Bioavailability enhancement of an active substance by supercritical antisolvent precipitation

Journal of Supercritical Fluids

Volumn 40, Issue 1, 2007, Pages 101-110

  Majerik, Viktor ^a   Charbit, Gérard ^b   Badens, Elisabeth ^b   Horváth, Géza ^a   Szokonya, László ^a   Bosc, Nathalie ^c   Teillaud, Eric ^c  

^a UNIVERSITY OF PANNONIA   (Hungary)

^b CNRS   (France)

^c Merck Santé sas ^*  (France)

Author keywords

Bioavailability; Dissolution rate; Polymorphic purity; Poorly water soluble drug; Supercritical antisolvent

Indexed keywords

BLOCK COPOLYMERS; CRYSTALLIZATION; DISSOLUTION; MORPHOLOGY; POLYETHYLENE GLYCOLS; PRECIPITATION (CHEMICAL); SOLUBILITY; SOLVENTS;

BIOAVAILABILITY; DISSOLUTION RATE; OXEGLITAZAR; POLYMORPHIC PURITY; POLYOXYPROPYLENES; SUPERCRITICAL ANTISOLVENT (SAS); TETRAHYDROFURAN (THF);

DRUG PRODUCTS;

EID: 33845484838     PISSN: 08968446     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.supflu.2006.03.027     Document Type: Article

References (31)

1. Majerik V., Horváth G., Charbit G., Badens E., Szokonya L., Bosc N., and Teillaud E. Novel particle engineering techniques in drug delivery: review of formulations using supercritical fluids and liquefied gases. Hun. J. Ind. Chem. 32 (2004) 41-56
2. Vemavarapu C., Mollan M.J., Lodaya M., and Needhamb T.E. Design and process aspects of laboratory scale SCF particle formation systems. Int. J. Pharm. 292 (2005) 1-16
3. Charbit G., Badens E., and Boutin O. Methods of particle production. In: York P., Kompella U.B., and Shekunov B.Y. (Eds). Supercritical Fluid Technology for Drug Product Development, Drugs and Pharmaceutical Sciences vol. 138 (2004), Marcel Dekker Inc., New York
4. 2 and cryogenic spray-freezing technologies. Drug Dev. Ind. Pharm. 27 10 (2001) 1003-1015
5. Jung J., and Perrut M. Particle design using supercritical fluids: literature and patent survey. J. Supercrit. Fluids 20 (2001) 179-219
6. Hannay J.B., and Hoghart J. On the solubility of solids in gases. Proc. Roy. Sec. 29 (1879) 324
7. Türk M., Hils P., Helfgen B., Schaber K., Martin H.-J., and Wahl M.A. Micronization of pharmaceutical substances by rapid expansion of supercritical solutions (RESS): a promising method to improve bioavailability of poorly soluble pharmaceutical agents. J. Supercrit. Fluids 22 (2002) 75-84
8. Perrut M., Jung J., and Leboeuf F. Enhancement of dissolution rate of poorly soluble active ingredients by supercritical fluid processes. Part II. Preparation of composite particles. Int. J. Pharm. 288 (2005) 11-16
9. V.J. Krukonis, P.M. Gallagher, M.P. Coffey, US Patent 5,360,478 (1994).
10. Moneghini M., Kikic I., Voinovich D., Perissutti B., and Filipovic-Grcic J. Processing of carbamazepine-PEG 4000 solid dispersions with supercritical carbon dioxide: preparation, characterisation, and in vitro dissolution. Int. J. Pharm. 222 (2001) 129-138
11. Corrigan O.I., and Crean A.M. Comparative physicochemical properties of hydrocortisone-PVP composites prepared using supercritical carbon dioxide by the GAS anti-solvent recrystallization process, by coprecipitation and by spray drying. Int. J. Pharm. 245 (2002) 75-82
12. Debenedetti P.G., and Roberts C.J. Engineering pharmaceutical stability with amorphous solids. AIChE J. 48 6 (2002) 1140-1144
13. Falk R., Randolph T.W., Meyer J.D., Kelly R.M., and Manning M.C. Controlled release of ionic compounds from poly (l-lactide) microspheres produced by precipitation with a compressed antisolvent. J. Cont. Rel. 44 (1997) 77-85
14. Taki S., Badens E., and Charbit G. Controlled release system formed by supercritical anti-solvent coprecipitation of a herbicide and a biodegradable polymer. J. Supercrit. Fluids 21 (2001) 61-70
15. P. York, M. Hanna, Patent WO 95/01221 (1995).
16. P. York, S.E. Walker, S.A. Wilkins, R.A. Storey, R.S. Harland, Patent WO 01/15664 (2001).
17. Juppo A.M., Boissier C., and Khoo C. Evaluation of solid dispersion particles prepared with SEDS. Int. J. Pharm. 250 (2003) 385-401
18. Kerc J., Srcic S., Knez Z., and Sencar-Bozic P. Micronization of drugs using supercritical carbon dioxide. Int. J. Pharm. 182 (1999) 33-39
19. 2. Int. J. Pharm. 148 (1997) 123-130
20. York P., Beach S., Lathan D., Sidgwick C., and Hanna M. Control of the physical form of Salmeterol Xinafoate. Org. Proc. Res. Dev. 3 (1999) 370-376
21. 2. Proceedings of the European Conference on Drug Delivery and Pharmaceutical Technology. Sevilla, Spain, 10-12 May (2004) 46
22. Fargeot C., Badens E., Charbit G., Bosc N., Teillaud E., and Veesler S. Cristallisation d'un prinicipe actif: comparaison des méthodes par voie liquide et supercritique. Proceedings of the Cristal2. Toulouse, France, 12-13 November (2003) 55-60
23. Shieh Y.-T., Su J.-H., Manivannan G., Lee P.H.C., Sawan S.P.S., and Spall W.D. Interaction of supercritical carbon dioxide with polymers. II. Amorphous polymers. J. Appl. Polym. Sci. 59 (1996) 707-717
24. Forster A., Hempenstall J., Tucker I., and Rades T. Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis. Int. J. Pharm. 226 (2001) 147-161
25. Tajber L., Corrigan O.I., and Healy A.M. Physicochemical evaluation of PVP-thiazide diuretic interactions in co-spray-dried composites-analysis of glass transition composition relationships. Eur. J. Pharm. Sci. 24 (2005) 553-563
26. Reverchon E., Della Porta G., De Rosa I., Subra P., and Letourneur D. Supercritical antisolvent micronization of some biopolymers. J. Supercrit. Fluids 18 (2000) 239-245
27. Jung J., Clavier J.Y., and Perrut M. Gram to kilogram scale-up of supercritical Anti-solvent process. Proceedings of the Sixth International Symposium on Supercritical Fluids. Versailles, France, 28-30 April (2003)
28. Sethia S., and Squillante E. Solid dispersions of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods. Int. J. Pharm. 272 (2004) 1-10
29. FDA. International Conference on Harmonisation, ICH Guidance on Impurities: Residual Solvents. Federal Register 62 247 (1997) 67377-67388
30. Bitz C., and Doelker E. Influence of the preparation method on residual solvents in biodegradable microspheres. Int. J. Pharm. 131 (1996) 171-181
31. Ruchatz F., Kleinebudde P., and Müller B.W. Residual solvents in biodegradable microparticles. Influence of process parameters on the residual solvent in microparticles produced by the aerosol solvent extraction system (ASES) process. Int. J. Pharm. Sci. 86 (1997) 101-105