1. Yamahira Y, Noguchi T, Takenaka H, Maeda T. Biopharmaceutical studies of lipid-containing oral dosage forms: relationship between drug absorption rate and digestibility of vehicles. Int J Pharm 1979; 3:23-31.
2. Fouad FM, Farrell PG, Marshall WD, van de Voort FR. In vitro model for lipase-catalysed lipophile release from fats. J Agric Food Chem 1991; 39(1):150-153.
3. Humberstone AJ, Charman WN. Lipid-based vehicles for the oral delivery of poorly water-soluble drugs. Adv Drug Deliv Rev 1997; 25(1):103-128.
4. 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.
5. Gershanik T, Benita S. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur J Pharm Biopharm 2000; 50(1):179-188.
6. Stuchlik M, Zak S. Lipid-based vehicle for oral drug delivery. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub 2001; 145(2):17-26.
7. Porter CJ, Charman WN. Uptake of drugs into the intestinal lymphatics after oral administration. Adv Drug Deliv Rev 1997; 25(1):71-89.
8. Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004; 58(3):173-182.
9. Constantinides PP. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm Res 1995; 12(11): 1561-1572.
10. Shah NH, Carvajal MT, Patel CI, Infeld MH, Malick AW. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int J Pharm 1994; 106(1):15-23.
11. Pouton CW. Self-emulsifying drug delivery systems:assessment of the efficiency of emulsification. Int J Pharm 1985; 27(2-3):335-348.
12. Wakerly MG, Pouton-CW, Meakin BJ. Evaluation of the self-emulsifying preformance of a non-ionic surfactant-vegetable oil mixture. J Pharm Pharmacol 1987; 39:6P.
13. Charman SA, Charman WN, Rogge MC, Wilson TD, Dutko FJ, Pouton CW. Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharm Res 1992; 9(1):87-93.
14. Grove M, Pedersen GP, Nielsen JL, Mullertz A. Bioavailability of seocalcitol I: relating solubility in biorelevant media with oral bioavailability in rats-effect of medium and long chain triglycerides. J Pharm Sci 2005; 94(8):1830-1838.
15. de Smidt PC, Campanero MA, Troconiz IF. Intestinal absorption of penclomedine from lipid vehicles in the conscious rat: contribution of emulsification versus digestibility. Int J Pharm 2004; 270(1-2):109-118.
16. Myers RA, Stella VJ. Systemic bioavailability of penclomedine (NSC-338720) from oil-in-water emulsions administered intraduodenally to rats. Int J Pharm 1992; 78(1-3):217-226.
17. FDA 2005. Guidance for Industry Nonclinical Studies for the Safety Evaluation of Pharmaceutical Excipients. U.S. Department of Health and Human Services.
18. FDA 2006. www.accessdata.fda.gov/scripts/cder/lig/index.cfm. U.S. Food and Drug Administration.
19. Lin JH, Chen IW, Lievens H. The effect of dosage form on oral absorption of L-365260, a potent CCKB receptor antagonist, in beagle dogs. Pharm Res 1991; 8:S-272.
20. Gallo-Torres H, Ludorf J, Brin M. The effect of medium-chain triglycerides on the bioavailability of vitamin E. Int J Vit Nutr Res 1978; 48(3):240-249.
21. Palin KJ, Wilson CG, Davis SS, Phillips AJ. The effect of oils on the lymphatic absorption of DDT. J Pharm Pharmacol 1982; 34(11):707-710.
22. Palin KJ, Winson CG. The effect of different oils on the absorption of probucol in the rat. J Pharm Pharmacol 1984; 36(9):641-643.
23. Deckelbaum RJ, Hamilton JA, Moser A, et al. Medium-chain versus long-chain tri-acylglycerol emulsion hydrolysis by lipoprotein lipase and hepatic lipase: implications for the mechanisms of lipase action. Biochemistry 1990; 29(5):1136-1142.
24. Khoo SM, Shackleford DM, Porter CJ, Edwards GA, Charman WN. Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit-dose lipid-based formulation to fasted dogs. Pharm Res 2003; 20(9):1460-1465.
