The effects of pharmaceutical excipients on drug disposition

Advanced Drug Delivery Reviews

Volumn 59, Issue 15, 2007, Pages 1482-1503

  Buggins, Talia R ^a   Dickinson, Paul A ^b   Taylor, Glyn ^b  

^a CARDIFF UNIVERSITY   (United Kingdom)

^b ASTRAZENECA   (United Kingdom)

Author keywords

Excipients; Formulation; Metabolism; Pharmacokinetics; Surfactants

Indexed keywords

CLINICAL PHARMACOKINETICS; DRUG DISPOSITION; PHARMACEUTICAL EXCIPIENTS; PHYSICOCHEMICAL EFFECTS;

DRUG PRODUCTS; INFORMATION ANALYSIS; METABOLISM; PHARMACOKINETICS; SURFACE ACTIVE AGENTS;

DRUG DELIVERY;

8 (2 NOR 1 ADAMANTYL) 1,3 DIPROPYLXANTHINE; ACETYLSALICYLIC ACID; ALCOHOL; AMINOPHENAZONE; AZITHROMYCIN; BENZO[A]PYRENE; BMS 310705; BUPIVACAINE; CARBON TETRACHLORIDE; CHLOROFORM; COCAINE; CREATININE; CREMOPHOR; CYCLODEXTRIN; DEXTROPROPOXYPHENE; DIMETHYL SULFOXIDE; ETHOXYCOUMARIN; ETHYLENE GLYCOL; ISONIAZID; MACROGOL; MIDAZOLAM; MORPHINE; PARACETAMOL; PENICILLIN G; POLYSORBATE 80; PROCAINAMIDE; PROPYLENE GLYCOL; SULINDAC; TETRYLAMMONIUM; THEOPHYLLINE; UNCLASSIFIED DRUG; UNINDEXED DRUG; WARFARIN;

DRUG ABSORPTION; DRUG DISPOSITION; DRUG DOSE INCREASE; DRUG FORMULATION; DRUG METABOLISM; HUMAN; LIVER BLOOD FLOW; NONHUMAN; PHARMACOKINETICS; PRIORITY JOURNAL; REVIEW; URINARY EXCRETION;

CYCLODEXTRINS; DRUG EVALUATION, PRECLINICAL; EMULSIONS; EXCIPIENTS; HUMANS; PHARMACOKINETICS; SOLUBILITY; SOLVENTS; SURFACE-ACTIVE AGENTS;

EID: 36248980358     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.addr.2007.08.017     Document Type: Review

References (157)

