Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats

Journal of Pharmacy and Pharmacology

Volumn 62, Issue 1, 2010, Pages 63-70

  Tønsberg, Henrik ^a,b   Holm, René ^b   Boll, Jette Bisgaard ^b   Jacobsen, Jette ^a   Müllertz, Anette ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b H LUNDBECK A S   (Denmark)

Author keywords

Oral bioavailability; Polyethylene glycol 400; Polysorbate 80; Poorly watersoluble drugs

Indexed keywords

HALOFANTRINE; MACROGOL 400; POLYSORBATE 80;

ANIMAL EXPERIMENT; ARTICLE; BLOOD SAMPLING; CONTROLLED STUDY; DILUTION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG SOLUBILITY; IN VITRO STUDY; INTESTINE FLUID; MALE; NONHUMAN; PRECIPITATION; RAT; TAIL; VEIN PUNCTURE; VENOUS BLOOD;

EID: 77949523821     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/jpp.62.01.0006     Document Type: Article

References (34)

1. Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004; 58: 173-182.
2. Hauss DJ. Oral lipid-based formulations. Adv Drug Deliv Rev 2007; 59: 667-676.
3. Dai WG et al. Evaluation of drug precipitation of solubilityenhancing liquid formulations using milligram quantities of a new molecular entity (NME). J Pharm Sci 2006; 96: 2957-2969.
4. LindML et al. Intestinal lymphatic transport of halofantrine in rats assessed using a chylomicron flowblocking approach: the influence of polysorbate 60 and 80. Eur J Pharm Sci 2008; 35: 211-218.
5. Porter CJH et al. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Disc 2007; 6: 231-248.
6. Hermansky SJ et al. Effects of polyethylene-glycol-400 (PEG-400) following 13 weeks of gavage treatment in Fischer-344 Rats. Food Chem Toxicol 1995; 33: 139-149.
7. Montaguti P et al. Acute intravenous toxicity of dimethyl-sulfoxide, polyethylene-glycol-400, dimethylformamide, absolute ethanol, and benzyl alcohol in inbred mouse strains. Arzm Forsch-Drug Res 1994; 1: 566-570.
8. Tejwani RW et al. Study of phase behavior of poly(ethylene glycol)-polysorbate 80 and poly(ethylene glycol)-polysorbate 80-water mixtures. J Pharm Sci 2000; 89: 946-950.
9. Rowe RC et al. Handbook of pharmaceutical excipients, 5th edn. London: Pharmaceutical Press, 2006.
10. Crivori P et al. Development and validation of in silico models for estimating drug preformulation risk in PEG400/water and Tween80/water systems. Eur J Pharm Sci 2007; 32: 169-181.
11. Yalkowsky SH et al. In vitro method for detecting precipitation of parenteral formulations after injection. J Pharm Sci 1983; 72: 1014-1017.
12. Yalkowsky SH, Valvani SC. Precipitation of solubilized drugs due to injection or dilution. Drug Intell Clin Pharm 1977; 11: 417-419.
13. Neervannan S. Preclinical formulations for discovery and toxicology: physicochemical challenges. Expert Opin Drug Metab Toxicol 2006; 2: 715-731.
14. Larsen A et al. Lipid-based formulations for Danazol containing a digestible surfactant, Labrafil M 2125CS: in vivo bioavail-ability and dynamic in vitro lipolysis. Pharm Res 2008; 25: 2769-2777.
15. Poelma FG et al. Intestinal absorption of drugs. The influence of mixed micelles on the disappearance kinetics of drugs from the small intestine of the rat. J Pharm Pharmacol 1991; 43: 317-324.
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. Li P, Zhao L. Developing early formulations: practice and perspective. Int J Pharm 2007; 341: 1-19.
18. Aronson H. Correction factor for dissolution profile calculations. J Pharm Sci 1993; 82: 1190
19. Humberstone AJ et al. A simplified liquid chromatography assay for the quantitation of halofantrine and desbutylhalofantrine in plasma and identification of a degradation product of desbutylhalofantrine formed under alkaline conditions. J Pharm Biomed Anal 1995; 13: 265-272.
20. Rowland M, Tozer T. Clinical pharmacokinetics: concepts and applications, 1st edn. Philadelphia: Lippincott Williams & Wilkins, 1995.
21. Humberstone AJ et al. A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine. J Pharm Sci 1996; 85: 525-529.
22. Kararli TT. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm Drug Dispos 1995; 16: 351-380.
23. Gao P et al. Enhanced oral bioavailability of a poorly water soluble drug PNU-91325 by supersaturable formulations. Drug Dev Ind Pharm 2004; 30: 221-229.
24. Basit AW et al. The effect of polyethylene glycol 400 on gastrointestinal transit: implications for the formulation of poorly water-soluble drugs. Pharm Res 2001; 18: 1146-1150.
25. Basit AW et al. Influence of polyethylene glycol 400 on the gastrointestinal absorption of ranitidine. Pharm Res 2002; 19: 1368-1374.
26. Hansford DT et al. The influence of formulation on the absorption of orally administered griseofulvin preparations in rabbits. Pharm Ind 1980; 42: 646-650.
27. Gao P et al. Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability. J Pharm Sci 2003; 92: 2386-2398.
28. Krantz JR. Toxicologic, pharmacodynamic and clinical observations on Tween 80. Bull Sch Med Univ 1949; 97: 48-56.
29. Seeballuck F et al. 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 2004; 21: 2320-2326.
30. LaugierR, Sarles H.Action of oleic acid on the exocrine pancreatic secretion of the conscious rat: evidence for an anti-cholecystokinin- pancreozymin factor. J Physiol 1977; 271: 81-92.
31. Brown NJ et al. Characteristics of lipid substances activating the ileal brake in the rat. Gut 1990; 31: 1126-1129.
32. Dobson CL et al. The effect of oleic acid on the human ileal brake and its implications for small intestinal transit of tablet formulations. Pharm Res 1999; 16: 92-96.
33. Croce G, Ferrini R. Modificazioni della coleresi nel ratto con alcuni solventi e disperdenti usati come veicoli de farmaci. Boll Soc Ital Biol Sper 1973; 49: 653-659.
34. Holm R et al. Comparison of the lymphatic transport of halofantrine from 3 different unsaturated triglycerides in lymph-cannulated conscious rats. Eur J Pharm Sci 2001; 14: 331-337.