Modeling gastrointestinal drug absorption requires more in vivo biopharmaceutical data: Experience from in vivo dissolution and permeability studies in humans

Current Drug Metabolism

Volumn 8, Issue 7, 2007, Pages 645-657

  Lennernäs, Hans ^a  

^a UPPSALA UNIVERSITY   (Sweden)

Author keywords

Bioavailability; Bioequivalence; Intestinal permeability; QSAR models; Solubilization

Indexed keywords

AMILORIDE; AMOXICILLIN; ATENOLOL; CARBAMAZEPINE; CEFALEXIN; CIMETIDINE; CYCLOSPORIN; DANAZOL; DESIPRAMINE; ENALAPRIL MALEATE; ENALAPRILAT; FELODIPINE; FEXOFENADINE; FLUINDOSTATIN; FUROSEMIDE; GRISEOFULVIN; HYDROCHLOROTHIAZIDE; INOGATRAN; ISOTRETINOIN; KETOPROFEN; LEVODOPA; LISINOPRIL; LOSARTAN POTASSIUM; METHYLDOPA; METOPROLOL; NAPROXEN; PHENAZONE; PROBUCOL; UBIQUINONE; UNINDEXED DRUG;

DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG METABOLISM; DRUG PENETRATION; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG TRANSPORT; EUROPE; FIRST PASS EFFECT; FOOD; FOOD DRUG INTERACTION; FOOD INTAKE; GASTROINTESTINAL ABSORPTION; GASTROINTESTINAL TRANSIT; HUMAN; IN VITRO STUDY; IN VIVO STUDY; INTESTINE FLUID; INTESTINE MUCOSA PERMEABILITY; LIPOPHILICITY; MODEL; PHYSICAL CHEMISTRY; REVIEW; SIMULATION; UNITED STATES;

ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; DRUG DESIGN; HUMANS; INTESTINAL ABSORPTION; INTESTINES; MODELS, BIOLOGICAL; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; SOLUBILITY;

EID: 35348860160     PISSN: 13892002     EISSN: None     Source Type: Journal    
DOI: 10.2174/138920007782109823     Document Type: Review

References (129)