1. Bittner B., and Mountfield R.J. Intravenous administration of poorly soluble new drug entities in early drug discovery: the potential impact of formulation on pharmacokinetic parameters. Curr. Opin. Drug Discov. Dev. 5 (2002) 59-71
2. Sparreboom A., van Tellingen O., Nooijen W.J., and Beijnen J.H. Nonlinear pharmacokinetics of paclitaxel in mice results from the pharmaceutical vehicle Cremophor EL. Cancer Res. 56 (1996) 2112-2115
3. van Tellingen O., Huizing M.T., Nannan Panday V.R., Schellens V.H.M., Nooije W.J., and Beijnen J.H. Cremophor EL causes (pseudo-) non-linear pharmacokinetics of paclitaxel in patients. Br. J. Cancer 81 (2000) 330-335
4. Brink J.J., and Stein D.G. Pemoline levels in brain: enhancement by dimethyl sulfoxide. Science 158 (1967) 1479-1480
5. Yoo J.S., Cheung R.J., Patten C.J., Wade D., and Yang C.S. Nature of N-nitrosodimethylamine demethylase and its inhibitors. Cancer Res. 47 (1987) 3378-3383
6. Chauret N., Gauthier A., and Nicoll-Griffith D.A. Effect of common organic solvents on in vitro cytochrome P450-mediated metabolic activities in human liver microsomes. Drug Metab. Dispos. 26 (1998) 1-4
7. Lee D.W., Lim H.B., Moon J.Y., and Park K.H. In vitro enhancement of microsomal cytochrome P450-dependent monooxygenases by organic solvents in rat liver. J. Biochem. Mol. Biol. 31 (1998) 391-398
8. Kawalec J.C., and Andrews A.W. The effect of solvents on drug metabolism in vitro. Drug Metab. Dispos. 8 (1980) 380-384
9. Kontir D.M., Glance C.A., Clolby H.D., and Miles P.R. Effects of organic-solvent vehicles on benzo(a)pyrene metabolism in rabbit lung microsomes. Biochem. Pharmacol. 35 (1986) 2569-2575
10. Zitting A., Vainiotal S., and Elovaara E. Dimethylsulfoxide induced activation of renal microsomal ethoxycoumarin O-deethylation. In: Rydstrom J., Montelius J., and Bengtsson M. (Eds). Extrahepatic Drug Metabolism and Chemical Carcinogenesis (1983), Elsevier Science Publishers, The Netherlands 241-242
11. Ratnayake H.J., Hanna P.E., Anders M.W., and Duggan D.E. In vitro reduction of sulindac by rat hepatic cytosolic enzymes. Drug Metab. Dispos. 9 (1981) 85-87
12. Swanson B.N., Mojaverian P., Boppana V.K., and Dudash M.R. Effect of dimethylsulfoxide on sulindac disposition in rats. Drug Metab. Dispos. 9 (1981) 499-502
13. Swanson B.N., Bappana V.K., Vlasses P.H., Rotmensch H.H., and Ferguson R.K. Dimethylsulfoxide inhibits bioactivation of sulindac. J. Lab. Clin. Med. 102 (1983) 95-101
14. Swanson B.N., Mojaverian P., and Boppana V.K. Inhibition of sulindac metabolism by dimethylsulfoxide in the rat. J. Toxicol. Environ. Health 12 (1983) 213-222
15. Buggins T.R., Dickinson P.A., DeMatas M., and Taylor G. The effects of pharmaceutical excipients on in vivo drug metabolism. J. Pharm. Pharmacol. 57 (2005) S104
16. Muther R.S., and Bennett W.M. Effects of dimethyl sulfoxide on renal function in man. JAMA 244 (1980) 2081-2083
17. Gunn I.R., and Acomb C. High plasma osmolality following intravenous dimethylsulfoxide in the treatment of postoperative hemiplegia. J. Neurol. Neurosurg. Psychiatry 49 (1986) 961-962
18. Ali B.H., and Mousa M.M. Effect of dimethyl sulfoxide on gentamicin-induced nephrotoxicity in rats. Human Exp. Toxicol. 20 (2001) 199-203
19. Pestel S., Martin H.J., Maier G.M., and Guth B. Effect of commonly used vehicles on gastrointestinal, renal, and liver function in rats. J. Pharmacol. Toxicol. Methods 54 (2006) 200-214
20. Passananti G.T., Shively C.A., and Vesell E.S. Orally administered dimethyl sulfoxide and its effects on blood concentrations of salicylic acid, sulfanilamide and warfarin. Ann. N.Y. Acad. Sci. 243 (1975) 311-316
21. Gross S.M., Reddy R.V., and Reddy C.S. Alteration in the tissue retention of [14C]-caffeine in pregnant mice by dimethylsulfoxide. Nat. Toxins 1 (1993) 376-380
22. Kassell N.F., Sprowell J.A., Boarini D.J., and Olin J.J. Effect of dimethyl sulfoxide on the cerebral and systemic circulations of the dog. Neurosurgery 12 (1983) 24-28
23. Iwen P.C., and Miller N.G. Enhancement of ketoconazole penetration across the blood-brain barrier of mice by dimethyl sulfoxide. Antimicrob. Agents Chemother. 30 (1986) 617-618
24. Rubinstein E., and Lev-El A. The effect of dimethyl sulfoxide on tissue distribution of gentamicin. Experientia 36 (1980) 92-93
25. Ivanovic Matic S., Dinic S., Mihailovic M., Grigorov I., Bogojevic D., and Poznanovic G. Acute-phase protein expression in DMSO-intoxicated rats. Toxicol. Lett. 147 (2004) 153-159
