Search Results - "MATHIAS, Neil R"

The Use of Modeling Tools to Drive Efficient Oral Product Design by Mathias, Neil R., Crison, John

“…Modeling and simulation of drug dissolution and oral absorption has been increasingly used over the last decade to understand drug behavior in vivo based on…”
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Utilization of In Vitro, In Vivo and In Silico Tools to Evaluate the pH-Dependent Absorption of a BCS Class II Compound and Identify a pH-Effect Mitigating Strategy by Gesenberg, Christoph, Mathias, Neil R., Xu, Yan, Crison, John, Savant, Ishani, Saari, Amy, Good, David J., Hemenway, Jeffrey N., Narang, Ajit S., Schartman, Richard R., Zheng, Naiyu, Buzescu, Adela, Patel, Jatin

“…Purpose To describe a stepwise approach to evaluate the pH effect for a weakly basic drug by in vitro , in vivo and in silico techniques and identify a viable…”
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Assessing the Risk of pH-Dependent Absorption for New Molecular Entities: A Novel in Vitro Dissolution Test, Physicochemical Analysis, and Risk Assessment Strategy by Mathias, Neil R, Xu, Yan, Patel, Dhaval, Grass, Michael, Caldwell, Brett, Jager, Casey, Mullin, Jim, Hansen, Luke, Crison, John, Saari, Amy, Gesenberg, Christoph, Morrison, John, Vig, Balvinder, Raghavan, Krishnaswamy

“…Weak base therapeutic agents can show reduced absorption or large pharmacokinetic variability when coadministered with pH-modifying agents, or in achlorhydria…”
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Permeability Characteristics of Calu-3 Human Bronchial Epithelial Cells: In Vitro - In Vivo Correlation to Predict Lung Absorption in Rats by Mathias, Neil R., Timoszyk, Julita, Stetsko, Paul I., Megill, John R., Smith, Ronald L., Wall, Doris A.

“…The goal of this study was to evaluate the permeability characteristics of Calu-3, human bronchial epithelial cells to passive and actively transported drugs…”
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Non-invasive systemic drug delivery: developability considerations for alternate routes of administration by Mathias, Neil R, Hussain, Munir A

“…Over the past few decades alternate routes of administration have gained significant momentum and attention, to complement approved drug products, or enable…”
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Rat nasal lavage biomarkers to assess preclinical irritation potential of nasal drug formulations and excipients by Mathias, Neil R, Moench, Paul, Heran, Christopher, Hussain, Munir A, Smith, Ronald L

“…The goal of this study was to evaluate biomarkers of nasal mucosal damage for rapid assessment of irritancy potential of formulations in the rat nasal lavage…”
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Respiratory epithelial cell culture models for evaluation of ion and drug transport by Mathias, Neil R., Yamashita, Fumiyoshi, Lee, Vincent H.L.

“…This review presents the advances in respiratory epithelial cell culture developed for biochemical, ion transport, and drug transport characterization in the…”
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Discovery of (R)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): A Potent Antagonist of the Human Calcitonin Gene-Related Peptide Receptor for Migraine with Rapid and Efficient Intranasal Exposure by Degnan, Andrew P, Chaturvedula, Prasad V, Conway, Charles M, Cook, Deborah A, Davis, Carl D, Denton, Rex, Han, Xiaojun, Macci, Robert, Mathias, Neil R, Moench, Paul, Pin, Sokhom S, Ren, Shelly X, Schartman, Richard, Signor, Laura J, Thalody, George, Widmann, Kimberly A, Xu, Cen, Macor, John E, Dubowchik, Gene M

“…Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant…”
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The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2 by Han, Xiaojun, Civiello, Rita L., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Degnan, Andrew P., Jiang, Xiang-Jun, Macci, Robert, Mathias, Neil R., Moench, Paul, Pin, Sokhom S., Schartman, Richard, Signor, Laura J., Thalody, George, Tora, George, Whiterock, Valerie, Xu, Cen, Macor, John E., Dubowchik, Gene M.

