Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability

Archives of Pharmacal Research

Volumn 33, Issue 8, 2010, Pages 1217-1225

  Park, Young Joon ^b   Xuan, Jing Ji ^a   Oh, Dong Hoon ^a   Balakrishnan, Prabagar ^a   Yang, Ho Joon ^a   Yeo, Woo Hyun ^a   Lee, Mi Kyung ^c   Choi, Han Gon ^a   Yong, Chul Soon ^a  

^a Yeungnam University   (South Korea)

^b Samil Pharmaceutical Co Ltd   (South Korea)

^c Woosuk University   (South Korea)

Author keywords

Bioavailability; Itraconazole; No changeable crystal; Solid dispersion; Solubility

Indexed keywords

CITRIC ACID; ITRACONAZOLE; POLOXAMER; POLYVINYLPYRROLINE; PYRROLINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSAGE FORM COMPARISON; DRUG FORMULATION; DRUG SOLUBILITY; DRUG STABILITY; HYDROPHILICITY; HYDROPHOBICITY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PHYSICAL CHEMISTRY; RAT; SCANNING ELECTRON MICROSCOPY; TIME TO MAXIMUM PLASMA CONCENTRATION; X RAY DIFFRACTION;

ANIMALS; ANTIFUNGAL AGENTS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CALORIMETRY, DIFFERENTIAL SCANNING; CITRIC ACID; CRYSTALLIZATION; DRUG CARRIERS; DRUG STABILITY; DRUG STORAGE; HYDROPHOBIC AND HYDROPHILIC INTERACTIONS; ITRACONAZOLE; MALE; MICROSCOPY, ELECTRON, SCANNING; POLOXAMER; POVIDONE; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; X-RAY DIFFRACTION;

EID: 77957295541     PISSN: 02536269     EISSN: 19763786     Source Type: Journal    
DOI: 10.1007/s12272-010-0812-2     Document Type: Article

References (35)