1. Kola, I. and Landis, I (2004) Nat. Rev. Drug Discov., 3, 711-716.
2. Van, de, Waterbeemd, H.; Gifford, E. (2003) Nat. Rev. Drug Discov., 2, 192-204.
3. Schmid, E.F. and Smith, D.A. (2006) Drug Discov. Today, 11(17-18), 775-94.
4. Skold, C.; Winiwarter, S.; Wernevik, J.; Bergstrom, F.; Engstrom, L.; Allen, R.; Box, K.; Comer, J.; Mole, J.; Hallberg, A.; Lennernas, H.; Lundstedt T.; Ungell, A.L. and Karlen, A. (2006) J. Med. Chem., 16, 49(23), 6660-71.
5. Westergren, J.; Lindfors, L.; Hoglund, T.; Luder, K.; Nordholm, S. and Kjellander, R. (2007) J. Phys. Chem. B, 22, 111(7), 1872-82.
6. Winiwarter, S.; Bonham, N., M.; Ax, F.; Hallberg, A.; Lennernaes, H. and Karlen, A. (1998) J. Med. Chem., 41, 4939-4949.
7. Palm, K.; Stenberg, P.; Luthman, K. and Artursson, P. (1997) Pharm. Res., 14, 568-571.
8. Bergstroem, C.A.S.; Wassvik, C.M.; Norinder, U.; Luthman, K. and Artursson, P. 42004) J. Chem. Inf. Comput. Sci., 44, 1477-1488.
9. Afzelius, L.; Zamora, I.; Masimirembwa, C., M.; Karlen, A.; Andersson, T., B.; Mecucci, S.; Baroni, M. and Cruciani, G. (2004) J. Med. Chem., 47, 907-914.
10. Kratochwil, N.A.; Huber, W.; Muller, F.; Kansy, M. and Gerber, P., R. (2002) Biochem. Pharmacol., 64, 1355-1374.
11. Afzelius, L.; Arnby, C.H.; Broo, A.; Carlsson, L.; Isaksson, C.; Jurva, U.; Kjellander, B.; Kolmodin, K.; Nilsson, K.; Raubacher, F. and Weidolf, L. (2007) Drug Metab. Rev., 39(1), 61-86
12. Mager, D.E. (2006) Adv. Drug Deliv. Rev., 30, 58 (12-13), 1326-56.
13. Luder, K.; Lindfors, L.; Westergren, J.; Nordholm, S. and Kjellander, R. (2007), J. Phys. Chem. B., 22, 111 (7), 1883-92.
14. Amidon, G.L.; Lennemas, H.; Shah, V.P. and Crison, J.R. (1995) Pharm. Res., 12, 413-420.
15. Lennernas, H. and Abrahamsson, B. (2005) J. Pharm. Pharmacol., 57, 273-285.
16. Dressman, J.B. and Fleisher, D. (1986) J. Pharm. Sci., 75(2), 109-116.
17. Sinko, P.J.; Leesman, G.D. and Amidon, G.L. (1991) Pharm. Res., 8, 979-988.
18. Yu, L.X.; Crison, J.R. and Amidon, G.L. (1996) Int. J. Pharmaceut., 140 (1), 111-118.
19. CDER, Waiver, of, in vivo, bioavailability, and bioequivalence, studies, for, immidiate-release, solid, oral, dosage, forms, based, on, a, biopharmaceutics, classification, system; Food, and Drug, Administration, 2000.
20. CPMP, Note for Guidance on the Investigation of bioavailability and bioequivalence (CPMP/EWP/QWP/1401/98); The, European, Agency, for, the, Evaluation, of, Medicinal, Products, 2001.
21. Yu, L.X.; Amidon, G.L.; Polli, J.E.; Zhao, H, Mehra, M.U.; Conner, D.P.; Shah, V.P.; Lesko, L.J.; Chen, M.L.; Lee, V.H. and Hussain, A.S. (2002) Pharm. Res., 19, 921-925.
22. Rekhi, G.S.; Eddington, N.D.; Fossler, M.J.; Schwartz, P.; Lesko, L.J. and Augsburger, L.L. (1997) Pharm. Dev. Technol., 2, 11-24.
23. Rowland M.; Tozer, T., N. (1995) In, Clinical Pharmacokinetics: Concepts and Applications; 3rd, ed., Williams, &, Wilkins:, Philadelphia, 1995; chapter, 9, pp. 119-134.