25. Laher JM, Rigler MW, Vetter RD, Barrowman JA, Patton JS. Similar bioavailability and lymphatic transport of benzo(a)pyrene when administered to rats in different amounts of dietary fat. J Lipid Res 1984; 25(12):1337-1342.
26. Gershanik T, Haltner E, Lehr CM, Benita S. Charge-dependent interaction of self-emulsifying oil formulations with Caco-2 cells monolayers: binding, effects on barrier function and cytotoxicity. Int J Pharm 2000; 211(1-2):29-36.
27. Gursoy N, Garrigue JS, Razafindratsita A, Lambert G, Benita S. Excipient effects on in vitro cytotoxicity of a novel paclitaxel self-emulsifying drug delivery system. J Pharm Sci 2003; 92(12):2411-2418.
28. Palamakula A, Khan MA. Evaluation of cytotoxicity of oils used in coenzyme Q10 self-emulsifying drug delivery systems (SEDDS). Int J Pharm 2004; 273(1-2):63-73.
29. Tenjarla S. Microemulsions: an overview and pharmaceutical applications. Crit Rev Ther Drug Carrier Syst 1999; 16(5):461-521.
30. Strickley RG. Solubilizing excipients in oral and injectable formulations. Pharm Res 2004; 21(2):201-230.
31. Grove M, Mullertz A, Nielsen JL, Pedersen GP. Bioavailability of seocalcitol II: development and characterisation of self microemulsifying drug delivery systems (SMEDDS) for oral administration containing medium and long chain triglycerides. Eur J Pharm Sci 2006; 28(3):233-242.
32. Khoo SM, Humberstone AJ, Porter CJ, Edwards GA, Charman WN. Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int J Pharm 1998; 167(12):155-164.
33. Christensen J0. Evaluation of an in vitro lipid digestion model—testing poorly soluble drug substances and lipid-based formulations. Ph.D. Thesis Ed., Department of Pharmaceutics, The Danish University of Pharmaceutical Science, Copenhagen, Denmark, 2004.
34. Gao P, Rush BD, Pfund WP, et al. Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability. J Pharm Sci 2003; 92(12):2386-2398.
35. Alander J, Wärnheim T. Model microemulsions containing vegetable oils part 1: nonionic surfactant systems. J Am Oil Chem Soc 1989; 66:1656-1660.
36. Tarr BD, Yalkowsky SH. Enhanced intestinal absorption of cyclosporine in rats through the reduction of emulsion droplet size. Pharm Res 1989; 6(1):40-43.
37. Odeberg JM, Kaufmann P, Kroon KG, Hoglund P. Lipid drug delivery and rational formulation design for lipophilic drugs with low oral bioavailability, applied to cyclosporine. Eur J Pharm Sci 2003; 20(4-5):375-382.
38. Mueller EA, Kovarik JM, van Bree JB, Grevel J, Lucker PW, 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 1994; 11(1):151-155.
39. Mueller EA, Kovarik JM, van Bree JB, Tetzloff W, Grevel J, Kutz K. Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharm Res 1994; 11(2):301-304.
40. Kang BK, Lee JS, Chon SK, et al. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm 2004; 274(1-2):65-73.
41. Julianto T, Yuen KH, Noor AM. Improved bioavailability of vitamin E with a self emulsifying formulation. Int J Pharm 2000; 200(1):53-57.
42. Hauss DJ, Fogal SE, Ficorilli JV, et al. Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor. J Pharm Sci 1998; 87(2):164-169.
43. Porter CJ, Kaukonen AM, Boyd BJ, Edwards GA, Charman WN. Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation. Pharm Res 2004; 21(8):1405-1412.
44. Grove M, Mullertz A, Pedersen GP, Nielsen JL. Bioavailability of seocalcitol III: administration of lipid-based formulations to mini-pigs in the fasted and the fed state. Eur J Pharm Sci 2007; in press.
