Formulation and in vivo human bioavailability of dissolving tablets containing a self-nanoemulsifying itraconazole solid dispersion without precipitation in simulated gastrointestinal fluid

European Journal of Pharmaceutical Sciences

Volumn 51, Issue 1, 2014, Pages 67-74

  Piao, Zong Zhu ^a   Choe, Jae Seung ^a   Oh, Kyung Teak ^c   Rhee, Yun Seok ^d   Lee, Beom Jin ^b  

^a EuraPharm Inc   (South Korea)

^b Ajou University   (South Korea)

^c Chung Ang University   (South Korea)

^d Gyeongsang National University   (South Korea)

Author keywords

Enhanced dissolution; In vivo oral bioavailability; Poorly water soluble drug; Precipitation and crystallisation; Self nanoemulsifying solid dispersion

Indexed keywords

ITRACONAZOLE; SILICON DIOXIDE; SURFACTANT; WATER;

ADSORPTION KINETICS; ADULT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CONTROLLED STUDY; CRYSTAL STRUCTURE; CRYSTALLIZATION; DISPERSION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG DELIVERY SYSTEM; DRUG DETERMINATION; DRUG SOLUBILITY; DRUG STABILITY; DRUG STORAGE; HUMAN; HUMAN EXPERIMENT; IN VIVO STUDY; INTESTINE FLUID; MALE; MAXIMUM PLASMA CONCENTRATION; NANOEMULSION; NORMAL HUMAN; PRECIPITATION; PRIORITY JOURNAL; SELF NANOEMULSIFYING SOLID DISPERSION; SOLID STATE; STOMACH JUICE; TABLET COMPRESSION; TABLET DISINTEGRATION; TABLET FORMULATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ENHANCED DISSOLUTION; IN VIVO ORAL BIOAVAILABILITY; POORLY WATER-SOLUBLE DRUG; PRECIPITATION AND CRYSTALLISATION; SELF-NANOEMULSIFYING SOLID DISPERSION;

ADULT; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; EMULSIFYING AGENTS; HUMANS; ITRACONAZOLE; MALE; NANOPARTICLES; SOLUBILITY; SURFACE-ACTIVE AGENTS; TABLETS; WATER; YOUNG ADULT;

EID: 84884921441     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2013.08.037     Document Type: Article

References (24)

