-
1
-
-
0034002261
-
Role of the development scientist in compound lead selection and optimization
-
DOI 10.1002/(SICI)1520-6017(200002)89:2<145::AID-JPS2>3.0.CO;2-6
-
S. Venkatesh, and R.A. Lipper Role of the development scientist in compound lead selection and optimization J. Pharm. Sci. 89 2000 145 154 (Pubitemid 30120795)
-
(2000)
Journal of Pharmaceutical Sciences
, vol.89
, Issue.2
, pp. 145-154
-
-
Venkatesh, S.1
Lipper, R.A.2
-
2
-
-
0031024171
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
DOI 10.1016/S0169-409X(96)00423-1, PII S0169409X96004231
-
C.A. Lipinski, F. Lombardo, B.W. Dominy, and P.J. Feeney Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings Adv. Drug Deliv. Rev. 23 1997 3 25 (Pubitemid 27046991)
-
(1997)
Advanced Drug Delivery Reviews
, vol.23
, Issue.1-3
, pp. 3-25
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
3
-
-
0030614844
-
Physicochemical and physiological mechanisms for the effects of food on drug absorption: The role of lipids and pH
-
DOI 10.1021/js960085v
-
W.N. Charman, C.J. Porter, S. Mithani, and J.B. Dressman Physiochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH J. Pharm. Sci. 86 1997 269 282 (Pubitemid 27113759)
-
(1997)
Journal of Pharmaceutical Sciences
, vol.86
, Issue.3
, pp. 269-282
-
-
Charman, W.N.1
Porter, C.J.H.2
Mithani, S.3
Dressman, J.B.4
-
4
-
-
77956847917
-
Recent advances in the generation of molecular diversity
-
(Chapter 33)
-
W.H. Moos, and G.D. Green Recent advances in the generation of molecular diversity Annu. Rep. Med. Chem. 28 1993 315 324 (Chapter 33)
-
(1993)
Annu. Rep. Med. Chem.
, vol.28
, pp. 315-324
-
-
Moos, W.H.1
Green, G.D.2
-
5
-
-
0000122370
-
Applications of small-molecule combinatorial chemistry to drug discovery
-
DOI 10.1016/1359-6446(96)89062-3
-
D.V. Patel, and E.M. Gordon Applications of small molecule combinatorial chemistry to drug discovery Drug Discov. Today 1 1996 134 144 (Pubitemid 126402198)
-
(1996)
Drug Discovery Today
, vol.1
, Issue.4
, pp. 134-144
-
-
Patel, D.V.1
Gordon, E.M.2
-
6
-
-
0021745755
-
Functional group contributions to drug-receptor interactions
-
DOI 10.1021/jm00378a021
-
P.R. Andrews, D.J. Craik, and J.L. Martin Functional group contributions to drug-receptor interactions J. Med. Chem. 27 1984 1648 1657 (Pubitemid 15177908)
-
(1984)
Journal of Medicinal Chemistry
, vol.27
, Issue.12
, pp. 1648-1657
-
-
Andrews, P.R.1
Craik, D.J.2
Martin, J.L.3
-
7
-
-
1042287180
-
Drug polymorphism and dosage form design: A practical perspective
-
DOI 10.1016/j.addr.2003.10.008
-
D. Singhal, and W. Curatolo Drug polymorphism and dosage form design: a practical perspective Adv. Drug Deliv. Rev. 56 2004 335 347 (Pubitemid 38201429)
-
(2004)
Advanced Drug Delivery Reviews
, vol.56
, Issue.3
, pp. 335-347
-
-
Singhal, D.1
Curatolo, W.2
-
8
-
-
0033805179
-
In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs
-
J.B. Dressman, and C. Reppas In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs J. Eur. Pharm. Sci. 11 Suppl. 2 2000 73 80
-
(2000)
J. Eur. Pharm. Sci.
, vol.11
, Issue.SUPPL. 2
, pp. 73-80
-
-
Dressman, J.B.1
Reppas, C.2
-
9
-
-
12844283957
-
High-throughput drug discovery: What can we expect from HTS?