26. Aasmundstad T.A., Lillekjendlie B., and Morland J. Ethanol interference with morphine metabolism in isolated guinea pig hepatocytes. Pharmacol. Toxicol. 79 (1996) 114-119
27. Rendic S., and Di Carlo F.J. Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors. Drug Metab. Rev. 29 (1997) 413-580
28. Wang P.Y., Kaneko T., Tsukada H., Nakano M., and Sato A. Dose-and route-dependent alterations in metabolism and toxicity of chemical compounds in ethanol-treated rats: difference between highly (Chloroform) and poorly (Carbon tetrachloride) metabolized hepatotoxic compounds. Toxicol. Appl. Pharmacol. 142 (1997) 13-21
29. Peng R., Tu Y.Y., and Yang C.S. The induction and competitive inhibition of a high affinity microsomal nitrosodimethylamine demethylase by ethanol. Carcinogenesis 3 (1982) 1457-1461
30. Parker R.B., Gades N., Mandrell T., and Laizure C. Effect of ethanol on oral cocaine pharmacokinetics. Pharmacotherapy 22 (2002) 246
31. Kambam J.R., Franks J.J., Janicki P.K., Mets B., van der Watt M., and Hickman R. Alcohol pretreatment alters the metabolic pattern and accelerates cocaine metabolism in pigs. Drug Alcohol Depend. 36 (1994) 9-13
32. Oguma T., and Levy G. Acute effect of ethanol on hepatic first-pass elimination of propoxyphene in rats. J. Pharmacol. Exp. Ther. 219 (1981) 7-13
33. Olsen H., Aune H., Lilleasen P., Gulliksen M., Bodd E., and Morland J. The effect of ethanol intake on propoxyphene absorption and biotransformation in dogs. Acta Pharmacol. Toxicol. 53 (1983) 21
34. Bodd E., Olsen H., Gulliksen M., and Mørland J. Ethanol does not increase lethality due to propoxyphene in rats. Alcohol 2 (1985) 293-296
35. Grauer G.F., Thrall M.A., Henre B.A., and Hjelle J.J. Comparison of the effects of ethanol and 4-methylpyrazole on the pharmacokinetics and toxicity of ethylene glycol in the dog. Toxicol. Lett. 35 (1987) 307-314
36. Kourtopoulos H., Bolander H., Holm S.E., and Wahlstrom G. Effect of ethanol on the pharmacokinetics of penicillin in the rat. Acta Pharmacol. Toxicol. 53 (1983) 200-204
37. Kim Y.K., Lee S.H., Goldinger J.M., and Hong S.K. Effect of ethanol on organic ion transport in rabbit kidney. Toxicol. Appl. Pharmacol. 86 (1986) 411-420
38. Preheim L.C., Olsen K.M., Yue M., Snitily M.U., and Gentry M.J. Ethanol feeding does not affect the efficacy or pharmacokinetics of azithromycin, trovafloxacin, or ceftriaxone in a rat model of pneumococcal pneumonia. Alcohol Clin. Exp. Res. 23 (1999) 842-849
39. Mets B., Kamban J.R., Janicki P.K., Franks J., Neveling U., and Hickman R. Alcohol pretreatment does not affect bupivacaine pharmacokinetics in the pig. Pharmacol. Res. 33 (1996) 291-295
40. Dattani R.G., Harry F., Hutchings A.D., and Routledge P.A. The effects of acute ethanol intake on isoniazid pharmacokinetics. Br. J. Clin. Pharmacol. 47 (1999) 591-592
41. Hoyo-Vadillo C., Mandema J.W., and Danhof M. Pharmacodynamic interaction between midazolam and a low dose of ethanol in vivo. Life Sci. 57 (1995) 325-333
42. Gole D.J., and Nagwekar J.B. Effects of chronic ethanol ingestion on pharmacokinetics of procainamide in rats. J. Pharm. Sci. 80 (1991) 232-238
43. Christensen J.M., Suvanakadt U., Ayres J.W., and Tavipatana W. Ethyl lactate-ethanol-water cosolvent for intravenous theophylline. Res. Commun. Chem. Pathol. Pharmacol. 50 (1985) 147-150
44. Walters K.M., Mason W.D., and Badr M.Z. Effect of propylene glycol on the disposition of dramamine in the rabbit. Drug Metab. Dispos. 21 (1993) 305-308
45. Dean M.E., and Stock H. Propylene glycol as a drug solvent in the study of hepatic microsomal enzyme metabolism in the rat. Toxicol. Appl. Pharmacol. 28 (1974) 44-52
46. Snawder J.E., Benson R.W., Leakey J.E., and Roberts D.W. The effect of propylene glycol on the P450-dependent metabolism of acetaminophen and other chemicals in subcellular fractions of mouse liver. Life Sci. 52 (1993) 183-189
47. Oshiro T.T., Texeira C.F.P., and Oga S. Propylene glycol enhances anti-inflammatory effects of phenylbutazone. Gen. Pharmacol. 21 (1990) 131-134
48. Hayman M., Seidl E.C., Ali M., and Malik K. Acute tubular necrosis associated with propylene glycol from concomitant administration of intravenous lorazepam and trimethoprim-sulfamethoxazole. Pharmacotherapy 23 (2003) 1190-1194
49. Yaucher N.E., Fish J.T., Smith H.W., and Wells J.A. Propylene glycol-associated renal toxicity from lorazepam infusion. Pharmacotherapy 23 (2003) 1094-1099
