Bioavailability of probucol from lipid and surfactant based formulations in minipigs: Influence of droplet size and dietary state

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 69, Issue 2, 2008, Pages 553-562

  Nielsen, Flemming Seier ^a   Petersen, Kamilla Buchberg ^a   Müllertz, Anette ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Bioavailability; Emulsion nanoemulsion; Food interactions; Oral absorption; Self emulsifying drug delivery system (SEDDS); Surfactants

Indexed keywords

FAT; LIPID; OIL; PROBUCOL; SURFACTANT; WATER;

ANIMAL EXPERIMENT; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; DIET; DIET RESTRICTION; DIGESTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG FORMULATION; EMULSION; ENERGY; FEEDING; FOOD; HUMAN; HUMAN CELL; MALE; MEAL; MINIPIG; NONHUMAN; PARTICLE SIZE;

ANIMALS; ANTICHOLESTEREMIC AGENTS; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; CHEMISTRY, PHARMACEUTICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DIET; DIETARY FATS; EMULSIONS; FASTING; HUMANS; INJECTIONS, INTRAVENOUS; LIPIDS; P-GLYCOPROTEIN; PARTICLE SIZE; POWDERS; PROBUCOL; SURFACE-ACTIVE AGENTS; SWINE; SWINE, MINIATURE;

EID: 43249122851     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2007.12.020     Document Type: Article

References (38)

