Dissolution enhancement of the anti-HIV drug UC 781 by formulation in a ternary solid dispersion with TPGS 1000 and Eudragit E100

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 70, Issue 3, 2008, Pages 861-868

  Goddeeris, C ^a   Willems, T ^a   Houthoofd, K ^a   Martens, J A ^a   Van den Mooter, G ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Dissolution; Drug carrier interaction; Powder properties; Solid dispersions

Indexed keywords

ALPHA TOCOPHEROL; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; DEXTRO ALPHA TOCOPHERYL POLYETHYLENE GLYCOL SUCCINATE 1000; EUDRAGIT; HYDROXYPROPYLMETHYLCELLULOSE; KOLLICOAT IR; MACROGOL; MACROGOL 6000; METHYL GROUP; N [4 CHLORO 3 (3 METHYL 2 BUTENYLOXY)PHENYL] 2 METHYL 3 FURANCARBOTHIOAMIDE; POLOXAMER; POLYETHYLENE GLYCOL 100000; POLYMER; POLYVINYLPYRROLIDONE CO VINYLACETATE 64; POVIDONE; SURFACTANT; UNCLASSIFIED DRUG;

ARTICLE; DRUG RELEASE; DRUG SOLUBILITY; FLUID FLOW; GASTROINTESTINAL TRACT; POWDER; SIMULATION; SOLID STATE; X RAY DIFFRACTION;

ACRYLATES; ANILIDES; ANTI-HIV AGENTS; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; FURANS; KINETICS; POLYETHYLENE GLYCOLS; POLYMERS; POWDERS; SOLUBILITY; SURFACE-ACTIVE AGENTS; TECHNOLOGY, PHARMACEUTICAL; TRANSITION TEMPERATURE; VITAMIN E;

EID: 54949118684     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2008.07.006     Document Type: Article

References (20)

1. Balzarini J., Brouwer W.G., Dao D.C., Osika E.M., and De Clercq E. Identification of novel thiocarboxanilide derivatives that surpress a variety of drug-resistant mutant human immunodeficiency virus type 1 strains at a potency similar to that for wild-type virus. Antimicrob. Agents Chemother. 40 (1996) 1454-1466
2. Balzarini J., Naesens L., Verbeken E., Laga M., Van Damme L., Parniak M., van Mellaert L., Anné J., and De Clercq E. Preclinical studies on the thiocarboxanilide UC781 as a virucidal agent. AIDS 12 (1998) 1129-1138
3. Barnard J., Borkow G., and Parniak M.A. The thiocarboxanilide non-nucleoside UC781 is a thight-binding inhibitor of HIV-1 reverse transcriptase. Biochemistry 36 (1997) 7786-7792
4. Borkow G., Barnard J., Belmonte A., Nguyen T.M., Wainberg M.A., and Parniak M.A. Chemical barriers to human immunodeficiency virus type 1 (HIV-1) infection: retrovirucidal activity of UC781, a thiocarboxanilide non-nucleoside inhibitor of HIV-1 reverse transcriptase. J. Virol. 71 (1997) 3023-3030
5. Damian F., Blaton N., Desseyn H., Clou K., Augustijns P., Naesens L., Balzarini J., Kinget R., and Van den Mooter G. Solid state properties of pure UC781 and solid dispersions with polyvinylpyrrolidone (PVPK30). J. Pharm. Pharmacol. 53 (2001) 1109-1116
6. Amidon G.L., Lennernäs H., Shah V.P., and Crison J.R. Theoretical basis for a biopharmaceutical drug classification: the correlation of in vivo drug product dissolution and in vivo bioavailability. Pharm. Res. 12 (1995) 413-420
7. Liu R. Water-insoluble Drug Formulation (2000), Interpharm Press, Denver, Colorado
8. Stupak E.I., and Bates T.R. Enhanced absorption and dissolution of reserpine-polyvinylpyrrolidone coprecipitates. J Pharm. Sci. 61 (1972) 400-404
9. Stupak E.I., and Bates T.R. Enhanced absorption of digitoxin from orally administered digitoxin-polyvonylpyrrolidone coprecipitates. J. Pharm. Sci. 62 (1973) 1806-1809
10. Chiou W.L., and Riegelmans S. Pharmaceutical applications of solid dispersion systems. J. Pharm. Sci. 60 (1971) 1281-1302
11. Ford J.L. The current status of solid dispersions. Pharm. Acta Helv. 61 (1986) 69-88
12. Ozeki T., Yuasa H., and Kanaya Y. Application of the solid dispersion method to the controlled release of medicine. IX. Difference in the release of flurbiprofen from solid dispersions with poly(ethylene oxide) and hydroxypropylcellulose and the interaction between medicine and polymers. Int. J. Pharm. 115 (1997) 209-217
13. Sekigushi K., and Obi N. Studies on absorption of eutectic mixtures. I. A comparison of the behavior of eutectic mixture of sulfathiazole and that of ordinary sulfathiazole in man. Chem. Pharm. Bull. 9 (1961) 866-872
14. Hancock B.C., and Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J. Pharm. Sci. 86 (1997) 1-12
15. Shin S.-C., and Kim J. Physicochemical characterisation of solid dispersion of furosemide with TPGS. Int. J. Pharm. 251 (2003) 79-84
16. Khoo S.-M., Porter C., and Charman W. The formulation of Halofantrine as either non-solubilising PEG 6000 or solubilising lipid based solid dispersions: physical stability and absolute bioavailability assessment. Int. J. Pharm. 205 (2000) 65-78
17. S. Janssens, S. Nagels, H. Novoa de Armas, W. D'Autry, A. Van Schepdael, G. Van den Mooter, Formulation and characterization of ternary solid dispersions made up of itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study, Eur. J. Pharm. Biopharm, doi: 10.1016/j.ejpb.2007.11.04.
18. Six K., Leuner Ch., Dressman J., Verreck G., Peeters J., Blaton N., Augustijns P., Kinget R., and Van den Mooter G. Thermal properties of hot-stage extrudates of itraconazole and eudragit E100. J. Therm. Anal. Cal. 68 (2002) 591-601
19. Van den Mooter G., Wuyts M., Blaton N., Busson R., Grobet P., Augustijns P., and Kinget R. Physical stabilisation of amorphous ketconazole in solid dispersions with polyvinylpyrrolidone K25. Eur. J. Pharm. Sc. 12 (2001) 261-269
20. Guyot M., Fawaz F., Bildet J., Bonini F., and Lagueny A.M. Physicochemical characterization and dissolution of norfloxacin/cyclodextrin inclusion compounds and PEG solid dispersions. Int. J. Pharm. 123 (1995) 53-63