Search Results - "Box, Karl J."

On the Usefulness of Two Small-Scale In Vitro Setups in the Evaluation of Luminal Precipitation of Lipophilic Weak Bases in Early Formulation Development by O'Dwyer, Patrick J, Imanidis, Georgios, Box, Karl J, Reppas, Christos

“…A small-scale biphasic dissolution setup and a small-scale dissolution-permeation (D-P) setup were evaluated for their usefulness in simulating the luminal…”
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Study of pH-dependent solubility of organic bases. Revisit of Henderson-Hasselbalch relationship by Völgyi, Gergely, Baka, Edit, Box, Karl J., Comer, John E.A., Takács-Novák, Krisztina

“…In this paper the pH-equilibrium solubility profiles of six organic drugs are presented. The equilibrium solubility values were determined using the saturation…”
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Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration by Box, Karl J., Comer, John, Taylor, Robert, Karki, Shyam, Ruiz, Rebeca, Price, Robert, Fotaki, Nikoletta

“…The purpose of this study was to better understand the dissolution properties and precipitation behavior of pharmaceutical cocrystals of poorly soluble drugs…”
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On the usefulness of four in vitro methods in assessing the intraluminal performance of poorly soluble, ionisable compounds in the fasted state by O'Dwyer, Patrick J, Box, Karl J, Imanidis, Georgios, Vertzoni, Maria, Reppas, Christos

“…A small-scale two-stage biphasic system, a small-scale two-stage dissolution-permeation system, the Erweka mini-paddle apparatus, and the BioGIT system were…”
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pH-Dependent Liquid–Liquid Phase Separation of Highly Supersaturated Solutions of Weakly Basic Drugs by Indulkar, Anura S, Box, Karl J, Taylor, Robert, Ruiz, Rebeca, Taylor, Lynne S

“…Supersaturated solutions of poorly aqueous soluble drugs can be formed both in vivo and in vitro. For example, increases in pH during gastrointestinal transit…”
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Predictions of biorelevant solubility change during dispersion and digestion of lipid-based formulations by Ejskjær, Lotte, Holm, René, Kuentz, Martin, Box, Karl J., Griffin, Brendan T., O'Dwyer, Patrick J.

“…Computational approaches are increasingly explored in development of drug products, including the development of lipid-based formulations (LBFs), to assess…”
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Biphasic drug release testing coupled with diffusing wave spectroscopy for mechanistic understanding of solid dispersion performance by Jankovic, Sandra, O'Dwyer, Patrick J., Box, Karl J., Imanidis, Georgios, Reppas, Christos, Kuentz, Martin

“…Amorphous solid dispersions (ASDs) represent an important formulation technique to achieve supersaturation in gastrointestinal fluids and to enhance absorption…”
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In vitro methods to assess drug precipitation in the fasted small intestine – a PEARRL review by O'Dwyer, Patrick J., Litou, Chara, Box, Karl J., Dressman, Jennifer B., Kostewicz, Edmund S., Kuentz, Martin, Reppas, Christos

“…Objectives Drug precipitation in vivo poses a significant challenge for the pharmaceutical industry. During the drug development process, the impact of drug…”
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Combining biorelevant in vitro and in silico tools to simulate and better understand the in vivo performance of a nano-sized formulation of aprepitant in the fasted and fed states by Litou, Chara, Patel, Nikunjkumar, Turner, David B., Kostewicz, Edmund, Kuentz, Martin, Box, Karl J., Dressman, Jennifer

“…When developing bio-enabling formulations, innovative tools are required to understand and predict in vivo performance and may facilitate approval by…”
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Combining biorelevant in vitro and in silico tools to investigate the in vivo performance of the amorphous solid dispersion formulation of etravirine in the fed state by Litou, Chara, Turner, David B., Holmstock, Nico, Ceulemans, Jens, Box, Karl J., Kostewicz, Edmund, Kuentz, Martin, Holm, Rene, Dressman, Jennifer

“…In the development of bio-enabling formulations, innovative in vivo predictive tools to understand and predict the in vivo performance of such formulations are…”
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Developing an in vitro lipolysis model for real-time analysis of drug concentrations during digestion of lipid-based formulations by Ejskjær, Lotte, O'Dwyer, Patrick J., Ryan, Callum D., Holm, René, Kuentz, Martin, Box, Karl J., Griffin, Brendan T.