24. Wu, C.Y.; Benet, L.Z.; Hebert, M.F.; Gupta, S.K.; Rowland M.; Gomez, D.Y.; Wacher, V.J. (1995) Clin. Pharmacol. Ther., 58, 492-497.
25. Lindahl, A.; Sandstrom, R.; Ungell, A.L.; Abrahamsson, B.; Knutson, T.W.; Knutson, L. and Lennernas, H. (1996) Clin. Pharmacol. Ther., 60 (5), 493-503.
26. Lennernäs, H (1998) J. Pharm. Sci., 87, 403-410.
27. Benet, L-Z.; Cummins, C.L. and Wu, C.Y. (2004) Int. J. Pharm., 11 (277), 3-9.
28. Wu, C.Y. and Benet, L.Z. (2005) Pharm. Res., 22 (1), 11-23.
29. Naritomi, Y.; Terashita, S.; Kagayama, A. and Sugiyama, Y. (2003) Drug Metab. Dispos., 31(5), 580-8.
30. Galetin, A.; Houston, J.B. (2006) J. Pharmacol. Exp. Ther., 318(3), 1220-9.
31. Nakamura, T.; Sakaeda, T.; Ohmoto, N.; Tamura, T.; Aoyama, N.; Shirakawa, T.; Kamigaki, T.; Nakamura, T.; Kim, K.I.; Kim, S.R.; Kuroda, Y.; Matsuo, M.; Kasuga, M., and Okumura, K. (2002) Drug Metab. Dispos., 30, 4-6.
32. Berggren, S.; Lennermäs, P.; Ekelund, M.; Weström, B.; Hoogstraate, J. and Lennernäs, H. (2003) J. Pharm. Pharmacol., 55, 963-972.
33. de, Waziers, I.; Cugnenc, P.H.; Yang, C.S.; Leroux, J.P. and Beaune, P.H. (1990) J. Pharmacol. Exp. Ther., 253, 387-394.
34. Berggren, S.; Gall, C.; Wollnitz, N.; Ekelund, M.; Karlbom, U, Hoogstraate, J.; Schrenk, D. and Lennernas,, H. (2007) Mol. Pharm., 2 (4) 252-257.
35. Englund, G.; Rorsman, F.; Ronnblom, A.; Kailbom, U.; Lazorova, L.; Graajo, J., Kindmark, A. and Artursson, P. (2006) Eur. J. Pharm. Sci., 29(3-4), 269-77.
36. Goldin, B.R. (1990) Ann. Med 22, 43-48.
37. Chandra, P. and Brouwer, K.L. (2004) Pharm. Res., 21, 719-735.
38. Tannergren, C.; Petri, N.; Knutson, L.; Hedeland M.; Bondesson, U. and Lennernas, H., (2003) Clin. Pharmacol. Ther., 74, 423-436.
39. Bonlokke, L.; Hovgaard, L.; Kristensen, HG.; Knutson, L. and Lennernas, H. (2001) Eur. J. Pharm. Sci., 12, 239-250.
40. Kossena, G.A.; Charman, W.N.; Boyd, R.J.; Dunstan, D.E. and, Porter, C.J. (2004) J. Pharm. Sci, 93, 332-348.
41. Porter, C.J.; Kaukonen, A.M.; Taillardat-Bertschinger, A.; Boyd, B.J.; O'Connor, J.M.; Edwards, G.A. and Charman, W.N. (2004) J. Pharm. Sci., 93, 1110-1421.
42. Kostewicz, E.S.; Brauns, U.; Becker, R.; Pressman, J.B. (2002) Pharm. Res., 19, 345-349.
43. Persson, E.; Lofgren, L.; Hansson, G:, Abrahamsson, B.; Lennernas, H. and Nilsson, R. (2007) J. Lipid Res., 48(1), 242-51.
44. Persson, E.M.; Nilsson, R.G., Hansson, G.I.; Lofgren, L.J.; Liback, F.; Knutson, L.; Abrahamsson, B. and Lennermas, H. (2006) Pharm. Res., 23(4), 742-51.
45. Persson, E.M.; Gustafsson, A.S.; Carlsson, A.S.; Nilsson, R.G.; Knutson, L.; Forsell, P.; Hanisch, G.; Lennernas, H. and Abrahamsson, B. (2005) Pharm. Res., 22(12), 2141-51.
46. Weitschies, W.; Wedemeyer, R.S.; Kosch, O.; Fach, K.; Nagel, S.; Soderlind, E.; Trahms, L.; Abrahamsson, B. and Monnikes, H. (2005) J. Control. Release, 28 (108), 375-85.
47. Abrahamsson, B.; Pal, A.; Sjoberg, M.; Carlsson, M.; Laurell, E. and Brasseur, J.G. (2005) Pharm. Res., 22(8), 1215-26.