50. Morshed K.M., Desjeux J.F., Nagpaul J.P., Majumdar S., and Amma M.K.P. The effect of propane-diols on the intestinal uptake of nutrients and brush-border membrane enzymes in the rat. Biochem. Med. Metabol. B 45 (1991) 161-170
51. Cornaire G., Woodley J.F., Hermann P., Cloarec A., 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
52. Schulze J.D., Peters E.E., Vickers A.W., Staton J.S., Coffin M.D., Parsons G.E., and Basit A.W. Excipient effects on gastrointestinal transit and drug absorption in beagle dogs. Int. J. Pharm. 300 (2005) 67-75
53. Johnson B.M., Charman W.N., and Porter C.J.H. An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-a-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine. AAPS PharmSci 4 (2002) 40
54. Hugger E.D., Novak B.L., Burton P.S., Audus K.L., and Borchardt R.T. A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J. Pharm. Sci. 91 (2002) 1991-2002
55. Issar M., Singh S.K., Mishra B., and Gupta R.C. Pharmacokinetics, in-situ absorption and protein binding studies of a new neuroleptic agent centbutindole in rats. Eur. J. Pharm. Sci. 19 (2003) 105-113
56. Basit A.W., Podczeck F., Newton J.M., Waddington W.A., Eli P.J., and Lacey L.F. Influence of polyethylene glycol 400 on the gastrointestinal absorption of ranitidine. Pharm. Res. 19 (2002) 1368-1374
57. Schulze J.D., Waddington W.A., Eli P.J., Parsons G.E., Coffin M.D., and Basit A.W. Concentration-dependent effects of polyethylene glycol 400 on gastrointestinal transit and drug absorption. Pharm. Res. 20 (2003) 1984-1988
58. Laine G.A., Hossain S.M., Solis R.T., and Adams S.C. Polyethylene glycol nephrotoxicity secondary to prolonged high-dose intravenous lorazepam. Ann. Pharmacother. 29 (1995) 1110-1114
59. Menicagli S., Longo V., Mazzaccaro A., and Gervasi P.G. Microsomal metabolism of N,N-diethylacetamide and N,N-dimethylacetamide and their effects on drug-metabolizing enzymes of rat liver. Biochem. Pharmacol. 48 (1994) 717-726
60. Tolando R., Zanovello A., Ferrara R., Iley J.N., and Manno M. Inactivation of rat liver cytochrome P450 by N,N-dimethylformamide and N,N-dimethylacetamide. Toxicol. Lett. 124 (2001) 101-111
61. Loscher W., Honack D., Richter A., Schulz H.U., Schurer M., Dusing R., and Brewster M.E. New injectable aqueous carbamazepine solution through complexing with 2-hydroxypropyl-beta-cyclodextrin - tolerability and pharmacolkinetics after intravenous injection in comparison to a glycofurol-based formulation. Epilepsia 36 (1995) 255-261
62. Yasaka W.J., Sasame H.A., Saul W., Maling H.M., and Gilette J.R. Mechanisms in potentiation and inhibition of pharmacological actions of hexobarbital and zoxazolamine by glycofurol. Biochem. Pharmacol. 27 (1978) 2851-2858
63. Stella V.J., and Rajewski R.A. Cyclodextrins: their future in drug formulation and delivery. Pharm. Res. 14 (1997) 556-567
64. Frijlink H.W., Franssen E.J.F., Eissens A.C., Oosting R., Lerk C.F., and Meijer D.K.F. The effects of cyclodextrins on the disposition of intravenously injected drugs in the rat. Pharm. Res. 8 (1991) 380-384
65. 11C]toluene. Nucl. Med. Biol. 29 (2002) 607-612
66. Ishikawa M., Yoshii H., and Furuta T. Interaction of modified cyclodextrins with cytochrome P-450. Biosci. Biotechnol. Biochem. 69 (2005) 246-248
67. Grosse P.Y., Bressolle F., Rouanet P., Joulia J.M., and Pinguet F. Methyl-beta-cyclodextrin and doxorubicin pharmacokinetics and tissue concentrations following bolus injection of these drugs alone or together in the rabbit. Int. J. Pharm. 180 (1999) 215-223
68. Arimori K., and Uekama K. Effects of beta-and gamma-cyclodextrins on the pharmacokinetic behavior of prednisolone after intravenous and intramuscular administrations to rabbits. J. Pharmacobio-dyn. 10 (1987) 390-395
69. Piel G., Evrard B., Van Hees T., and Delattre L. Comparison of the IV pharmacokinetics in sheep of miconazole-cyclodextrin solutions and a micellar solution. Int. J. Pharm. 180 (1999) 41-45
70. Egan T.D., Kern S.E., Johnson K.B., and Pace N.L. The pharmacokinetics and pharmacodynamics of propofol in a modified cyclodextrin formulation (Captisol) versus propofol in a lipid formulation (Diprivan): an electroencephalographic and hemodynamic study in a porcine model. Anesth. Analg. 97 (2003) 72-79
71. Doenicke A., Roizen M.F., Nebauer A.E., Kugler A., Hoernecke R., and Beger-Hintzen H. A comparison of two formulations for etomidate, 2-hydroxypropyl-beta-cyclodextrin (HPCD) and propylene glycol. Anesth. Analg. 79 (1994) 933-939
