Absorption Rate Limit Considerations for Oral Phosphate Prodrugs

作者: Tycho Heimbach , Doo-Man Oh , Lilian Y Li , Markus Forsberg , Jouko Savolainen

DOI: 10.1023/A:1023827017224

关键词:

摘要: Purpose. To evaluate the potential of phosphate ester prodrugs to significantly improve absorptive flux poorly soluble parent drugs.

参考文章(32)
Albert S. Kearney, Valentine J. Stella, The in vitro enzymic labilities of chemically distinct phosphomonoester prodrugs. Pharmaceutical Research. ,vol. 9, pp. 497- 503 ,(1992) , 10.1023/A:1015840329786
Bruce J Aungst, Nhung H Nguyen, James P Bulgarelli, Kristi Oates-Lenz, The Influence of Donor and Reservoir Additives on Caco-2 Permeability and Secretory Transport of HIV Protease Inhibitors and Other Lipophilic Compounds Pharmaceutical Research. ,vol. 17, pp. 1175- 1180 ,(2000) , 10.1023/A:1026402410783
Gordon L. Amidon, Hans Lennernäs, Vinod P. Shah, John R. Crison, A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability Pharmaceutical Research. ,vol. 12, pp. 413- 420 ,(1995) , 10.1023/A:1016212804288
David Fleisher, Neel Sheth, Heidi Griffin, Martin McFadden, Gregory Aspacher, Nutrient influences on rat intestinal phenytoin uptake. Pharmaceutical Research. ,vol. 6, pp. 332- 337 ,(1989) , 10.1023/A:1015906726365
M. A. Boogaerts, A. Van Hoof, D. Catovsky, M. Kovacs, M. Montillo, P. L. Zinzani, J. L. Binet, W. Feremans, R. Marcus, F. Bosch, G. Verhoef, M. Klein, Activity of oral fludarabine phosphate in previously treated chronic lymphocytic leukemia. Journal of Clinical Oncology. ,vol. 19, pp. 4252- 4258 ,(2001) , 10.1200/JCO.2001.19.22.4252
V Phung-Ba, A Warnery, P Wils, S Legrain, D Scherman, High lipophilicity decreases drug transport across intestinal epithelial cells. Journal of Pharmacology and Experimental Therapeutics. ,vol. 269, pp. 654- 658 ,(1994)
Peter Rohdewald, Helmut Möllmann, Jürgen Barth, Jörg Rehder, Hartmut Derendorf, Pharmacokinetics of dexamethasone and its phosphate ester. Biopharmaceutics & Drug Disposition. ,vol. 8, pp. 205- 212 ,(1987) , 10.1002/BDD.2510080302
Yasushi MATSUNAGA, Ryoko OHTA, Nobuyuki BANDO, Hiroaki YAMADA, Hiroshi YUASA, Yoshio KANAYA, Effects of Water Content on Physical and Chemical Stability of Tablets Containing an Anticancer Drug TAT-59. Chemical & Pharmaceutical Bulletin. ,vol. 41, pp. 720- 724 ,(1993) , 10.1248/CPB.41.720
Lilian Y. Li, Gordon L. Amidon, Jae Seung Kim, Tycho Heimbach, Filippos Kesisoglou, John T. Topliss, David Fleisher, Intestinal Metabolism Promotes Regional Differences in Apical Uptake of Indinavir: Coupled Effect of P-Glycoprotein and Cytochrome P450 3A on Indinavir Membrane Permeability in Rat Journal of Pharmacology and Experimental Therapeutics. ,vol. 301, pp. 586- 593 ,(2002) , 10.1124/JPET.301.2.586
Jouko Savolainen, Markus Forsberg, Hannu Taipale, Pekka T. M�nnist�, Kristiina J�rvinen, Jukka Gynther, Pekka Jarho, Tomi J�rvinen, Effects of aqueous solubility and dissolution characteristics on oral bioavailability of entacapone Drug Development Research. ,vol. 49, pp. 238- 244 ,(2000) , 10.1002/1098-2299(200004)49:4<238::AID-DDR2>3.0.CO;2-V