48. Abrahamsson, B.; Albery, T.; Eriksson, A.; Gustafsson, I. and Sjoberg, M. (2004) Eur. J. Pharm. Sci., 22(2-3), 165-72.
49. Balakrishnan, A.; Rege, B.D.; Amidon, G.L. and Polli, J.E. (2004) J. Pharm. Sci., 93(8), 2064-75.
50. Scholz, A.; Abrahamsson, B.; Diebold, S.M.; Kostewicz, E.; Polentarutti, B.I.; Ungell, A.L. and Dressman, J.B. (2002) Pharm. Res., 19 (1), 42-6.
51. Bonlokke, L.; Hovgaard, L.; Kristensen, H.G.; Knutson, L.; Lindahl, A. and Lennernas, H. (1999) Eur. J. Pharm. Sci., 8(1), 19-27.
52. Bonlokke, L.; Christensen, F.N.; Knutson, L.; Kristensen, H.G. and Lennernas, H. (1997) Pharm. Res., 14(10), 1490-2.
53. Kalantzi, L.; Persson, E.; Polentarutti, B.; Abrahamsson, B.; Goumas, K.; Dressman, JB. and Reppas, C. (2006) Pharm. Res., 23(6), 1373-81.
54. Schiller, C.; Frohlich, C.P.; Giessmann, T.; Siegmund, W.; Monnikes, H.; Hosten, N. and Weitschies, W. (2005) Aliment. Pharmacol. Ther., 22(10), 971-9.
55. Higuchi, W.I.; Prakongpan, S.; Surpuriya, V. and Young, F. (1972) Science., 178, 633-4.
56. Hörter, D. and Dressmann, J.B. (1997) Adv. Drug Deliv. Rev., 25(1), 3-14.
57. Mithani, S., D., Bakatselou, V.; TenHoor, C.N.; Dressman, J.B. (1996) Pharm. Res., 13, 163-167.
58. Jack, D., B. (1992) Handbook of Clinical Pharmacokinetic Data; Macmillan, Publishers, Ltd:, Basingtoke.
59. Wassvik, C.M.; Holmen, A.G.; Bergstrom, C.A.; Zamora, I. and Artursson, P. (2006) Eur. J. Pharm. Sci., 29(3-4), 294-305.
60. Glaeser, H.; Bailey, D.G.; Dresser, G.K.; Gregor, J.C.; Schwarz, U.I.; McGrath, J.S.; Jolicoeur, E.; Lee, W.; Leake, B.F.; Tirona, R.G. and Kim, R.B. (2007) Clin. Pharmacol. Ther., 81 (3), 362-70.
61. Ho, R.H. and Kim, R.B. (2005) Clin. Pharmacol. Ther., 78 (3), 260-77.
62. Cao, X.; Gibbs, S.T.; Fang, L.; Miller, H.A.; Landowski, C.P.; Shin, H.C.; Lennernas, H.; Zhong, Y.; Amidon, G.L.; Yu, L.X. and Sun, D. (2006) Pharm. Res., 23 (8), 1675-86.
63. Oh, D.M.; Han, H.K. and Amidon, G.L., R (1999) Pharm. Biotechnol., 12, 59-88.
64. Benet, L.Z. and Cummins, C.L. (2001) Adv. Drug Deliv. Rev., 50, Suppl, 1, S3-11.
65. Borst, P. and Elferink, R.O. (2002) Ann. Rev. Biochem., 71, 537-92.
66. Suzuki, H. and Sugiyama, Y. (2000) Eur. J. Pharm. Sci., 12, 3-12.
67. Soldner, A.; Christians, U.; Susanto, M.; Wacher, V.J.; Silverman, J.A. et al. (1999) Pharm. Res., 16, 478-485.
68. Schwarz, U.I.; Gramatte, T.; Krappweis, J.; Oertel, R. and Kirch, W. (2000) Int. J. Clin. Pharmacol. Ther., 38, 161-167
69. Spahn-Langguth, H. and Langguth, P. (2001) Eur. J. Pharm. Sci., 4, 361-7.
70. Wacher, V.J.; Wu, C.Y. and Benet, L.Z. (1995) Mol. Carcinog., 13, 129-134.
71. Zhang, Y. and Benet, L. Z. (2001) Clin. Pharmacokinet., 40, 159-168.
72. van Zuylen, L.; Verweij, J.; Nooter, K.; Brouwer, E.; Stoter, G. and Sparreboom, A. (2000) Clin. Cancer Res., 7, 2598-603.
73. Hunter, J.; Hirst, B.H. and Simmons, N.L. (1993) Pharm. Res., 10, 743-749.
74. Kim, R.B.; Fromm, M.F.; Wandel, C.; Leake, B.; Wood, A.J,; Roden, DM. and Wilkinson, G.R. (1998) J. Clin. Invest., 15, 101, 289-94.