-
DOI 10.1016/S1359-6446(04)03275-1, PII S1359644604032751
-
P. Gribbon, and A. Sewing High-throughput drug discovery: what can we expect from HTS? Drug Discov. Today 10 2005 17 22 (Pubitemid 40164815)
-
(2005)
Drug Discovery Today
, vol.10
, Issue.1
, pp. 17-22
-
-
Gribbon, P.1
Andreas, S.2
-
10
-
-
36549042006
-
Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs
-
DOI 10.1016/j.drudis.2007.09.005, PII S1359644607003753
-
T. Vasconcelos, B. Sarmento, and P. Costa Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs Drug Discov. Today 12 2007 1068 1075 (Pubitemid 350186132)
-
(2007)
Drug Discovery Today
, vol.12
, Issue.23-24
, pp. 1068-1075
-
-
Vasconcelos, T.1
Sarmento, B.2
Costa, P.3
-
11
-
-
58049193000
-
Microemulsions: A novel approach to enhanced drug delivery
-
S. Talegaonkar, A. Azeem, F.J. Ahmad, R.K. Khar, S.A. Pathan, and Z.I. Khan Microemulsions: a novel approach to enhanced drug delivery Recent Pat. Drug Deliv. Formul. 2 2008 238 257
-
(2008)
Recent Pat. Drug Deliv. Formul.
, vol.2
, pp. 238-257
-
-
Talegaonkar, S.1
Azeem, A.2
Ahmad, F.J.3
Khar, R.K.4
Pathan, S.A.5
Khan, Z.I.6
-
12
-
-
79960609478
-
-
Tripos, St. Louis, MO, Biobyte Software ClogP/CRMTM
-
Tripos, St. Louis, MO, Biobyte Software ClogP/CRMTM.
-
-
-
-
13
-
-
0034609833
-
Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties
-
P. Ertl, and B. Rohde Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties J. Med. Chem. 43 2000 3714 3717
-
(2000)
J. Med. Chem.
, vol.43
, pp. 3714-3717
-
-
Ertl, P.1
Rohde, B.2
-
14
-
-
37749011993
-
Epik: A software program for pK(a) prediction and protonation state generation for drug-like molecules
-
J.C. Shelley, A. Cholleti, L.L. Frye, J.R. Greenwood, M.R. Timlin, and M. Uchimaya Epik: a software program for pK(a) prediction and protonation state generation for drug-like molecules J. Comput. Aided Mol. Des. 21 2007 681 691
-
(2007)
J. Comput. Aided Mol. Des.
, vol.21
, pp. 681-691
-
-
Shelley, J.C.1
Cholleti, A.2
Frye, L.L.3
Greenwood, J.R.4
Timlin, M.R.5
Uchimaya, M.6
-
16
-
-
84856604841
-
-
adopted July 27 1995 (last accessed 10.08.10)
-
OECD Guideline for the Testing of Chemicals, 107, adopted July 27 1995 (last accessed 10.08.10). < http://www.oecd.org/dataoecd/17/35/1948169. pdf>.
-
OECD Guideline for the Testing of Chemicals
, vol.107
-
-
-
18
-
-
62649166527
-
PDE2A reporter cell line: Characterization of the cellular activity of PDE inhibitors
-
F. Wunder, M.J. Gnoth, A. Geerts, D. Barufe, and A. Novel PDE2A reporter cell line: characterization of the cellular activity of PDE inhibitors Mol. Pharm. 6 2008 326 336
-
(2008)
Mol. Pharm.
