Literature DB >> 18222563

Advanced screening assays to rapidly identify solubility-enhancing formulations: high-throughput, miniaturization and automation.

Wei-Guo Dai1, Crystal Pollock-Dove, Liang C Dong, Shu Li.   

Abstract

Development of solubility-enhancing formulations for poorly water-soluble compounds always poses a challenge. Conventional formulation screening assays are potentially time-consuming and labor-intensive and, moreover, require a large amount of a compound; they are not ideal when compound availability and testing time are limited. In recent years, in-vitro screening assays that are rapid, inexpensive, minimally labor-intensive, and require only small quantities of a compound have become available. These advanced assays allow high-throughput automation, miniaturization, and parallel processing, thereby enabling scientists to rapidly identify solubility-enhancing formulations with milligram or sub-milligram quantities of an active pharmaceutical ingredient (API). This article reviews these assays for rapidly screening the aqueous solubility of lead compounds and the solubility-enhancing formulations with limited quantities of API.

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Year:  2007        PMID: 18222563     DOI: 10.1016/j.addr.2007.10.017

Source DB:  PubMed          Journal:  Adv Drug Deliv Rev        ISSN: 0169-409X            Impact factor:   15.470


  10 in total

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Review 2.  Fluorescence techniques for determination of the membrane potentials in high throughput screening.

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Journal:  J Fluoresc       Date:  2010-11       Impact factor: 2.217

3.  Attenuated total reflection-Fourier transform infrared spectroscopic imaging of pharmaceuticals in microfluidic devices.

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Journal:  Biomicrofluidics       Date:  2016-04-20       Impact factor: 2.800

4.  Synthesis of N3-substituted carboranyl thymidine bioconjugates and their evaluation as substrates of recombinant human thymidine kinase 1.

Authors:  Hitesh K Agarwal; Craig A McElroy; Elena Sjuvarsson; Staffan Eriksson; Michael V Darby; Werner Tjarks
Journal:  Eur J Med Chem       Date:  2012-12-05       Impact factor: 6.514

5.  Miniaturized transfer models to predict the precipitation of poorly soluble weak bases upon entry into the small intestine.

Authors:  Sandra Klein; Norma L Buchanan; Charles M Buchanan
Journal:  AAPS PharmSciTech       Date:  2012-09-12       Impact factor: 3.246

6.  Prediction of Phase Behavior of Spray-Dried Amorphous Solid Dispersions: Assessment of Thermodynamic Models, Standard Screening Methods and a Novel Atomization Screening Device with Regard to Prediction Accuracy.

Authors:  Aymeric Ousset; Pierre-François Chavez; Joke Meeus; Florent Robin; Martin Alexander Schubert; Pascal Somville; Kalliopi Dodou
Journal:  Pharmaceutics       Date:  2018-03-07       Impact factor: 6.321

7.  A Novel Protocol Using Small-Scale Spray-Drying for the Efficient Screening of Solid Dispersions in Early Drug Development and Formulation, as a Straight Pathway from Screening to Manufacturing Stages.

Authors:  Aymeric Ousset; Rosanna Chirico; Florent Robin; Martin Alexander Schubert; Pascal Somville; Kalliopi Dodou
Journal:  Pharmaceuticals (Basel)       Date:  2018-08-27

8.  A Fully Integrated Assay Panel for Early Drug Metabolism and Pharmacokinetics Profiling.

Authors:  Johan Wernevik; Fredrik Bergström; Anna Novén; Johan Hulthe; Linda Fredlund; Dan Addison; Jan Holmgren; Per-Erik Strömstedt; Erika Rehnström; Thomas Lundböck
Journal:  Assay Drug Dev Technol       Date:  2020-05-14       Impact factor: 1.738

9.  Evaluation of Influence of Various Polymers on Dissolution and Phase Behavior of Carbamazepine-Succinic Acid Cocrystal in Matrix Tablets.

Authors:  Majeed Ullah; Hanif Ullah; Ghulam Murtaza; Qaisar Mahmood; Izhar Hussain
Journal:  Biomed Res Int       Date:  2015-08-24       Impact factor: 3.411

Review 10.  Revealing facts behind spray dried solid dispersion technology used for solubility enhancement.

Authors:  Bhavesh B Patel; Jayvadan K Patel; Subhashis Chakraborty; Dali Shukla
Journal:  Saudi Pharm J       Date:  2013-12-23       Impact factor: 4.330

  10 in total

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