1. A.A. Attama, I.T. Nzekwe, P.O. Nnamani, M.U. Adikwu, and C.O. Onugu The use of solid self-emulsifying systems in the delivery of diclofenac Int. J. Pharm. 262 2003 23 28 (Pubitemid 36966690)
2. E.B. Basalius, W. El-Sebuie, and O. El-Gazayerly Application of pharmaceutical QbD for enhancement of the solubility and dissolution of a class II BCS drug using polymeric surfactants and crystallization inhibitors development of controlled-release tablets AAPS Pharm. Sci. Technol. 12 3 2011 799 810
3. R. Cai, L. Zhu, and L. Yu Crystallization of organic glasses: effects of polymer additives on bulk and surface crystal growth in amorphous nifedipine Pharm. Res. 28 2011 2458 2466
4. K.P.R. Chowdary, and S. Rao Investigation of dissolution enhancement of itraconazole by solid dispersion in superdisintegrants Drug Dev. Ind. Pharm. 26 11 2000 1207 1211
5. H. de Waard, W.L. Hinrichs, M.R. Visser, C. Bologna, and H.W. Frijlink Unexpected differences in dissolution behavior of tablets prepared from solid dispersions with a surfactant physically mixed or incorporated Int. J. Pharm. 349 2008 66 73 (Pubitemid 350299690)
6. J.C. Dinunzio, C. Brough, D.A. Miller, R.O. Williams III, and J.W. McGinity Applications of kinetisol® dispersing for the production of plasticizer free amorphous solid dispersions Eur. J. Pharm. Sci. 40 2010 179 187
7. G. Dumortier, J.L. Grossiord, F. Agnely, and J.C. Chaumeil A review of Poloxamer 407 pharmaceutical and pharmacological characteristics Pharm. Res. 23 12 2006 2709 2728 (Pubitemid 44885361)
8. E. Franceschinisa, D. Voinovicha, M. Grassib, B. Perissuttia, J. Filipovic-Grcicc, A. Martinacc, and F. Meriani-Merloa Self-emulsifying pellets prepared by wet granulation in high-shear mixer: influence of formulation variables and preliminary study on the in vitro absorption Int. J. Pharm. 291 2005 87 97
9. M.-Y. Heo, Z.-Z. Piao, T.-W. Kim, Q.-R. Cao, A. Kim, and B.-J. Lee Effect of solubilizing and microemulsifying excipients in polyethylene glycol 6000 solid dispersion on enhanced dissolution and bioavailability of ketoconazole Arch. Pharm. Res. 28 2005 604 611 (Pubitemid 44698739)
10. S. Nazzal, and M. Khan Controlled release of a self-nanoemulsifying formulation from a tablet dosage form: stability assessment and optimization of some processing parameters Int. J. Pharm. 315 2006 110 121 (Pubitemid 43674113)
11. V. Nekkanti, P. Karatgi, R. Prabhu, and R. Pillai Solid self-microemulsifying formulation for candesartan cilexetil AAPS Pharm. Sci. Technol. 11 1 2010 9 17
12. K.A. Overhoff, A. Moreno, D.A. Miller, K.P. Johnston, and R.O. Williama Solid dispersions of itraconazole and enteric polymers made by ultra-rapid freezing Int. J. Pharm. 336 2007 122 132 (Pubitemid 46551563)
13. M.-J. Park, S. Ren, and B.-J. Lee In vitro and in vivo comparative study of itraconazole bioavailability when formulated in highly soluble self-emulsifying system and in solid dispersion Biopharm. Drug Dispos. 28 4 2007 199 207 (Pubitemid 46824855)
14. J. Peeters, P. Neeslens, J.P. Tollenaere, P. Van Remoortere, and M. Brewster Characterization of the interaction of 2-hydroxypropyl-β- cyclodextrin with itraconazole at pH 2, 4 and 7 J. Pharm. Sci. 91 2002 1414 1422
15. Z.-Z. Piao, M.-K. Lee, and B.-J. Lee Colonic release and reduced intestinal tissue damage of coated tablets containing naproxen inclusion complex Int. J. Pharm. 350 2008 205 211
16. S.-Y. Shim, C.-W. Ji, H.-K. Sah, E.-S. Park, and B.-J. Lee Characterization of itraconazole semisolid dosage forms prepared by hot melt technique Arch. Pharm. Res. 29 2006 1055 1060 (Pubitemid 44885785)
17. Y. Shono, E. Jantratid, and J.B. Dressman Precipitation in the small intestine may play a more important role in the in vivo performance of poorly soluble weak bases in the fasted state: case example nelfinavir Eur. J. Pharm. Biopharm. 79 2011 2011 349 356
18. M.V. Speybroeck, R. Mols, R. Mellaerts, T.D. Thi, J.A. Martens, J.V. Humbeeck, P. Annaert, G.V. Mooter, and P. Augustijns Combined use of ordered mesoporous silica and precipitation inhibitors for improved oral absorption of the poorly soluble weak base itraconazole Eur. J. Pharm. Biopharm. 75 2010 354 365
19. B. Tang, G. Cheng, J.C. Gu, and C.H. Xu Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms Drug Discovery Today 13 2008 606 612
20. T. Tokumura, Y. Tsushima, and K. Tatsuishi Enhancement of the oral bioavailability of cinnarizine in oleic acid in beagle dogs J. Pharm. Sci. 76 1987 286 288 (Pubitemid 17118155)
21. P.H. Tran, H.T. Tran, and B.-J. Lee Modulation of microenvironmental pH and crystallinity of ionizable telmisartan using alkalizers in solid dispersions for controlled release J. Controlled Release 129 1 2008 59 65
22. T.T. Tran, P.H. Tran, and B.-J. Lee Dissolution-modulating mechanism of alkalizers and polymers in nanoemulsifying solid dispersion containing acidic drug Eur. J. Pharm. Biopharm. 72 2009 83 90
23. P.H. Tran, T.T. Tran, Z.Z. Piao, T.V. Vo, J.B. Park, J. Lim, K.T. Oh, Y.-S. Rhee, and B.-J. Lee Physical properties and in vivo bioavailability in human volunteers of isradipine using controlled release matrix tablet containing self-emulsifying solid dispersion Int. J. Pharm. 450 2013 79 86
24. J.-S. Woo, Y.-K. Song, J.-Y. Hong, S.-J. Lim, and C.-K. Kim Reduced food-effect and enhanced bioavailability of a self-microemulsifying formulation of itraconazole in healthy volunteers Eur. J. Pharm. Sci. 33 2008 159 165