Co-crystals of non-steroidal anti-inflammatory drugs(NSAIDs):Insight toward formation,methods,and drug enhancement

作     者：Andre L.C.S.Nascimento Richard P.Fernandes Maxime D.Charpentier Joop H.ter Horst Flavio J.Caires Marius Chorilli André L.C.S.Nascimento;Richard P.Fernandes;Maxime D.Charpentier;Joop H.ter Horst;Flávio J.Caires;Marlus Chorilli

作者机构：Sao Paulo State University(UNESP)School of Pharmaceutical Sciences14800-903 AraraquaraSao PauloBrazil São Paulo State University(UNESP)Institute of Chemistry14800-060 AraraquaraSao PauloBrazil EPSRC Centre for Innovative Manufacturing in Continuous Manufacturing and CrystallisationUniversity of StrathclydeGlasgowUK Sao Paulo State University(UNESP)School of Sciences17033-260 BauruSao PauloBrazil 

出 版 物：《Particuology》 (颗粒学报（英文版）)

年 卷 期：2021年第19卷第5期

页      面：227-241页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：FAPESP(Proc.n 2013/09022-7,2017/14936-9,2018/12463-9,2018/24378-6 and 2018/23357-5) CNPq(Proc.141829/2017-6)for financial support the European Union's Horizon 2020 research and innovation programme under the Marie Sklodowska-Curie grant agreement No.722456 CORE ITN for funding as part of the CORE project(October 2016-September 2020) the EPSRC Centre for Innovative Manufacturing in Continuous Manufacturing and Crystallization(http://www.cmac.ac.uk)for supporting this work(EPSRC funding under Grant Reference:EP/1033459/1) 

主　　题：Pharmaceutical co-crystals NSAIDs Supramolecular synthons Co-crystal discovery Bioavailability 

摘      要：Pharmaceutical co-crystals have been explored by many researchers as a strategy to optimize physicochemical properties of solid-state *** improvements of solubility,bioavailability,and the reduced tendency for phase transformation occurrence,are factors that highlight benefits of pharmaceutical co-crystals among other solid *** to the Biopharmaceutical Classification System(BCS),non-steroidal anti-inflammatory drugs(NSAIDs)are class Ⅱ drugs,which have low aqueous solubility and therefore co-crystallization has the potential to optimize NSAID product *** this review,we highlight the recent progress made on NSAIDs co-crystals,their co-formers,synthesis,methods and use,while we underline some promising results on in vitro and in vivo co-crystal properties.A celecoxib-tramadol co-crystal reaches phase Ⅲ clinical trials,showing greater analgesic activity than both individual *** aqueous solubility of the co-crystal formed between l-proline and diclofenac is very high in comparison with the pure *** co-crystals with urea and thiourea have an increase of drug release of almost 60%.Co-crystal design brings a new perspective in drug development since the co-former used can also be a biologically active component allowing to combine different anti-inflammatory drugs,which have an incredible spectrum of application due to the analgesic,anti-pyretic and anti-inflammatory properties.