Itraconazole/TPGS/Aerosil®200 solid dispersions. Characterization, physical stability and in vivo performance

European Journal of Pharmaceutical Sciences

Volumn 38, Issue 3, 2009, Pages 270-278

  Van Eerdenbrugh, Bernard ^a   Van Speybroeck, Michiel ^a   Mols, Raf ^a   Houthoofd, Kristof ^b   Martens, Johan A ^b   Froyen, Ludo ^b   Van Humbeeck, Jan ^b   Augustijns, Patrick ^a   Van den Mooter, Guy ^a  

^a DEPARTMENT OF PHARMACEUTICAL AND PHARMACOLOGICAL SCIENCES   (Belgium)

^b UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Aerosil 200; Itraconazole; Solid dispersion; Spray drying

Indexed keywords

AEROSIL; ITRACONAZOLE; TOCOFERSOLAN; ALPHA TOCOPHEROL; ALPHA TOCOPHERYL POLYETHYLENE GLYCOL SUCCINATE; ALPHA-TOCOPHERYL POLYETHYLENE GLYCOL SUCCINATE; DRUG CARRIER; DRUG DERIVATIVE; MACROGOL DERIVATIVE; SILICON DIOXIDE;

ADSORPTION; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG SOLUBILITY; DRUG STABILITY; DRUG STORAGE; HEAT TREATMENT; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; PRIORITY JOURNAL; RAT; SPRAY DRYING; SUSPENSION; TIME TO MAXIMUM PLASMA CONCENTRATION; X RAY POWDER DIFFRACTION; ANIMAL; BLOOD; CHEMISTRY; COMPARATIVE STUDY; METABOLISM; METHODOLOGY; POWDER; WISTAR RAT; X RAY DIFFRACTION;

ANIMALS; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; DRUG CARRIERS; DRUG STABILITY; ITRACONAZOLE; MALE; POLYETHYLENE GLYCOLS; POWDERS; RATS; RATS, WISTAR; SILICON DIOXIDE; VITAMIN E; X-RAY DIFFRACTION;

EID: 70349112222     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2009.08.002     Document Type: Article

References (34)