, vol.6
, pp. 326-336
-
-
Wunder, F.1
Gnoth, M.J.2
Geerts, A.3
Barufe, D.4
Novel, A.5
-
20
-
-
0033973754
-
Caco-2 versus Caco-2/HT29-MTX co-cultured cell lines: Permeabilities via diffusion, inside- and outside-directed carrier-mediated transport
-
DOI 10.1002/(SICI)1520-6017(200001)89:1<63::AID-JPS7>3.0.CO;2-6
-
C. Hilgendorf, H. Spahn-Langguth, C.G. Regardh, E. Lipka, G.L. Amidon, and P. Langguth Caco-2 versus Caco-2/HT29-MTX co-cultured cell lines: permeabilities via diffusion, inside- and outside-directed carrier-mediated transport J. Pharm. Sci. 89 2000 63 75 (Pubitemid 30080155)
-
(2000)
Journal of Pharmaceutical Sciences
, vol.89
, Issue.1
, pp. 63-75
-
-
Hilgendorf, C.1
Spahn-Langguth, H.2
Regardh, C.G.3
Lipka, E.4
Amidon, G.L.5
Langguth, P.6
-
21
-
-
0030990079
-
In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man - Fact or myth
-
DOI 10.1023/A:1012102522787
-
S. Yee In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man-fact or myth Pharm. Res. 14 1997 763 766 (Pubitemid 27281671)
-
(1997)
Pharmaceutical Research
, vol.14
, Issue.6
, pp. 763-766
-
-
Yee, S.1
-
22
-
-
0037122748
-
Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates
-
DOI 10.1021/jm010152k
-
K. Mandagere, T.N. Thompson, and K.K. Hwang Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates J. Med. Chem. 45 2002 304 311 (Pubitemid 34073449)
-
(2002)
Journal of Medicinal Chemistry
, vol.45
, Issue.2
, pp. 304-311
-
-
Mandagere, A.K.1
Thompson, T.N.2
Hwang, K.-K.3
-
23
-
-
31344451056
-
Development and evaluation of an in vitro method for prediction of human drug absorption: II. Demonstration of the method suitability
-
DOI 10.1016/j.ejps.2005.11.005, PII S0928098705003350
-
G. Corti, F. Maestrelli, M. Cirri, N. Zerrouk, and P. Mura Development and evaluation of an in vitro method for prediction of human drug absorption. II. Demonstration of the method suitability Eur. J. Pharm. Sci. 27 2006 354 362 (Pubitemid 43143261)
-
(2006)
European Journal of Pharmaceutical Sciences
, vol.27
, Issue.4
, pp. 354-362
-
-
Corti, G.1
Maestrelli, F.2
Cirri, M.3
Zerrouk, N.4
Mura, P.5
-
24
-
-
1242337282
-
The "High Solubility" Definition of the Current FDA Guidance on Biopharmaceutical Classification System May Be Too Strict for Acidic Drugs
-
DOI 10.1023/B:PHAM.0000016242.48642.71
-
M. Yazdanian, K. Briggs, C. Jankowsky, and A. Hawi The "high solubility" definition of the current FDA guidance on biopharmaceutical classification system may be too strict for acidic drugs Pharm. Res. 21 2004 293 299 (Pubitemid 38221975)
-
(2004)
Pharmaceutical Research
, vol.21
, Issue.2
, pp. 293-299
-
-
Yazdanian, M.1
Briggs, K.2
Jankovsky, C.3
Hawi, A.4
-
25
-
-
3142687675
-
Fluvastatin: Clinical and safety profile
-
DOI 10.2165/00003495-200464120-00004
-
A. Corsini, T.A. Jacobson, and C.M. Ballantyne Fluvastatin: clinical and safety profile Drugs 64 2004 1305 1323 (Pubitemid 38916344)
-
(2004)
Drugs
, vol.64
, Issue.12
, pp. 1305-1323
-
-
Corsini, A.1
Jacobson, T.A.2
Ballantyne, C.M.3
-
26
-
-
0027134778
-
Mechanism of intestinal absorption of ranitidine and ondansetron: Transport across Caco-2 cell monolayers
-
DOI 10.1023/A:1018965929419
-
L.S. Gan, P.H. Hsyu, J.F. Pritchard, and D. Thakker Mechanism of intestinal absorption of ranitidine and ondansetron: transport across Caco-2 cell monolayers Pharm. Res. 10 1993 1722 1725 (Pubitemid 24000355)
-
(1993)
Pharmaceutical Research
, vol.10
, Issue.12
, pp. 1722-1725
-
-
Gan, L.-S.1
Hsyu, P.-H.2
Pritchard, J.F.3
Thakker, D.4
-
27
-
-
0034031969
-
Optimized conditions for prediction of intestinal drug permeability using Caco-2 cells
-
DOI 10.1016/S0928-0987(00)00076-2, PII S0928098700000762
-
S. Yamashita, T. Furubayashi, M. Kataoka, T. Sakane, H. Sezaki, and H. Tokuda Optimized conditions for prediction of intestinal drug permeability using Caco-2 cells Eur. J. Pharm. Sci. 10 2000 195 204 (Pubitemid 30190095)
-
(2000)
European Journal of Pharmaceutical Sciences
, vol.10
, Issue.3
, pp. 195-204
-
-
Yamashita, S.1
Furubayashi, T.2
Kataoka, M.3
Sakane, T.4
Sezaki, H.5
Tokuda, H.6
-
28
-
-
72449122816
-
Measurement and prediction of oral absorption
-
J. Keldenich Measurement and prediction of oral absorption Chem. Biodivers. 6 2009 2000 2013
-
(2009)
Chem. Biodivers.
