Insight into Concept and Progress on Pharmaceutical Co-Crystals: An overview

Vemuri, Venkata Deepthi; Srinivas, Leela

doi:10.5530/ijper.53.4s.147

Cited by 18 publications

(25 citation statements)

References 141 publications

(208 reference statements)

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“…The studies pointed out the increased dissolution performance of RSC upon co-crystallization with L-asparagine and L-glutamine, which is in good agreement with apparent solubility studies. The strategy of converting the idea of cocrystals into the application was well explained in the previous literatures, which may be helpful for process development in the future investigation [62][63][64].…”

Section: Discussionmentioning

confidence: 99%

Rosuvastatin cocrystals: an attempt to modulate physicochemical parameters

Vemuri

Srinivas

2021

Futur J Pharm Sci

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Background The meager physicochemical properties like low solubility and low dissolution rate of rosuvastatin calcium remain as an obstruction for formulation development. In the present work, we explore the evolution of rosuvastatin cocrystal, which may offer the synergetic physico-chemical properties of the drug. Cocrystal crafting depends on two possible intermolecular interactions; heteromeric and the homomeric selection of compounds with complementary functional groups are contemplated as a possible cause of supramolecular synthons in cocrystal formation. Specifically, cocrystals of rosuvastatin with l-asparagine and l-glutamine with molar ratio (1:1) were fabricated by using slow solvent evaporation and slow evaporation techniques. Novel cocrystals of rosuvastatin-asparagine (RSC-C) and rosuvastatin-glutamine (RSC-G) cocrystals obtained by slow solvent evaporation were utilized for preliminary investigation and further scale-up was done by using the solvent evaporation technique. Results The novel cocrystals showed a new characteristic of powder X-ray diffraction, thermograms of differential scanning calorimetry, 1H liquid FT-NMR spectra, and scanning electron microscopy. These results signify the establishment of intermolecular interaction within the cocrystals. In both the novel cocrystals, rosuvastatin was determined to be engaged in the hydrogen bond interaction with the complementary functional groups of l-asparagine and l-glutamine. Compared with the pure rosuvastatin, RSC-C and RSC-G cocrystal showed 2.17-fold and 1.60-fold improved solubility respectively. The dissolution test showed that the RSC-C and RSC-G cocrystal exhibited 1.97-fold and 1.94-fold higher dissolution rate than the pure rosuvastatin in pH6.8 phosphate buffer respectively. Conclusion Modulation in the chemical environment, improvement in the solubility, and dissolution rate demonstrated the benefit of co-crystallization to improve the physicochemical properties of the drug. Graphical abstract

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Section: Discussionmentioning

confidence: 99%

Rosuvastatin cocrystals: an attempt to modulate physicochemical parameters

Vemuri

Srinivas

2021

Futur J Pharm Sci

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“…Hereafter, stability properties are undoubtedly the big challenge in co-crystallization. Practically, stability testing is carried out on various aspects, namely moisture stress, thermal stress, and chemical stability [ 119 ].…”

Section: Challenges In Nsaid Co-crystal Developmentmentioning

confidence: 99%

“…The stability test results at a temperature of 40 °C and a humidity of 75% RH, 82% RH, and 96% RH for two weeks showed no change in the mefenamic acid-N-methyl- d -glucamine (MFA–MG) co-crystal, indicating that the co-crystal was stable in high humidity [ 66 ]. This test provides information that the water content caused molecular damage to determine co-crystal shelf life and storage [ 119 ]. Moisture can cause co-crystal distortion, conversion to a hydrate form, or dissociation [ 19 ].…”

Section: Challenges In Nsaid Co-crystal Developmentmentioning

confidence: 99%

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Challenges and Progress in Nonsteroidal Anti-Inflammatory Drugs Co-Crystal Development

Nugrahani

Parwati

2021

Molecules

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Co-crystal innovation is an opportunity in drug development for both scientists and industry. In line with the “green pharmacy” concept for obtaining safer methods and advanced pharmaceutical products, co-crystallization is one of the most promising approaches to find novel patent drugs, including non-steroidal anti-inflammatory drugs (NSAID). This kind of multi-component system improves previously poor physicochemical and mechanical properties through non-covalent interactions. Practically, there are many challenges to find commercially viable co-crystal drugs. The difficulty in selecting co-formers becomes the primary problem, followed by unexpected results, such as decreased solubility and dissolution, spring and parachute effect, microenvironment pH effects, changes in instability, and polymorphisms, which can occur during the co-crystal development. However, over time, NSAID co-crystals have been continuously updated regarding co-formers selection and methods development.

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“…Solvent-assisted grinding is one of the most used methods for cocrystal synthesis. In this method, the API and the coformer are ground together (manually using a mortar and pestle, or with a ball mill) with a small amount of solvent (Vemuri & Lankalapalli, 2019). This method allows the rapid determination of the formation of cocrystals if the grinding process is monitored by infrared (IR) spectroscopy or powder X-ray diffraction (PXRD) (Pindelska et al, 2017).…”

Section: Introductionmentioning

confidence: 99%

Crystal structures of cocrystals of 2,7-dihydroxynaphthalene with isoniazid and piracetam

González-González¹,

Flores²,

Flores-Álamo³

et al. 2022

Acta Crystallogr C

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Cocrystals of 2,7-dihydroxynaphthalene (DHN, or naphthalene-2,7-diol) with isoniazid (pyridine-4-carbohydrazide) (INH), denoted DHN–INH [C10H8O2·C6H7N3O, (I)], and piracetam [2-(2-oxopyrrolidin-1-yl)acetamide] (PIR), denoted DHN–PIR [C10H8O2·C6H10N2O2, (II)], were obtained by the solvent-assisted grinding method and characterized by IR spectroscopy, powder X-ray diffraction and single-crystal X-ray diffraction. Cocrystal (I) crystallized in the triclinic space group P\overline{1} and showed a 2:2 stoichiometry. DHN and INH molecules are connected by O—H...N(pyridine) and O—H...N(hydrazide) hydrogen bonds. Cocrystal (II) crystallized in the space group Pca21 with a 1:1 stoichiometry. DHN and PIR molecules are connected by O—H...O=C hydrogen bonds. The supramolecular architecture of cocrystal (I) showed interlinked supramolecular tapes; meanwhile, in cocrystal (II), interlinked supramolecular sheets were observed.

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Insight into Concept and Progress on Pharmaceutical Co-Crystals: An overview

Cited by 18 publications

References 141 publications

Rosuvastatin cocrystals: an attempt to modulate physicochemical parameters

Rosuvastatin cocrystals: an attempt to modulate physicochemical parameters

Challenges and Progress in Nonsteroidal Anti-Inflammatory Drugs Co-Crystal Development

Crystal structures of cocrystals of 2,7-dihydroxynaphthalene with isoniazid and piracetam

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