Applying Hot-Stage Microscopy to Co-Crystal Screening: A Study of Nicotinamide with Seven Active Pharmaceutical Ingredients

Berry, David J.; Seaton, Colin C.; Clegg, William; Harrington, Ross W.; Coles, Simon J.; Horton, Peter N.; Hursthouse, Michael B.; Storey, Richard; Jones, William; Friščić, Tomislav; Blagden, Nicholas

doi:10.1021/cg800035w

Cited by 307 publications

(250 citation statements)

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“…18 Also, Myz et al have studied a 1 : 1 citric acid-meloxicam cocrystal. 19 A number of paracetamol cocrystals have been reported to date; [20][21][22] Lemmerer et al have studied cocrystal of citric acid and nicotinamide formation of four hydrogen bonding heterosynthons in one cocrystal; 23 Schantz et al have studied citric acid anhydrous and paracetamol, prepared as crystalline physical mixtures using solid-state NMR, 24 but a systematic synthesis and vibrational spectroscopy characterization of the citric acid-paracetamol (CIT-Pa) cocrystal have not to our knowledge been studied hitherto.…”

Section: 4mentioning

confidence: 99%

Identification of a new cocrystal of citric acid and paracetamol of pharmaceutical relevance

et al. 2011

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Cocrystals have been increasingly recognized as an attractive alternative delivery form for solid drug products. In this work, Raman spectroscopy, X-ray powder diffraction/X-ray crystallography, and differential scanning calorimetry have been used to study the phenomenon of cocrystal formation in stoichiometric mixtures of citric acid with paracetamol. Raman spectroscopy was particularly useful for the characterization of the products and was used to determine the nature of the interactions in the cocrystals. It was observed that little change in the vibrational modes associated with the phenyl groups of the respective reactants took place upon cocrystal formation but changes in intensities of the vibrational modes associated with the amide and the carboxylic acid groups were observed upon cocrystal formation. Several new vibrational bands were identified in the cocrystal which were not manifest in the raw material and could be used as diagnostic features of cocrystal formation. An understanding of the effects of cocrystal formation on the vibrational modes was obtained by the complete assignment of the spectra of the starting materials and of the cocrystal component. The results show that the cocrystals was obtained in a 2 : 1 molar ratio of paracetamol to citric acid. The asymmetric unit of the crystal contains two paracetamol molecules hydrogen-bonded to the citric acid; one of these acts as a phenolic-OH hydrogen bond donor to the carbonyl of a carboxylic acid arm of citric acid. In contrast, the other phenolic-OH acts as a hydrogen bond acceptor from the quaternary C-OH of citric acid.

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Section: 4mentioning

confidence: 99%

Identification of a new cocrystal of citric acid and paracetamol of pharmaceutical relevance

et al. 2011

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“…So, some researchers used DSC with other techniques for the screening of the cocrystals [76] . Hot stage microscopy was also used for identification of cocrystals and found to increase the overall screening efficiency [77] . This method offers identification of number of phases present in the system by direct visualization when two components were heated.…”

Section: Thermal Analysismentioning

confidence: 99%

“…Nicotinamide was selected as coformer and hot stage microscopy was used for screening of cocrystals' formation with different APIs. Hot stage microscopy is also known as Kofler contact method [77,78] .…”

Section: Thermal Analysismentioning

confidence: 99%

Pharmaceutical Cocrystals: An Overview

Kumar¹,

Nanda²

2017

pharmaceutical-sciences

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“…Diversas abordagens são utilizadas nos processos de cocristalização na área farmacêutica, dentre elas destacam-se a cristalização em solução, 67-69 a moagem, 70 a cristalização por fusão 51,71 e o método de cristalização por reação (MCR). 68 Entre os diferentes métodos, o MCR 68 apresenta grande vantagem na triagem e obtenção de cocristais, uma vez que é capaz de formar cocristais sem que ocorra a cristalização dos componentes individuais.…”

Section: Estratégias De Formação De Cocristaisunclassified

Cocristais: uma estratégia promissora na área farmacêutica

et al. 2016

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COCRYSTALS: A PROMISING STRATEGY IN PHARMACEUTICAL SCIENCES. Pharmaceutical cocrystals have emerged as a useful strategy to improve the aqueous solubility of poorly water soluble drugs by aiming to enhance their oral absorption and bioavailability. Aqueous cocrystal solubility can be orders of magnitude higher than that of the constituent drug and this solubility advantage can be fine-tuned based on environmental conditions such as pH and the presence of drug solubilizing agents. This review presents a brief overview of pharmaceutical cocrystals regarding cocrystal design, obtainment methods, with particular focus on cocrystal solubility, and the solubility modulation by solution phase chemistry.Keywords: cocrystals; drug; solubility; transition point; thermodynamic stability. INTRODUÇÃOO setor de fármaco-medicamentos representa uma área estratégica sob o ponto de vista tecnológico/produtivo nacional. Vários são os desafios da produção de medicamentos competitivos e de qualidade no Brasil, como a oferta de insumos, a pesquisa de novas moléculas ativas e a sua inserção no mercado. Neste sentido, a utilização de inovações incrementais surge como alternativa à problemática do setor, destacando-se a manipulação da forma cristalina dos fármacos, síntese de polimorfos, sais, complexos e, mais recentemente, os cocristais. 1 Cocristais são materiais cristalinos homogêneos, compostos por dois ou mais compostos em proporção estequiométrica definida e que são sólidos em condições ambientes (25 ºC/1 atm). 2,3 Ao longo das últimas décadas, os cocristais têm recebido atenção significativa por parte da indústria farmacêutica, e diversos cocristais farmacêuticos têm sido relatados. Cocristais farmacêuticos, por sua vez, são compostos por um ingrediente farmacêutico ativo (IFA) e uma molécula não tóxica ou outro IFA, chamado de coformador. Ligações de hidrogênio entre as moléculas neutras do fármaco e do coformador orientam a formação do cocristal. 2,4 A síntese de cocristais tem sido uma estratégia cada vez mais utilizada para melhorar a solubilidade, a taxa de dissolução in vitro, e consequentemente, a biodisponibilidade de fármacos pouco solúveis, sem a necessidade de mudar a estrutura molecular e/ou a interação farmacológica. [5][6][7] No entanto, a avaliação da solubilidade e estabilidade dos cocristais em solução ainda não está consolidada. Um levantamento realizado no período de 1999 a 2015 (Figura 1) revelou um crescente número de publicações envolvendo a síntese e a caracterização dos cocristais, mas um reduzido número de publicações envolvendo outros aspectos essenciais no desenvolvimento de formulações contendo cocristais, como estudos de solubilidade, química em solução, estabilidade e a influência de excipientes.Considerando que a baixa solubilidade aquosa é um dos principais problemas associados às entidades químicas farmacêuticas, os

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Applying Hot-Stage Microscopy to Co-Crystal Screening: A Study of Nicotinamide with Seven Active Pharmaceutical Ingredients

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Cited by 307 publications

References 50 publications

Identification of a new cocrystal of citric acid and paracetamol of pharmaceutical relevance

Identification of a new cocrystal of citric acid and paracetamol of pharmaceutical relevance

Pharmaceutical Cocrystals: An Overview

Cocristais: uma estratégia promissora na área farmacêutica

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