Production of advanced solid dispersions for enhanced bioavailability of itraconazole using KinetiSol® Dispersing

References

• Breitenbach J. (2009). The Kaletra® Meltrex story: Turning scientific challenges into patient benefit, Soliqs, May92009.
   Google Scholar
• Gao P, Morozowich W. (2006). Development of supersaturatable self-emulsifying drug delivery system formulations for improving the oral absorption of poorly soluble drugs. Expert Opin Drug Deliv, 3(1):97–110.
   PubMedGoogle Scholar
• Gao P, Morozowich W. (2006). Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability. United States of America Patent US 7,115,565 B22006.
   Google Scholar
• Brewster ME, Vandecruys R, Peeters J, Neeskens P, Verreck G, Loftsson T. (2008). Comparative interaction of 2-hydroxypropyl-β-cyclodextrin and sulfobutylether-β-cyclodextrin with itraconazole: Phase-solubility behavior and stabilization of supersaturated drug solutions. Eur J Pharm Sci, doi:10.1016/j.ejps.2008.02.007.
   PubMed Web of Science ®Google Scholar
• Buchanan CM, Buchanan NL, Edgar KJ, Klein S, Little JL, Ramsey MG, . (2007). Pharmacokinetics of itraconazole after intravenous and oral dosing of itraconazole-cyclodextrin formulations. J Pharm Sci, 96(11):3100–16.
   PubMed Web of Science ®Google Scholar
• Peeters J, Neeskens P, Tollenaere JP, Van Remoortere P, Brewster ME. (2002). Characterization of the interaction of 2‐hydroxypropyl-β-cyclodextrin with itraconazole at pH 2, 4, and 7. J Pharm Sci, 91(6):1414–22.
   PubMed Web of Science ®Google Scholar
• Loftsson T, Brewster ME. (1996). Pharmaceutical applications of cyclodextrins. 1. Drug solubilization and stabilization. J Pharm Sci, 85(10):1017–25.
   PubMed Web of Science ®Google Scholar
• Glasmacher A, Hahn C, Molitor E, Marklein G, Sauerbruch T, Schmidt-Wolf IGH. (1999). Itraconazole trough concentrations in antifungal prophylaxis with six different dosing regimens using hydroxypropyl-β-cyclodextrin oral solution or coated-pellet capsules. Mycoses 42(11–12):591–600.
   PubMed Web of Science ®Google Scholar
• Gao P, Rush BD, Pfund WP, Huang T, Bauer JM, Morozowich W, . (2003). Development of a supersaturable SEDDS (S‐SEDDS) formulation of paclitaxel with improved oral bioavailability. J Pharm Sci, 92(12):2386–98.
   PubMed Web of Science ®Google Scholar
• Keown P, Niese D. (1998). Cyclosporine microemulsion increases drug exposure and reduces acute rejection without incremental toxicity in de novo renal transplantation. Kidney Int, 54(3):938–44.
   PubMed Web of Science ®Google Scholar
• Bhardwaj V, Hariharan S, Bala I, Lamprecht A, Kumar N, Panchagnula R, . (2005). Pharmaceutical aspects of polymeric nanoparticles for oral drug delivery. J Biomed Nanotechnol, 1(3):235–58.
   Web of Science ®Google Scholar
• Jia L. (2005). Nanoparticle formulation increases oral bioavailability of poorly soluble drugs: Approaches, experimental evidences and theory. Curr Nanosci, 1(3):237–43.
   PubMed Web of Science ®Google Scholar
• Overhoff KA, McConville JT, Yang W, Johnston KP, Peters JI, Williams III RO. (2008). Effect of stabilizer on the maximum degree and extent of supersaturation and oral absorption of Tacrolimus made by ultra-rapid freezing. Pharm Res, 25(1):167–75.
   PubMed Web of Science ®Google Scholar
• Vaughn JM, McConville JT, Crisp MT, Johnston KP, Williams III RO. (2006). Supersaturation produces high bioavailability of amorphous danazol particles formed by evaporative precipitation into aqueous solution and spray freezing into liquid technologies. Drug Dev Ind Pharm, 32(5):559–67.
   PubMed Web of Science ®Google Scholar
• Kayser O, Olbrich C, Yardley V, Kiderlen AF, Croft SL. (2003). Formulation of amphotericin B nanosuspension for oral administration. Int J Pharm, 254(1):73–5.
   PubMed Web of Science ®Google Scholar
• Yin SX, Franchini M, Chen J, Hsieh A, Jen S, Lee T, . (2005). Bioavailability enhancement of a COX-2 inhibitor, BMS-347070, from a nanocrystalline dispersion prepared by spray-drying. J Pharm Sci, 94(7):1598–607.