72. Vora J., Wu Z., Montague M., Penn M., and Erow K. Influence of dosing vehicles on the preclinical pharmacokinetics of phenolic antioxidants. Res. Commun. Mol. Pathol. 104 (1999) 93-106
73. Liu J., Qiu L., Gao J., and Jin Y. Preparation, characterization and in vivo evaluation of formulation of baicalein with hydroxypropyl-beta-cyclodextrin. Int. J. Pharm. 312 (2006) 137-143
74. Stella V.J., Lee H.K., and Thompson D.O. The effect of SBE4-β-CD on i.v. methylprednisolone pharmacokinetics in rats: comparison to a co-solvent solution and two water-soluble prodrugs. Int. J. Pharm. 120 (1995) 189-195
75. Stella V.J., Lee H.K., and Thompson D.O. The effect of SBE4-β-CD on i.m. prednisolone pharmacokinetics and tissue damage in rabbits: comparison to a co-solvent solution and a water-soluble prodrug. Int. J. Pharm. 120 (1995) 197-204
76. Muller B.W., and Albers E. Effect of hydrotropic substances on the complexation of sparingly soluble drugs with cyclodextrin derivatives and the influence of cyclodextrin complexation on the pharmacokinetics of the drugs. J. Pharm. Sci. 80 (1991) 599-604
77. Pitha J., Gerloczy A., and Olivi A. Parenteral hydroxypropyl cyclodextrins: intravenous and intracerebral administration of lipophiles. J. Pharm. Sci. 83 (1994) 833-837
78. García J.J., Bolás F., and Torrado J.J. Bioavailability and efficacy characteristics of two different oral liquid formulations of albendazole. Int. J. Pharm. 250 (2003) 351-358
79. Piette M., Evrard B., Frankenne F., Chiap P., Bertholet P., Castagne D., Foidart J.M., Delattre L., and Piel G. Pharmacokinetic study of a new synthetic MMP inhibitor (Ro 28-2653) after IV and oral administration of cyclodextrin solutions. Eur. J. Pharm. Sci. 28 (2006) 189-195
80. Lee P.S., Han J.Y., Song T.W., Sung J.H., Kwon O.S., Song S., and Chung Y.B. Physicochemical characteristics and bioavailability of a novel intestinal metabolite of ginseng saponin (IH901) complexed with beta-cyclodextrin. Int. J. Pharm. 316 (2006) 29-36
81. Westerberg G., and Wiklund L. Beta-cyclodextrin reduces bioavailability of orally administered [3H]benzo[a]pyrene in the rat. J. Pharm. Sci. 94 (2005) 114-119
82. He Z.G., Li Y.S., Zhang T.H., Tang X., Zhao C., and Zhang R.H. Effects of 2-hydroxypropyl-beta-cyclodextrin on pharmacokinetics of digoxin in rabbits and humans. Pharmazie 59 (2004) 200-202
83. BASF Aktiengesellschaft, Solubilizers, solvents and co-solvents, [WWW](2004) [accessed 21 July 2007].
84. ten Tije A.J., Verweij J., Loos W.J., and Sparreboom A. Pharmacological effects of formulation vehicles - implications for cancer chemotherapy. Clin. Pharmacokinet. 42 (2003) 665-685
85. Gelderblom H., Verweij J., Nooter K., and Sparreboom A. Cremophor EL: the drawbacks and advantages of vehicle selection for drug formulation. Eur. J. Cancer 37 (2001) 1590-1598
86. Fetterly G.J., and Straubinger R.M. Pharmacokinetics of paclitaxel-containing liposomes in rats. AAPS PharmSci 5 (2003) 32
87. Kim S.C., Kim D.W., Shim Y.H., Bang J.S., Oh H.S., Kim S.W., and Seo M.H. In vivo evaluation of polymeric micellar paclitaxel formulation: toxicity and efficacy. J. Control. Release 72 (2001) 191-202
88. Webster L.K., Cosson E.J., Stokes K.H., and Millward M.J. Effect of the paclitaxel vehicle, Cremophor EL, on the pharmacokinetics of doxorubicin and doxorubicinol in mice. Br. J. Cancer 73 (1996) 522-524
89. Brasseur N., Ouellet R., Lewis K., Potter W.R., and van Lier J.E. Photodynamic activities and skin photosensitivity of the bis(dimethylthexylsiloxy)silicon 2,3-naphthalocyanine in mice. Photochem. Photobiol. 62 (1995) 1058-1065
90. Yokogawa K., Jin M., Furui N., Yamazak M., Yoshihara H., Nomura M., Furukawa H., Ishizaki J., Fushida S., Miwa K., and Miyamoto K.I. Disposition kinetics of taxanes after intraperitoneal administration in rats and influence of surfactant vehicles. J. Pharm. Pharmacol. 56 (2004) 629-634
91. Jin M., Shimada T., Yokogaw K., Nomura M., Mizuhara Y., Furukawa J., Ishizaki, and Miyamoto K.I. Cremophor EL releases cyclosporin A adsorbed on blood cells and blood vessels, and increases apparent plasma concentration of cyclosporin A. Int. J. Pharm. 293 (2005) 137-144
92. Sparreboom A., van Zuylen L., Brouwer E., Loos W.J., de Bruijn P., Gelderblom H., Pillay M., Nooter K., Stoter G., and Verweij J. Cremophor EL-mediated alteration of paclitaxel distribution in human blood: clinical pharmacokinetic implications. Cancer Res. 59 (1999) 1454-1457
93. Sykes E., Woodburn K., Decker D., and Kessel D. Effects of cremophor EL on distribution of taxol to serum lipoproteins. Br. J. Cancer 70 (1994) 401-404
