Physicochemical properties and oral bioavailability of amorphous atorvastatin hemi-calcium using spray-drying and SAS process

International Journal of Pharmaceutics

Volumn 359, Issue 1-2, 2008, Pages 211-219

  Kim, Jeong Soo ^a   Kim, Min Soo ^a   Park, Hee Jun ^a   Jin, Shun Ji ^a   Lee, Sibeum ^a   Hwang, Sung Joo ^a  

^a Chungnam National University   (South Korea)

Author keywords

Amorphous; Atorvastatin; Bioavailability; SAS process; Spray drying

Indexed keywords

ACETONE; ATORVASTATIN; CALCIUM; CRYSTALLIN; TETRAHYDROFURAN;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; DISSOLUTION; DRUG BIOAVAILABILITY; DRUG DOSAGE FORM COMPARISON; MALE; NONHUMAN; PARTICLE SIZE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RAT; SOLUBILITY; SPRAY DRYING;

ACETONE; ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CRYSTALLIZATION; FURANS; HEPTANOIC ACIDS; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; MALE; PARTICLE SIZE; PYRROLES; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; SOLVENTS;

EID: 44749087764     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2008.04.006     Document Type: Article

References (40)

1. Al-Marzouqi A., Shehatta I., Jobe B., and Dowaidar A. Phase solubility and inclusion complex of itraconazole with beta-cyclodextrin. J. Pharm. Sci. 95 (2006) 292-304
2. Anzai K., Mizoguchi J., Yanagi T., Hirayama F., Arima H., and Uekama K. Improvement of dissolution properties of a new Helicobacter pylori eradicating agent (TG44) by inclusion complexation with beta-cyclodextrin. Chem. Pharm. Bull. (Tokyo) 55 (2007) 1466-1470
3. Brittain H. Physical Characterization of Pharmaceutical Solids (1995), Marcel Dekker, New York
4. Chawla G., and Bansal A. A comparative assessment of solubility advantage from glassy and crystalline forms of a water-insoluble drug. Eur. J. Pharm. Sci. 32 (2007) 45-57
5. Chen Y., Zhang G., Neilly J., Marsh K., Mawhinney D., and Sanzgiri Y. Enhancing the bioavailability of ABT-963 using solid dispersion containing Pluronic F-68. Int. J. Pharm. 286 (2004) 69-80
6. Choi W.S., Kim H.I., Kwak S.S., Chung H.Y., Chung H.Y., Yamamoto K., Oguchi T., Tozuka Y., Yonemochi E., and Terada K. Amorphous ultrafine particle preparation for improvement of bioavailability of insoluble drugs: grinding characteristics of fine grinding mills. Int. J. Miner. Process. 74 (2004) S165-S172
7. Corsini A., Bellosta S., Baetta R., Fumagalli R., Paoletti R., and Bernini F. New insights into the pharmacodynamic and pharmacokinetic properties of statins. Pharmacol. Ther. 84 (1999) 413-428
8. Di Martino P., Barthelemy C., Palmieri G., and Martelli S. Physical characterization of naproxen sodium hydrate and anhydrate forms. Eur. J. Pharm. Sci. 14 (2001) 293-300
9. Elamin A.A., Ahlneck C., Alderborn G., and Nystrom C. Increased metastable solubility of milled griseofulvin, depending on the formation of a disordered surface structure. Int. J. Pharm. 111 (1994) 159-170
10. Engel G., Farid N., Faul M., Richardson L., and Winneroski L. Salt form selection and characterization of LY333531 mesylate monohydrate. Int. J. Pharm. 198 (2000) 239-247
11. Farinha A., Bica A., and Tavares P. Improved bioavailability of a micronized megestrol acetate tablet formulation in humans. Drug Dev. Ind. Pharm. 26 (2000) 567-570
12. Grau M.J., Kayser O., and Muller R.H. Nanosuspensions of poorly soluble drugs-reproducibility of small scale production. Int. J. Pharm. 196 (2000) 155-159
13. Han H.-K., and Choi H.-K. Improved absorption of meloxicam via salt formation with ethanolamines. Eur. J. Pharm. Biopharm. 65 (2007) 99-103
14. Hancock B., and Parks M. What is the true solubility advantage for amorphous pharmaceuticals?. Pharm. Res. 17 (2000) 397-404
15. Hancock B.C., and Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J. Pharm. Sci. 86 (1997) 1-12
16. Hermann M., Christensen H., and Reubsaet J. Determination of atorvastatin and metabolites in human plasma with solid-phase extraction followed by LC-tandem MS. Anal. Bioanal. Chem. 382 (2005) 1242-1249