   PubMed Web of Science ®Google Scholar
• Breitenbach J. (2006). Melt extrusion can bring new benefits to HIV therapy: The example of Kaletra tablets. Am J Drug Deliv, 4(2):61–4.
   Google Scholar
• Six K, Daems T, de Hoon J, Van Hecken A, Depre M, Bouche M‐P, . (2005). Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion. Eur J Pharm Sci, 24(2–3):179–86.
   PubMed Web of Science ®Google Scholar
• Zheng X, Yang R, Zhang Y, Wang Z, Tang X, Zheng L. (2007). Part II: Bioavailability in beagle dogs of Nimodipine solid dispersions prepared by hot-melt extrusion. Drug Dev Ind Pharm, 33(7):783–9.
   PubMed Web of Science ®Google Scholar
• Yamashita K, Nakate T, Okimoto K, Ohike A, Tokunaga Y, Ibuki R, . (2003). Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int J Pharm, 267(1–2):79–91.
   PubMed Web of Science ®Google Scholar
• DiNunzio JC, Miller DA, Yang W, McGinity JW, Williams III RO. (2008). Amorphous compositions using concentration enhancing polymers for improved bioavailability. Mol Pharm, 5(6):968–80.
   PubMed Web of Science ®Google Scholar
• Kondo N, Iwao T, Hirai K, Fukuda M, Yamanouchi K, Yokoyama K, . (1994). Improved oral absorption of enteric coprecipitates of a poorly soluble drug. J Pharm Sci, 83(4):566–70.
   PubMed Web of Science ®Google Scholar
• Miller DA, DiNunzio JC, Yang W, McGinity JW, Williams III RO. (2008). Enhanced in vivo absorption of itraconazole via stabilization of supersaturation following acidic-to-neutral pH transition. Drug Dev Ind Pharm, 34(8):890–902.
   PubMed Web of Science ®Google Scholar
• Gad SC. (2007). Introduction: The gastrointestinal tract as barrier and as absorptive and metabolic organ. In: Gad SC, ed. Toxicology of the gastrointestinal tract. Boca Raton, FL: CRC Press, 1–34.
   Google Scholar
• Kapp Jr RW. (2007). 2 Gastrointestinal tract as major route of pharmaceutical administration. In: Gad SC, ed. Toxicology of the gastrointestinal tract. Boca Raton, FL: CRC Press, 107–33.
   Google Scholar
• Wagner D, Spahn-Langguth H, Hanafy A, Koggel A, Langguth P. (2001). Intestinal drug efflux: Formulation and food effects. Adv Drug Deliv Rev, 50(Suppl 1):S13–31.
   Google Scholar
• Karalis V, Macheras P, Van Peer A, Shah VP. (2008). Bioavailability and bioequivalence: Focus on physiological factors and variability. Pharm Res, 25(8):1956–62.
   PubMed Web of Science ®Google Scholar
• McConnell EL, Fadda HM, Basit AW. (2008). Gut instincts: Explorations in intestinal physiology and drug delivery. Int J Pharm, 364(2):213–26.
   PubMed Web of Science ®Google Scholar
• Miller DA, DiNunzio JC, Yang W, McGinity JW, Williams III RO. (2008). Targeted intestinal delivery of supersaturated itraconazole for improved oral absorption. Pharm Res, 25(6):1450–9.
   PubMed Web of Science ®Google Scholar
• Guzmán HR, Tawa M, Zhang Z, Ratanabanangkoon P, Shaw P, Gardner CR, . (2007). Combined use of crystalline salt forms and precipitation inhibitors to improve oral absorption of Celecoxib from solid oral formulations. J Pharm Sci, 96(10):2686–702.
   PubMed Web of Science ®Google Scholar
• Gao P, Guyton ME, Huang T, Bauer JM, Stefanski KJ, Lu Q. (2004). Enhanced oral bioavailability of a poorly water soluble drug PNU-91325 by supersaturatable formulations. Drug Dev Ind Pharm, 30(2):221–9.
   PubMed Web of Science ®Google Scholar
• Usui F, Maeda K, Kusai A, Nishimura K, Yamamoto K. (1997). Inhibitory effects of water-soluble polymers on precipitation of RS-8359. Int J Pharm, 154(1):59–66.
   Web of Science ®Google Scholar
• De Beule K, Van Gestel J. (2001). Pharmacology of itraconazole. Drugs, 61(1):27–37.
   PubMedGoogle Scholar
• Willems L, van der Geest R, de Beule K. (2001). Itraconazole oral solution and intravenous formulations: A review of pharmacokinetics and pharmacodynamics. J Clin Pharm Ther, 26:159–69.