“…•In-line real-time in vitro lipolysis model.•Investigations of dynamic drug concentrations upon dispersion and digestion of LBFs.•Ready-to-use liquid Palatase®…”
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Novel Biphasic Lipolysis Method To Predict in Vivo Performance of Lipid-Based Formulations by O’Dwyer, Patrick J, Box, Karl J, Koehl, Niklas J, Bennett-Lenane, Harriet, Reppas, Christos, Holm, Rene, Kuentz, Martin, Griffin, Brendan T

“…The absence of an intestinal absorption sink is a significant weakness of standard in vitro lipolysis methods, potentially leading to poor prediction of in…”
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pH-Induced Precipitation Behavior of Weakly Basic Compounds: Determination of Extent and Duration of Supersaturation Using Potentiometric Titration and Correlation to Solid State Properties by Hsieh, Yi-Ling, Ilevbare, Grace A., Van Eerdenbrugh, Bernard, Box, Karl J., Sanchez-Felix, Manuel Vincente, Taylor, Lynne S.

“…ABSTRACT Purpose To examine the precipitation and supersaturation behavior of ten weak bases in terms of the relationship between pH-concentration-time…”
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Oral biopharmaceutics tools: recent progress from partnership through the Pharmaceutical Education and Research with Regulatory Links collaboration by O’Dwyer, Patrick J, Box, Karl J, Dressman, Jennifer, Griffin, Brendan T, Henze, Laura J, Litou, Chara, Pentafragka, Christina, Statelova, Marina, Vertzoni, Maria, Reppas, Christos

“…Abstract Objectives To summarise key contributions of the Pharmaceutical Education and Research with Regulatory Links (PEARRL) project (2016–2020) to the…”
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Effects of medicines used to treat gastrointestinal diseases on the pharmacokinetics of coadministered drugs: a PEARRL Review by Litou, Chara, Effinger, Angela, Kostewicz, Edmund S., Box, Karl J., Fotaki, Nikoletta, Dressman, Jennifer B.

“…Objectives Drugs used to treat gastrointestinal diseases (GI drugs) are widely used either as prescription or over‐the‐counter (OTC) medications and belong to…”
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Diclofenac Solubility:  Independent Determination of the Intrinsic Solubility of Three Crystal Forms by Llinàs, Antonio, Burley, Jonathan C, Box, Karl J, Glen, Robert C, Goodman, Jonathan M

“…The solubility in water of diclofenac ({2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid), a potent nonsteroidal anti-inflammatory drug, has been investigated…”
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Acidity and Hydrophobicity of Several New Potential Antitubercular Drugs: Isoniazid and Benzimidazole Derivatives by Ràfols, Clara, Bosch, Elisabeth, Ruiz, Rebeca, Box, Karl J, Reis, Marina, Ventura, Cristina, Santos, Susana, Araújo, M. Eduarda, Martins, Filomena

“…Hydrophobicity values (log P o/w) determined both by potentiometry and by the conventional shake-flask method and aqueous pK a values obtained by potentiometry…”
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Equilibrium versus kinetic measurements of aqueous solubility, and the ability of compounds to supersaturate in solution--a validation study by Box, Karl J, Völgyi, Gergely, Baka, Edit, Stuart, Martin, Takács-Novák, Krisztina, Comer, John E A

“…A novel potentiometric procedure has recently been described for rapid measurement of equilibrium aqueous solubility values of organic acids, bases, and…”
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A new method for the reproducible generation of polymorphs: two forms of sulindac with very different solubilities by Llinàs, Antonio, Box, Karl J., Burley, Jonathan C., Glen, Robert C., Goodman, Jonathan M.

“…Polymorphism of drugs has been the subject of intense interest in the pharmaceutical industry for over forty years. Although identical in chemical composition,…”
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Physicochemical Properties of a New Multicomponent Cosolvent System for the pKa Determination of Poorly Soluble Pharmaceutical Compounds by Box, Karl J., Völgyi, Gergely, Ruiz, Rebeca, Comer, John E., Takács-Novák, Krisztina, Bosch, Elisabeth, Ràfols, Clara, Rosés, Martí

“…A mixture of cosolvents is described that significantly improves the solubility of most pharmaceutical compounds. The mixture consists of equal volumes of…”
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