PubRank

Gordon L Amidon

Author PubWeight™ 101.34‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol Pharm 2004 2.63
2 A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan. Mol Pharm 2006 2.07
3 A mechanistic approach to understanding the factors affecting drug absorption: a review of fundamentals. J Clin Pharmacol 2002 1.85
4 Biopharmaceutics classification system: the scientific basis for biowaiver extensions. Pharm Res 2002 1.74
5 Polymer degradation and in vitro release of a model protein from poly(D,L-lactide-co-glycolide) nano- and microparticles. J Control Release 2003 1.72
6 The use of BDDCS in classifying the permeability of marketed drugs. Pharm Res 2008 1.57
7 Lessons learned from marketed and investigational prodrugs. J Med Chem 2004 1.43
8 Summary workshop report: biopharmaceutics classification system--implementation challenges and extension opportunities. J Pharm Sci 2004 1.43
9 Comparison of human duodenum and Caco-2 gene expression profiles for 12,000 gene sequences tags and correlation with permeability of 26 drugs. Pharm Res 2002 1.37
10 Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs. AAPS J 2009 1.37
11 Why is it challenging to predict intestinal drug absorption and oral bioavailability in human using rat model. Pharm Res 2006 1.26
12 Amino acid ester prodrugs of the anticancer agent gemcitabine: synthesis, bioconversion, metabolic bioevasion, and hPEPT1-mediated transport. Mol Pharm 2005 1.21
13 Identification of a human valacyclovirase: biphenyl hydrolase-like protein as valacyclovir hydrolase. J Biol Chem 2003 1.19
14 Physiological parameters for oral delivery and in vitro testing. Mol Pharm 2010 1.18
15 The suitability of an in situ perfusion model for permeability determinations: utility for BCS class I biowaiver requests. Mol Pharm 2006 1.16
16 The BCS, BDDCS, and regulatory guidances. Pharm Res 2011 1.11
17 Pharmacokinetics of an immediate release, a controlled release and a two pulse dosage form in dogs. Eur J Pharm Biopharm 2005 1.10
18 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol 2009 1.08
19 A novel nucleoside prodrug-activating enzyme: substrate specificity of biphenyl hydrolase-like protein. Mol Pharm 2005 1.04
20 Molecular basis of prodrug activation by human valacyclovirase, an alpha-amino acid ester hydrolase. J Biol Chem 2008 1.04
21 Floxuridine amino acid ester prodrugs: enhancing Caco-2 permeability and resistance to glycosidic bond metabolism. Pharm Res 2005 1.04
22 Targeted delivery to PEPT1-overexpressing cells: acidic, basic, and secondary floxuridine amino acid ester prodrugs. Mol Cancer Ther 2005 1.03
23 Summary workshop report: bioequivalence, biopharmaceutics classification system, and beyond. AAPS J 2008 1.01
24 G.L. Amidon, H. Lennernas, V.P. Shah, and J.R. Crison. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability, Pharm Res 12, 413-420, 1995--backstory of BCS. AAPS J 2014 1.00
25 Multiple efflux pumps are involved in the transepithelial transport of colchicine: combined effect of p-glycoprotein and multidrug resistance-associated protein 2 leads to decreased intestinal absorption throughout the entire small intestine. Drug Metab Dispos 2009 1.00
26 Amino acid ester prodrugs of floxuridine: synthesis and effects of structure, stereochemistry, and site of esterification on the rate of hydrolysis. Pharm Res 2003 1.00
27 Gene expression in the human intestine and correlation with oral valacyclovir pharmacokinetic parameters. J Pharmacol Exp Ther 2003 0.99
28 High-permeability criterion for BCS classification: segmental/pH dependent permeability considerations. Mol Pharm 2010 0.99
29 Comparative gene expression profiles of intestinal transporters in mice, rats and humans. Pharmacol Res 2007 0.98
30 Segmental dependent transport of low permeability compounds along the small intestine due to P-glycoprotein: the role of efflux transport in the oral absorption of BCS class III drugs. Mol Pharm 2009 0.98
31 In vitro testing of drug absorption for drug 'developability' assessment: forming an interface between in vitro preclinical data and clinical outcome. Curr Opin Drug Discov Devel 2004 0.97