94. Woodburn K., Chang C.K., Lee S., Henderson B., and Kessel D. Biodistribution and PDT efficacy of a ketochlorin photosensitizer as a function of the delivery vehicle. Photochem. Photobiol. 60 (1994) 154-159
95. Woodburn K., Sykes E., and Kessel D. Interactions of Solutol HS 15 and Cremophor EL with plasma lipoproteins. Int. J. Biochem. Cell Biol. 27 (1995) 693-699
96. Bravo Gonzalez R.C., Huwyler J., Boess F., Walter I., and Bittner B. In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam. Biopharm. Drug Dispos. 25 (2004) 37-49
97. Wandel C., Kim R.B., and Stein C.M. "Inactive" excipients such as Cremophor can affect in vivo drug disposition. Clin. Pharmacol. Ther. 73 (2003) 394-396
98. Ellis A.G., Crinis N.A., and Webster L.K. Inhibition of etoposide elimination in the isolated perfused rat liver by Cremophor EL and Tween 80. Cancer Chemother. Pharmacol. 38 (1996) 81-87
99. Ellis A.G., and Webster L.K. Inhibition of paclitaxel elimination in the isolated perfused rat liver by Cremophor EL. Cancer Chemother. Pharmacol. 43 (1999) 13-18
100. Speeg K.V., Maldonado A.L., Liaci J., and Muirhead D. Effect of cyclosporine on colchicine secretion by the kidney multidrug transporter studied in vivo. J. Pharmacol. Exp. Ther. 261 (1992) 50-55
101. Tibell A., Larsso M., and Alvestrand A. Dissolving intravenous cyclosporin A in a fat emulsion carrier prevents acute renal side effects in the rat. Transpl. Int. 6 (1993) 69-72
102. Besarab A., Jarrell B.E., Hirsch S., Carabasi R.A., Cressman M.D., and Green P. Use of the isolated perfused kidney model to assess the acute pharmacologic effects of cyclosporine and its vehicle, cremophor EL. Transplantation 44 (1987) 195-201
103. Bogman K., Erne-Brand F., Alsenz J., and Drewe J. The role of surfactants in the reversal of active transport mediated by multidrug resistance proteins. J. Pharm. Sci. 92 (2003) 1250-1261
104. Sparreboom A., Verweij J., van der Burg M.E., Loos W.J., Brouwer E., Vigano L., Locatelli A., de Vos A.I., Nooter K., Stoter G., and Gianni L. Disposition of Cremophor EL in humans limits the potential for modulation of the multidrug resistance phenotype in vivo. Clin. Cancer Res. 4 (1998) 1937-1942
105. Cornaire G., Woodley J.F., Saivin S., Legendre J.Y., Decourt S., Cloarec A., and Houin G. Effect of polyoxyl 35 castor oil and Polysorbate 80 on the intestinal absorption of digoxin in vitro. Arzneim.-Forsch. 50 (2000) 576-579
106. Tayrouz Y., Ding R., Burhenne J., Riedel K.D., Weiss J., Hoppe-Tichy T., Haefeli W.E., and Mikus G. Pharmacokinetic and pharmaceutic interaction between digoxin and Cremophor RH40. Clin. Pharmacol. Ther. 73 (2003) 397-405
107. Martin-Facklam M., Burhenne J., Ding R., Fricker R., Mikus G., Walter-Sack I., and Haefeli W.E. Dose-dependent increase of saquinavir bioavailability by the pharmaceutic aid cremophor EL. Br. J. Clin. Pharmacol. 53 (2002) 576-581
108. 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
109. Malingre M.M., Schellens J.H., van Tellingen O., Ouwehand M., Bardelmeijer H.A., Rosing H., Koopman F.J., Schot M.E., Ten 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
110. 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
111. Kamath A.V., Chang M., Lee F.Y., Zhang Y., and Marathe P.H. Preclinical pharmacokinetics and oral bioavailability of BMS-310705, a novel epothilone B analog. Cancer Chemother. Pharmacol. 56 (2005) 145-153
112. Millward M.J., Webster L.K., Rischin D., Ellis A.G., Linahan B.M., Maisano R., Toner G.C., and Stokes K.H. Randomised, cross-over trial to determine the effect of Cremophor on the pharmacokinetics and pharmacodynamics of carboplatin-based therapy. Ann. Oncol. 9 Suppl 2 (1998) 499
113. Tibell A., Lindholm A., Sawe J., Chen G., and Norrlind B. Cyclosporin A in fat emulsion carriers: experimental studies on pharmacokinetics and tissue distribution. Pharmacol. Toxicol. 76 (1995) 115-121
114. Kurlansky P.A., Sadeghi A.M., Michler R.E., Coppey L.J., Re L.P., Thomas W.G., Smith C.R., Reemtsma K., and Rose E.A. Role of the carrier solution in cyclosporine pharmacokinetics in the baboon. J. Heart Transplant. 5 (1986) 312-316
115. Badary O.A., Al-Shabanah O.A., Al-Gharably N.M., and Elmazar M.N.A. Effect of Cremophor EL on the pharmacokinetics, antitumor activity and toxicity of doxorubicin in mice. Anti-Cancer Drugs 9 (1998) 809-815
116. Colombo T., Parisi I., Zucchetti M., Sessa C., Goldhirsch A., and D'Incalci M. Pharmacokinetic interactions of paclitaxel, docetaxel and their vehicles with doxorubicin. Ann. Oncol. 10 (1999) 391-395
