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Research Article

Determination of the Aqueous Solubility of Drugs Using a Convenient 96-Well Plate-Based Assay

Pages 107-109 | Published online: 29 Jan 2001

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Ardita Veseli, Simon Žakelj & Albin Kristl. (2019) A review of methods for solubility determination in biopharmaceutical drug characterization. Drug Development and Industrial Pharmacy 45:11, pages 1717-1724.
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J. Huuskonen, D.J. Livingstone & D.T. Manallack. (2008) Prediction of drug solubility from molecular structure using a drug-like training set. SAR and QSAR in Environmental Research 19:3-4, pages 191-212.
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Kouki Obata, Kiyohiko Sugano, Minoru Machida & Yoshinori Aso. (2004) Biopharmaceutics Classification by High Throughput Solubility Assay and PAMPA. Drug Development and Industrial Pharmacy 30:2, pages 181-185.
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Articles from other publishers (30)

M Vertzoni, J Alsenz, P Augustijns, A Bauer-Brandl, CAS Bergström, J Brouwers, A Müllerz, G Perlovich, C Saal, K Sugano & C Reppas. (2022) UNGAP best practice for improving solubility data quality of orally administered drugs. European Journal of Pharmaceutical Sciences 168, pages 106043.
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Long Chen, Jing Zhang, Xinjing Wang, Yu Li, Lu Zhou, Xiongxiong Lu, Guoqiang Dong & Chunquan Sheng. (2022) Discovery of novel KRAS‒PDEδ inhibitors with potent activity in patient-derived human pancreatic tumor xenograft models. Acta Pharmaceutica Sinica B 12:1, pages 274-290.
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Mai Shimizu, Tatsuki Fukami, Toshio Taniguchi, Yukihiro Nomura & Miki Nakajima. (2020) A Novel Systematic Approach for Selection of Prodrugs Designed to Improve Oral Absorption. Journal of Pharmaceutical Sciences 109:5, pages 1736-1746.
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Árpád Könczöl & Gergő Dargó. (2018) Brief overview of solubility methods: Recent trends in equilibrium solubility measurement and predictive models. Drug Discovery Today: Technologies 27, pages 3-10.
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Tomás Sou & Christel A.S. Bergström. (2018) Automated assays for thermodynamic (equilibrium) solubility determination. Drug Discovery Today: Technologies 27, pages 11-19.
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Kofi Asare-Addo & Barbara R. Conway. 2017. Poorly Soluble Drugs. Poorly Soluble Drugs 19 84 .
Ahmad Ghanbari, Yashar SArbaz, Vahid Jouyban-Gharamaleki, Karim Jouyban-Gharamaleki, Jafar Soleymani & Abolghasem Jouyban. (2016) An Improved Automated Setup for Solubility Determination of Drugs. Pharmaceutical Sciences 22:3, pages 210-214.
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Sonali S. Bharate & Ram A. Vishwakarma. (2015) Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. Bioorganic & Medicinal Chemistry Letters 25:7, pages 1561-1567.
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Vahid Jouyban-Gharamaleki, Karim Jouyban-Gharamaleki, Ali Shayanfar, Mehry Khoubnasabjafari & Abolghasem Jouyban. (2015) An Automated System for Determining Drug Solubility Based on Laser Monitoring Technique. Journal of Laboratory Automation 20:1, pages 3-9.
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Shreyans K. Jain, Surjeet Singh, Anamika Khajuria, Santosh K. Guru, Prashant Joshi, Samdarshi Meena, Janhavi R. Nadkarni, Amarinder Singh, Sonali S. Bharate, Shashi Bhushan, Sandip B. Bharate & Ram A. Vishwakarma. (2014) Pyrano-isochromanones as IL-6 Inhibitors: Synthesis, in Vitro and in Vivo Antiarthritic Activity. Journal of Medicinal Chemistry 57:16, pages 7085-7097.
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João M. M. Araújo, Catarina Florindo, Ana B. Pereiro, Nicole S. M. Vieira, Ana A. Matias, Catarina M. M. Duarte, Luís P. N. Rebelo & Isabel M. Marrucho. (2014) Cholinium-based ionic liquids with pharmaceutically active anions. RSC Adv. 4:53, pages 28126-28132.
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Li Di, Bo Feng, Theunis C. Goosen, Yurong Lai, Stefanus J. Steyn, Manthena V. Varma & R. Scott Obach. (2013) A Perspective on the Prediction of Drug Pharmacokinetics and Disposition in Drug Research and Development. Drug Metabolism and Disposition 41:12, pages 1975-1993.
