Pharmaceutical cocrystal: a game changing approach for the administration of old drugs in new crystalline form

Panzade, Prabhakar; Shendarkar, Giridhar R

doi:10.1080/03639045.2020.1810270

Cited by 30 publications

(19 citation statements)

References 105 publications

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“…Pharmaceutical cocrystals are composed of an API and one or more pharmaceutically acceptable cocrystal formers (CCFs) with a well-defined stoichiometry, interacting through hydrogen bond, π–π conjugation, and other noncovalent bonds . Pharmaceutical applications of cocrystals lie in their ability to modify physicochemical properties, such as solubility, dissolution rate, physical stability, tabletability, , and bioavailability, , without altering the pharmacological activity of the API. − Cocrystals formed between APIs, i.e. , drug–drug cocrystals, can overcome problems in physicochemical properties of individual APIs and, sometimes, even exhibit synergistic pharmacological effects .…”

Section: Introductionmentioning

confidence: 99%

Drug–Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

Liu

Song

et al. 2021

Crystal Growth & Design

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The oral delivery of genistein (GEN) is hindered by its low bioavailability. The delivery of tetramethylpyrazine (TMP or ligustrazine) is faced with physical instability challenges due to its high sublimation tendency. We tackled respective challenges of the two drugs by forming a cocrystal. The GEN-TMP cocrystal exhibits a significantly reduced sublimation tendency than TMP and a significant enhancement in both the in vitro release rate and bioavailability in rats than GEN. Thus, cocrystallization simultaneously improves pharmaceutical properties of both parent drugs.

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Section: Introductionmentioning

confidence: 99%

Drug–Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

Liu

Song

et al. 2021

Crystal Growth & Design

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“…Formulations such as Suglat ® (Ipragliflozin L-Proline) (Astellas Pharma and Kotobuki Pharmaceutical, Japan), Entresto ® (sacubitril and valsartan) (Novartis, Switzerland), Steglatro ® (ertugliflozin) (Merck Sharp and Dohme B.V, Netherlands), and Steglujan ® (ertugliflozin and sitagliptin) (Pfizer, USA) were marketed between the years 2014 to 2017 [61,97]. Some products were identified as co-crystals at a later stage, while already being on the market, such as Lexapro ® (Escitalopram oxalate oxalic acid) (Lundbeck, Denmark) and Beta-chlor ® (Chloral hydrate and betaine) (Franklin Laboratories, India) [26,60,101]. TAK 020 co-crystal (a tyrosine kinase inhibitor), indicated for the potential treatment of rheumatoid arthritis, is still at its phase I clinical trials [98].…”

Section: Regulatory Limitations Of Crystalline Productsmentioning

confidence: 99%

“…Physicochemical and mechanical properties of a co-crystal formulation should be investigated prior to selecting a suitable co-crystal [100]. Melting point, hygroscopicity, solubility, hardness, plasticity, and elasticity are all examples of physical properties of solid-state materials [101]. Hygroscopicity of a drug impacts the physicochemical properties such as solubility, dissolution rate, stability, bioavailability, and mechanical properties [102].…”

Section: Regulatory Limitations Of Crystalline Productsmentioning

confidence: 99%

“…The co-crystal should overcome API chemical instability in the solid form. Elasticity, plasticity, viscoelasticity, and fragmentation mechanisms are among the mechanical deformation mechanisms for solid materials [101]. Many organic chemicals, on the other hand, have poor mechanical characteristics, making tablet formation difficult [102].…”

Section: Regulatory Limitations Of Crystalline Productsmentioning

confidence: 99%

“…The application will then be reviewed by the FDA to ensure that the safety and effectiveness of the drug comply with the method of manufacturing. Once evidence on dissociation of drug from co-crystal before reaching the targeted site of action has been provided, the USFDA will accept the new drug applications [101].…”

Section: Regulatory Limitations Of Crystalline Productsmentioning

confidence: 99%

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Nano- and Crystal Engineering Approaches in the Development of Therapeutic Agents for Neoplastic Diseases

et al. 2022

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Cancer is a leading cause of death worldwide. It is a global quandary that requires the administration of many different active pharmaceutical ingredients (APIs) with different characteristics. As is the case with many APIs, cancer treatments exhibit poor aqueous solubility which can lead to low drug absorption, increased doses, and subsequently poor bioavailability and the occurrence of more adverse events. Several strategies have been envisaged to overcome this drawback, specifically for the treatment of neoplastic diseases. These include crystal engineering, in which new crystal structures are formed to improve drug physicochemical properties, and/or nanoengineering in which the reduction in particle size of the pristine crystal results in much improved physicochemical properties. Co-crystals, which are supramolecular complexes that comprise of an API and a co-crystal former (CCF) held together by non-covalent interactions in crystal lattice, have been developed to improve the performance of some anti-cancer drugs. Similarly, nanosizing through the formation of nanocrystals and, in some cases, the use of both crystal and nanoengineering to obtain nano co-crystals (NCC) have been used to increase the solubility as well as overall performance of many anticancer drugs. The formulation process of both micron and sub-micron crystalline formulations for the treatment of cancers makes use of relatively simple techniques and minimal amounts of excipients aside from stabilizers and co-formers. The flexibility of these crystalline formulations with regards to routes of administration and ability to target neoplastic tissue makes them ideal strategies for effectiveness of cancer treatments. In this review, we describe the use of crystalline formulations for the treatment of various neoplastic diseases. In addition, this review attempts to highlight the gaps in the current translation of these potential treatments into authorized medicines for use in clinical practice.

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Technical and Formulation Aspects of Pharmaceutical Co‐Crystallization: A Systematic Review

et al. 2022

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Crystal engineering provides a unique approach to modulating the physicochemical properties of forming active drug molecules so nowadays pharmaceutical companies and researchers have shown interest in designing and building cocrystals. Creating new crystalline solid structures with altered physicochemical properties such as solubility, bioavailability, tabletability, melting point, stability, and so on. The intermolecular interactions of molecules in the crystal lattice are used to investigate these properties. Numbers of methods for crystallizing the drug are summarised and analyzed, pointing to the advantages and disadvantages that have been highlighted in the literature. This literature review discusses in detail the different types of cocrystals, their mechanisms, methods of cocrystals, applications of cocrystals, and their characterization. The main purpose of this article is to look at what has changed in this field in the last ten years and show what could be learned from better research on cocrystal formation and how it can be used.

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Pharmaceutical cocrystal: a game changing approach for the administration of old drugs in new crystalline form

Cited by 30 publications

References 105 publications

Drug–Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

Drug–Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

Nano- and Crystal Engineering Approaches in the Development of Therapeutic Agents for Neoplastic Diseases

Technical and Formulation Aspects of Pharmaceutical Co‐Crystallization: A Systematic Review

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