117. Kemper E.M., van Zandbergen A.E., Cleypool C., Mos H.A., Boogerd W., Beijnen J.H., and van Tellingen O. Increased penetration of paclitaxel into the brain by inhibition of P-glycoprotein. Clin. Cancer Res. 9 (2003) 2849-2855
118. Gelderblom H., Verweij J., van Zomeren D.M., Buijs D., Ouwens L., Nooter K., Stoter G., and Sparreboom A. Influence of Cremophor El on the bioavailability of intraperitoneal paclitaxel. Clin. Cancer Res. 8 (2002) 1237-1241
119. Dutta S., Matsumoto Y., and Ebling W.F. Propofol pharmacokinetics and pharmacodynamics assessed from a Cremophor EL formulation. J. Pharm. Sci. 86 (1997) 967-969
120. Zhang H., Yao M., Morrison R.A., and Chong S. Commonly used surfactant, Tween 80, improves absorption of P-glycoprotein substrate, digoxin, in rats. Arch. Pharm. Res. 26 (2003) 768-772
121. Azmin M.N., Stuart J.F.B., and Florence A.T. The distribution and elimination of methotrexate in mouse blood and brain after concurrent administration of polysorbate 80. Cancer Chemother. Pharmacol. 14 (1985) 238-242
122. Mountfield R.J., Senepin S., Schleimer M., Walter I., and Bittner B. Potential inhibitory effects of formulation ingredients on intestinal cytochrome P450. Int. J. Pharm. 211 (2000) 89-92
123. van Tellingen O., Beijnen J.H., Verweij J., Scherrenburg E.J., Nooijen W.J., and Sparreboom A. Rapid esterase-sensitive breakdown of polysorbate 80 and its impact on the plasma pharmacokinetics of docetaxel and metabolites in mice. Clin. Cancer Res. 5 (1999) 2918-2924
124. Loos W.J., Baker S.D., Verweij J., Boonstra J.G., and Sparreboom A. Clinical pharmacokinetics of unbound docetaxel: role of polysorbate 80 and serum proteins. Clin. Pharmacol. Ther. 74 (2003) 364-371
125. Dimitrijevic D., Whitton P.S., Domin M., Welham K., and Florence A.T. Increased vigabatrin entry into the brain by polysorbate 80 and sodium caprate. J. Pharm. Pharmacol. 53 (2001) 149-154
126. Gulyaev A.E., Gelperina S.E., Skidan I.N., Antropov A.S., Kivman G.Y., and Kreuter J. Significant transport of doxorubicin into the brain with polysorbate 80-coated nanoparticles. Pharm. Res. 16 (1999) 1564-1569
127. Kreuter J. Influence of the surface properties on nanoparticle-mediated transport of drugs to the brain. J. Nanosci. Nanotechnol. 4 (2004) 484-488
128. Harrison S.D., Cusic A.M., and McAfee S.M. Tween 80 increases plasma adriamycin concentrations in mice by a apparent reduction of plasma volume. Eur. J. Cancer 17 (1981) 387-389
129. Cummings J., Forrest G.J., Cunningham D., Gilchrist N.L., and Soukop M. Influence of polysorbate-80 (Tween-80)and etoposide (VP-16-213) on the pharmacokinetics and urinary excretion of adriamycin and its metabolites in cancer patients. Cancer Chemother. Pharmacol. 17 (1986) 80-84
130. Bravo Gonzalez R.C., Boess F., Durr E., Schaub N., and Bittner B. In vitro investigation on the impact of Solutol HS 15 on the uptake of colchicine into rat hepatocytes. Int. J. Pharm. 279 (2004) 27-31
131. Alyautdin R.N., Teziko E.B., Ramge P., Kharkevich D.A., Begley D.J., and Kreuter J. Significant entry of tubocurarine into the brain of rats by adsorption to polysorbate 80-coated polybutylcyanoacrylate nanoparticles: an in situ brain perfusion study. J. Microencapsul. 15 (1998) 67-74
132. Bravo Gonzalez R.C., Mountfield R.J., Walter I., Delobel F., and Bittner B. Impact of Solutol HS 15 on the clearance of midazolam in rat hepatocytes. Drug Metab. Rev. 33 S1 (2001) 364
133. Bittner B., Bravo Gonzalez R.C., Isel H., and Flament C. Impact of Solutol HS 15 on the pharmacokinetic behaviour of midazolam upon intravenous administration to male Wistar rats. Eur. J. Pharm. Biopharm. 56 (2003) 143-146
134. Bittner B., Gonzalez R.C., Walter I., Kapps M., and Huwyler J. Impact of Solutol HS 15 on the pharmacokinetic behaviour of colchicine upon intravenous administration to male Wistar rats. Biopharm. Drug Dispos. 24 (2003) 173-181
135. Desrayaud S., Guntz P., Scherrmann J.M., and Lemaire M. Effect of the P-glycoprotein inhibitor, SDZ PSC 833, on the blood and brain pharmacokinetics of colchicine. Life Sci. 61 (1997) 153-163
136. Coon J.S., Knudson W., Clodfelter K., Lu B., and Weinstein R.S. Solutol HS 15, nontoxic polyoxyethylene esters of 12-hydroxystearic acid, reverses multidrug resistance. Cancer Res. 51 (1991) 897-902
137. Woodcock D.M., Linsenmeyer M.E., Chojnowski G., Kriegler A.B., Nink V., Webster L.K., and Sawyer W.H. Reversal of multidrug resistance by surfactants. Br. J. Cancer 66 (1992) 62-68
