A novel stable supersaturated submicron lipid emulsion of Tirilazad

Pharmaceutical Development and Technology

Volumn 4, Issue 3, 1999, Pages 333-345

  Wang, Youmin ^a,b   Cory, Andrea L ^a  

^a Pharmaceutical Development   (United States)

^b PFIZER INC   (United States)

Author keywords

Amphiphile; Parenteral drug delivery; Submicron lipid emulsion; Supersaturation; Tirilazad

Indexed keywords

TIRILAZAD;

ARTICLE; CONTROLLED STUDY; DRUG CONCENTRATION; DRUG DELIVERY SYSTEM; DRUG SOLUBILITY; DRUG STABILITY; DRUG STORAGE; DRUG STRUCTURE; EMULSION; FLOW KINETICS; LIGHT SCATTERING; PARENTERAL DRUG ADMINISTRATION; PARTICLE SIZE; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPY; SPECTROSCOPY; VISCOSITY;

ANTIOXIDANTS; DRUG STABILITY; ELECTROCHEMISTRY; EMULSIONS; LIPIDS; PARTICLE SIZE; PREGNATRIENES; RHEOLOGY; SOLUBILITY; SOLVENTS; STERILIZATION;

EID: 0032782228     PISSN: 10837450     EISSN: None     Source Type: Journal    
DOI: 10.1081/PDT-100101369     Document Type: Article

References (26)

1. S. Benita and M. Y. Levy, Submicron emulsions as colloidal drug carriers for intravenous administration: comprehensive physicochemical characterization, J. Pharm. Sci., 82(11), 1069-1079 (1993).
2. L. C. Colliins-Gold, R. T. Lyons, and L. C. Bartholow, Parenteral emulsions for drug delivery, Adv. Drug Delivery Rev., 5, 189-208 (1990).
3. B. Lundberg, Preparation of drug-carrier emulsions stabilized with phosphatidylcholine-surfactant mixtures, J. Pharm. Sci., 83, 72-75 (1994).
4. R. H. Muller and S. Heinemann, Emulsions for intravenous administration, Pharm. Ind., 55(9), 853-856 (1993).
5. A. Wretlind, Development of fat emulsions, J. Parenter. Enteral Nutr., 5230-235 (1981).
6. A. J. Prankerd and V. J. Stella, The use of oil-in-water emulsions as a vehicle for parenteral drug administration, J. Parenter. Sci. Technol., 44, 139-149 (1990).
7. S. Buxser, Optimizing biological activity of lipophilic compounds in cultured cells by improving delivery: theoretical and practical considerations, Neuroprotocols, 3, 167-174 (1993).
8. D. E. Decker, S. M. Vroegop, T. G. Goodman, T. Peterson, and S. E. Buxser, Kinetics and thermodynamics of emulsion delivery of lipophilic antioxidants to cells in culture, Chem. Phys. Lipids, 76, 7-25 (1995).
9. E. H. Cox, C. A. J. Knibbe, V. S. Koster, M. W. E. Langemeijer, E. E. Tukker, R. Lange, P. F. M. Fukes, and M. Danhof, Influence of different fat emulsion-based intravenous formulations on the pharmacokinetics and pharmacodynamics of propofol, Pharm. Res., 15, 442-448 (1998).
10. M. Y. Levy and S. Benita, Design and characterization of a submicron o/w emulsion of diazepam for parenteral use, Int. J. Pharm., 54, 103-112 (1989).
11. K. J. Steffens, A. Lich, and H. Perschbacher, O/W emulsions as carriers for micronized drug particles, Manuf. Chem., 63, 23-26 (1992).
12. P. C. Schmidt, H. Perschbacher, K. J. Steffens, and H. P. Kraemer, Development of a suspension-emulsion system for parenteral application in animals, Acta Pharm. Technol., 35(1), 34-37 (1989).
13. D. E. Epps and J. M. McCall, Physical and chemical mechanisms of the antioxidant action of tirilazad mesylate, in Handbook of Synthetic Antioxidants (L. Packer and E. Cadenas, eds.), Marcel Dekker, Inc., New York. 1997. pp. 95-137.
14. D. F. Nicoli, in Nicomp 370 Submicron Particle Sizer, Version 5.0, Instruction Manual, Pacific Scientific, Instruments Division, Silver Spring, MD, 1987.
15. R. W. Duke and L. L. Chapoy, The rheology and structure of lecithin in concentrated solution and the liquid crystalline state, Rheol. Acta, 15, 548-557 (1976).
16. M. Rotenberg, M. Rubin, A. Bor, D. Meyuhas, Y. Talmon, and D. Lichtenberg, Physico-chemical characterization of intralipid emulsions, Biochim. Biophys. Acta, 1086, 265-272 (1991).
17. M. J. Groves, M. Wineberg, and A. P. R. Brain, The presence of liposomal materials in phosphatide stabilized emulsion, J. Dispersion Sci. Technol, 6, 237-243 (1985).
18. K. Westesen and T. Wehler, Physicochemical characterization of a model intravenous oil-in-water emulsion, J. Pharm. Sci., 81, 777-786 (1992).
19. 1H-NMR techniques, Chem. Pharm. Bull., 42, 1715-1719 (1994).
20. A. D. Bangham, Membrane models with phospholipids, Prog. Biophys. Mol. Biol., 18, 29 (1968).
21. P. J. Spooner, S. B. Clark, D. L. Gantz, J. A. Hamilton, and D. M. Small, The ionization and distribution behavior of oleic acid in chylomicron and chylomicron-like emulsion particles and the influence of serum albumin, J. Biol. Chem., 263, 1444-1453 (1988).
22. J. G. Lessard and M. Fragata, Micropolarities of lipid bilayers and micelles. # Effect of monovalent ions on the dielectric constant of the water-membrane interface of unilamellar phosphatidylcholine vesicles, J. Phys. Chem., 90(5), 811-817 (1986).
23. G. Zografi, Physical stability assessment of emulsions and related disperse systems: a critical review, J. Soc. Cosmet. Chem., 33, 345-358 (1982).
24. I. Hakansson, Physicochemical changes in artificial fat emulsions during storage: studies of the hydrolysis and its physiological effects, Acta Chem. Scand., 30, 2267-2281 (1966).
25. P. R. Chaturvedi, N. M. Patel, and S. A. Lodhi, Effect of terminal heat sterilization on the stability of phospholipid-stabilized submicron emulsions, Acta Pharm. Nord., 4, 51-55 (1992).
26. A. O. Dekker and R. G. Dickinson, Oxidation of ascorbic acid by oxygen with cupric ion as catalyst, J. Am. Chem. Soc., 62, 2165 (1940).