   PubMed Web of Science ®Google Scholar
• Quinney SK, Galinsky RE, Jiyamapa-Serna VA, Chen Y, Hamman MA, Hall SD, . (2008). Hydroxyitraconazole, formed during intestinal first-pass metabolism of itraconazole, controls the time course of hepatic CYP3A inhibition and the bioavailability of itraconazole in rats. Drug Metab Dispos, 36(6):1097–101.
   PubMed Web of Science ®Google Scholar
• Li L, Mathias NR, Heran CLH, Moench P, Wall DA, Smith RL. (2006). Carbopol-mediated paracellular transport enhancement in Calu-3 cell layers. J Pharm Sci, 95(2):326–35.
   PubMed Web of Science ®Google Scholar
• Peppas NA, Thomas BJ, McGinity J. (2009). Molecular aspects of mucoadhesive carrier development for drug delivery and improved absorption. J Biomater Sci Polym Ed, 20(1):1–20.
   PubMed Web of Science ®Google Scholar
• Borchard G, LeuBen HL, de Boer AG, Verhoef JC, Lehr C-M, Junginger HE. (1996). The potential of mucoadhesive polymers in enhancing intestinal peptide drug absorption. III: Effects of chitosan-glutamate and carbomer on epithelial tight junctions in vitro. J Control Release, 39(2–3):131–8.
   Web of Science ®Google Scholar
• DiNunzio JC, Brough C, Miller DA, Williams III RO, McGinity JW. (2010). Fusion processing of itraconazole solid dispersions by KinetiSol® dispersing: A comparative study to hot melt extrusion. J Pharm Sci, 99(3):1239.
   PubMed Web of Science ®Google Scholar
• DiNunzio JC, Brough C, Miller DA, Williams III RO, McGinity JW. (2009). Applications of KinetiSol® dispersing for the production of plasticizer free amorphous solid dispersions. Eur J Pharm Sci, Submitted.
   Web of Science ®Google Scholar
• Mellaerts R, Mols R, Kayaert P, Annaert P, Van Humbeeck J, Van den Mooter G, . (2008). Ordered mesoporous silica induces pH-independent supersaturation of the basic low solubility compound itraconazole resulting in enhanced transepithelial transport. Int J Pharm, 357(1–2):169–79.
   PubMed Web of Science ®Google Scholar
• Fukasawa M, Obara S. (2004). Molecular weight determination of hypromellose acetate succinate (HPMCAS) using size exclusion chromatography with a multi-angle laser light scattering detector. Chem Pharm Bull (Tokyo), 52(11):1391–3.
   PubMed Web of Science ®Google Scholar
• Vandecruys R, Peeters J, Verreck G, Brewster ME. (2007). Use of a screening method to determine excipients which optimize the extent and stability of supersaturated drug solutions and application of this system to solid formulation design. Int J Pharm, 342(1–2):168–75.
   PubMedGoogle Scholar
• DiNunzio JC, Brough C, Hughey JR, Miller DA, Williams III RO, McGinity JW. (2010). Fusion production of solid dispersions containing heat sensitive active ingredient by hot melt extrusion and KinetiSol® dispersing. Eur J Pharm Biopharm, 74(2):340.
   PubMed Web of Science ®Google Scholar
• Six K, Verreck G, Peeters J, Augustijns P, Kinget R, Van den Mooter G. (2001). Characterization of glassy itraconazole: A comparative study of its molecular mobility below Tg with that of structural analogues using MTDSC. Int J Pharm, 213(1–2):163–73.
   PubMedGoogle Scholar
• Young CR, Dietzsch C, Cerea M, Farrell T, Fegely KA, Rajabi-Siahboomi A, . (2005). Physicochemical characterization and mechanisms of release of theophylline from melt-extruded dosage forms based on a methacrylic acid copolymer. Int J Pharm, 301(1–2):112–20.
   PubMed Web of Science ®Google Scholar
• Dressman JB, Thelen K, Jantratid E. (2008). Towards quantitative prediction of oral drug absorption. Clin Pharmacokinet, 47(10):655–67.
   PubMed Web of Science ®Google Scholar
• Dressman JB, Vertzoni M, Goumas K, Reppas C. (2007). Estimating drug solubility in the gastrointestinal tract. Adv Drug Deliv Rev, 59(7):591–602.
   PubMed Web of Science ®Google Scholar
• McConnell EL, Basit AW, Murdan S. (2008). Measurements of rat and mouse gastrointestinal pH, fluid and lymphoid tissue, and implications for in-vivo experiments. J Pharm Pharmacol, 60(1):63–70.
   PubMed Web of Science ®Google Scholar