1. G. L. Amidon H. Lennernas V. P. Shah J. R. Crison 1995 A theoretical basis for a biopharmaceutics durg classification: the correlation of in vitro drug product dissolution and in vivo bioavailability Pharm. Res. 12 413 420 1:CAS:528:DyaK2MXksVGqur8%3D 10.1023/A:1016212804288 7617530
2. M. A. Bogaerts J. Maertens R. Van der Geest A. Bosly J. L. Michaux A. Van Hoof M. Cleeren R. Woestenborghs K. De Beule 2001 Pharmacokinetics and safety of a 7-day administration of intravenous itraconazole followed by a 14-day administration of itraconazole oral solution in patients with hematologic malignancy Antimicrob. Agents Chemother. 45 981 985 10.1128/AAC.45.3.981-985. 2001 (Pubitemid 32182062)
3. C. M. Buchanan N. L. Buchanan K. J. Edgar S. Klein J. L. Little M. G. Ramsey K. M. Ruble V. J. Wacher M. F. Wempe 2007 Pharmacokinetics of itraconazole after intravenous and oral dosing of itraconazole-cyclodextrin formulations J. Pharm. Sci. 96 3100 3116 1:CAS:528:DC%2BD2sXht12jtrrL 10.1002/jps.20878 17712849 (Pubitemid 350221205)
4. W. L. Chiou S. Riegelman 1971 Pharmaceutical application of solid dispersion systems J. Pharm. Sci. 60 1281 1302 1:STN:280:DyaE3M3otFersQ%3D%3D 10.1002/jps.2600600902 4935981
5. H. G. Choi Y. K. Oh C. K. Kim 1998 In-situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability Int. J. Pharm. 165 23 32 1:CAS:528:DyaK1cXis1Wru74%3D 10.1016/S0378-5173(97)00385-2 (Pubitemid 28218341)
6. H. G. Choi B. J. Lee C. S. Yong J. D. Rhee J. H. Han M. K. Lee K. M. Park C. K. Kim 2001 Terfenadine-β-cyclodextrin inclusion complex with the anti-histaminic activity enhancement Drug Dev. Ind. Pharm. 27 857 862 1:CAS:528:DC%2BD3MXosVKks7o%3D 10.1081/DDC-100107250 11699838 (Pubitemid 33029512)
7. D. Q. M. Craig 2002 The mechanism of drug release from solid dispersion in water-soluble polymers Int. J. Pharm. 231 131 144 1:CAS:528: DC%2BD3MXptlaitL0%3D 10.1016/S0378-5173(01)00891-2 11755266 (Pubitemid 34033673)
8. C. Doherty P. York 1987 Mechanisms of dissolution of frusemide/PVP solid dispersions Int. J. Pharm. 34 197 205 1:CAS:528:DyaL2sXht1Gkur8%3D 10.1016/0378-5173(87)90180-3 (Pubitemid 17227496)
9. C. Holvoet Y. Vander Heyden J. Plaizier-Vercammen 2007 Influence of preparation method on itraconazole oral solutions using cyclodextrins as complexing agents Pharmazie 62 510 514 1:CAS:528:DC%2BD2sXnvFCksb4%3D 17718191
10. J. Y. Hong J. K. Kim Y. K. Song J. S. Park C. K. Kim 2006 A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption J. Control. Release 110 332 338 1:CAS:528:DC%2BD2MXhtlert7nM 10.1016/j.jconrel.2005.10.002 16297483 (Pubitemid 41827486)
11. J. Y. Jung S. D. Yoo S. H. Lee K. H. Kim D. S. Yoon K. H. Lee 1999 Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique Int. J. Pharm. 187 209 218 1:CAS:528:DyaK1MXmt1Sgsbk%3D 10.1016/S0378-5173(99)00191-X 10502627 (Pubitemid 29443901)
12. K. Kachrimanis I. Nikolakakis S. Malamataris 2000 Spherical crystal agglomeration of ibuprofen by the solvent-change technique in presence of methacrylic polymers J. Pharm. Sci. 89 250 259 1:CAS:528:DC%2BD3cXit1Knt78%3D 10.1002/(SICI)1520-6017(200002)89:2<250::AID-JPS12>3.0.CO;2-W 10688754 (Pubitemid 30120805)
13. G. M. Khan Z. Jiabi 1998 Preparation, characterization, and dissolution studies of ibuprofen solid dispersions using polyethylene glycol (PEG), talc, and PEG-talc as dispersion carriers Drug Dev. Ind. Pharm. 24 455 462 1:CAS:528:DyaK1cXjt1eqsrs%3D 10.3109/03639049809085643 9876608
14. J. E. Kipp 2004 The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs Int. J. Pharm. 284 109 122 1:CAS:528:DC%2BD2cXnvVCjurw%3D 10.1016/j.ijpharm.2004.07.019 15454302 (Pubitemid 39349144)
15. S. W. Lee M. H. Kim C. K. Kim 1999 Encapsulation of ethanol by spray drying technique: effects of sodium lauryl sulfate Int. J. Pharm. 187 193 198 1:CAS:528:DyaK1MXmt1Sgsbs%3D 10.1016/S0378-5173(99)00185-4 10502625 (Pubitemid 29443899)
16. C. Leuner J. Dressman 2000 Improving drug solubility for oral delivery using solid dispersions Eur. J. Pharm. Biopharm. 50 47 60 1:CAS:528: DC%2BD3cXjslyju7c%3D 10.1016/S0939-6411(00)00076-X 10840192 (Pubitemid 30326688)
17. D. X. Li Y. K. Oh S. J. Lim J. O. Kim H. J. Yang J. H. Sung C. S. Yong H. G. Choi 2008 Novel gelatin microcapsule with bioavailability enhancement of ibuprofen using spray drying technique Int. J. Pharm. 355 277 284 1:CAS:528:DC%2BD1cXkt1ygs7c%3D 10.1016/j.ijpharm.2007.12.020 18243606
18. D. A. Miller J. T. McConville W. Yang R. O. Williams 3rd J. W. McGinity 2007 Hot-melt extrusion for enhanced delivery of drug particles J. Pharm. Sci. 96 361 376 1:CAS:528:DC%2BD2sXhsFGmtbw%3D 10.1002/jps.20806 17075869 (Pubitemid 46363567)