1. Amidon G.L., Lennernäs H., Shah V.P., and Crison J.R. Theoretical basis for a biopharmaceutical drug classification; the correlation of in vivo drug product dissolution and in vivo bioavailability. Pharm. Res. 12 (1995) 413-420
2. Bahl D., and Bogner R.H. Amorphization of indomethacin by co-grinding with neusilin US2: amorphization kinetics, physical stability and mechanism. Pharm. Res. 23 (2006) 2317-2325
3. Bahl D., Hudak J., and Bogner R.H. Comparison of the ability of various pharmaceutical silicates to amorphize and enhance dissolution of indomethacin upon co-grinding. Pharm. Dev. Technol. 13 (2008) 255-269
4. Gupta M.K., Goldman D., Bogner R.H., and Tseng Y.C. Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent. Pharm. Dev. Technol. 6 (2001) 563-572
5. Gupta M.K., Bogner R.H., Goldman D., and Tseng Y.C. Mechanism for further enhancement in drug dissolution from solid-dispersion granules upon storage more options. Pharm. Dev. Technol. 7 (2002) 103-112
6. Gupta M.K., Tseng Y.C., Goldman D., and Bogner R.H. Hydrogen bonding with adsorbent during storage governs drug dissolution from solid-dispersion granules. Pharm. Res. 19 (2002) 1663-1672
7. Gupta M.K., Vanwert A., and Bogner R.H. Formation of physically stable amorphous drugs by milling with neusilin. J. Pharm. Sci. 92 (2003) 536-551
8. Hancock B.C., and Parks M. What is the true solubility advantage for amorphous pharmaceuticals?. Pharm. Res. 17 (2000) 397-404
9. Kinoshita M., Baba K., Nagayasu A., Yarnabe K., Azuma M., Houchi H., and Minakuchi K. Highly stabilized amorphous 3-bis(4-methoxyphenyl)methylene-2-indolinone (TAS-301) in melt-adsorbed products with silicate compounds. Drug. Dev. Ind. Pharm. 29 (2003) 523-529
10. Leuner C., and Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm. 50 (2000) 47-60
11. Mackie C., Wuyts K., Haseldonckx M., Blokland S., Gysemberg P., Verhoeven I., Timmerman P., and Nijsen M. New model for intravenous drug administration and blood sampling in the awake rat, designed to increase quality and throughput for in vivo pharmacokinetic analysis. J. Pharmacol. Toxicol. Methods 52 (2005) 293-301
12. Mellaerts R., Mols R., Jammaer J.A.G., Aerts C.A., Annaert P., Van Humbeeck J., Van den Mooter G., Augustijns P., and Martens J.A. Increasing the oral bioavailability of the poorly water soluble drug itraconazole with ordered mesoporous silica. Eur. J. Pharm. Biopharm. 69 (2008) 223-230
13. Morefield E., and Seyer J. Colloidal silicon dioxide. In: Rowe R.C., Sheskey P.J., and Weller P.J. (Eds). Handbook of Pharmaceutical Excipients. 4th Edition (2003), Pharmaceutical Press, London 161-164
14. Nernst W. Theorie der Reaktionsgeschwindigkeit in heterogenen Systemen. Zeitschrift f Physik Chemie 47 (1904) 52-55
15. Noyes A.A., and Whitney W.R. The rate of solution of solid substances in their own solutions. J. Am. Chem. Soc. 19 (1897) 930-934
16. Peeters J., Neeskens P., Tollenaere J.P., Van Remoortere P., and Brewster M.E. Characterization of the Interaction of 2-hydroxypropyl-beta-cyclodextrin with itraconazole at pH 2, 4, and 7. J. Pharm. Sci. 91 (2002) 1414-1422
17. Serajuddin A.T.M. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J. Pharm. Sci. 88 (1999) 1058-1066
18. Six K., Verreck G., Peeters J., Binnemans K., Berghmans H., Augustijns P., Kinget R., and Van den Mooter G. Investigation of thermal properties of glassy itraconazole: identification of a monotropic mesophase. Thermochim. Acta 376 (2001) 171-181
19. Six K., Daems T., de Hoon J., Van Hecken A., Depre M., Bouche M., Prinsen P., Verreck G., Peeters J., Brewster M.E., and Van den Mooter G. Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion. Eur. J. Pharm. Sci. 24 (2005) 179-186
20. Takeuchi H., Handa T., and Kawashima Y. Spherical solid dispersion containing amorphous tolbutamide embedded in enteric coating polymers or colloidal silica prepared by spray-drying technique. Chem. Pharm. Bull. 35 (1987) 3800-3806
21. Takeuchi H., Nagira S., Yamamoto H., and Kawashima Y. Solid dispersion particles of tolbutamide prepared with fine silica particles by the spray-drying method. Powder Technol. 141 (2004) 187-195
22. Takeuchi H., Nagira S., Yamamoto H., and Kawashima Y. Solid dispersion particles of amorphous indomethacin with fine porous silica particles by using spray-drying method. Int. J. Pharm. 293 (2005) 155-164
23. Uchino T., Yasuno N., Yanagihara Y., and Suzuki H. Solid dispersion of spironolactone with porous silica prepared by the solvent method. Pharmazie 62 (2007) 599-603
24. Van Eerdenbrugh B., Froyen L., Martens J.A., Blaton N., Augustijns P., Brewster M., and Van den Mooter G. Characterization of physico-chemical properties and pharmaceutical performance of sucrose co-freeze-dried solid nanoparticulate powders of the anti-HIV agent loviride prepared by media milling. Int. J. Pharm. 338 (2007) 198-206
25. Van Eerdenbrugh B., Froyen L., Van Humbeeck J., Martens J.A., Augustijns P., and Van den Mooter G. Alternative matrix formers for nanosuspension solidification: dissolution performance and X-ray microanalysis as an evaluation tool for powder dispersion. Eur. J. Pharm. Sci. 35 (2008) 344-353
26. Van Eerdenbrugh B., Froyen L., Van Humbeeck J., Martens J.A., Augustijns P., and Van den Mooter G. Drying of crystalline drug nanosuspensions - the importance of surface hydrophobicity on dissolution behavior upon redispersion. Eur. J. Pharm. Sci. 35 (2008) 127-135
27. Van Eerdenbrugh B., Vercruysse S., Martens J.A., Vermant J., Froyen L., Van Humbeeck J., Van den Mooter G., and Augustijns P. Microcrystalline cellulose, a useful alternative for sucrose as a matrix former during freeze-drying of drug nanosuspensions - a case study with itraconazole. Eur. J. Pharm. Biopharm. 70 (2008) 590-596
28. Van Eerdenbrugh B., Vermant J., Martens J.A., Froyen L., Van Humbeeck J., Augustijns P., and Van den Mooter G. A Screening study of surface stabilization during the production of drug nanocrystals. J. Pharm. Sci. 98 (2009) 2091-2130
29. Wang L., De Cui F., and Sunada H. Preparation and evaluation of solid dispersions of nitrendipine prepared with fine silica particles using the melt-mixing method. Chem. Pharm. Bull. 54 (2006) 37-43
30. Watanabe T., Wakiyama N., Usui F., Ikeda M., Isobe T., and Senna M. Stability of amorphous indomethacin compounded with silica. Int. J. Pharm. 226 (2001) 81-91
31. Watanabe T., Hasegawa S., Wakiyama N., Kusai A., and Senna M. Prediction of apparent equilibrium solubility of indomethacin compounded with silica by C-13 solid state NMR. Int. J. Pharm. 248 (2002) 123-129
32. Watanabe T., Ohno I., Wakiyama N., Kusal A., and Senna M. Controlled dissolution properties of indomethacin by compounding with silica. STP Pharm. Sci. 12 (2002) 363-367
33. Watanabe T., Ohno I., Wakiyama N., Kusai A., and Senna M. Stabilization of amorphous indomethacin by co-grinding in a ternary mixture. Int. J. Pharm. 241 (2002) 103-111
34. Watanabe T., Hasegawa S., Wakiyama N., Kusai A., and Senna M. Comparison between polyvinylpyrrolidone and silica nanoparticles as carriers for indomethacin in a solid state dispersion. Int. J. Pharm. 250 (2003) 283-286