-
1
-
-
77955915185
-
Strategies at the Interface of Drug Discovery and Development: Early Optimization of the Solid State Phase and Preclinical Toxicology Formulation for Potential Drug Candidates
-
Palucki, M.; Higgins, J.; Kwong, E.; Templeton, A. C. Strategies at the Interface of Drug Discovery and Development: Early Optimization of the Solid State Phase and Preclinical Toxicology Formulation for Potential Drug Candidates J. Med. Chem. 2010, 53, 5897-5905
-
(2010)
J. Med. Chem.
, vol.53
, pp. 5897-5905
-
-
Palucki, M.1
Higgins, J.2
Kwong, E.3
Templeton, A.C.4
-
2
-
-
84926658174
-
Strategic Use of Preclinical Pharmacokinetics Studies and in Vitro Models in optimizing ADME Properties of Lead Compounds
-
Borchardt, R. T. Hageman, M. J. Stevens, J. L. Kerns, E. H. Thakker, D. R. Springer: New York
-
Thakker, D. R. Strategic Use of Preclinical Pharmacokinetics Studies and In Vitro Models in optimizing ADME Properties of Lead Compounds. In Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "Drug-Like" Properties of Leads in Drug Discovery; Borchardt, R. T.; Hageman, M. J.; Stevens, J. L.; Kerns, E. H.; Thakker, D. R., Eds.; Springer: New York, 2006; pp 1-24.
-
(2006)
Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "drug-Like" Properties of Leads in Drug Discovery
, pp. 1-24
-
-
Thakker, D.R.1
-
3
-
-
84860777045
-
Case History-Use of ADME Studies for Optimization of Drug Candidates
-
Borchardt, R. T. Hageman, M. J. Stevens, J. L. Kerns, E. H. Thakker, D. R. Springer: New York
-
Gan, L.-S.; Lee, F. W.; Nelamangala, N.; Li, P.; Labutti, J.; Yin, W.; Xia, C.; Yang, H.; Uttamsingh, V.; Lu, C.; Pulsakar, S.; Daniels, J. S.; Huang, R.; Qian, M.; Wu, J.-T.; Cardoza, K.; Balani, S. K.; Miwa, G. T. Case History-Use of ADME Studies for Optimization of Drug Candidates. In Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "Drug-Like" Properties of Leads in Drug Discovery; Borchardt, R. T.; Hageman, M. J.; Stevens, J. L.; Kerns, E. H.; Thakker, D. R., Eds.; Springer: New York, 2006; pp 81-98.
-
(2006)
Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "drug-Like" Properties of Leads in Drug Discovery
, pp. 81-98
-
-
Gan, L.-S.1
Lee, F.W.2
Nelamangala, N.3
Li, P.4
Labutti, J.5
Yin, W.6
Xia, C.7
Yang, H.8
Uttamsingh, V.9
Lu, C.10
Pulsakar, S.11
Daniels, J.S.12
Huang, R.13
Qian, M.14
Wu, J.-T.15
Cardoza, K.16
Balani, S.K.17
Miwa, G.T.18
-
4
-
-
46949094595
-
Solubility, Solubilization and Dissolution in Drug Delivery during Lead Optimization
-
Borchardt, R. T. Hageman, M. J. Stevens, J. L. Kerns, E. H. Thakker, D. R. Springer: New York
-
Hageman, M. J. Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization. In Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "Drug-Like" Properties of Leads in Drug Discovery; Borchardt, R. T.; Hageman, M. J.; Stevens, J. L.; Kerns, E. H.; Thakker, D. R., Eds.; Springer: New York, 2006; pp 99-130.
-
(2006)
Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "drug-Like" Properties of Leads in Drug Discovery
, pp. 99-130
-
-
Hageman, M.J.1
-
5
-
-
0033952168
-
Compound optimization in early- and late-phase drug discovery; Acceptable pharmacokinetic properties utilizing combined physicocohemical, in vitro and in vivo screens
-
Caldwell, G. W. Compound optimization in early- and late-phase drug discovery; acceptable pharmacokinetic properties utilizing combined physicocohemical, in vitro and in vivo screens Curr. Opin. Drug Discovery Dev. 2000, 3, 30-41
-
(2000)
Curr. Opin. Drug Discovery Dev.
, vol.3
, pp. 30-41
-
-
Caldwell, G.W.1
-
6
-
-
33745070265
-
Discovery Pharmaceutics - Challenges and Opportunities
-
Article 46
-
Chen, X.-Q.; Antman, M. D.; Christoph, G.; Gudmundson, O. S. Discovery Pharmaceutics - Challenges and Opportunities. AAPS J. 2006, 8, Article 46, E402-E407.
-
(2006)
AAPS J.
