Hygroscopicity of Celiprolol Hydrochloride Polymorphs

Narurkar, Arvind; Purkaystha, Auditi; Sheen, Pai‐Chang; Augustine, Matthew A.

doi:10.3109/03639048809151877

Cited by 7 publications

(4 citation statements)

References 1 publication

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“…More than three decades ago, in 1988, Narurkar et al [146] investigated the hydration stability of a polymorphic drug celiprolol hydrochloride (Scheme 11) using thermal measurements. Celiprolol is a beta-blocker used for the treatment of high blood pressure.…”

Section: Polymorphism In Pharmaceutical Materialsmentioning

confidence: 99%

Polymorphs with Remarkably Distinct Physical and/or Chemical Properties

Saha

Nath

Thakuria

2022

The Chemical Record

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Polymorphism in crystals is known since 1822 and the credit goes to Mitscherlich who realized the existence of different crystal structures of the same compound while working with some arsenate and phosphate salts. Later on, this phenomenon was observed also in organic crystals. With the advent of different technologies, especially the easy availability of single crystal XRD instruments, polymorphism in crystals has become a common phenomenon. Almost 37 % of compounds (single component) are polymorphic to date. As the energies of the different polymorphic forms are very close to each other, small changes in crystallization conditions might lead to different polymorphic structures. As a result, sometimes it is difficult to control polymorphism. For this reason, it is considered to be a nuisance to crystal engineering. It has been realized that the property of a material depends not only on the molecular structure but also on its crystal structure. Therefore, it is not only of interest to academia but also has widespread applications in the materials science as well as pharmaceutical industries. In this review, we have discussed polymorphism which causes significant changes in materials properties in different fields of solid-state science, such as electrical, magnetic, SHG, thermal expansion, mechanical, luminescence, color, and pharmaceutical. Therefore, this review will interest researchers from supramolecular chemistry, materials science as well as medicinal chemistry.

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Section: Polymorphism In Pharmaceutical Materialsmentioning

confidence: 99%

Polymorphs with Remarkably Distinct Physical and/or Chemical Properties

Saha

Nath

Thakuria

2022

The Chemical Record

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“…Finding as many solid forms as possible is an essential step in the active pharmaceutical ingredient (API) development, as different polymorphs, hydrates, and solvates show different properties, such as densities, hygroscopicity, stability, mechanical properties, solubility, and bioavailability. − In addition, solvates may inevitably be formed during the solution crystallization process, causing considerable interest to study. Although many solvates cannot be used directly due to the toxicity, it is still an important part to develop the polymorph landscape of API, and some are the precursors to form specific polymorphs .…”

Section: Introductionmentioning

confidence: 99%

Structural Insights into the Highly Solvating System of Axitinib via Binary and Ternary Solvates

Zhang

et al. 2022

Crystal Growth & Design

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Axitinib is a well-known model in crystal engineering, exhibiting a high tendency to form various solvates, and more than 70 kinds of solvates have been reported. Therefore, it is a challenge to elucidate the effect of solvents on the crystallization of Axitinib and develop the polymorph or solvate landscape of Axitinib. Here, we illustrate an uncommon and complicated solvation behavior of Axitinib from the structural analysis and theoretical characterization. The structures of two new ternary solvates and five binary solvates are reported for the first time. Experimental and theoretical calculation and studies on phase transition are performed to rationalize and understand the formation of solvates and the transformation of polymorphisms. Crystal structure analysis and molecular properties reveal that shape, size, the hydrogen bond donor of the solvents, and the chance to lower crystal free energy are the main factors to drive solvates. Three sets of isostructural binary solvate are distinguished and calculated quantitatively to prove that the intermolecular interactions, strong hydrogen bond donor, CH−π, and orientation force control the classification results of binary solvates. Stability of solvates is found to be associated with the intermolecular interaction energies of solvent molecules with surrounding molecules. The polymorphic behavior of the desolventized product is attributed to the two-dimensional isostructurality between form IV and solvate.

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“…Phase transitions including polymorph interconversion, hydrate formation, and solvate desolvation − may happen under different processes, such as crystallization, granulation, compaction, drying, storage, and transport. It will further affect the performance (stability, − particle size and shape, − flowability, hygroscopicity, − and solubility − ) of the active pharmaceutical ingredients . Consequently, a thorough characterization of all possible pharmaceutical polymorphs and investigation of the phase transformation process are crucial for selecting the optimal solid form for development. − Furthermore, mapping the solid form landscapes will increase the understanding of the physicochemical properties and crystallization behavior of crystal forms, which can contribute to product design and process development.…”

Section: Introductionmentioning

confidence: 99%

Exploring Solid Form Landscape of Anticancer Drug Dimethylaminomicheliolide Fumarate: Crystal Structures Analysis, Phase Transformation Behavior, and Physicochemical Properties Characterization

Wang

et al. 2021

Crystal Growth & Design

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Brain tumors are still the deadliest among all types of cancer even after decades of extensive research. Glioblastoma is the most common and aggressive form of primary malignant brain tumors. As an efficient NF-κB inhibitor, dimethylaminomicheliolide fumarate has shown excellent therapeutic effect for glioblastoma in clinical trials. To date, no reports about the solid forms of dimethylaminomicheliolide fumarate have been disclosed. Dimethylaminomicheliolide fumarate was thus an interesting subject for polymorphism exploration. In this work, four solid forms (Forms B, C, D, and E) were successfully obtained. The crystal structures exhibit similarity in molecular conformation and packing arrangements between Form C and Form E. The PXRD patterns and phase transition behavior suggest that Form B and Form D are likely to have similarities. Hirshfeld surfaces were generated for a better understanding of the relationships of different crystal forms. They were also characterized and evaluated by thermal analysis, polarizing microscope, and dynamic vapor sorption as well as powder properties tests. The comprehensive exploration of the solid form landscape provided essential knowledge for product development and quality control of this potential drug.

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Hygroscopicity of Celiprolol Hydrochloride Polymorphs

Cited by 7 publications

References 1 publication

Polymorphs with Remarkably Distinct Physical and/or Chemical Properties

Polymorphs with Remarkably Distinct Physical and/or Chemical Properties

Structural Insights into the Highly Solvating System of Axitinib via Binary and Ternary Solvates

Exploring Solid Form Landscape of Anticancer Drug Dimethylaminomicheliolide Fumarate: Crystal Structures Analysis, Phase Transformation Behavior, and Physicochemical Properties Characterization

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