, vol.6
, pp. 2000-2013
-
-
Keldenich, J.1
-
29
-
-
3242778534
-
A physiological model for the estimation of the fraction dose absorbed in humans
-
DOI 10.1021/jm030999b
-
S. Willmann, W. Schmitt, J. Keldenich, J. Lippert, and J.B. Dressman A physiological model for the estimation of the fraction dose absorbed in humans J. Med. Chem. 47 2004 4022 4031 (Pubitemid 38970963)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.16
, pp. 4022-4031
-
-
Willmann, S.1
Schmitt, W.2
Keldenich, J.3
Lippert, J.4
Dressman, J.B.5
-
30
-
-
34250769986
-
Improvement of the oral drug absorption of topotecan through the inhibition of intestinal xenobiotic efflux transporter, breast cancer resistance protein, by excipients
-
DOI 10.1124/dmd.106.014217
-
T. Yamagata, H. Kusuhara, M. Morishita, K. Takayama, H. Benameur, and Y. Sugiyama Improvement of the oral drug absorption of topotecan through the inhibition of intestinal xenobiotic efflux transporter, breast cancer resistance protein, by excipients Drug Metab. Dispos. 35 2007 1142 1148 (Pubitemid 46956435)
-
(2007)
Drug Metabolism and Disposition
, vol.35
, Issue.7
, pp. 1142-1148
-
-
Yamagata, T.1
Kusuhara, H.2
Morishita, M.3
Takayama, K.4
Benameur, H.5
Sugiyama, Y.6
-
31
-
-
79960578455
-
In vitro and in vivo evaluation of pharmaceutical excipients: Interaction potential with biological barriers
-
November 2005, Nashville (M1135)
-
J. Schulze, A. Sacher, T. Backensfeld, A. Reichel, P. Lienau, In vitro and in vivo evaluation of pharmaceutical excipients: interaction potential with biological barriers, 2005 AAPS Annual Meeting and Exposition, November 2005, Nashville (M1135).
-
2005 AAPS Annual Meeting and Exposition
-
-
Schulze, J.1
Sacher, A.2
Backensfeld, T.3
Reichel, A.4
Lienau, P.5
-
32
-
-
0027275566
-
Physicological parameters in laboratory animals and humans
-
B. Davies, and T. Morris Physicological parameters in laboratory animals and humans Pharm. Res. 10 1993 1093 1099
-
(1993)
Pharm. Res.
, vol.10
, pp. 1093-1099
-
-
Davies, B.1
Morris, T.2
-
33
-
-
0029055473
-
Comparison of the gastrointestinal anatomy, physiology and biochemistry of humans and commonly used laboratory animals
-
T.T. Kararli Comparison of the gastrointestinal anatomy, physiology and biochemistry of humans and commonly used laboratory animals Biopharm. Drug Dispos. 16 1995 351 380
-
(1995)
Biopharm. Drug Dispos.
