Anti-solvent co-crystallization of carbamazepine and saccharin

Wang, In Chun; Lee, Min-Jeong; Sim, Sang Jun; Kim, Woo Sik; Chun, Nan Hee; Choi, Guang J.

doi:10.1016/j.ijpharm.2013.04.012

Cited by 62 publications

(45 citation statements)

References 36 publications

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“…Disadvantages of this method are its lower performance compared to grinding that uses a solvent, as well as the large volume of solvent used. Antisolvent crystallization has been reported for the production of carbamazepine-saccharin and indomethacin-saccharin cocrystals [ 98 , 99 ]. In both studies, the construction of phase solubility diagrams was an integral part of the methodology for identifying the optimal conditions (e.g., ratio of solvent to antisolvent) for the formation of cocrystals.…”

Section: Methods Of Cocrystal Preparationmentioning

confidence: 99%

Pharmaceutical Cocrystals: New Solid Phase Modification Approaches for the Formulation of APIs

2018

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Cocrystals can be used as an alternative approach based on crystal engineering to enhance specific physicochemical and biopharmaceutical properties of active pharmaceutical ingredients (APIs) when the approaches to salt or polymorph formation do not meet the expected targets. In this article, an overview of pharmaceutical cocrystals will be presented, with an emphasis on the intermolecular interactions in cocrystals and the methods for their preparation. Furthermore, cocrystals of direct pharmaceutical interest, along with their in vitro properties and available in vivo data and characterization techniques are discussed, highlighting the potential of cocrystals as an attractive route for drug development.

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Section: Methods Of Cocrystal Preparationmentioning

confidence: 99%

Pharmaceutical Cocrystals: New Solid Phase Modification Approaches for the Formulation of APIs

2018

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“…Improvement of dissolution profiles can be obtained by particle size reduction techniques (Choi and Park, 2017;Dizaj et al, 2015;Khadka et al, 2014;Sironi et al, 2017), crystal morphology/polymorphism modifications (Amodwala et al, 2017;Jain et al, 2017;Keraliya et al, 2010;Maghsoodi, 2015) or multicomponent A C C E P T E D M A N U S C R I P T crystals synthesis (Ross et al, 2016;Schultheiss and Newman, 2009;Yadav et al, 2009). The latter approach including bi-component cocrystallization deserves particular attention due to the variety of cocrystal preparation methods such as solvent evaporation techniques (Bag et al, 2011;Bag and Reddy, 2012;Cysewski et al, 2016;Przybyłek et al, 2016aPrzybyłek et al, , 2016b, antisolvent crystallization (Chun et al, 2014;Lee et al, 2015;Wang et al, 2013), mechanochemical co-grinding (Hasa et al, 2015;Karki et al, 2007;Li et al, 2016;Tröbs and Emmerling, 2014) or slurry methods (Apshingekar et al, 2017;Kojima et al, 2010;Takata et al, 2008). Furthermore, the variety of cocrystals formers applicable for pharmaceutical formulations offers fine tuning of physicochemical properties of new multicomponent solids ood and Rodr guez-Hornedo, 2009).…”

Section: Introductionmentioning

confidence: 99%

Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index

Cysewski

Przybyłek

2017

European Journal of Pharmaceutical Sciences

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New theoretical screening procedure was proposed for appropriate selection of potential cocrystal formers possessing the ability of enhancing dissolution rates of drugs. The procedure relies on the training set comprising 102 positive and 17 negative cases of cocrystals found in the literature. Despite the fact that the only available data were of qualitative character, performed statistical analysis using binary classification allowed to formulate quantitative criterions. Among considered 3679 molecular descriptors the relative value of lipoaffinity index, expressed as the difference between values calculated for active compound and excipient, has been found as the most appropriate measure suited for discrimination of positive and negative cases. Assuming 5% precision, the applied classification criterion led to inclusion of 70% positive cases in the final prediction. Since lipoaffinity index is a molecular descriptor computed using only 2D information about a chemical structure, its estimation is straightforward and computationally inexpensive. The inclusion of an additional criterion quantifying the cocrystallization probability leads to the following conjunction criterions H<-0.18 and ΔLA>3.61, allowing for identification of dissolution rate enhancers. The screening procedure was applied for finding the most promising coformers of such drugs as Iloperidone, Ritonavir, Carbamazepine and Enthenzamide.

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“…It is difficult to obtain cocrystal product with high purity and good quality using the grinding method [ 15 , 16 , 17 ]. The solution method has been applied in many cases to prepare cocrystal [ 18 , 19 ]. In the solution method, the selection of solvent is very important.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Carbamazepine Cocrystal in Polymer Solution

et al. 2017

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In this study, we attempted to prepare carbamazepine (CBZ) cocrystal through the solution method in ethanol-water solvent mixture (volume ratio 1:1) and polyvinyl pyrrolidone (PVP) solution. Nicotinamide (NIC) and saccharin (SAC) were selected as cocrystal coformers. Cocrystal screening products were characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD) techniques. Characterization results show that in ethanol-water solvent mixture, pure CBZ-NIC cocrystal can be prepared, while CBZ-SAC cocrystal cannot be obtained. The addition of PVP can inhibit CBZ-NIC cocrystal formation and facilitate CBZ-SAC cocrystal formation.

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Anti-solvent co-crystallization of carbamazepine and saccharin

Cited by 62 publications

References 36 publications

Pharmaceutical Cocrystals: New Solid Phase Modification Approaches for the Formulation of APIs

Pharmaceutical Cocrystals: New Solid Phase Modification Approaches for the Formulation of APIs

Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index

Preparation and Characterization of Carbamazepine Cocrystal in Polymer Solution

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