The pharmaceutical availability of nitrofurantoin in three commercial urinary antiseptic preparations for oral use was assessed by an in vitro determination of drug release into a strongly acidic, a weakly acidic and a weakly basic medium. The following parameters are reported: t87.5%, tdiss, X0 (percentage released immediately on contact with medium), krel (relative dissolution rate constant), and dissolution efficiency (DE).
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Deep learning-based design and experimental validation of a medicine-like human antibody library.
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Antibody generation requires the use of one or more time-consuming methods, namely animal immunization, and in vitro display technologies. However, the recent availability of large amounts of antibody sequence and structural data in the public domain along with the advent of generative deep learning algorithms raises the possibility of computationally generating novel antibody sequences with desirable developability attributes. Here, we describe a deep learning model for computationally generating libraries of highly human antibody variable regions whose intrinsic physicochemical properties resemble those of the variable regions of the marketed antibody-based biotherapeutics (medicine-likeness).
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Department of Neurological Surgery, Nippon Medical School, Tokyo, Japan.
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National Vaccine Innovation Platform, Scholl of Pharmacy, Nanjing Medical University, Nanjing 211166, China.
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Front Pharmacol
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Institute of Pharmacology and the Gaston H. Glock Research Laboratories for Exploratory Drug Development, Centre of Physiology and Pharmacology, Medical University of Vienna, Vienna, Austria.
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Laboratory of Drug Discovery and Ecotoxicology, Department of Pharmacy, Guru Ghasidas Vishwavidyalaya, Bilaspur, 495009 India.
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