75. Fromm, M.F.; Kauffmann, H.M.; Fritz, P.; Burk; O.; Kroemer, H.K.; Warzok, R.W.; Eichelbaum, M.; Siegmund, W. and Schrenk, D. (2000) Am. J. Pathol., 157, 1575-1580.
76. Fricker, G. and Miller, D.S. (2002) Pharmacol. Toxicol., 90, 5-13.
77. Sandstrom, R.; Karlsson, A.; Knutson, L. and Lennernas, H. (1998) Pharm. Res., 15, 856-862.
78. Sandstrom, R.; Knutson, T., W.; Knutson, L.; Jansson, B. and Lennernas, H. (1999) Br. J. Clin. Pharmacol., 48, 180-189.
79. Chiou, W.L.; Chung, S.M.; Wu, T.C. and Ma, C. (2001) Int. J. Clin. Pharmacol. Ther., 39(3), 93-101.
80. Yu, L.X.; Amidon, G.L.; Polli, J.E.; Zhao, H.; Mehra, M.U.; Conner, D.P.; Shah, V.P.; Lesko, L.J.; Chen, M.L.; Lee, V.H. and Hussain, A.S. (2002) Pharm. Res., 19, 921-925.
81. Tucker, G.T.; Houston, J.B.; Huang, S.M. (2001) Br. J. Clin. Pharmacol., 52, 107-117
82. Gramatte, T. and Oertel, R. (1999) Clin. Pharmacol. Ther., 66, 239-245.
83. Lennernäs, H.; Ahrenstedt, Ö.; Hällgren, R.; Knutson, L.; Ryde, M. and Paalzow, L.K. (1992) Pharm. Res., 9, 1243-1251.
84. Ghibellini, G.; Leslie, E.M. and Brouwer, KL. (2006) Mol. Pharm., 3(3), 198-211.
85. Hedman, A.; Angelin, B.; Arvidsson, A.; Dahlqvist, R. and Nilsson, B. (1990) Clin. Pharmacol. Ther., 47(1), 20-6.
86. Hedman, A.; Angelin, B.; Arvidsson, A.; Beck, O.; Dahlqvist, R.; Nilsson, B.; Olsson, M. and Schenck-Gustafsson, K. (1991) Clin. Pharmacol. Ther., 49(3), 256-62.
87. Bergman, E.; Forsell, P.; Tevell, A.;Persson, E.M.; Hedeland M.; Bondesson, U.; Knutson, L. and Lennernäs, H. (2006) Eur. J. Pharm. Sci., 29, 205-14.
88. Lennernas, H. (1997) J. Pharm. Pharmacol., 49, 627-38.
89. Lennernas, H. (2003) J. Pharm. Pharmacol., 55, 429-33.
90. Lennernäs, H.; Palm, K.; Fagerholm, U. and Artursson. (1996) Int. J. Pharm., 127, 103-7.
91. Sun, D.; Lennernäs, H.; Welage, L.S.; Barnett, J.L.; Landowski, C.P.; Foster, D.; Fleisher, D.; Lee, K.-D. and Amidon, G.L. (2002) Pharm. Res., 19, 1400-16.
92. Bourdet, D.L. and Thakker, D.R. (2006) Pharm. Res., 23, 1165-77.
93. Bourdet, D.L.; Pollack, G.M. and Thakker, D.R. (2006) Pharm. Res., 23, 1178-87.
94. Kalvass, J.C. and Pollack, G.M. (2007) Pharm. Res., 24, 265-76.
95. Petri, N.; Tannergren, C.; Rungstad, D. and Lennernäs, H. (2004) Pharm. Res., 21, 1398-1404.
96. Kalvass, J.C.; Maurer, T.S. and Pollack, G.M. (2007) Drug Metab. Dispos., 35, 660-6.
97. Petri, N.; Tannergren, C.; Holst, B.; Mellon, F.A.; Bao, Y.; Plumb, G.W.; Bacon, J., O'Leary, K.A.; Kroon, P.A.; Knutson, L.; Forsell, P.; Eriksson, T.; Lennernas, H. and Williamson, G. (2003) Drug Metab. Dispos., 31, 805-13.
98. Tannergren, C.; Knutson, T.; Knutson, L. and Lennernas, H. (2003) Br. J. Clin. Pharmacol., 55, 182-90.
99. Zhang, L.; Strong, J.M.; Qiu, W.; Lesko, L.J. and Huang, S.M. (2006) Mol. Pharm., 3, 62-9.
100. Huang, S.M.; Temple, R.; Throckmorton, D.C. and Lesko, L.J. (2007) Clin. Pharmacol. Ther., 81, 298-304.
101. Rautio, J.; Humphreys, J.E.; Webster, L.O.; Balakrishnan, A.; Keogh, J.P.; Kunta, J.R.; Serabjit-Singh, C.J. and Polli, J.W. (2006) Drug Metab. Dispos., 34, 786-92