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Qian Ru, Hala M. Fadda, Chung Li, Daniel Paul, Peng T. Khaw, Steve Brocchini & Mire Zloh. (2013) Molecular Dynamic Simulations of Ocular Tablet Dissolution. Journal of Chemical Information and Modeling 53:11, pages 3000-3008.
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Christoph Saal & Anna Christine Petereit. (2012) Optimizing solubility: Kinetic versus thermodynamic solubility temptations and risks. European Journal of Pharmaceutical Sciences 47:3, pages 589-595.
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Alexander V. LyubimovJochem Alsenz. 2011. Encyclopedia of Drug Metabolism and Interactions. Encyclopedia of Drug Metabolism and Interactions 1 70 .
Manthena V. Varma, Iain GardnerStefanus J. Steyn, Paul Nkansah, Charles J. Rotter, Carrie Whitney-Pickett, Hui Zhang, Li Di, Michael CramKatherine S. FennerAyman F. El-Kattan. (2012) pH-Dependent Solubility and Permeability Criteria for Provisional Biopharmaceutics Classification (BCS and BDDCS) in Early Drug Discovery. Molecular Pharmaceutics 9:5, pages 1199-1212.
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Kirstin Thelen, Katrin Coboeken, Stefan Willmann, Rolf Burghaus, Jennifer B. Dressman & Jörg Lippert. (2011) Evolution of a detailed physiological model to simulate the gastrointestinal transit and absorption process in humans, Part 1: Oral solutions. Journal of Pharmaceutical Sciences 100:12, pages 5324-5345.
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Samuel Yalkowshy, Yan He & Parijat Jain. 2010. Handbook of Aqueous Solubility Data, Second Edition. Handbook of Aqueous Solubility Data, Second Edition 1367 1440 .
Abolghasem Jouyban. 2009. Handbook of Solubility Data for Pharmaceuticals. Handbook of Solubility Data for Pharmaceuticals 1 67 .
Yveline Henchoz, Bruno Bard, Davy Guillarme, Pierre-Alain Carrupt, Jean-Luc Veuthey & Sophie Martel. (2009) Analytical tools for the physicochemical profiling of drug candidates to predict absorption/distribution. Analytical and Bioanalytical Chemistry 394:3, pages 707-729.
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Bettina Hoelke, Sabine Gieringer, Michael Arlt & Christoph Saal. (2009) Comparison of Nephelometric, UV-Spectroscopic, and HPLC Methods for High-Throughput Determination of Aqueous Drug Solubility in Microtiter Plates. Analytical Chemistry 81:8, pages 3165-3172.
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Arimichi Okazaki, Takashi Mano & Kiyohiko Sugano. (2008) Theoretical Dissolution Model of Poly-Disperse Drug Particles in Biorelevant Media. Journal of Pharmaceutical Sciences 97:5, pages 1843-1852.
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Jochem Alsenz & Manfred Kansy. (2007) High throughput solubility measurement in drug discovery and development. Advanced Drug Delivery Reviews 59:7, pages 546-567.
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Jochem Alsenz, E.v.a. Meister & Elisabeth Haenel. (2007) Development of a partially automated solubility screening (PASS) assay for early drug development. Journal of Pharmaceutical Sciences 96:7, pages 1748-1762.
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Nicole Wyttenbach, Jochem Alsenz & Olaf Grassmann. (2007) Miniaturized Assay for Solubility and Residual Solid Screening (SORESOS) in Early Drug Development. Pharmaceutical Research 24:5, pages 888-898.
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Kiyohiko Sugano, Arimichi Okazaki, Shohei Sugimoto, Sumitra Tavornvipas, Atsushi Omura & Takashi Mano. (2007) Solubility and Dissolution Profile Assessment in Drug Discovery. Drug Metabolism and Pharmacokinetics 22:4, pages 225-254.
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Kiyohiko Sugano, Teruhisa Kato, Kentaro Suzuki, Kako Keiko, Tetsujo Sujaku & Takashi Mano. (2006) High throughput solubility measurement with automated polarized light microscopy analysis. Journal of Pharmaceutical Sciences 95:10, pages 2115-2122.
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Joseph J. Goodwin. (2006) Rationale and benefit of using high throughput solubility screens in drug discovery. Drug Discovery Today: Technologies 3:1, pages 67-71.
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Yung-Chi Lee, Philip D Zocharski & Brian Samas. (2003) An intravenous formulation decision tree for discovery compound formulation development. International Journal of Pharmaceutics 253:1-2, pages 111-119.
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