Characteristics of indomethacin–saccharin (IMC–SAC) co-crystals prepared by an anti-solvent crystallization process

Chun, Nan-Hee; Wang, In-Chun; Lee, Min‐Jeong; Jung, Yun-Taek; Lee, Sang Kil; Kim, Woo‐Sik; Choi, Guang J.

doi:10.1016/j.ejpb.2013.02.007

Cited by 51 publications

(27 citation statements)

References 20 publications

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“…To realize the objective of the study, widely investigated co-crystals of indomethacin with saccharin [ 8 , 10 , 16 , 18 , 19 , 20 , 21 ] and furosemide with p -aminobenzoic acid [ 12 , 14 , 22 ] were chosen as the model samples. Their crystal structure is already known to consist of ingredient dimers connected via hydrogen bonds.…”

Section: Resultsmentioning

confidence: 99%

DSC, FTIR and Raman Spectroscopy Coupled with Multivariate Analysis in a Study of Co-Crystals of Pharmaceutical Interest

Garbacz

Wesołowski

2018

Molecules

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Co-crystals have garnered increasing interest in recent years as a beneficial approach to improving the solubility of poorly water soluble active pharmaceutical ingredients (APIs). However, their preparation is a challenge that requires a simple approach towards co-crystal detection. The objective of this work was, therefore, to verify to what extent a multivariate statistical approach such as principal component analysis (PCA) and cluster analysis (CA) can be used as a supporting tool for detecting co-crystal formation. As model samples, physical mixtures and co-crystals of indomethacin with saccharin and furosemide with p-aminobenzoic acid were prepared at API/co-former molar ratios 1:1, 2:1 and 1:2. Data acquired from DSC curves and FTIR and Raman spectroscopies were used for CA and PCA calculations. The results obtained revealed that the application of physical mixtures as reference samples allows a deeper insight into co-crystallization than is possible with the use of API and co-former or API and co-former with physical mixtures. Thus, multivariate matrix for PCA and CA calculations consisting of physical mixtures and potential co-crystals could be considered as the most profitable and reliable way to reflect changes in samples after co-crystallization. Moreover, complementary interpretation of results obtained using DSC, FTIR and Raman techniques is most beneficial.

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Section: Resultsmentioning

confidence: 99%

DSC, FTIR and Raman Spectroscopy Coupled with Multivariate Analysis in a Study of Co-Crystals of Pharmaceutical Interest

Garbacz

Wesołowski

2018

Molecules

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“…As for the production of co-crystals, the drugs can be dissolved into different miscible organic solvents, premixed, and then added to aqueous solution to result into saturated drugs solutions with the controlled precipitation of the paired drug molecules [120,121]. The precipitation conditions can be predicted by analyzing the phase solubility diagrams: micrococrystals of saccharin and indomethacin were prepared by adding water to drug-cofomer solutions in different organic solvents, to evaluate the effect of the solvent characteristics on the precipitation process [122]. The yield is quite high, with a recovery of 70-80% [123].…”

Section: Conventional Methodsmentioning

confidence: 99%

Production of pure drug nanocrystals and nano co-crystals by confinement methods

Fontana

Figueiredo

Zhang

et al. 2018

Advanced Drug Delivery Reviews

134

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The use of drug nanocrystals in the drug formulation is increasing due to the large number of poorly water-soluble drug compounds synthetized and due to the advantages brought by the nanonization process. The downsizing processes are done using a top-down approach (milling and homogenization currently employed at the industrial level), while the crystallization process is performed by bottom-up techniques (e.g., antisolvent precipitation, use of supercritical fluids or spray and freeze drying). In addition, the production of nanocrystals in confined environment can be achieved within microfluidics channels. This review analyzes the processes for the preparation of nanocrystals and co-crystals, divided by top-down and bottom-up approaches, together with their combinations. The combination of both strategies merges the favorable features of each process and avoids the disadvantages of single processes. Overall, the applicability of drug nanocrystals is highlighted by the widespread research on the production processes at the engineering, pharmaceutical, and nanotechnology level.

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“…41 The reaction rate is depended on used solvent; the preformulation testing by evaporation method using various solvents is useful. 41,43 However, the granulation should be carried out using green chemicals for pharmaceutical industry; therefore, water and ethanol are preferable and used in this study. Figure 3 shows the XRD pattern of each starting material, the reference IND-SAC cocrystal, and each dried granule sample using a one-step wet granulation method.…”

Section: Effect Of the High-shear Wet Granulation Processmentioning

confidence: 99%

“…40 Indomethacin (IND) is known as a typical weakly acidic model drug (pKa 4.5) of BCS class II and was reported to form a cocrystal with saccharin (SAC), which can enhance solubility and bioavailability of IND. [41][42][43] In this study for the purpose of making the IND-SAC cocrystal product during the consistent process, and the granules were prepared using a high-shear wet granulation method without the preprocess of cocrystal formation. The methodology allows the continuous manufacture of pharmaceutical products as a cocrystal; therefore, it is required to monitor any crystalline structure changes in the API and control the processes by in situ analysis.…”

Section: Introductionmentioning

confidence: 99%

Kinetics Study of Cocrystal Formation Between Indomethacin and Saccharin Using High-Shear Granulation With In Situ Raman Spectroscopy

Tanaka

Hattori

Ashizawa

et al. 2019

Journal of Pharmaceutical Sciences

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Characteristics of indomethacin–saccharin (IMC–SAC) co-crystals prepared by an anti-solvent crystallization process

Cited by 51 publications

References 20 publications

DSC, FTIR and Raman Spectroscopy Coupled with Multivariate Analysis in a Study of Co-Crystals of Pharmaceutical Interest

DSC, FTIR and Raman Spectroscopy Coupled with Multivariate Analysis in a Study of Co-Crystals of Pharmaceutical Interest

Production of pure drug nanocrystals and nano co-crystals by confinement methods

Kinetics Study of Cocrystal Formation Between Indomethacin and Saccharin Using High-Shear Granulation With In Situ Raman Spectroscopy

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