Pharmaceutical Co-crystals: A Systematic Review

Jayram, Puneeth; Sudheer, Preethi

doi:10.5530/ijpi.2020.3.45

Cited by 7 publications

(6 citation statements)

References 27 publications

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“…In solution, it has led to the development of molecular receptors [2,3]; meanwhile, in solid state, it has been applied in the design and synthesis of pharmaceutical cocrystals. Pharmaceutical cocrystals are multi-component crystalline solids formed by a pharmaceutical active ingredient (API) and a cocrystal former, stabilized by noncovalent interactions, principally hydrogen bonds [4].…”

Section: Introductionmentioning

confidence: 99%

Mechanochemical Synthesis of the Catechol-Theophylline Cocrystal: Spectroscopic Characterization and Molecular Structure

González-González¹,

Jiménez-López²,

Ortegón-Reyna³

et al. 2021

Applied Sciences

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Pharmaceutical cocrystallization offers the possibility to modify the physicochemical and biopharmaceutical properties of active pharmaceutical ingredients. The mechanochemical synthesis and spectroscopic characterization of the catechol-theophylline (CAT-TEO) cocrystal is reported. The cocrystal was prepared by the solvent-assisted grinding method. The ATR-IR spectroscopy study allowed to determine the formation of the cocrystal because the O-H and C=O stretching bands in the CAT-TEO cocrystal were shifted with respect to the starting materials, suggesting the formation of the C=O···H-O hydrogen bond interaction. Infrared spectroscopy also allowed to discard hydration of the cocrystal, and polymorphic transitions of the starting products as a consequence of the mechanochemical grinding. The X-ray powder diffraction and thermal studies confirmed the formation of a new solid phase. In the solid state 13C NMR spectra of the cocrystal, the signals were shifted with respect to the starting products. The 13C NMR chemical shifts of the CAT-TEO cocrystal were simulated by using the gauge including the atomic orbital (GIAO) method. These results showed a good correlation between the experimental and calculated 13C NMR results. Theoretical calculations and natural bonding orbital analysis (NBO) at a B3LYP/6-31G(d,p) level of theory were performed to obtain structural information of the cocrystal.

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Section: Introductionmentioning

confidence: 99%

Mechanochemical Synthesis of the Catechol-Theophylline Cocrystal: Spectroscopic Characterization and Molecular Structure

González-González¹,

Jiménez-López²,

Ortegón-Reyna³

et al. 2021

Applied Sciences

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“…34 The increased solubility of cocrystals enhances the rate of dissolution, which is the rate limiting step in the absorption of drug in the gastrointestinal tract. 35 Sugandha et al synthesized ezetimibe cocrystals using three different techniques: solution crystallization, liquid aided grinding, and reaction crystallization, with methyl paraben serving as the coformer. In the case of a cocrystal created through solution crystallization, equilibrium water solubility of ezetimibe was increased by 2-fold The solubility of cocrystals generated during reaction crystallization was strikingly similar to that of pure ezetimibe.…”

Section: Melting Point (Mp)mentioning

confidence: 99%

Pharmaceutical Cocrystals: An Emerging Approach to Modulate Physicochemical Properties of Active Pharmaceutical Ingredients

Tupe

Khandagale

Jadhav

2023

J. Drug Delivery Ther.

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Most of the Active Pharmaceutical Ingredients (APIs) are typically formulated and administered to patients in oral solid dosage forms due to ease of administration, patient compliance and cost effectiveness. Poor water solubility, low permeability and low bioavailability of APIs are major hurdles in development of oral solid dosage forms. In recent years, cocrystal development has evolved as a feasible approach for enhancing the solubility and bioavailability of poorly soluble drugs. Crystal engineering strategies have been asserted to enhance the likelihood of discovering new solid forms of an API. A pharmaceutical cocrystal is made up of two basic components, an API and a harmless material known as a coformer in stoichiometric ratio. Cocrystallization of an API with a pharmaceutically acceptable coformer can improve the physical characteristics of the API, such as solubility, hygroscopicity, and compaction behavior, without affecting the API's pharmacological efficacy. This review article offers a comprehensive overview of pharmaceutical cocrystals, their physiochemical characteristics, and methods of preparation, with an emphasis on cocrystal screening and cocrystal characterization. The review also included recent FDA and EMA guidance on pharmaceutical cocrystals as well as an outline of multidrug cocrystals. Keywords: Pharmaceutical co-crystals, crystal engineering, coformers, supramolecular synthons, Solubility

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“…The surface morphology and properties of the cocrystals can be studied using a scanning electron microscope (SEM) 37 . The samples are sputtered with gold at ambient temperature in an argon environment.…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Pharmaceutical cocrystal-a deft technique for solubility enhancement

Bhattacharyya,

Manjunath

2023

Pharm Sci Asia

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Solubility enhancement of active pharmaceutical ingredients is a challenging field in the pharmaceutical industry. Several methods and excipients are employed in the solubility improvement process of poorly soluble drugs. Crystal engineering is one of the novel strategies to alter the physicochemical properties of the molecule without causing significant changes in its structural integrity. Cocrystals are single-phase or homogeneous crystalline structures composed of two or more compounds bound noncovalently with the active pharmaceutical ingredient in a definite stoichiometric ratio. The cocrystallization technique is effective not only in improving the problems associated with solubility, and bioavailability, in addition, it enhances permeability, stability, hygroscopicity, flowability, and processability of the materials. This review represents the concept, characterization, and application of cocrystals in a systematic way. The review focuses on the requisite and mechanism of cocrystal formation, different preparation methods of cocrystals, and stages of screening. The growing interest in this technique has led the regulatory bodies to implement the guidelines, hence, a brief on regulatory perspectives is discussed here. The cocrystallization method establishes its potential in the pharmaceutical field through an increasing number of patents and market approvals.

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Pharmaceutical Co-crystals: A Systematic Review

Cited by 7 publications

References 27 publications

Mechanochemical Synthesis of the Catechol-Theophylline Cocrystal: Spectroscopic Characterization and Molecular Structure

Mechanochemical Synthesis of the Catechol-Theophylline Cocrystal: Spectroscopic Characterization and Molecular Structure

Pharmaceutical Cocrystals: An Emerging Approach to Modulate Physicochemical Properties of Active Pharmaceutical Ingredients

Pharmaceutical cocrystal-a deft technique for solubility enhancement

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