Co-Crystals: A Review

Chaudhari, Shilpa P.; Nikam, Sarika Ankushrao; Khatri, Neetu; Wakde, Shubham

doi:10.22270/jddt.v8i6-s.2194

Cited by 32 publications

(29 citation statements)

References 28 publications

(32 reference statements)

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“…This fact makes co-crystals more accessible than other methods, such as micronization [ 25 ], solid dispersion [ 26 ], salt formation [ 27 ], nanoparticle formation [ 28 ], and others. Important factors that need to be considered in changing the physicochemical properties of a drug without changing its pharmacological activities are the character of the API and the co-former used, the molecular interactions that occur, and the synthesis procedure [ 2 ]. In contrast to salt formation, which can only be applied to ionizable API and involve the transfer of hydrogen atoms between acidic and basic functional groups, the co-crystallization technique can be used for both ionizable and non-ionizable API.…”

Section: Co-crystalsmentioning

confidence: 99%

“…On the other hand, recently discovered drugs (around 60% to 70%) are considered to be BCS (Biopharmaceutics Classification System) class II (low solubility, high permeability) and BCS class IV (low solubility, low permeability). Poor solubility may lead to problems in bioavailability and therapeutic efficacy [ 2 ]. Accordingly, many researchers have been developing ways to modulate API physicochemical properties to enhance their therapeutic effectiveness [ 3 ].…”

Section: Introductionmentioning

confidence: 99%

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Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review

Nugrahani

Jessica

2021

Molecules

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Co-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological activity through non-covalent interactions with one or more co-formers. A “green method” has recently prompted many researchers to develop solvent-free techniques or minimize solvents for arranging the eco-friendlier process of co-crystallization. Researchers have also been looking for less-risk co-formers that produce the desired API’s physicochemical properties. This review purposed to collect the report studies of amino acids as the safe co-former and explored their advantages. Structurally, amino acids are promising co-former candidates as they have functional groups that can form hydrogen bonds and increase stability through zwitterionic moieties, which support strong interactions. The co-crystals and deep eutectic solvent yielded from this natural compound have been proven to improve pharmaceutical performance. For example, l-glutamine could reduce the side effects of mesalamine through an acid-base stabilizing effect in the gastrointestinal fluid. In addition, some amino acids, especially l-proline, enhances API’s solubility and absorption in its natural deep eutectic solvent and co-crystals systems. Moreover, some ionic co-crystals of amino acids have also been designed to increase chiral resolution. Therefore, amino acids are safe potential co-formers, which are suitable for improving the physicochemical properties of API and prospective to be developed further in the dosage formula and solid-state syntheses.

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Section: Co-crystalsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review

Nugrahani

Jessica

2021

Molecules

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“…In this method, drugs and coformer are dissolved in a common solvent and kept for sonication at a constant temperature. 54 Cold water is provided in order to maintain a constant temperature of sonicator. 22 The air bubbles or voids are produced due to the high energy, that makes size reduction and supersaturation, causes crystallization.…”

Section: Sonocrystallizationmentioning

confidence: 99%

“…The partners are dissolved in a common evaporating solvent and sprayed to a hot stream of air for evaporation of the solvent to yield good co-crystals. 22,54 Once after the preparation of the co-crystals, a rigorous scrutiny has been carried out for the confirmation and purity of the prepared cocrystals. The following section covers some of the characterization techniques that can be adopted for the assessment of co-crystals.…”

Section: Spray Dryingmentioning

confidence: 99%

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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“…In pharmaceutical field more than 60 % are synthesized drug. Overall synthesized drug upto 40 % have bioavailability problem due to its poor solubility [4]. Pharmaceutical cocrystal is a building tool to improve the solubility, dissolution of the drug, and physicochemical properties of the drug.…”

Section: Introductionmentioning

confidence: 99%

Design, Formulation, and Characterization of Apremilast-Saccharin Cocrystals Loaded With Topical Gel

Mane¹,

Mohite²

2020

Asian J Pharm Clin Res

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Objective: Most of the drugs are relevant to BSC class II and class IV having solubility problems. Cocrystallization of drug with conformer is an immense approach used to explore the physicochemical properties of drug. The objective of the present work was to design formulate and evaluate the drug cocrystals of poorly soluble drug apremilast (APR) with saccharin. Methods: Cocrystals of APR were prepared using the solvent evaporation technique. The saturated solubility study and in vitro dissolution study of cocrystals were carried out. The prepared cocrystals were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy. The topical gel of APR cocrystals was formulated optimized and evaluated using three-level factorial design. Results: The cocrystals of APR were prepared in 1:1 molar ratio with saccharin. APR cocrystals showed the improvement in solubility and dissolution as compared to pure APR. The formation of cocrystals was confirmed from change in endothermic peak of DSC and from shifting of FTIR spectra of cocrystals. Crystallinity of cocrystal was confirmed from XRD pattern and noteworthy change in 2θ values of the intense peak. The topical gel of APR cocrystals was formulated and optimized using three-level factorial design using Carbapol-940 and hydroxypropyl methylcellulose (HPMC) as a gelling agent. Conclusion: The cocrystals with altered physicochemical properties of APR were prepared with saccharin and formulated as a topical gel to overcome the problems related to oral administration.

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Co-Crystals: A Review

Cited by 32 publications

References 28 publications

Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review

Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review

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

Design, Formulation, and Characterization of Apremilast-Saccharin Cocrystals Loaded With Topical Gel

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