32 Enhancing the intestinal membrane permeability of zanamivir: a carrier mediated prodrug approach. Mol Pharm 2011 0.96
33 The solubility-permeability interplay in using cyclodextrins as pharmaceutical solubilizers: mechanistic modeling and application to progesterone. J Pharm Sci 2010 0.95
34 Feasibility of biowaiver extension to biopharmaceutics classification system class III drug products: cimetidine. Clin Pharmacokinet 2006 0.95
35 Blockade of interleukin-6 receptor suppresses the proliferation of H460 lung cancer stem cells. Int J Oncol 2012 0.95
36 Surfactant-mediated dissolution: contributions of solubility enhancement and relatively low micelle diffusivity. J Pharm Sci 2004 0.94
37 Grapefruit juice and its constituents augment colchicine intestinal absorption: potential hazardous interaction and the role of p-glycoprotein. Pharm Res 2008 0.94
38 Tacrolimus is a class II low-solubility high-permeability drug: the effect of P-glycoprotein efflux on regional permeability of tacrolimus in rats. J Pharm Sci 2002 0.93
39 Enhanced cancer cell growth inhibition by dipeptide prodrugs of floxuridine: increased transporter affinity and metabolic stability. Mol Pharm 2008 0.93
40 Enabling the intestinal absorption of highly polar antiviral agents: ion-pair facilitated membrane permeation of zanamivir heptyl ester and guanidino oseltamivir. Mol Pharm 2010 0.93
41 Stability of valacyclovir: implications for its oral bioavailability. Int J Pharm 2006 0.92
42 The biowaiver extension for BCS class III drugs: the effect of dissolution rate on the bioequivalence of BCS class III immediate-release drugs predicted by computer simulation. Mol Pharm 2010 0.92
43 Increasing oral absorption of polar neuraminidase inhibitors: a prodrug transporter approach applied to oseltamivir analogue. Mol Pharm 2013 0.92
44 A novel high-throughput pepT1 transporter assay differentiates between substrates and antagonists. Mol Pharm 2004 0.92
45 Nucleoside ester prodrug substrate specificity of liver carboxylesterase. J Pharmacol Exp Ther 2005 0.92
46 Human jejunal permeability of cyclosporin A: influence of surfactants on P-glycoprotein efflux in Caco-2 cells. Pharm Res 2003 0.92
47 Enhanced absorption and growth inhibition with amino acid monoester prodrugs of floxuridine by targeting hPEPT1 transporters. Molecules 2008 0.92
48 Permeability dominates in vivo intestinal absorption of P-gp substrate with high solubility and high permeability. Mol Pharm 2005 0.91
49 Summary of the National Institute of Child Health and Human Development-best pharmaceuticals for Children Act Pediatric Formulation Initiatives Workshop-Pediatric Biopharmaceutics Classification System Working Group. Clin Ther 2012 0.90
50 Mechanistic understanding of time-dependent oral absorption based on gastric motor activity in humans. Eur J Pharm Biopharm 2008 0.90
51 The solubility-permeability interplay: mechanistic modeling and predictive application of the impact of micellar solubilization on intestinal permeation. Mol Pharm 2011 0.89
52 Segmental-dependent membrane permeability along the intestine following oral drug administration: Evaluation of a triple single-pass intestinal perfusion (TSPIP) approach in the rat. Eur J Pharm Sci 2008 0.89
53 Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter. J Med Chem 2005 0.88
54 Chemical and enzymatic stability of amino acid prodrugs containing methoxy, ethoxy and propylene glycol linkers. Mol Pharm 2009 0.88
55 Solubilization and dissolution of insoluble weak acid, ketoprofen: effects of pH combined with surfactant. Eur J Pharm Sci 2006 0.88
56 Purely in silico BCS classification: science based quality standards for the world's drugs. Mol Pharm 2013 0.88
57 Feasibility studies of utilizing disk intrinsic dissolution rate to classify drugs. Int J Pharm 2004 0.87
58 Amino acid ester prodrugs of 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole enhance metabolic stability in vitro and in vivo. J Pharmacol Exp Ther 2005 0.87
59 Comparison of the permeability of metoprolol and labetalol in rat, mouse, and Caco-2 cells: use as a reference standard for BCS classification. Mol Pharm 2013 0.86
60 Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach. J Med Chem 2010 0.86
