Pharmaceutical cocrystallization: an effective approach to modulate the physicochemical properties of solid-state drugs

Pharmaceutical cocrystallization affords an opportunity to modify the physicochemical properties of a solid-state drug without covalent modification of its molecular structure. This review presents an update on various applications of pharmaceutical cocrystallization with considerations on both cocr...

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Published inCrystEngComm Vol. 2; no. 36; pp. 5292 - 5316
Main Authors Dai, Xia-Lin, Chen, Jia-Mei, Lu, Tong-Bu
Format Journal Article
LanguageEnglish
Published Cambridge Royal Society of Chemistry 2018
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Abstract Pharmaceutical cocrystallization affords an opportunity to modify the physicochemical properties of a solid-state drug without covalent modification of its molecular structure. This review presents an update on various applications of pharmaceutical cocrystallization with considerations on both cocrystals and salts, focusing on the property modification relevant to clinical efficacy and safety, and manufacturability of drugs. Some prominent examples of drug cocrystals/salts, which exhibit improved solubility and/or permeability and pharmacokinetics, stability and mechanic properties, are highlighted. This highlight presents an update on applications of cocrystallization to modify properties relevant to efficacy, safety, and manufacturability of drugs.
AbstractList Pharmaceutical cocrystallization affords an opportunity to modify the physicochemical properties of a solid-state drug without covalent modification of its molecular structure. This review presents an update on various applications of pharmaceutical cocrystallization with considerations on both cocrystals and salts, focusing on the property modification relevant to clinical efficacy and safety, and manufacturability of drugs. Some prominent examples of drug cocrystals/salts, which exhibit improved solubility and/or permeability and pharmacokinetics, stability and mechanic properties, are highlighted. This highlight presents an update on applications of cocrystallization to modify properties relevant to efficacy, safety, and manufacturability of drugs.
Pharmaceutical cocrystallization affords an opportunity to modify the physicochemical properties of a solid-state drug without covalent modification of its molecular structure. This review presents an update on various applications of pharmaceutical cocrystallization with considerations on both cocrystals and salts, focusing on the property modification relevant to clinical efficacy and safety, and manufacturability of drugs. Some prominent examples of drug cocrystals/salts, which exhibit improved solubility and/or permeability and pharmacokinetics, stability and mechanic properties, are highlighted.
Author Dai, Xia-Lin
Chen, Jia-Mei
Lu, Tong-Bu
AuthorAffiliation Institute for New Energy Materials and Low Carbon Technologies
Tianjin University of Technology
School of Chemistry and Chemical Engineering
Sun Yat-Sen University
School of Pharmaceutical Sciences
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  name: Tianjin University of Technology
– sequence: 0
  name: School of Pharmaceutical Sciences
Author_xml – sequence: 1
  givenname: Xia-Lin
  surname: Dai
  fullname: Dai, Xia-Lin
– sequence: 2
  givenname: Jia-Mei
  surname: Chen
  fullname: Chen, Jia-Mei
– sequence: 3
  givenname: Tong-Bu
  surname: Lu
  fullname: Lu, Tong-Bu
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Notes 2
reduction catalysts and pharmaceutical polymorphs and cocrystals.
a crystal engineering based approach.
Jia-Mei Chen currently serves as a professor in the School of Chemistry and Chemical Engineering at Tianjin University of Technology. She was born in 1979 and obtained her PhD (2008) from Sun Yat-Sen University under the supervision of Professor Tong-Bu Lu. After a short industrial stint as a chemist at Lonza R&D, China, she served as a faculty member at Yat-Sen University from 2010-2018. Her areas of research interest focus upon pharmaceutical cocrystallization and polymorphism
Tong-Bu Lu (1964) obtained his B.S. in 1988 and PhD in 1993 under the supervision of Prof. Min-Yu Tan from Lanzhou University. After two years of postdoctoral fellowship at Sun Yat-Sen University, he joined the faculty at the same university and became a professor in 2000. He moved to Tianjin University of Technology in 2016. His current research interest lies in energy materials including water splitting and CO
Xia-Lin Dai (1993) obtained her BSc in Pharmaceutical Science from Nankai University in 2015. Currently she is a PhD student at the School of Pharmaceutical Sciences, Sun Yat-Sen University, supervised by Professor Tong-Bu Lu. Her current research revolves around pharmaceutical cocrystallization, including cocrystals and salts, with the intention of improving the solubility and permeability of active pharmaceutical ingredients.
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Snippet Pharmaceutical cocrystallization affords an opportunity to modify the physicochemical properties of a solid-state drug without covalent modification of its...
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SubjectTerms Cocrystallization
Drugs
Manufacturability
Molecular structure
Pharmaceuticals
Solid state
Title Pharmaceutical cocrystallization: an effective approach to modulate the physicochemical properties of solid-state drugs
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