19. M. Newa K. H. Bhandari D. X. Li T. H. Kwon J. A. Kim B. K. Yoo J. S. Woo W. S. Lyoo C. S. Yong H. G. Choi 2007 Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188 Int. J. Pharm. 343 228 237 1:CAS:528:DC%2BD2sXpsl2iur8%3D 10.1016/j.ijpharm.2007.05.031 17597315 (Pubitemid 47321028)
20. M. Newa K. H. Bhandari D. X. Li J. O. Kim D. S. Yoo J. A. Kim B. K. Yoo J. S. Woo W. S. Lyoo C. S. Yong H. G. Choi 2008 Preparation and evaluation of immediate release ibuprofen solid dispersions using polyethylene glycol 4000 Biol. Pharm. Bull. 31 939 945 1:CAS:528:DC%2BD1cXotF2mt7g%3D 10.1248/bpb.31.939 18451523 (Pubitemid 351732002)
21. K. Okimoto M. Miyake R. Ibuki M. Yasumura N. Ohnishi T. Nakai 1997 Dissolution mechanism and rate of solid dispersion particles of nilvadipine with hydroxypropyl-methylcellulose Int. J. Pharm. 159 85 93 1:CAS:528: DyaK2sXnvFSgtLo%3D 10.1016/S0378-5173(97)00274-3 (Pubitemid 28062813)
22. K. A. Overhoff A. Moreno D. A. Miller K. P. Johnston R. O. Williams III 2007 Solid dispersions of itraconazole and enteric polymers made by ultra-rapid freezing Int. J. Pharm. 336 122 132 1:CAS:528:DC%2BD2sXktFOmt7c%3D 10.1016/j.ijpharm.2006.11.043 17184938 (Pubitemid 46551563)
23. Society of Toxicology (SOT), Guilding Priciples in the Use of Animals in Toxicology, www.toxicology.org/AI/FA/guidingprinciples.pdf. (2008).
24. M. H. Sung J. S. Kim W. S. Kim I. Hirasawa 2002 Modification of crystal growth mechanism of yttrium oxalate in metastable solution J. Cryst. Growth 235 529 540 1:CAS:528:DC%2BD38XmsFejtg%3D%3D 10.1016/S0022-0248(01)01837-1 (Pubitemid 34070406)
25. L. S. Taylor G. Zografi 1997 Spectroscopic characterization interactions between PVP and indomethacin in amorphous molecular dispersions Pharm. Res. 14 1691 1698 1:CAS:528:DyaK1cXktFKjtQ%3D%3D 10.1023/A:1012167410376 9453055 (Pubitemid 28062912)
26. R. Vandecruys J. Peeters G. Verreck M. E. Brewster 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. 342 168 175 1:CAS:528:DC%2BD2sXptFymtrk%3D 10.1016/j.ijpharm.2007.05.006 17573214 (Pubitemid 47259339)
27. V. Venkateswarlu K. Manjunath 2004 Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles J. Control. Release 95 627 638 1:CAS:528:DC%2BD2cXitVKgtLw%3D 10.1016/j.jconrel.2004.01.005 15023472 (Pubitemid 38344153)
28. S. Walser R. Hruby E. Hesse H. Heinzl H. Mascher 1997 Preliminary toxicokinetic study with different crystal forms of S (+)-ibuprofen (dexibuprofen) and R,S-ibuprofen in rats Arzneimittelforschung 47 750 754 1:CAS:528:DyaK2sXktlGnsb8%3D 9239454
29. M. F. Wempe V. J. Wacher K. M. Ruble M. G. Ramsey K. J. Edgar N. L. Buchanan C. M. Buchanan 2008 Pharmacokinetics of raloxifene in male Wistar-Hannover rats: influence of complexation with hydroxybutenyl-beta- cyclodextrin Int. J. Pharm. 346 25 37 1:CAS:528:DC%2BD2sXhtlWmsLbK 10.1016/j.ijpharm.2007.06.002 17644287 (Pubitemid 350110509)
30. L. Willems R. Van Der Geest K. De Beule 2001 Itraconazole oral solution and intravenous formulations: A review of pharmacokinetics and pharmacodynamics J. Clin. Pharm. Ther. 26 159 169 1:CAS:528:DC%2BD3MXlt1yksbw%3D 10.1046/j.1365-2710.2001.00338.x 11422598 (Pubitemid 32592545)
31. K. Yamashita T. Nakate K. Okimoto A. Ohike Y. Tokunaga R. Ibuki K. Higaki T. Kimura 2003 Establishment of new preparation method for solid dispersion formulation of tacrolimus Int. J. Pharm. 267 79 91 1:CAS:528: DC%2BD3sXosFOqtLw%3D 10.1016/j.ijpharm.2003.07.010 14602386 (Pubitemid 37352952)
32. Y. Yi H. J. Yoon B. O. Kim M. Shim S. O. Kim S. J. Hwang M. H. Seo 2007 A mixed polymeric micellar formulation of itraconazole: Characteristics, toxicity and pharmacokinetics J. Control. Release 117 59 67 1:CAS:528: DC%2BD2sXht1Cmsr4%3D 10.1016/j.jconrel.2006.10.001 17097755 (Pubitemid 46161866)
33. C. S. Yong C. H. Yang J. D. Rhee B. J. Lee D. C. Kim D. D. Kim C. K. Kim J. S. Choi H. G. Choi 2004 Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol Int. J. Pharm. 269 169 176 1:CAS:528: DC%2BD3sXpvFektL8%3D 10.1016/j.ijpharm.2003.09.013 14698588 (Pubitemid 38032832)
34. C. S. Yong D. X. Li D. H. Oh J. A. Kim B. K. Yoo J. S. Woo J. D. Rhee H. G. Choi 2006 Retarded dissolution of ibuprofen in gelatin microcapsule by cross-linking with glutaradehyde Arch. Pharm. Res. 29 520 524 1:CAS:528:DC%2BD28XntFGmsrs%3D 10.1007/BF02969427 16833022
35. S. D. Yoo S. H. Lee E. Kang H. Jun J. Y. Jung J. W. Park K. H. Lee 2000 Bioavailability of itraconazole in rats and rabbits after administration of tablets containing solid dispersion particles Drug Dev. Ind. Pharm. 26 27 34 1:CAS:528:DC%2BD3cXhtVSqtr8%3D 10.1081/DDC-100100324 10677807 (Pubitemid 30075299)