61 The fraction dose absorbed, in humans, and high jejunal human permeability relationship. Mol Pharm 2012 0.86
62 Quasi-equilibrium analysis of the ion-pair mediated membrane transport of low-permeability drugs. J Control Release 2009 0.85
63 Comparative gene expression of intestinal metabolizing enzymes. Biopharm Drug Dispos 2009 0.84
64 MRP2 mediated drug-drug interaction: indomethacin increases sulfasalazine absorption in the small intestine, potentially decreasing its colonic targeting. Int J Pharm 2009 0.84
65 The low/high BCS permeability class boundary: physicochemical comparison of metoprolol and labetalol. Mol Pharm 2014 0.83
66 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. J Pharmacol Exp Ther 2002 0.83
67 Toward an in vivo dissolution methodology: a comparison of phosphate and bicarbonate buffers. Mol Pharm 2009 0.83
68 A fluorescent hPept1 transporter substrate for uptake screening. Pharm Res 2003 0.83
69 The H2 receptor antagonist nizatidine is a P-glycoprotein substrate: characterization of its intestinal epithelial cell efflux transport. AAPS J 2009 0.83
70 In silico prediction of drug dissolution and absorption with variation in intestinal pH for BCS class II weak acid drugs: ibuprofen and ketoprofen. Biopharm Drug Dispos 2012 0.82
71 Drug targeting strategies for the treatment of inflammatory bowel disease: a mechanistic update. Expert Rev Clin Immunol 2010 0.82
72 Transporter and ion channel gene expression after Caco-2 cell differentiation using 2 different microarray technologies. AAPS J 2004 0.81
73 Mechanistic analysis of solute transport in an in vitro physiological two-phase dissolution apparatus. Biopharm Drug Dispos 2012 0.81
74 N-methylpurine DNA glycosylase and 8-oxoguanine dna glycosylase metabolize the antiviral nucleoside 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole. Drug Metab Dispos 2006 0.81
75 Possibility of enterohepatic recycling of ketoprofen in dogs. Int J Pharm 2007 0.81
76 Interferon-gamma increases expression of the di/tri-peptide transporter, h-PEPT1, and dipeptide transport in cultured human intestinal monolayers. Pharmacol Res 2008 0.80
77 Specificity of a prodrug-activating enzyme hVACVase: the leaving group effect. Mol Pharm 2010 0.80
78 Mechanistic enhancement of the intestinal absorption of drugs containing the polar guanidino functionality. Expert Opin Drug Metab Toxicol 2011 0.79
79 Possible degradative process of cholecystokinin analogs in rabbit jejunum brush-border membrane vesicles. Life Sci 2002 0.79
80 The achievement of mass balance by simultaneous quantification of floxuridine prodrug, floxuridine, 5-fluorouracil, 5-dihydrouracil, α-fluoro-β-ureidopropionate, α-fluoro-β-alanine using LC-MS. J Chromatogr B Analyt Technol Biomed Life Sci 2011 0.79
81 Pharmacokinetics of the CYP 3A substrate simvastatin following administration of delayed versus immediate release oral dosage forms. Pharm Res 2008 0.79
82 The feasibility of enzyme targeted activation for amino acid/dipeptide monoester prodrugs of floxuridine; cathepsin D as a potential targeted enzyme. Molecules 2012 0.78
83 Establishing the pharmaceutical quality of Chinese herbal medicine: a provisional BCS classification. Mol Pharm 2013 0.78
84 Potential of amino acid/dipeptide monoester prodrugs of floxuridine in facilitating enhanced delivery of active drug to interior sites of tumors: a two-tier monolayer in vitro study. Pharm Res 2011 0.78
85 Particle diffusional layer thickness in a USP dissolution apparatus II: a combined function of particle size and paddle speed. J Pharm Sci 2008 0.78
86 Mechanistic understanding of food effects: water diffusivity in gastrointestinal tract is an important parameter for the prediction of disintegration of solid oral dosage forms. Mol Pharm 2013 0.78
87 Ion pairing with bile salts modulates intestinal permeability and contributes to food-drug interaction of BCS class III compound trospium chloride. Mol Pharm 2013 0.78
88 Mechanistic investigation of food effect on disintegration and dissolution of BCS class III compound solid formulations: the importance of viscosity. Biopharm Drug Dispos 2012 0.78
