Pharmaceutical Cocrystals: An Overview

Kumar, Selvamuthu R; Nanda, Amita

doi:10.4172/pharmaceutical-sciences.1000302

Cited by 85 publications

(95 citation statements)

References 97 publications

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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].…”

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

127

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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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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

127

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“…Greenhalgh suggests the formation of co-crystals if the difference is ≤ 7 MPa 1/2 . 22,29 In addition to this, Salem et al have recently contributed cut-off value 8.18 MPa 1/2 , which is more dependable due to the relaxation of the cut-off value compared to the previous values. 30…”

Section: Hansen Solubility Parameter (Hsp)mentioning

confidence: 97%

“…The equation involved in the prediction of cocrystal formation is ΔpKa=[pKa(base) -pKa(acid)]. 22 The transfer of proton can be seen if the difference in the pKa value is more than 3. If the ΔpKa value is less than zero, then co-crystal might be formed and the higher value that is more than 3 results in the formation of salts.…”

Section: Pka Based Modelmentioning

confidence: 99%

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Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

et al. 2020

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Pharmaceutical co-crystals are novel class of pharmaceutical substances, which possess an apparent probability of advancement of polished physical properties offering stable and patentable solid forms. These multi-component crystalline forms influence pertinent physicochemical parameters like solubility, dissolution rate, chemical stability, physical stability, etc. which in turn result in the materials with superior properties to those of the free drug. Co-crystallization is a process by which the molecular interactions can be altered to optimize the drug properties. Co-crystals comprise a multicomponent system of active pharmaceutical ingredient (API) with a stoichiometric amount of a pharmaceutically acceptable coformer incorporated in the crystal lattice. By manufacturing pharmaceutical co-crystals, the physicochemical properties of a drug can be improved thus multicomponent crystalline materials have received renewed interest in the current scenario due to the easy administration in the pharmaceutical industry. There is an immense amount of literature available on co-crystals. However, there is a lack of an exhaustive review on a selection of coformers and regulations on co-crystals. The review has made an attempt to bridge this gap. The review also describes the methods used to prepare co-crystals with their characterization. Brief description on the pharmaceutical applications of co-crystals has also been incorporated here. Efforts are made to include reported works on co-crystals, which further help to understand the concept of co-crystals in depth.

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“…This technique mainly includes: Solvent evaporation [12], solvent drop grinding [13], liquid-assisted grinding [14], solution crystallization [15], cooling crystallization [16], supercritical fluids [17], slurry method [18], antisolvent method [19], reaction crystallization method [20], ultrasound-assisted solution technique [21], supercritical fluid atomization techniques [22], and spray drying techniques [23].…”

Section: Liquid-based Techniquementioning

confidence: 99%

Cocrystals: A Complete Review on Conventional and Novel Methods of Its Formation and Its Evaluation

Yadav

Khursheed

Singh

2019

Asian J Pharm Clin Res

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The active moiety with poor solubility is posing a challenge in drug development which may reduce the effectiveness in patients when administered orally. Cocrystal formation is one of the latest approaches for improving the various parameters of a drug molecule such as solubility, melting point, pharmacokinetic, pharmacodynamic, and bioavailability. Cocrystals are crystalline single state materials composed of two or more than two different molecular amalgams held together in a fixed stoichiometric ratio. There are various techniques used for the preparation of cocrystals such as solvent evaporation, grinding, and cooling crystallization. The quantitative and qualitative aspects of these cocrystals are evaluated using various validated instruments such as nuclear magnetic resonance, powder X-ray diffraction, and differential scanning calorimetry.

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Pharmaceutical Cocrystals: An Overview

Cited by 85 publications

References 97 publications

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

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

Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

Cocrystals: A Complete Review on Conventional and Novel Methods of Its Formation and Its Evaluation

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