Journal ArticleDOI
Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019.
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TLDR
The five-year drug-approval database contains 61 pharmaceutical salts, featuring a diverse range of counterions; however, hydrochlorides are the most abundant.About:
This article is published in Drug Discovery Today.The article was published on 2021-02-01. It has received 47 citations till now.read more
Citations
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Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs.
TL;DR: A review on the design, synthesis, and applications of pharmaceutical cocrystals to afford improved drug products and drug substances will interest researchers in crystal engineering, supramolecular chemistry, medicinal chemistry, process development, and pharmaceutical and materials sciences as discussed by the authors .
Journal ArticleDOI
Pharmaceutical Salts of Fenbendazole with Organic Counterions: Structural Analysis and Solubility Performance
Artem O. Surov,Nikita A. Vasilev,Mikhail V. Vener,Olga D. Parashchuk,Andrei V. Churakov,Oxana V. Magdysyuk,German L. Perlovich +6 more
Journal ArticleDOI
Carboxylic Acid Counterions in FDA-Approved Pharmaceutical Salts.
TL;DR: A review of carboxylic acid counterions used in FDA-approved pharmaceutical salts from 1939 to 2020 is presented in this paper, showing that carboxylate counterions have a major contribution of acetate, maleate, tartrate, and succinate.
Journal ArticleDOI
Trends in small molecule drug properties: a developability molecule assessment perspective.
TL;DR: In this article , a comprehensive analysis was conducted on molecules in the drug repurposing hub dataset to systematically uncover knowledge obtained from recent trends in physicochemical properties and the corresponding impact on chemistry manufacturing controls (CMC) development.
Journal ArticleDOI
Combining enabling formulation strategies to generate supersaturated solutions of delamanid: In situ salt formation during amorphous solid dispersion fabrication for more robust release profiles
TL;DR: In this paper , a dual strategy combining salt formation with ASD formation is proposed to alter the crystallization tendency and to improve drug release of problematic poorly water-soluble compounds, including delamanid.
References
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Journal ArticleDOI
Salt formation to improve drug solubility.
TL;DR: Physicochemical principles of salt solubility are presented, with special reference to the influence of pH-solubility profiles of acidic and basic drugs on salt formation and dissolution.
Journal ArticleDOI
Polymorphs, Salts, and Cocrystals: What’s in a Name?
Srinivasulu Aitipamula,Rahul Banerjee,Arvind K. Bansal,Kumar Biradha,Miranda L. Cheney,Angshuman Roy Choudhury,Gautam R. Desiraju,Amol G. Dikundwar,Ritesh Dubey,Naga Kiran Duggirala,Preetam P. Ghogale,Soumyajit Ghosh,Pramod Kumar Goswami,N. Rajesh Goud,Ram K. R. Jetti,Piotr H. Karpinski,Poonam Kaushik,Dinesh Kumar,Vineet Kumar,Brian Moulton,Arijit Mukherjee,Gargi Mukherjee,Allan S. Myerson,Vibha Puri,Arunachalam Ramanan,T. Rajamannar,C. Malla Reddy,Naír Rodríguez-Hornedo,Robin D. Rogers,T. N. Guru Row,Palash Sanphui,Ning Shan,Ganesh Shete,Amit Singh,Changquan Calvin Sun,Jennifer A. Swift,Ram Thaimattam,Tejender S. Thakur,Rajesh Kumar Thaper,Sajesh P. Thomas,Srinu Tothadi,Venu R. Vangala,Narayan Variankaval,Peddy Vishweshwar,David R. Weyna,Michael J. Zaworotko +45 more
TL;DR: A discussion of the FDA guidance on regulatory classification of pharmaceutical cocrystals of active pharmaceutical ingredients (APIs) was held in Manesar near Delhi, India, from February 2-4, 2012 as mentioned in this paper.
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Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities
TL;DR: In this article, a range of salts should be prepared for each new substance and their properties compared during a suitable pre-formulation program, where possible, where the salt form selected will influence other properties such as melting point, hygroscopicity, chemical stability, dissolution rate, solution pH, crystal form, and mechanical properties.
Book
Drug Delivery Strategies for Poorly Water-Soluble Drugs
Alfred Fahr,Xiangli Liu +1 more
TL;DR: The emerging formulation designs for delivering of poorly water-soluble drugs, including the massive use of surface-active excipients for solubilisation, are addressed.
Journal ArticleDOI
The expanding role of prodrugs in contemporary drug design and development
TL;DR: This Review highlights prodrug design strategies for improved formulation and pharmacokinetic and targeting properties, with a focus on the most recently marketed prodrugs.