45. Porter CJ, Charman SA, Charman WN. Lymphatic transport of halofantrine in the triple-cannulated anesthetized rat model: effect of lipid vehicle dispersion. J Pharm Sci 1996; 85(4):351-356.
46. Porter CJ, Charman SA, Humberstone AJ, Charman WN. Lymphatic transport of halofantrine in the conscious rat when administered as either the free base or the hydrochloride salt: effect of lipid class and lipid vehicle dispersion. J Pharm Sci 1996; 85(4):357-361.
47. Karpf DM, Holm R, Kristensen HG, Mullertz A. Influence of the type of surfactant and the degree of dispersion on the lymphatic transport of halofantrine in conscious rats. Pharm Res 2004; 21(8):1413-1418.
48. Ichihashi T, Kinoshita H, Takagishi Y, Yamada H. Effect of oily vehicles on absorption of mepitiostane by the lymphatic system in rats. J Pharm Pharmacol 1992; 44(7):560-564.
49. Clark SB, Lawergren B, Martin JV. Regional intestinal absorptive capacities for triolein: an alternative to markers. Am J Physiol 1973; 225(3):574-585.
50. Holm R, Porter CJ, Edwards GA, Mullertz A, Kristensen HG, Charman WN. 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 2003; 20(1):91-97.
51. Colburn WA, Gibson DM, Wiens RE, Hanigan JJ. Food increases the bioavailability of isotretinoin. J Clin Pharmacol 1983; 23(11-12):534-539.
52. Charman WN, Rogge MC, Boddy AW, Berger BM. Effect of food and a monoglyc-eride emulsion formulation on danazol bioavailability. J Clin Pharmacol 1993; 33(4):381-386.
53. Sunesen VH, Vedelsdal R, Kristensen HG, Christrup L, Mullertz A. Effect of liquid volume and food intake on the absolute bioavailability of danazol, a poorly soluble drug. Eur J Pharm Sci 2005; 24(4):297-303.
54. Matuszewska B, Hettrick L, Bondi JV, Storey DE. Comparative bioavailability of L-683,453, a 5a-reductase inhibitor, from a self-emulsifying drug delivery system in Beagle dogs. Int J Pharm 1996; 136(1-2):147-154.
55. Aungst BJ, Nguyen NH, Taylor NJ, Bindra DS. Formulation and food effects on the oral absorption of a poorly water-soluble, highly permeable antiretroviral agent. J Pharm Sci 2002; 91(6):1390-1395.
56. Humberstone AJ, Porter CJ, Charman WN. A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine. J Pharm Sci 1996; 85(5):525-529.
57. Charman WN, Porter CJ, Mithani S, Dressman JB. Physiochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J Pharm Sci 1997; 86(3):269-282.
58. Pope DG. Accelrated stability testing for prediction of drug product stability. Drug Cosmetic Industry 1980; 1276:48-116.
59. Gursoy N, Garrigue JS, Razafindratsita A, Lambert G, Benita S. Excipient effects on in vitro cytotoxicity of a novel paclitaxel self-emulsifying drug delivery system. J Pharm Sci 2003; 92(12):2411-2418.
60. Kommuru TR, Gurley B, Khan MA, Reddy IK. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int J Pharm 2001; 212(2):233-246.
61. Kovarik JM, Mueller EA, van Bree JB, Tetzloff W, Kutz K. Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation. J Pharm Sci 1994; 83(3):444-446.
62. O'Driscoll CM. Lipid-based formulations for intestinal lymphatic delivery. Eur J Pharm Sci 2002; 15(5):405-415.
63. Attwood D. Microemulsions. In: Kreutted J, ed, Colloid Drug Delivery Systems, 1st ed. New York: Marcel Dekker Inc., 1994:31-71.
64. Wu AL, Clark SB, Holt PR. Transmucosal triglyceride transport rates in proximal and distal rat intestine in vivo. J Lipid Res 1975; 16(4):251-257.
65. Charman WN, Stella VJ. Effect of lipid class and lipid vehicle volume on the intestinal lymphatic transport of DDT. Int J Pharm 1986; 33(1-3):165-172.
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