and solubility. Properties of Polymers. Their Correlation with Chemical Structure: Their Numerical Estimation and Prediction from Additive Group Contributions (1997), Elsevier, Amsterdam, The Netherlands 189-225
26. Nair R., Nyamweya N., Gönen S., Martinez-Miranda L.J., and Hoag S.W. Influence of various drugs on the glass transition temperature of poly(vinylpyrrolidone): a thermodynamic and spectroscopic investigation 225 (2001) 83-96
27. Langer M., Höltje M., Urbanetz N.A., Brandt B., Höltje H.D., and Lippold B.C. Investigations on the predictability of the formation of glassy solid solutions of drugs in sugar alcohols. Int. J. Pharm. 252 (2003) 167-179
28. Mura P., Moyano J.R., Gonzales-Rodriquez M.L., Rabasco-Alvarez A.M., Cirri M., and Maestrelli F. Characterization and dissolution properties of ketoprofen in binary and ternary solid dispersions with polyethylene glycol and surfactants. Drug. Dev. Ind. Pharm. 31 (2005) 425-434
29. Sethia S., and Squillante E. Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods. Int. J. Pharm. 272 (2004) 1-10
30. Ruan L.P., Yu B.Y., Fu G.M., and Zhu D. Improving the solubility of ampelopsin by solid dispersions and inclusion complexes. J. Pharm. Biomed. Anal. 38 (2005) 457-464
31. Murray C.B., Kagan C.R., and Bawendi M.G. Synthesis and characterization of monodisperse nanocrystals and close-packed nanocrystal assemblies. Annu. Rev. Mater. Sci. 30 (2000) 545-610
32. Finnie K.S., Bartlett J.R., Barbe C.J., and Kong L. Formation of silica nanoparticles in microemulsions. Langmuir 23 (2007) 3017-3024
33. Craig D.Q.M. The mechanisms of drug release from solid dispersions in water-soluble polymers. Int. J. Pharm. 231 (2002) 131-144
34. Craig D.Q.M. Polyethylene glycols and drug release. Drug. Dev. Ind. Pharm. 16 (1990) 2501-2526
35. Gordon M., and Taylor J.S. Ideal copolymers and the second order transition of synthetic rubbers 1. Non-crystalline co-polymers. J. Appl. Chem. 2 (1952) 493-500
36. Lu Q., and Zografi G. Phase behavior of binary and ternary amorphous mixtures containing indomethacin, citric acid and PVP. Pharm. Res. 15 (1998) 1202-1206
37. Van den Mooter G., Augustinjs P., Blaton N., and Kinget R. Physico-chemical characterization of solid dispersions of temazepam with polyethylene glycol 6000 and PVP K30. Int. J. Pharm. 164 (1998) 67-80
38. Matsumoto T., and Zografi G. Physical properties of solid molecular dispersions of indomethacin with poly(vinylpyrrolidone) and poly(vinylpyrrolidone-co-vinylacetate) in relation to indomethacin crystallization. Pharm. Res. 14 (1999) 1722-1728
39. Karavas E., Ktistis G., Xenakis A., and Georgarakis E. Miscibility behavior and formation mechanism of stabilized felodipine-polyvinylpyrrolidone amorphous solid dispersions. Drug. Dev. Ind. Pharm. 31 (2005) 473-489
40. Paradkar A., Ambike A.A., Jadhav B., and Mahadik K.R. Characterization of curcumin-PVP solid dispersion obtained by spray drying. Int. J. Pharm. 271 (2004) 281-286
41. Shah J., Chen J., and Chow D. Preformulation study of etoposide. II: increased solubility and dissolution rate by solid-solid dispersion. Int. J. Pharm. 113 (1995) 103-111
42. Lin C.W., and Cham T.M. Effect of particle size on the available surface area of nifedipine from nifedipine-polyethylene glycol 600 solid dispersions. Int. J. Pharm. 127 (1996) 261-272
43. Vijaya Kumar S.G., and Mishra D.N. Preparation, characterization and in vitro dissolution studies of solid dispersion of meloxicam with PEG 6000. Yakugaku Zasshi 126 (2006) 657-664
44. Perng C.Y., Kearney A.S., Patel K., Palepu N.R., and Zuber G. Investigation of formulation approaches to improve the dissolution of SB-210661, a poorly water soluble 5-lipoxygenase inhibitor. Int. J. Pharm. 176 (1998) 31-38
45. Patel R.P., and Patel M.M. Physicochemical characterization, dissolution study of solid dispersions of lovastatin with polyethylene glycol 4000 and polyvinylpyrrolidone K30, Pharm. Dev. Technol. 12 (2007) 21-33
46. Elkhider N., Chan K.L.A., and Kazarian S.G. Effect of moisture and pressure on tablet compaction studied with FTIR spectroscopic imaging. J. Pharm. Sci. 96 (2007) 351-360
47. Bansal S.S., Kaushal A.M., and Bansal A.K. Molecular and thermodynamic aspects of solubility advantage from solid dispersions. Mol. Pharm. 4 (2007) 794-802
48. Mura P., Faucci M.T., Manderioli A., Bramanti G., and Parrini P. Thermal behavior and dissolution properties of naproxen from binary and ternary solid dispersions. Drug Dev. Ind. Pharm. 25 (1999) 257-264
49. Tong P., and Zografi G. Solid-state characterization of amorphous sodium indomethacin relative to its free acid. Pharm. Res. 16 (1999) 1186-1192
50. Tong P., Taylor L.S., and Zografi G. Influence of alkali metal counterions on the glass transition temperature of amorphous indomethacin salts. Pharm. Res. 19 (2002) 649-654
51. Usui F., Maeda K., Kusai A., Ikeda M., Nishimura K., and Yamamoto K. Dissolution improvement of RS-8350 by the solid dispersion prepared by the solvent method. Int. J. Pharm. 170 (1998) 247-256
52. Tran P.H., Tran H.T., and Lee B.J. Modulation of microenvironmental pH and crystallinity of ionizable telmisartan using alkalizers in solid dispersions for controlled release. J. Control. Rel. 129 (2008) 59-65