, vol.8
-
-
Chen, X.-Q.1
Antman, M.D.2
Christoph, G.3
Gudmundson, O.S.4
-
7
-
-
12444301371
-
-
Hilgers, A. R.; Smith, D. P.; Biermacher, J. J.; Day, J. S.; Jensen, J. L.; Sims, S. M.; Adams, W. J.; Fiis, J. M.; Palandra, J.; Hosley, J. D.; Shobe, E. M.; Burton, P. S. Pharm. Res. 2003, 20, 1149-1155
-
(2003)
Pharm. Res.
, vol.20
, pp. 1149-1155
-
-
Hilgers, A.R.1
Smith, D.P.2
Biermacher, J.J.3
Day, J.S.4
Jensen, J.L.5
Sims, S.M.6
Adams, W.J.7
Fiis, J.M.8
Palandra, J.9
Hosley, J.D.10
Shobe, E.M.11
Burton, P.S.12
-
8
-
-
69949109727
-
Using the Golden Triangle to optimize clearance and oral absorption
-
Johnson, T. W.; Dress, K. R.; Edwards, M. Using the Golden Triangle to optimize clearance and oral absorption Bio. Med. Chem. Lett. 2009, 19, 5560-5564
-
(2009)
Bio. Med. Chem. Lett.
, vol.19
, pp. 5560-5564
-
-
Johnson, T.W.1
Dress, K.R.2
Edwards, M.3
-
9
-
-
33846290338
-
Preclinical formulations for discovery and toxicology: Physicochemical challenges
-
Neervannan, S. Preclinical formulations for discovery and toxicology: physicochemical challenges Expert Opin. Drug Metab. Toxicol. 2006, 2, 715-731
-
(2006)
Expert Opin. Drug Metab. Toxicol.
, vol.2
, pp. 715-731
-
-
Neervannan, S.1
-
10
-
-
39149113817
-
Formulation of Lipid Based Delivery Systems for Oral Administration: Materials, Methods, and Strategy
-
Pouton, C. W.; Porter, C. J. Formulation of Lipid Based Delivery Systems for Oral Administration: Materials, Methods, and Strategy Adv. Drug Delivery Rev. 2008, 60, 673-691
-
(2008)
Adv. Drug Delivery Rev.
, vol.60
, pp. 673-691
-
-
Pouton, C.W.1
Porter, C.J.2
-
11
-
-
41949100244
-
Drug Nanoparticles: Formulating Poorly Water-Soluble Compounds
-
Merisko-Liversidge, E. M.; Liversidge, G. G. Drug Nanoparticles: Formulating Poorly Water-Soluble Compounds Toxicol. Pathol. 2008, 36, 43-48
-
(2008)
Toxicol. Pathol.
, vol.36
, pp. 43-48
-
-
Merisko-Liversidge, E.M.1
Liversidge, G.G.2
-
12
-
-
64649100465
-
Hydroxypropyl methylcellulose acetate succinate based spray-dried dispersions: An overview
-
Friesen, D.; Shankar, R.; Crew, M.; Smithey, D.; Curatolo, W.; Nightingale, J. A. S. Hydroxypropyl methylcellulose acetate succinate based spray-dried dispersions: An overview Mol. Pharmaceutics 2008, 5, 1003-1009
-
(2008)
Mol. Pharmaceutics
, vol.5
, pp. 1003-1009
-
-
Friesen, D.1
Shankar, R.2
Crew, M.3
Smithey, D.4
Curatolo, W.5
Nightingale, J.A.S.6
-
13
-
-
0034461768
-
Drug-like properties and the causes of poor solubility and poor permeability
-
Lipinski, C. Drug-like properties and the causes of poor solubility and poor permeability J. Pharm. Toxicol. 2000, 44, 235-249
-
(2000)
J. Pharm. Toxicol.
, vol.44
, pp. 235-249
-
-
Lipinski, C.1
-
14
-
-
0031741846
-
Physical Chemical Properties of Oral Drug Candidates in the Discovery and Exploratory Development Settings
-
Curatolo, W. Physical Chemical Properties of Oral Drug Candidates in the Discovery and Exploratory Development Settings Pharm. Sci. Technol. Today 1998, 1, 387-393
-
(1998)
Pharm. Sci. Technol. Today
, vol.1
, pp. 387-393
-
-
Curatolo, W.1
-
15
-
-
2942585051
-
In-vitro testing of drug absorption for drug "developability" assessment: Forming an interface between in-vitro preclinical data and clinical outcomes
-
Sun, D.; Yu, L. X.; Hussain, M. A.; Wall, D. A.; Smith, R. L.; Amidon, G. L. In-vitro testing of drug absorption for drug "developability" assessment: Forming an interface between in-vitro preclinical data and clinical outcomes Curr. Opin. Drug Discovery Dev. 2004, 7, 75-85
-
(2004)
Curr. Opin. Drug Discovery Dev.
