Polymorphs, Solvates and Hydrates

Threlfall, Terry L.

doi:10.1002/0470027320.s8301

Cited by 4 publications

(3 citation statements)

References 114 publications

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“…Polymorphism is the ability of a molecule to arrange itself in a different spatial arrangement which results in differential physicochemical, stability and biopharmaceutical properties. More than 50% of known pharmaceutical small molecules exist as polymorph, still, this covers only 0.0001% of reported polymorphism in the scientific literature (Threlfall, ). Despite this, polymorphism can have a profound influence on pharmaceutical formulation development, storage stability, and biopharmaceutical performance of the API (Bauer, ).…”

Section: Pharmaceutical Applicationsmentioning

confidence: 99%

“…The stable polymorphs are preferred, but they may have limitations vis‐a‐vis biopharmaceutical performance for poorly water‐soluble compounds. The metastable polymorph provides solubility and dissolution advantage which could translate into improved in vivo performance (Threlfall, ). Apart from that some metastable forms may possess better processability as compared to their stable counterpart and hence are desirable for pharmaceutical formulation development.…”

Section: Pharmaceutical Applicationsmentioning

confidence: 99%

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Emerging role of primary heterogeneous nucleation in pharmaceutical crystallization

Thakore

Sood

Bansal

2019

Drug Development Research

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Crystallization is an important and difficult to control unit operation in the pharmaceutical industry. Crystallization can control molecular (i.e., polymorphism) and particulate (i.e., particle size and crystal habit) properties of active pharmaceutical ingredient (API). Moreover, these molecular and particulate properties govern the manufacturability, stability, and biopharmaceutical performance of the API and drug product. Nucleation is a key step and primary heterogeneous nucleation is a common mode of nucleation during crystallization. Hence, it is important to understand the parameters affecting primary heterogeneous nucleation, to achieve desirable properties in crystalline APIs. Primary heterogeneous crystallization has usually been linked to the surface characteristics like topography and functionality of the heteronucleant. The review outlines recent findings in the primary heterogeneous crystallization with specific emphasis on its pharmaceutical applications including regulatory considerations. Molecular‐level mechanisms governing heteronucleation and subsequent outcome in terms of molecular as well as particulate‐level properties of API have also been discussed. Moreover, general guidance for the selection of heteronucleant has also been included. Heterogeneous crystallization is a promising tool for efficient crystallization of API having properties for optimal pharmaceutical performance.

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Section: Pharmaceutical Applicationsmentioning

confidence: 99%

Section: Pharmaceutical Applicationsmentioning

confidence: 99%

Emerging role of primary heterogeneous nucleation in pharmaceutical crystallization

Thakore

Sood

Bansal

2019

Drug Development Research

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“…API solvates are generally prepared by recrystallization, but hydrates may also appear during formulation of a drug while being exposed to air. But while pharmaceutical hydrates are viable forms for drug products because there is no safety concern about water as a crystal adduct, solvates are rarely formulated because of safety concerns due to solvent toxicity. , However, the phenomenon of pseudopolymorphism can have a significant impact in the development of a pharmaceutical drug since the pharmaceutical drugs are usually in contact with organic solvent during the purification and processing stages . Particularly relevant is the case of sulfathiazole, which forms over 100 solvates.…”

Section: Introductionmentioning

confidence: 99%

Polymorphism of Sildenafil: A New Metastable Desolvate

Barbas

Font-Bardı́a

Prohens

2018

Crystal Growth & Design

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A new anhydrous polymorph of the free base of sildenafil and two solvates (acetonitrile and propanenitrile) have been discovered and fully characterized. The new polymorph can be considered a desolvate of the acetonitrile solvate and is related to the most stable form I by morphotropism. The new polymorph can only be obtained by desolvation of the acetonitrile solvate. Thus, this study is a new example of the importance of this multicomponent family of solid forms in the discovery of new polymorphs of active pharmaceutical ingredients.

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Two-component self-assembly with solvent leading to “wet” and microcrystalline organogel fibers

Löfman

Lahtinen

Sievänen

2015

Journal of Colloid and Interface Science

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Polymorphs, Solvates and Hydrates

Abstract: The sections in this article are Introduction – The Nature of Polymorphism and Solvation Mid‐Infrared Spectroscopy Quantitative Mid‐Infrared Measurements Burger's Infrared Rule Stability Near‐Infrared Spectroscopy R aman Spectroscopy … Show more

Cited by 4 publications

References 114 publications

Emerging role of primary heterogeneous nucleation in pharmaceutical crystallization

Emerging role of primary heterogeneous nucleation in pharmaceutical crystallization

Polymorphism of Sildenafil: A New Metastable Desolvate

Two-component self-assembly with solvent leading to “wet” and microcrystalline organogel fibers

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