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Crystals
Special Issues
Pharmaceutical Cocrystals
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Pharmaceutical Cocrystals

A special issue of Crystals (ISSN 2073-4352).

Deadline for manuscript submissions: closed (30 November 2015)

Special Issue Editor

Prof. Dr. Sitaram Velaga

E-Mail Website
Guest Editor
Department of Health Sciences, Luleå University of Technology, Luleå, Sweden
Interests: pharmaceutical materials; polymorphs; physical stability; solubility; salts; cocrystals; crystallization; phase diagrams; drug formulation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Pharmaceutical cocrystals are structurally homogeneous multicomponent solids comprising active pharmaceutical ingredient (API) in a stoichiometric ratio, with a second component that is solid at ambient temperature. Cocrystals can exhibit enhanced physical, mechanical and biopharmaceutical properties of a drug, due to changes in their crystal and solid structure. Consequently, pharmaceutical cocrystallization has emerged as an alternative and viable strategy to address development issues of APIs in the pharmaceutical industry.

This Special Issue intends to provide a unique forum to gather research results and scientific advances in the entire field of Pharmaceutical cocrystals. We welcome research as well as review articles covering topics including, but not limited to: cocrystal theoretical prediction tools, screening methods, design, crystal engineering, solid state characterization, structural analysis, scale-up processes, solubility, stability, manufacturability and pharmacokinetics.

Prof. Dr. Sitaram Velaga
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Crystals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2600 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


 

Keywords

  • pharmaceutical solid forms
  • cocrystals and salts
  • intermolecular interactions
  • physicochemical and mechanical properties
  • bioavailability

Published Papers (2 papers)

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Research

3395 KiB  
Article
Crystal Structures, Thermal Analysis, and Dissolution Behavior of New Solid Forms of the Antiviral Drug Arbidol with Dicarboxylic Acids
by Alex N. Manin, Artem O. Surov, Andrei V. Churakov and German L. Perlovich
Crystals 2015, 5(4), 650-669; https://doi.org/10.3390/cryst5040650 - 04 Dec 2015
Cited by 20 | Viewed by 7709
Abstract
Salts of the antiviral drug arbidol (umifenovir) (Arb) with maleate (Mlc) and fumarate (Fum) anions have been obtained, and their crystal structures have been described. The crystal structure of arbidol maleate has been redetermined by single crystal [...] Read more.
Salts of the antiviral drug arbidol (umifenovir) (Arb) with maleate (Mlc) and fumarate (Fum) anions have been obtained, and their crystal structures have been described. The crystal structure of arbidol maleate has been redetermined by single crystal X-ray diffraction at 180K. A new arbidol cocrystal in zwitterion form with succinic acid (Suc) has also been found and characterized. The arbidol zwitterion was not previously seen in any of the drug crystal forms, and the [Arb + Suc] cocrystal seems to be the first found instance. Analysis of the conformational preferences of the arbidol molecule in the crystal structures has shown that it adopts two types of conformations, namely “open” and “closed” ones. Thermal stability of the arbidol salts and cocrystal have been analyzed by means of differential scanning calorimetry, thermogravimetric, and mass-spectrometry analysis. The dissolution study of the arbidol salts and cocrystal performed in aqueous buffer solutions with pH 1.2 and 6.8 has shown that both the salts and the cocrystal dissolve incongruently to form an arbidol hydrochloride monohydrate at pH 1.2 and an arbidol base at pH 6.8, respectively. The cocrystal reaches the highest solubility level in both pH 1.2 and pH 6.8 solutions. Full article
(This article belongs to the Special Issue Pharmaceutical Cocrystals)
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4672 KiB  
Article
Liquid-Assisted Grinding to Prepare a Cocrystal of Adefovir Dipivoxil Thermodynamically Less Stable than Its Neat Phase
by Sungyup Jung, Insil Choi and Il Won Kim
Crystals 2015, 5(4), 583-591; https://doi.org/10.3390/cryst5040583 - 19 Nov 2015
Cited by 17 | Viewed by 6050
Abstract
Liquid-assisted grinding was employed to generate a cocrystal of adefovir dipivoxil (AD) and glutaric acid (GLU), which had not been successfully obtained through solution crystallization. The cocrystal formation was confirmed with powder X-ray diffraction, and its thermal stability and release behavior were studied [...] Read more.
Liquid-assisted grinding was employed to generate a cocrystal of adefovir dipivoxil (AD) and glutaric acid (GLU), which had not been successfully obtained through solution crystallization. The cocrystal formation was confirmed with powder X-ray diffraction, and its thermal stability and release behavior were studied through differential scanning calorimetry and dissolution experiments, respectively. The AD/GLU cocrystal was less stable than neat AD phase and the previously reported AD cocrystals with other dicarboxylic acids, such as suberic acid and succinic acid. This suggests that the intermolecular interactions of the AD/GLU cocrystal are probably weaker than the other crystal phases. The release behavior of the AD/GLU was comparable with the cocrystal with suberic acid. The current study verifies the effectiveness of the liquid-assisted grinding for the preparation of the thermodynamically less stable cocrystal phase. Full article
(This article belongs to the Special Issue Pharmaceutical Cocrystals)
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