, vol.7
, pp. 75-85
-
-
Sun, D.1
Yu, L.X.2
Hussain, M.A.3
Wall, D.A.4
Smith, R.L.5
Amidon, G.L.6
-
16
-
-
34249037098
-
Predicting Effect of Food on Extent of Drug Absorption Based on Physicochemical Properties
-
Gu, C.-H.; Li, H.; Levons, J.; Lentz, K.; Ganghi, R. B.; Raghavan, K.; Smith, R. L. Predicting Effect of Food on Extent of Drug Absorption Based on Physicochemical Properties Pharm. Res. 2007, 24, 1118-1130
-
(2007)
Pharm. Res.
, vol.24
, pp. 1118-1130
-
-
Gu, C.-H.1
Li, H.2
Levons, J.3
Lentz, K.4
Ganghi, R.B.5
Raghavan, K.6
Smith, R.L.7
-
17
-
-
0030444550
-
Guidance in the Setting of Drug Particle Size Specifications to Minimize Variability in Absorption
-
Johnson, K. C.; Swindell, A. C. Guidance in the Setting of Drug Particle Size Specifications to Minimize Variability in Absorption Pharm. Res. 1996, 13, 1795-1798
-
(1996)
Pharm. Res.
, vol.13
, pp. 1795-1798
-
-
Johnson, K.C.1
Swindell, A.C.2
-
18
-
-
0027473738
-
Estimating the Fraction Dose Absorbed from Suspensions of Poorly Soluble Compounds in Humans: A Mathematical Model
-
Oh, D. M.; Curl, R.; Amidon, G. Estimating the Fraction Dose Absorbed from Suspensions of Poorly Soluble Compounds in Humans: A Mathematical Model Pharm. Res. 1993, 10, 264-270
-
(1993)
Pharm. Res.
, vol.10
, pp. 264-270
-
-
Oh, D.M.1
Curl, R.2
Amidon, G.3
-
19
-
-
78149338125
-
Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure
-
Borchardt, R. T. Hageman, M. J. Stevens, J. L. Kerns, E. H. Thakker, D. R. Springer: New York
-
Rohrs, B. Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure. In Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "Drug-Like" Properties of Leads in Drug Discovery; Borchardt, R. T.; Hageman, M. J.; Stevens, J. L.; Kerns, E. H.; Thakker, D. R., Eds.; Springer: New York, 2006; pp 151-166.
-
(2006)
Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "drug-Like" Properties of Leads in Drug Discovery
, pp. 151-166
-
-
Rohrs, B.1
-
20
-
-
84872616831
-
-
GastroPlus from Simulationsplus Inc. Information at (accessed June 12, 2011)
-
GastroPlus from Simulationsplus Inc. Information at www.simulations-plus. com/ (accessed June 12, 2011).
-
-
-
-
21
-
-
84872604393
-
-
Intellipharm Software, LLC. Informationat (accessed June 12, 2011)
-
Intellipharm Software, LLC. Informationat www.intellipharm.com (accessed June 12, 2011).
-
-
-
-
22
-
-
77957735669
-
A pH-Dilution Method for Estimation of Biorelevant Drug Solubility Along the Gastrointestinal Tract: Application to Physiologically Based Pharmacokinetic Modeling
-
Gao, Y.; Carr, R.; Spence, J. K.; Wang, W. W.; Turner, T. M.; Lipari, J. M.; Miller, J. M. A pH-Dilution Method for Estimation of Biorelevant Drug Solubility Along the Gastrointestinal Tract: Application to Physiologically Based Pharmacokinetic Modeling Mol. Pharmaceutics 2010, 5, 1516-1526
-
(2010)
Mol. Pharmaceutics
, vol.5
, pp. 1516-1526
-
-
Gao, Y.1
Carr, R.2
Spence, J.K.3
Wang, W.W.4
Turner, T.M.5
Lipari, J.M.6
Miller, J.M.7
-
23
-
-
70349645327
-
Estimation of the Extent of the Oral Absorption in Animals from Oral and Intravenous Pharmacokinetic Data in Drug Discovery
-
Nomier, A. A.; Morrison, R.; Prelusky, D.; Korfmacher, W.; Broske, V.; Hesk, D.; McNamara, P.; Mei., H. Estimation of the Extent of the Oral Absorption in Animals from Oral and Intravenous Pharmacokinetic Data in Drug Discovery J. Pharm. Sci. 2009, 98, 4027-4037
-
(2009)
J. Pharm. Sci.
, vol.98
, pp. 4027-4037
-
-
Nomier, A.A.1
Morrison, R.2
Prelusky, D.3
Korfmacher, W.4
Broske, V.5
Hesk, D.6
McNamara, P.7
Mei, H.8
-
24
-
-
79151476463
-
Fraction of a dose absoprbed estimation for structurally diverse low solubility compounds
-
Sugano, K. Fraction of a dose absoprbed estimation for structurally diverse low solubility compounds Int. J. Pharm. 2011, 405, 79-80
-
(2011)
Int. J. Pharm.