17. Imaizumi H. Stability and several physical properties of amorphous and crystalline forms of indomethacin. Chem. Pharm. Bull. (Tokyo) 29 (1980) 983-987
18. Jun S., Kim M., Kim J., Park H., Lee S., Woo J., and Hwang S. Preparation and characterization of simvastatin/hydroxypropyl-beta-cyclodextrin inclusion complex using supercritical antisolvent (SAS) process. Eur. J. Pharm. Biopharm. 66 (2007) 413-421
19. Kaplan S.A. Biopharmaceutical considerations in drug formulation design and evaluation. Drug Metab. Rev. 1 (1972) 15-34
20. Khankari R.K., and Grant D.J.W. Pharmaceutical hydrates. Thermochim. Acta 248 (1995) 61-79
21. Kim M.-S., Lee S., Park J.-S., Woo J.-S., and Hwang S.-J. Micronization of cilostazol using supercritical antisolvent (SAS) process: effect of process parameters. Powder Technol. 177 (2007) 64-70
22. Kim M.-S., Jin S.-J., Kim J.-S., Park H.J., Song H.-S., Neubertb R.H.H., and Hwang S.-J. Preparation, characterization and in vivo evaluation of amorphous atorvastatin calcium nanoparticles using supercritical antisolvent (SAS) process. Eur. J. Pharm. Biopharm. (2007)
23. Lee L.Y., Wang C.H., and Smith K.A. Supercritical antisolvent production of biodegradable micro- and nanoparticles for controlled delivery of paclitaxel. J. Control. Release 125 (2008) 96-106
24. Lennernas H. Human jejunal effective permeability and its correlation with preclinical drug absorption models. J. Pharm. Pharmacol. 49 (1997) 627-638
25. Lennernas H. Clinical pharmacokinetics of atorvastatin. Clin. Pharmacokinet. 42 (2003) 1141-1160
26. Lipinski C., Lombardo F., Dominy B., and Feeney P. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 46 (2001) 3-26
27. Marco I.D., and Reverchon E. Supercritical antisolvent micronization of cyclodextrins. Powder Technol. 183 (2008) 239-246
28. Mullins J., and Macek T. Some pharmaceutical properties of novobiocin. J. Am. Pharm. Assoc. 49 (1960) 245-248
29. Nirogi R., Kandikere V., Shukla M., Mudigonda K., Maurya S., Boosi R., and Anjaneyulu Y. Simultaneous quantification of atorvastatin and active metabolites in human plasma by liquid chromatography-tandem mass spectrometry using rosuvastatin as internal standard. Biomed. Chromatogr. 20 (2006) 924-936
30. Paradkar A., Ambike A., Jadhav B., and Mahadik K. Characterization of curcumin-PVP solid dispersion obtained by spray drying. Int. J. Pharm. 271 (2004) 281-286
31. Park M., Ren S., and Lee B. 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 (2007) 199-207
32. Perng C., Kearney A., Palepu N., Smith B., and Azzarano L. Assessment of oral bioavailability enhancing approaches for SB-247083 using flow-through cell dissolution testing as one of the screens. Int. J. Pharm. 250 (2003) 147-156
33. Reverchon E., and Porta G.D. Production of antibiotic micro- and nano-particles by supercritical antisolvent precipitation. Powder Technol. 106 (1999) 23-29
34. Sato T., Okada A., Sekiguchi K., and Tsuda Y. Difference in physico-pharmaceutical properties between crystalline and non-crystalline 9,3″-diacetylmidecamycin. Chem. Pharm. Bull. (Tokyo) 29 (1981) 2675-2682
35. 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
36. Shen H., and Zhong M. Preparation and evaluation of self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin. J. Pharm. Pharmacol. 58 (2006) 1183-1191
37. Snavely W.K., Subramaniam B., Rajewski R.A., and Defelippis M.R. Micronization of insulin from halogenated alcohol solution using supercritical carbon dioxide as an antisolvent. J. Pharm. Sci. 91 (2002) 2026-2039
38. Taylor L., and Zografi G. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm. Res. 14 (1997) 1691-1698
39. Vaughn J., McConville J., Crisp M., Johnston K., and Williams III R. 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 (2006) 559-567
40. Wu X., Whitfield L.R., and Stewart B.H. Atorvastatin transport in the Caco-2 Cell Model: contributions of P-glycoprotein and the proton-monocarboxylic acid co-transporter. Pharm. Res. 17 (2000) 209-215