89 Functional expression and characterization of a sodium-dependent nucleoside transporter hCNT2 cloned from human duodenum. Biochem Biophys Res Commun 2003 0.78
90 Dedication to professor Leslie Z. Benet: 50 years of scientific excellence and still going strong! Pharm Res 2012 0.78
91 Molecular pharmaceutics: the NIH Roadmap and the FDA pipeline problem. Mol Pharm 2005 0.78
92 Proline prodrug of melphalan targeted to prolidase, a prodrug activating enzyme overexpressed in melanoma. Pharm Res 2007 0.77
93 Improved intestinal transport of PD 158473, an N-methyl-D-aspartate (NMDA) antagonist, by involvement of multiple transporters. J Pharm Sci 2002 0.77
94 Cytomegalovirus protease targeted prodrug development. Mol Pharm 2013 0.77
95 The site-specific transport and metabolism of tacrolimus in rat small intestine. J Pharmacol Exp Ther 2003 0.77
96 Fetal and maternal tissue distribution of the new fluoroquinolone DW-116 in pregnant rats. Comp Biochem Physiol C Toxicol Pharmacol 2003 0.77
97 Intestinal metabolism and absorption of cholecystokinin analogs in rats. Biochem Biophys Res Commun 2002 0.77
98 The effect of enzyme inhibitor and absorption site following [D-ala2, D-leu5]enkephalin oral administration in rats. Biopharm Drug Dispos 2002 0.77
99 Oral absorption of phytosterols and emulsified phytosterols by Sprague-Dawley rats. J Nutr Biochem 2004 0.76
100 Puromycin-sensitive aminopeptidase: an antiviral prodrug activating enzyme. Antiviral Res 2009 0.76
101 Transporter mRNA expression in a conditionally immortalized rat small intestine epithelial cell line (TR-SIE). Drug Metab Pharmacokinet 2004 0.76
102 Prolidase, a potential enzyme target for melanoma: design of proline-containing dipeptide-like prodrugs. Mol Pharm 2005 0.76
103 Selection of suitable prodrug candidates for in vivo studies via in vitro studies; the correlation of prodrug stability in between cell culture homogenates and human tissue homogenates. J Pharm Pharm Sci 2012 0.76
104 Quantification of gastrointestinal liquid volumes and distribution following a 240 mL dose of water in the fasted state. Mol Pharm 2014 0.76
105 Characteristics of gastrointestinal absorption of DX-9065a, a new synthetic anticoagulant. Drug Metab Pharmacokinet 2007 0.76
106 Dipeptidyl peptidase IV as a potential target for selective prodrug activation and chemotherapeutic action in cancers. Mol Pharm 2014 0.75
107 Dissolution and solubility behavior of fenofibrate in sodium lauryl sulfate solutions. Drug Dev Ind Pharm 2005 0.75
108 Intestinal dipeptide absorption is preserved during thermal injury and cytokine treatment. JPEN J Parenter Enteral Nutr 2009 0.75
109 In vivo predictive dissolution: transport analysis of the CO2 , bicarbonate in vivo buffer system. J Pharm Sci 2014 0.75
110 Structure and specificity of a human valacyclovir activating enzyme: a homology model of BPHL. Mol Pharm 2005 0.75
111 Biowaiver monographs for immediate-release solid oral dosage forms: codeine phosphate. J Pharm Sci 2014 0.75
112 Intestinal permeability study of minoxidil: assessment of minoxidil as a high permeability reference drug for biopharmaceutics classification. Mol Pharm 2014 0.75
113 Variability in cimetidine absorption and plasma double peaks following oral administration in the fasted state in humans: correlation with antral gastric motility. Eur J Pharm Biopharm 2002 0.75
114 Finding the "Magic". Mol Pharm 2004 0.75
115 In vitro Characterization of the Biomimetic Properties of Poly(dimethyl siloxane) to Simulate Oral Drug Absorption. Mol Pharm 2017 0.75
116 Provisional biopharmaceutical classification of some common herbs used in Western medicine. Mol Pharm 2012 0.75
117 Collaborative research training. Mol Pharm 2005 0.75
118 Lack of interaction between the peptidomimetic substrates captopril and cephradine. J Clin Pharmacol 2009 0.75
119 Evaluation of a three compartment in vitro gastrointestinal simulator dissolution apparatus to predict in vivo dissolution. J Pharm Sci 2014 0.75
120 Effect of experimental acute renal and hepatic failure on absorption of tacrolimus in rat small intestine. Drug Metab Pharmacokinet 2004 0.75
121 Proline prodrug of melphalan, prophalan-L, demonstrates high therapeutic index in a murine melanoma model. Eur J Pharm Biopharm 2007 0.75