, vol.16
, pp. 351-380
-
-
Kararli, T.T.1
-
34
-
-
0031786518
-
Linear correlation of the fraction of oral dose absorbed of 64 drugs between humans and rats
-
DOI 10.1023/A:1011981317451
-
W.L. Chiou, and A. Barve Linear correlation of the fraction of oral dose absorbed of 64 drugs between humans and rat Pharm. Res. 15 1998 1792 1795 (Pubitemid 28524594)
-
(1998)
Pharmaceutical Research
, vol.15
, Issue.11
, pp. 1792-1795
-
-
Chiou, W.L.1
Barve, A.2
-
35
-
-
0004116615
-
-
Lewis Publisher, Chelsea, MI
-
E.J. Calabrese, Table 33.9, Principles of animal extrapolation, Lewis Publisher, Chelsea, MI, 1991.
-
(1991)
Table 33.9, Principles of Animal Extrapolation
-
-
Calabrese, E.J.1
-
36
-
-
34447337731
-
Prediction of human pharmacokinetics-gastrointestinal absorption
-
U. Fagerholm Prediction of human pharmacokinetics-gastrointestinal absorption J. Pharm. Pharmacol. 59 2007 905 916
-
(2007)
J. Pharm. Pharmacol.
, vol.59
, pp. 905-916
-
-
Fagerholm, U.1
-
37
-
-
0022070123
-
Absorption potential: Estimating the fraction absorbed for orally administered drugs
-
J.B. Dressman, G.L. Amidon, and G.L. Fleisher Absorption potential: estimating the fraction absorbed for orally administered drugs J. Pharm. Sci. 74 1985 588 589
-
(1985)
J. Pharm. Sci.
, vol.74
, pp. 588-589
-
-
Dressman, J.B.1
Amidon, G.L.2
Fleisher, G.L.3
-
38
-
-
0027473738
-
Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: A mathematical model
-
DOI 10.1023/A:1018947113238
-
D.-M. Oh, R.M. Curl, and G.L. Amidon Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: a mathematical model Pharm. Res. 10 1993 264 270 (Pubitemid 23041742)
-
(1993)
Pharmaceutical Research
, vol.10
, Issue.2
, pp. 264-270
-
-
Oh, D.-M.1
Curl, R.L.2
Amidon, G.L.3
-
39
-
-
3242728351
-
Molecular properties of WHO essential drugs and provisional biopharmaceutical classification
-
N.A. Kasim, M. Whitehouse, C. Ramachandran, M. Bermejo, H. Lennernäs, A.S. Hussain, H.E. Junginger, S.A. Stavchansky, K.K. Midha, V.P. Shah, and G.L. Amidon Molecular properties of WHO essential drugs and provisional biopharmaceutical classification Mol. Pharm. 1 2004 5 96
-
(2004)
Mol. Pharm.
, vol.1
, pp. 5-96
-
-
Kasim, N.A.1
Whitehouse, M.2
Ramachandran, C.3
Bermejo, M.4
Lennernäs, H.5
Hussain, A.S.6
Junginger, H.E.7
Stavchansky, S.A.8
Midha, K.K.9
Shah, V.P.10
Amidon, G.L.11
-
40
-
-
0035292910
-
Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract
-
D. Hörter, and J.B. Dressman Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract Adv. Drug Deliv. Rev. 46 2001 75 87
-
(2001)
Adv. Drug Deliv. Rev.
, vol.46
, pp. 75-87
-
-
Hörter, D.1
Dressman, J.B.2
-
41
-
-
1842689072
-
Pharmaceutical evaluation of early development candidates "the 100 mg-approach"
-
DOI 10.1016/j.ijpharm.2004.01.034, PII S0378517304000699
-
S. Balbach, and C. Korn Pharmaceutical evaluation of early development candidates; the 100 mg-approach Int. J. Pharm. 275 2004 1 12 (Pubitemid 38481515)
-
(2004)
International Journal of Pharmaceutics
, vol.275
, Issue.1-2
, pp. 1-12
-
-
Balbach, S.1
Korn, C.2
-
42
-
-
51649104303
-
Towards quantitative prediction of oral drug absorption
-
J.B. Dressman, K. Thelen, and E. Jantratid Towards quantitative prediction of oral drug absorption Clin. Pharmacokin. 47 2008 655 667
-
(2008)
Clin. Pharmacokin.
, vol.47
, pp. 655-667
-
-
Dressman, J.B.1
Thelen, K.2
Jantratid, E.3
|