Oral bioavailability of ketoprofen in suspension and solution formulations in rats: The influence of poloxamer 188

Journal of Pharmacy and Pharmacology

Volumn 64, Issue 11, 2012, Pages 1631-1637

  Fischer, Sarah Maud ^a,b   Parmentier, Johannes ^b   Buckley, Stephen Timothy ^a   Reimold, Isolde ^b   Brandl, Martin ^a   Fricker, Gert ^b  

^a UNIVERSITY OF SOUTHERN DENMARK   (Denmark)

^b UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

ketoprofen; oral bioavailability; pluronic; poorly soluble drug; solubilisation

Indexed keywords

BUFFER; KETOPROFEN; LUTROL F 68; P 188; POLOXAMER; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG SOLUBILITY; DRUG SOLUTION; IN VIVO STUDY; INTESTINE FLUID; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT; SUSPENSION; WISTAR RAT;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; EXCIPIENTS; HUMANS; INTESTINAL SECRETIONS; KETOPROFEN; MALE; POLOXAMER; RATS; RATS, WISTAR; SOLUBILITY;

EID: 84867582563     PISSN: 00223573     EISSN: 20427158     Source Type: Journal    
DOI: 10.1111/j.2042-7158.2012.01541.x     Document Type: Article

References (35)

1. Lipinski CA, et al,. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 2001; 46: 3-26.
2. Friesen DT, et al,. Hydroxypropyl methylcellulose acetate succinate-based spray-dried dispersions: an overview. Mol Pharm 2008; 5: 1003-1019.
3. Davis ME, Brewster ME,. Cyclodextrin-based pharmaceutics: past, present and future. Nat Rev Drug Discov 2004; 3: 1023-1035.
4. Merisko-Liversidge EM, Liversidge GG,. Drug nanoparticles: formulating poorly water-soluble compounds. Toxicol Pathol 2008; 36: 43-48.
5. Pouton CW,. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur J Pharm Sci 2000; 11 (Suppl. 2): S93-S98.
6. Serajuddin AT,. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J Pharm Sci 1999; 88: 1058-1066.
7. Serajuddin AT,. Salt formation to improve drug solubility. Adv Drug Deliv Rev 2007; 59: 603-616.
8. Torchilin VP,. Micellar nanocarriers: pharmaceutical perspectives. Pharm Res 2007; 24: 1-16.
9. Amidon GL, et al,. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995; 12: 413-420.
10. Vasconcelos T, et al,. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today 2007; 12: 1068-1075.
11. Barakat NS,. Enhanced oral bioavailability of etodolac by self-emulsifying systems: in-vitro and in-vivo evaluation. J Pharm Pharmacol 2010; 62: 173-180.
12. Tonsberg H, et al,. Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats. J Pharm Pharmacol 2010; 62: 63-70.
13. Yang SG,. Biowaiver extension potential and IVIVC for BCS Class II drugs by formulation design: case study for cyclosporine self-microemulsifying formulation. Arch Pharm Res 2010; 33: 1835-1842.
14. Suzuki Y, et al,. The effects of emulsifying agents on disposition of lipid-soluble drugs included in fat emulsion. Drug Metab Pharmacokinet 2004; 19: 62-67.
15. Mudra DR, Borchardt RT,. Absorption barriers in the rat intestinal mucosa. 3: effects of polyethoxylated solubilizing agents on drug permeation and metabolism. J Pharm Sci 2010; 99: 1016-1027.
16. Nerurkar MM, et al,. Mechanistic roles of neutral surfactants on concurrent polarized and passive membrane transport of a model peptide in Caco-2 cells. J Pharm Sci 1997; 86: 813-821.
17. Katneni K, et al,. Permeability assessment of poorly water-soluble compounds under solubilizing conditions: the reciprocal permeability approach. J Pharm Sci 2006; 95: 2170-2185.
18. Fischer SM, et al,. In-vitro permeability of poorly water soluble drugs in the phospholipid vesicle-based permeation assay: the influence of nonionic surfactants. J Pharm Pharmacol 2011; 63: 1022-1030.
19. Fischer SM, et al,. Effect of the non-ionic surfactant Poloxamer 188 on passive permeability of poorly soluble drugs across Caco-2 cell monolayers. Eur J Pharm Biopharm 2011; 79: 416-422.
20. Miller JM, et al,. The solubility-permeability interplay: mechanistic modeling and predictive application of the impact of micellar solubilization on intestinal permeation. Mol Pharm 2011; 8: 1848-1856.
21. Di L, et al,. High throughput artificial membrane permeability assay for blood-brain barrier. Eur J Med Chem 2003; 38: 223-232.
22. Albalak A, et al,. Effects of submicellar bile salt concentrations on biological membrane permeability to low molecular weight non-ionic solutes. Biochemistry 1996; 35: 7936-7945.
23. Delbarre F, et al,. Pharmacokinetic study of ketoprofen (19.583 R.P.) in man using the tritiated compound. Scand J Rheumatol Suppl 1976; 1976: 45-52.
24. Ishizaki T, et al,. Pharmacokinetics of ketoprofen following single oral, intramuscular and rectal doses and after repeated oral administration. Eur J Clin Pharmacol 1980; 18: 407-414.
25. Sigfridsson K, et al,. Particle size reduction for improvement of oral absorption of the poorly soluble drug UG558 in rats during early development. Drug Dev Ind Pharm 2009; 35: 1479-1486.
26. Sigfridsson K, et al,. Particle size reduction and pharmacokinetic evaluation of a poorly soluble acid and a poorly soluble base during early development. Drug Dev Ind Pharm 2011; 37: 243-251.
27. Butler JM, Dressman JB,. The developability classification system: application of biopharmaceutics concepts to formulation development. J Pharm Sci 2010; 99: 4940-4954.
28. Dahan A, Hoffman A,. The effect of different lipid based formulations on the oral absorption of lipophilic drugs: the ability of in vitro lipolysis and consecutive ex vivo intestinal permeability data to predict in vivo bioavailability in rats. Eur J Pharm Biopharm 2007; 67: 96-105.
29. Bhattachar SN, et al,. Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus, simulations to predict absorption. J Pharm Sci 2011; 100: 4756-4765.
30. Shaik N, et al,. Interactions of pluronic block copolymers on P-gp efflux activity: experience with HIV-1 protease inhibitors. J Pharm Sci 2008; 97: 5421-5433.
31. Poelma FG, et al,. Intestinal absorption of drugs. The influence of mixed micelles on on the disappearance kinetics of drugs from the small intestine of the rat. J Pharm Pharmacol 1991; 43: 317-324.
32. Behrens I, et al,. Transport of lipophilic drug molecules in a new mucus-secreting cell culture model based on HT29-MTX cells. Pharm Res 2001; 18: 1138-1145.
33. Choi JS, et al,. Role of monocarboxylic acid transporters in the cellular uptake of NSAIDs. J Pharm Pharmacol 2005; 57: 1185-1189.
34. Legen I, et al,. Polarised transport of monocarboxylic acid type drugs across rat jejunum in vitro: the effect of mucolysis and ATP-depletion. Int J Pharm 2003; 256: 161-166.
35. Legen I, Kristl A,. pH and energy dependent transport of ketoprofen across rat jejunum in vitro. Eur J Pharm Biopharm 2003; 56: 87-94.