1. Porter C.J., and Charman W.N. In vitro assessment of oral lipid based formulations. Adv. Drug Deliv. Rev. 50 Suppl. 1 (2001) S127-S147
2. Pouton C.W. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur. J. Pharm. Sci. 11 Suppl. 2 (2000) S93-S98
3. Drewe J., Meier R., Vonderscher J., Kiss D., Posanski U., Kissel T., and Gyr K. Enhancement of the oral absorption of cyclosporin in man. Br. J. Clin. Pharmacol. 34 (1992) 60-64
4. Kovarik J.M., Mueller E.A., van Bree J.B., Tetzloff W., and Kutz K. Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation. J. Pharm. Sci. 83 (1994) 444-446
5. Gao Z.G., Choi H.G., Shin H.J., Park K.M., Lim S.J., Hwang K.J., and Kim C.K. Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosporin A. Int. J. Pharm. 161 (1998) 75-86
6. Odeberg J.M., Kaufmann P., Kroon K.G., and Hoglund P. Lipid drug delivery and rational formulation design for lipophilic drugs with low oral bioavailability, applied to cyclosporine. Eur. J. Pharm. Sci. 20 (2003) 375-382
7. Charman W.N. Lipids, lipophilic drugs, and oral drug delivery - some emerging concepts. J. Pharm. Sci. 89 (2000) 967-978
8. Gershanik T., and Benita S. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur. J. Pharm. Biopharm. 50 (2000) 179-188
9. de Smidt P.C., Campanero M.A., and Troconiz I.F. Intestinal absorption of penclomedine from lipid vehicles in the conscious rat: contribution of emulsification versus digestibility. Int. J. Pharm. 270 (2004) 109-118
10. Khossravi M., Kao Y.H., Mrsny R.J., and Sweeney T.D. Analysis methods of polysorbate 20: a new method to assess the stability of polysorbate 20 and established methods that may overlook degraded polysorbate 20. Pharm. Res. 19 (2002) 634-639
11. Seeballuck F., Lawless E., Ashford M.B., and O'Driscoll C.M. Stimulation of triglyceride-rich lipoprotein secretion by polysorbate 80: in vitro and in vivo correlation using Caco-2 cells and a cannulated rat intestinal lymphatic model. Pharm. Res. 21 (2004) 2320-2326
12. Porter C.J., Kaukonen A.M., Boyd B.J., Edwards G.A., and Charman W.N. Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation. Pharm. Res. 21 (2004) 1405-1412
13. Cornaire G., Woodley J., Hermann P., Cloarec A., Arellano C., and Houin G. Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo. Int. J. Pharm. 278 (2004) 119-131
14. Gursoy R.N., and Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed. Pharmacother. 58 (2004) 173-182
15. Schmidt L.E., and Dalhoff K. Food-drug interactions. Drugs 62 (2002) 1481-1502
16. Yagi N., Terashima Y., Kenmotsu H., Sekikawa H., and Takada M. Dissolution behavior of probucol from solid dispersion systems of probucol-polyvinylpyrrolidone. Chem. Pharm. Bull. (Tokyo) 44 (1996) 241-244
17. Nielsen F.S., Gibault E., Ljusberg-Wahren H., Arleth L., Pedersen J.S., and Mullertz A. Characterization of prototype self-nanoemulsifying formulations of lipophilic compounds. J. Pharm. Sci. 96 (2007) 876-892
18. Karpf D.M., Holm R., Kristensen H.G., and Mullertz A. Influence of the type of surfactant and the degree of dispersion on the lymphatic transport of halofantrine in conscious rats. Pharm. Res. 21 (2004) 1413-1418
19. Center for Drug Evaluation and Research (CDER), Guidance for Industry, Food-Effect Bioavailability and Fed Bioequivalence Studies, 2002.
20. Nourooz-Zadeh J., Gopaul N.K., Forster L.A., Ferns G.A., and Anggard E.E. Measurement of plasma probucol levels by high-performance liquid chromatography. J. Chromatogr. B. Biomed. Appl. 654 (1994) 55-60
21. Nielsen C.U., Amstrup J., Steffansen B., Frokjaer S., and Brodin B. Epidermal growth factor inhibits glycylsarcosine transport and hPepT1 expression in a human intestinal cell line. Am. J. Physiol. Gastrointest. Liver Physiol. 281 (2001) G191-G199
22. Palin K.J., and Wilson C.G. The effect of different oils on the absorption of probucol in the rat. J. Pharm. Pharmacol. 36 (1984) 641-643
23. de Campo L., Yaghmur A., Garti N., Leser M.E., Folmer B., and Glatter O. Five-component food-grade microemulsions: structural characterization by SANS. J. Colloid Interface Sci. 274 (2004) 251-267
24. Kokue E., Shimoda M., Sakurada K., and Wada J. Pharmacokinetics of oral sulfa drugs and gastric emptying in the pig. J. Pharmacobiodyn. 11 (1988) 549-554
25. Witkamp R.F., and Monshouwer M. Pharmacokinetics in vivo and in vitro in swine. Scand. J. Lab. Anim. Sci. 25 (1998) 45-56
26. Davis S.S., Illum L., and Hinchcliffe M. Gastrointestinal transit of dosage forms in the pig. J. Pharm. Pharmacol. 53 (2001) 33-39
27. Khoo S.M., Humberstone A.J., Porter C.J.H., Edwards G.A., and Charman W.N. Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int. J. Pharm. 167 (1998) 155-164
28. Holm R., Porter C.J., Edwards G.A., Mullertz A., Kristensen H.G., and Charman W.N. Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides. Eur. J. Pharm. Sci. 20 (2003) 91-97
29. Malingre M.M., Schellens J.H., van Tellingen O., Ouwehand M., Bardelmeijer H.A., Rosing H., Koopman F.J., Schot M.E., Bokkel Huinink W.W., and Beijnen J.H. The co-solvent Cremophor EL limits absorption of orally administered paclitaxel in cancer patients. Br. J. Cancer 85 (2001) 1472-1477
30. Bardelmeijer H.A., Ouwehand M., Malingre M.M., Schellens J.H., Beijnen J.H., and van Tellingen O. Entrapment by Cremophor EL decreases the absorption of paclitaxel from the gut. Cancer Chemother. Pharmacol. 49 (2002) 119-125
31. Gonzalez-Llaven J., Palma-Aguirre J.A., Garcia-Arreola R., Brizuela V., Nava-Rangel J., Moran-Lira S., Vela-Ojeda J., Castaneda-Hernandez G., and Flores-Murrieta F.J. Comparative bioavailability evaluation of two cyclosporine oral formulations in healthy Mexican volunteers. Arch. Med. Res. 30 (1999) 315-319
32. Klyashchitsky B.A., and Owen A.J. Drug delivery systems for cyclosporine: achievements and complications. J. Drug Target 5 (1998) 443-458
33. Mueller E.A., Kovarik J.M., van Bree J.B., Grevel J., Lucker P.W., and Kutz K. Influence of a fat-rich meal on the pharmacokinetics of a new oral formulation of cyclosporine in a crossover comparison with the market formulation. Pharm. Res. 11 (1994) 151-155
34. Kawakami K., Yoshikawa T., Hayashi T., Nishihara Y., and Masuda K. Microemulsion formulation for enhanced absorption of poorly soluble drugs. II. In vivo study. J. Control. Release 81 (2002) 75-82
35. Wagner D., Spahn-Langguth H., Hanafy A., Koggel A., and Langguth P. Intestinal drug efflux: formulation and food effects. Adv. Drug Deliv. Rev. 50 Suppl. 1 (2001) S13-S31
36. Shono Y., Nishihara H., Matsuda Y., Furukawa S., Okada N., Fujita T., and Yamamoto A. Modulation of intestinal P-glycoprotein function by cremophor EL and other surfactants by an in vitro diffusion chamber method using the isolated rat intestinal membranes. J. Pharm. Sci. 93 (2004) 877-885
37. Makhey V.D., Guo A., Norris D.A., Hu P., Yan J., and Sinko P.J. Characterization of the regional intestinal kinetics of drug efflux in rat and human intestine and in Caco-2 cells. Pharm. Res. 15 (1998) 1160-1167
38. Sugimoto K., Sudoh T., Tsuruoka S., Yamamoto Y., Maezono S., Watanabe Y., and Fujimura A. Effect of probucol on the oral bioavailability of cyclosporine A. Eur. J. Pharm. Sci. 22 (2004) 71-77