138. Bittner B., Bravo Gonzalez R.C., Walter I., and Huwyler J. Impact of oral administration of the surface-active excipient Solutol HS 15 on the pharmacokinetics of intravenously administered colchicine. Lett. Drug Des. Discov. 2 (2005) 193-195
139. Bravo Gonzalez R.C., Huwyler J., Walter I., Mountfield R., and Bittner B. Improved oral bioavailability of cyclosporin A in male Wistar rats. Comparison of a Solutol HS15 containing self-dispersing formulation and a microsuspension. Int. J. Pharm. 245 (2002) 143-151
140. Bittner B., Guenzi A., Fullhardt P., Zuercher G., Gonzalez R.C., and Mountfield R.J. Improvement of the bioavailability of colchicine in rats by co-administration of d-alpha-tocopherol polyethylene glycol 1000 succinate and a polyethoxylated derivative of 12-hydroxy-stearic acid. Arzneim-Forsch. 52 (2002) 684-688
141. Dutta S., and Ebling W.F. Formulation-dependent pharmacokinetics and pharmacodynamics of propofol in rats. J. Pharm. Pharmacol. 50 (1998) 37-42
142. Dutta S., and Ebling W.F. Formulation-dependent brain and lung distribution kinetics of propofol in rats. Anesthesiology 89 (1998) 678-685
143. Bettschart-Wolfensberger R., Semder A., Alibhai H., Demuth D., Aliabadi F.S., and Clarke K.W. Cardiopulmonary side-effects and pharmacokinetics of an emulsion of propofol (Disoprivan (R)) in comparison to propofol solved in polysorbate 80 in goats. J. Vet. Med., Ser. A 47 (2000) 341-350
144. Kim S.J., Choi H.K., and Lee Y.B. Pharmacokinetic and pharmacodynamic evaluation of cyclosporin A O/W-emulsion in rats. Int. J. Pharm. 249 (2002) 149-156
145. Park K.M., Lee M.K., Hwang K.J., and Kim C.K. Phospholipid-based microemulsions of flurbiprofen by the spontaneous emulsification process. Int. J. Pharm. 183 (1999) 145-154
146. Kurihara A., Shibayama Y., Mizota A., Yasuno A., Ikeda M., and Hisaoka M. Pharmacokinetics of highly lipophilic antitumor agent palmitoyl rhizoxin incorporated in lipid emulsions in rats. Biol. Pharm. Bull. 19 (1996) 252-258
147. Sakaeda T., and Hirano K. O/W lipid emulsions for parenteral drug delivery. II. Effect of composition on pharmacokinetics of incorporated drug. J. Drug Target. 3 (1995) 221-230
148. Woolfrey S.G., Palin K.J., and Davis S.S. The effect of Miglycol 812 oil on the oral absorption of propranolol in the rat. J. Pharm. Pharmacol. 41 (1989) 579-581
149. Brime B., Frutos P., Bringas P., Nieto A., Ballesteros M.P., and Frutos G. Comparative pharmacokinetics and safety of a novel lyophilized amphotericin B lecithin-based oil-water microemulsion and amphotericin B deoxycholate in animal models. J. Antimicrob. Chemother. 52 (2003) 103-109
150. Guo J.X., Ping Q.N., and Chen Y. Pharmacokinetic behavior of cyclosporin A in rabbits by oral administration of lecithin vesicle and sandimmun neoral. Int. J. Pharm. 216 (2001) 17-21
151. Park K.M., and Kim C.K. Preparation and evaluation of flurbiprofen-loaded microemulsion for parenteral delivery. Int. J. Pharm. 181 (1999) 173-179
152. Hosokawa T., Yamauchi M., Yamamoto Y., Iwata K., Mochizuki H., and Kato Y. Role of the lipid emulsion on an injectable formulation of lipophilic KW-3902, a newly synthesized adenosine A1-receptor antagonist. Biol. Pharm. Bull. 25 (2002) 492-498
153. Cox E.H., Knibbe C.A.J., Koster V.S., Langemeijer M.W.E., Tukker E.E., Lange R., Kuks P.F.M., Langemeijer H.J.M., Lie-A-Huen L., and Danhof M. Influence of different fat emulsion-based intravenous formulations on the pharmacokinetics and pharmacodynamics of propofol. Pharm. Res. 15 (1998) 442-448
154. Doenicke A.W., Roizen M.F., Rau J., O'Connor M., Kugler J., Klotz U., and Babl J. Pharmacokinetics and pharmacodynamics of propofol in a new solvent. Anesth. Analg. 85 (1997) 1399-1403
155. Paul M., Dueck M., Kampe S., Fruendt H., and Kasper S.M. Pharmacological characteristics and side effects of a new galenic formulation of propofol without soyabean oil. Anaesthesia 58 (2003) 1056-1062
156. Ward D.S., Norton J.R., Guivarc'h P.H., Litman R.S., and Bailey P.L. Pharmacodynamics and pharmacokinetics of propofol in a medium-chain triglyceride emulsion. Anesthesiology 97 (2002) 1401-1408
157. Knibbe C.A.J., Aarts L.P.H.J., Kuks P.F.M., Voortman H.J., Lie-A-Huen L., Bras L.J., and Danhof M. Pharmacokinetics and pharmacodynamics of propofol 6% SAZN versus propofol 1% SAZN and Diprivan-10 for short-term sedation following coronary artery bypass surgery. Eur. J. Clin. Pharmacol. 56 (2000) 89-95