“…Various substituted indazole and benzoxazolone amino acids were investigated as d-tyrosine surrogates in highly potent CGRP receptor antagonists. Compound 3,…”
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Modulation of Tight Junctions does Not Predict Oral Absorption of Hydrophilic Compounds: Use of Caco-2 and Calu-3 Cells by Kamath, Amrita V, Morrison, Richard A, Mathias, Neil R, Dando, Sandra A, Marino, Anthony M, Chong, Sae-Ho

“…Permeability estimates using Caco-2 cells do not accurately predict the absorption of hydrophilic drugs that are primarily absorbed via the paracellular…”
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Carbopol-mediated paracellular transport enhancement in Calu-3 cell layers by Li, Lianli, Mathias, Neil R, Heran, Christopher L, Moench, Paul, Wall, Doris A, Smith, Ronald L

“…The interaction of Carbopol polymers with mucus producing Calu-3 human bronchial epithelial cells was evaluated to test for potential paracellular transport…”
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A rabbit model for sublingual drug delivery: comparison with human pharmacokinetic studies of propranolol, verapamil and captopril by Dali, Manisha M, Moench, Paul A, Mathias, Neil R, Stetsko, Paul I, Heran, Christopher L, Smith, Ronald L

“…A rabbit model for investigating sublingual drug absorption was established yielding results consistent with clinical data reported in the literature. Using…”
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Modulation of tight junctions does not predict oral absorption of hydrophilic compounds: use of Caco-2 and Calu-3 cells by Kamath, Amrita V, Morrison, Richard A, Mathias, Neil R, Dando, Sandra A, Marino, Anthony M, Chong, Saeho

“…Permeability estimates using Caco-2 cells do not accurately predict the absorption of hydrophilic drugs that are primarily absorbed via the paracellular…”
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Functional and pharmacological mechanisms of nucleoside transport across the basolateral membrane of rabbit tracheal epithelial cells by Wu, Sharon K., Mathias, Neil R., Kim, Kwang-Jin, Lee, Vincent H.L.

“…The role of basolateral membrane nucleoside transport in primary cultured rabbit tracheal epithelial cells (RTEC) was studied. Primary cultured RTEC were grown…”
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Nucleoside transport in primary cultured rabbit tracheal epithelial cells by Mathias, Neil R., Wu, Sharon K., Kim, Kwang-Jin, Lee, Vincent H.L.

“…The present study aimed at elucidating the mechanisms of nucleoside transport in primary cultured rabbit tracheal epithelial cells (RTEC) grown on a permeable…”
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The effect of anesthesia on the pharmacokinetics of sublingually administered verapamil in rabbits by Moench, Paul A, Heran, Christopher L, Stetsko, Paul I, Mathias, Neil R, Wall, Doris A, Hussain, Munir A, Smith, Ronald L

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Corrigendum to “The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2” [Bioorg. Med. Chem. Lett. 23 (2013) 1870–1873] by Han, Xiaojun, Civiello, Rita L., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Degnan, Andrew P., Jiang, Xiang-Jun, Macci, Robert, Mathias, Neil R., Moench, Paul, Pin, Sokhom S., Schartman, Richard, Signor, Laura J., Thalody, George, Tora, George, Whiterock, Valerie, Xu, Cen, Macor, John E., Dubowchik, Gene M.

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Discovery of (R)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidm-1-yl)piperidin-1-yl)propan-2-ylpiperidine-1-carboxamide (BMS-694153) : A Potent Antagonist of the Human Calcitonin Gene-Related Peptide Receptor for Migraine with Rapid and Efficient Intranasal Exposure by DEGNAN, Andrew P, CHATURVEDULA, Prasad V, PIN, Sokhom S, REN, Shelly X, SCHARTMAN, Richard, SIGNOR, Laura J, THALODY, George, WIDMANN, Kimberly A, CEN XU, MACOR, John E, DUBOWCHIK, Gene M, CONWAY, Charles M, COOK, Deborah A, DAVIS, Carl D, DENTON, Rex, XIAOJUN HAN, MACCI, Robert, MATHIAS, Neil R, MOENCH, Paul

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Development and characterization of rabbit tracheal epithelial cell monolayer models for drug transport studies by MATHIAS, N. R, KWANG-JIN KIM, ROBISON, T. W, LEE, V. H. L

“…The objective of this study was to investigate how culture conditions would affect the morphological, functional, and permeability characteristics of rabbit…”
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Targeted drug delivery to the respiratory tract: solute permeability of air-interface cultured rabbit tracheal epithelial cell monolayers by Mathias, N R, Kim, K J, Lee, V H

“…The permeability characteristics of air-interfaced rabbit tracheal epithelial cell monolayers to model macromolecules and low molecular weight solutes were…”
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