, vol.405
, pp. 79-80
-
-
Sugano, K.1
-
25
-
-
37849031379
-
Measurements of rat and mouse gastrointestinal pH, fluid, lymphoid tissue, and implications for in-vivo experiments
-
McConnell, E. L.; Basit, A. W.; Murdan, S. Measurements of rat and mouse gastrointestinal pH, fluid, lymphoid tissue, and implications for in-vivo experiments J. Pharm. Pharmacol. 2008, 60, 63-70
-
(2008)
J. Pharm. Pharmacol.
, vol.60
, pp. 63-70
-
-
McConnell, E.L.1
Basit, A.W.2
Murdan, S.3
-
26
-
-
33846408581
-
Role of Mechanistic Transport Studies in Lead Optimization
-
Borchardt, R. T. Hageman, M. J. Stevens, J. L. Kerns, E. H. Thakker, D. R. Springer: New York
-
Hochman, J.; Mei, Q.; Yamazaki, M.; Tang, C.; Prueksaritanont, T.; Bock, M.; Ha, S.; Lin, J. Role of Mechanistic Transport Studies in Lead Optimization. In Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "Drug-Like"Properties of Leads in Drug Discovery; Borchardt, R. T.; Hageman, M. J.; Stevens, J. L.; Kerns, E. H.; Thakker, D. R., Eds.; Springer: New York, 2006; pp 25-48.
-
(2006)
Biotechnology: Pharmaceutical Aspects, Vol. IV: Optimizing the "drug-Like"Properties of Leads in Drug Discovery
, pp. 25-48
-
-
Hochman, J.1
Mei, Q.2
Yamazaki, M.3
Tang, C.4
Prueksaritanont, T.5
Bock, M.6
Ha, S.7
Lin, J.8
-
27
-
-
0031913402
-
Dissolution Testing as a Prognostic Tool for Oral Drug Absorption: Immediate Release Oral Dosage Forms
-
Dressman, J. B.; Amidon, G. L.; Reppas, C.; Shah, V. P. Dissolution Testing as a Prognostic Tool for Oral Drug Absorption: Immediate Release Oral Dosage Forms J. Pharm. Sci. 1998, 1, 11-22
-
(1998)
J. Pharm. Sci.
, vol.1
, pp. 11-22
-
-
Dressman, J.B.1
Amidon, G.L.2
Reppas, C.3
Shah, V.P.4
-
28
-
-
74049147801
-
Absorption Barriers in the Rat Intestinal Mucosa. 3: Effects of Polyethoxylated Solubilizing Agents on Drug Permeation and Metabolism
-
Mudra, D.; Borchardt, R. T. Absorption Barriers in the Rat Intestinal Mucosa. 3: Effects of Polyethoxylated Solubilizing Agents on Drug Permeation and Metabolism J. Pharm. Sci. 2010, 99, 1016-1027
-
(2010)
J. Pharm. Sci.
, vol.99
, pp. 1016-1027
-
-
Mudra, D.1
Borchardt, R.T.2
-
29
-
-
39149091886
-
Evaluation of the impact of surfactant digestion on the bioavailability of danazol after oral administration of lipidic self-emulsifying formulations to dogs
-
Cuine, J. F.; McEvoy, C. L.; Charman, W. N.; Pouton, C. W.; Edwards, G. A.; Benameur, H.; Porter, C. J. H. Evaluation of the impact of surfactant digestion on the bioavailability of danazol after oral administration of lipidic self-emulsifying formulations to dogs J. Pharm. Sci. 2008, 97, 995-1012
-
(2008)
J. Pharm. Sci.
, vol.97
, pp. 995-1012
-
-
Cuine, J.F.1
McEvoy, C.L.2
Charman, W.N.3
Pouton, C.W.4
Edwards, G.A.5
Benameur, H.6
Porter, C.J.H.7
-
30
-
-
34247638077
-
Comparative study on digestive lipase activities on the self emulsifying excipient Labrasol, medium chain triglycerides and PEG esters
-
Fernandez, S.; Jannin, V.; Rodier, J.-D.; Ritter, N.; Mahler, B.; Carriere, F. Comparative study on digestive lipase activities on the self emulsifying excipient Labrasol, medium chain triglycerides and PEG esters Biochem. Biophys. Acta 2007, 1771, 633-640
-
(2007)
Biochem. Biophys. Acta
, vol.1771
, pp. 633-640
-
-
Fernandez, S.1
Jannin, V.2
Rodier, J.-D.3
Ritter, N.4
Mahler, B.5
Carriere, F.6
|