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Pharmaceutics
Special Issues
Controlled Crystallization of Active Pharmaceutical Ingredients, 2nd Edition
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Controlled Crystallization of Active Pharmaceutical Ingredients, 2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: 20 June 2024 | Viewed by 3025

Special Issue Editors

Prof. Dr. Il Won Kim

E-Mail Website
Guest Editor
Department of Chemical Engineering, Soongsil University, Seoul 06978, Republic of Korea
Interests: biomineralization; pharmaceutical crystallization; interfacial phenomena
Special Issues, Collections and Topics in MDPI journals
Dr. Varin Titapiwatanakun

E-Mail Website
Guest Editor
Pharmaceutical Sciences and Technology Program, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand
Interests: crystal engineering; 3D-printing; drug delivery; pharmaceutical process development

Special Issue Information

Dear Colleagues,

Crystallization is an important separation process that generates crystalline materials with high purity and yield. In the area of pharmaceutical research, the crystallization of active pharmaceutical ingredients (APIs) has been vigorously studied because of its great influence on the physicochemical properties of APIs. The size, shape, and phase of the crystals are some of the features frequently controlled during crystallization and they are closely related to the solubility, dissolution rate, and stability of the resulting API solid forms.

The aim of this Special Issue is to provide a forum for researchers in the broad field of pharmaceutical crystallization. While the focus is specifically on the crystallization of APIs, this Special Issue is open to original research and review articles on all aspects of pharmaceutical crystallization.

Prof. Dr. Il Won Kim
Dr. Varin Titapiwatanakun
Guest Editors

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. Pharmaceutics 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 2900 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

  • active pharmaceutical ingredients
  • crystal shape and size (e.g., nanodrug)
  • crystal phases (e.g., polymorph, salt, cocrystal)
  • separation processes (e.g., purity, chirality)
  • industrial process development

Published Papers (2 papers)

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Research

20 pages, 6068 KiB  
Article
Polymorphism and Multi-Component Crystal Formation of GABA and Gabapentin
by Daniel Komisarek, Fulya Demirbas, Takin Haj Hassani Sohi, Klaus Merz, Carsten Schauerte and Vera Vasylyeva
Pharmaceutics 2023, 15(9), 2299; https://doi.org/10.3390/pharmaceutics15092299 - 10 Sep 2023
Viewed by 831
Abstract
This study exploits the polymorphism and multi-component crystal formation of γ-amino butanoic acid (GABA) and its pharmaceutically active derivative, gabapentin. Two polymorphs of GABA and both polymorphs of gabapentin are structurally revisited, together with gabapentin monohydrate. Hereby, GABA form II is only accessible [...] Read more.
This study exploits the polymorphism and multi-component crystal formation of γ-amino butanoic acid (GABA) and its pharmaceutically active derivative, gabapentin. Two polymorphs of GABA and both polymorphs of gabapentin are structurally revisited, together with gabapentin monohydrate. Hereby, GABA form II is only accessible under special conditions using additives, whereas gabapentin converts to the monohydrate even in the presence of trace amounts of water. Different accessibilities and phase stabilities of these phases are still not fully clarified. Thus, indicators of phase stability are discussed involving intermolecular interactions, molecular conformations, and crystallization environment. Calculated lattice energy differences for polymorphs reveal their similar stability. Quantification of the hydrogen bond strengths with the atoms-in-molecules (AIM) model in conjunction with non-covalent interaction (NCI) plots also shows similar hydrogen bond binding energy values for all polymorphs. We demonstrate that differences in the interacting modes, in an interplay with the intermolecular repulsion, allow the formation of the desired phase under different crystallization environments. Salts and co-crystals of GABA and gabapentin with fumaric as well as succinic acid further serve as models to highlight how strongly HBs act as the motif-directing force in the solid-phase GABA-analogs. Six novel multi-component entities were synthesized, and structural and computational analysis was performed: GABA fumarate (2:1); two gabapentin fumarates (2:1) and (1:1); two GABA succinates (2:1) and (1:1); and a gabapentin:succinic acid co-crystal. Energetically highly attractive carboxyl/carboxylate interaction overcomes other factors and dominates the multi-component phase formation. Decisive commonalities in the crystallization behavior of zwitterionic GABA-derivatives are discussed, which show how they can and should be understood as a whole for possible related future products. Full article
(This article belongs to the Special Issue Controlled Crystallization of Active Pharmaceutical Ingredients, 2nd Edition)
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16 pages, 10935 KiB  
Article
Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples
by Meitong Shen, Ling Zheng and Leo H. Koole
Pharmaceutics 2023, 15(8), 2146; https://doi.org/10.3390/pharmaceutics15082146 - 15 Aug 2023
Viewed by 1052
Abstract
Injectable polymer microparticles with the ability to carry and release pharmacologically active agents are attracting more and more interest. This study is focused on the chemical synthesis, characterization, and preliminary exploration of the utility of a new type of injectable drug-releasing polymer microparticle. [...] Read more.
Injectable polymer microparticles with the ability to carry and release pharmacologically active agents are attracting more and more interest. This study is focused on the chemical synthesis, characterization, and preliminary exploration of the utility of a new type of injectable drug-releasing polymer microparticle. The particles feature a new combination of structural and physico-chemical properties: (i) their geometry deviates from the spherical in the sense that the particles have a cavity; (ii) the particles are porous and can therefore be loaded with crystalline drug formulations; drug crystals can reside at both the particle’s surfaces and inside cavities; (iii) the particles are relatively dense since the polymer network contains covalently bound iodine (approximately 10% by mass); this renders the drug-loaded particles traceable (localizable) by X-ray fluoroscopy. This study presents several examples. First, the particles were loaded with crystalline voriconazole, which is a potent antifungal drug used in ophthalmology to treat fungal keratitis (infection/inflammation of the cornea caused by penetrating fungus). Drug loading as high as 10% by mass (=mass of immobilized drug/(mass of the microparticle + mass of immobilized drug) × 100%) could be achieved. Slow local release of voriconazole from these particles was observed in vitro. These findings hold promise regarding new approaches to treat fungal keratitis. Moreover, this study can help to expand the scope of the transarterial chemoembolization (TACE) technique since it enables the use of higher drug loadings (thus enabling higher local drug concentration or extended therapy duration), as well as application of hydrophobic drugs that cannot be used in combination with existing TACE embolic particles. Full article
(This article belongs to the Special Issue Controlled Crystallization of Active Pharmaceutical Ingredients, 2nd Edition)
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