102. Steffansen, B. et al. (2004) Eur. J. Pharm. Sci., 21, 3-16
103. Ettmayer, P. et al. (2004)., J. Med. Chem., 47, 2393-404.
104. Tannergren, C.; Engman, H.; Knutson, L.; Hedeland M.; Bondesson, U. and Lennernas, H. (2004) Clin. Pharmacol. Ther., 75, 298-309.
105. Schwarz, U.I.; Hanso, H.; Oertel, R.; Miehlke, S.; Kuhlisch, E.; Glaeser, H.; Hitzl, M.; Dresser, G.K.; Kim, R.B. and Kirch, W. (2007) Clin. Pharmacol. Ther., Mar, 28;
106. Han, H. et al. (1998) Pharm. Res., 15, 1154-9.
107. Swaan, P.W. et al. (1998) Receptors Channels, 6, 189-200
108. Lannernäs, H.; Knutson, L.; Knutson, T.; Husssain, A.; Lesko, L.; Salmonson, T. and Amidon, G.L. (2002) Eur. J. Pharm. Sci., 15, 271-7.
109. Eriksson, B.I. et al. (2002) Thromb. Haemost., 87, 231-7.
110. Masimirembwa, C.M.; Bredberg, U. and Andersson, T.B. (2003) Clin. Pharmacokinet., 42, 515-28.
111. Rostami-Hodjegan, A. and Tucker, G.T. (2007) Nat. Rev. Drug Discov., 6, 140-8.
112. Kasim, N.A.; Whitehouse, M.; Ramachandran, C.; Bermejo, M.; Lennernäs, H.; Hussain, A.S.; Amidon, G.L. (2004) Mol. Pharm., 1, 85-96.
113. Lipinski, C.A.; Lombardo, F.; Dominy, B.W.; Feeney, P.J. (2001) Adv. Drug Deliv. Rev., 46, 3-26.
114. van de Waterbeemd, H. (1998) Eur. J. Pharm. Sci., 7, 1-3.
115. Winiwarter, S.; Ax, F.; Lennernäs, H.; Hallberg, A.; Pettersson, C.; Karlén, A.J. (2003) Mol. Graph. Model., 21, 283-287.
116. Bergstrom, C.A.; Norinder, U.; Luthman, K. and Artursson, P. (2003) J. Chem. Inf. Comput. Sci., 43, 1177-1185.
117. Fichert, T.; Yazdanian, M. and Proudfoot, J.R. (2003) Bioorg. Med. Chem. Lett., 13, 719-722.
118. Sanghvi, T.; Jain, N.; Yang, G. and Yalkowsky, S.H. (2003) QSAR Comb. Sci., 22, 258-262.
119. Agoram, B.; Woltosz, W.S. and Bolger, M.B. (2003) Adv. Drug Deliv. Rev., 50 (Suppl, 1), S41-S67.,,
120. Grass, G.M. and Sinko, P.J. (2002) Adv. Drug Deliv. Rev., 54, 433-451.
121. Rowland, M.; Balant, L. and Peck, C. (2004) Pharm. Sci, 6(l), E6.
122. Lindahl, A.; Sjöberg, Å.; Bredberg, U.; Toreson, H.; Ungell, A.L.; Lennernäs, H. (2004) Mol. Pharm., 1, 347-356.
123. Soderholm, J.D.; Olaison, G.; Kald, A.; Tagesson, C.; Sjodahl, R. (1997) Dig. Dis. Sci., 42, 853-857.
124. Fagerholm, U.; Borgström, L.; Ahrenstedt, Ö.; Lennernäs, H. (1995)J. Drug Target., 3, 191-200.
125. Lennernäs, H.; Nilsson, D.; Aquilonius, S-M.; Ahrenstedt, Ö.; Knutson, L.; Paalzow, L.K. (1992) Br. J. Clin. Pharmacol., 35, 243-250.
126. Lennernäs, H.; Ahrenstedt, Ö.; Ungell, A-L. (1994) Br. J. Clin. Pharmacol., 37, 589-596.
127. Nilsson, D.; Fagerholm, U.; Lennernäs, H. (1994) Pharm. Res., 11, 1540-1544.
128. Takamatsu, N.; Welage, L.S.; Liu, D.-Y.; Idkaidek, N.M.; Lee, P.I.-D.; Hayashi, Y.; Rhie, J.K.; Lennernäs, H.; Barnett, J.L.; Shah, V.P.; Lesko, L.; Amidon, G.L. (1997) Pharm. Res.. 14, 1127-1132.
129. Takamatsu, N.; Kim, O.-N.; Welage, L.S.; Idkaidek, N.M.; Lennernas, H.; Barnett, J.L.; Amidon, G.L. (2001) Pharm. Res., 18, 742-744.