Crystalline Polymorphism of Organic Compounds

Caira, Mino R.

doi:10.1007/3-540-69178-2_5

Cited by 113 publications

(71 citation statements)

References 114 publications

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“…Among traditional methods to generate polymorphs (as well as hydrates and solvates), manual techniques [58] are time and material consuming, and sometimes fail to identify all possible polymorphs for a compound.…”

Section: Polymorph Screeningmentioning

confidence: 99%

Polymorph Impact on the Bioavailability and Stability of Poorly Soluble Drugs

2015

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Drugs with low water solubility are predisposed to poor and variable oral bioavailability and, therefore, to variability in clinical response, that might be overcome through an appropriate formulation of the drug. Polymorphs (anhydrous and solvate/hydrate forms) may resolve these bioavailability problems, but they can be a challenge to ensure physicochemical stability for the entire shelf life of the drug product. Since clinical failures of polymorph drugs have not been uncommon, and some of them have been entirely unexpected, the Food and Drug Administration (FDA) and the International Conference on Harmonization (ICH) has required preliminary and exhaustive screening studies to identify and characterize all the polymorph crystal forms for each drug. In the past, the polymorphism of many drugs was detected fortuitously or through manual time consuming methods; today, drug crystal engineering, in particular, combinatorial chemistry and high-throughput screening, makes it possible to easily and exhaustively identify stable polymorphic and/or hydrate/dehydrate forms of poorly soluble drugs, in order to overcome bioavailability related problems or clinical failures. This review describes the concepts involved, provides examples of drugs characterized by poor solubility for which polymorphism has proven important, outlines the state-of-the-art technologies and discusses the pertinent regulations.

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Section: Polymorph Screeningmentioning

confidence: 99%

Polymorph Impact on the Bioavailability and Stability of Poorly Soluble Drugs

2015

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“…3 The importance of polymorphism knowledge for pharmaceutical industry lies on having reliable and robust processes. 4,5 Among different processes to suffer by drug substances, they can be subjected to particle size reduction, grinding, and compression before they are finally blended with excipients to produce the final formulation. The milling process results in a reduction in the particle size of a given material.…”

Section: Introductionmentioning

confidence: 99%

Conformational Polymorphism on Imatinib Mesylate: Grinding Effects

Grillo

Polla

Vega

2012

Journal of Pharmaceutical Sciences

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“…[3][4][5] The middle of the last century witnessed a waning in passion in polymorphism. Thanks to McCrone's unyielding compassion in this phenomenon, 1,6,7 and also the importance of polymorphism in the field of pharmaceuticals (individual cases of polymorphism of pharmaceuticals are numerous [8][9][10][11][12][13][14][15][16] ), the study of polymorphism is now enjoying a renaissance.…”

Section: Introductionmentioning

confidence: 99%

Polymorphism and Phase Behaviors of 2-(Phenylamino)nicotinic Acid

Long

Parkin

Siegler

et al. 2008

Crystal Growth & Design

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ABSTRACT:The discovery and phase transition studies of four polymorphs of 2-(phenylamino)nicotinic acid are described in this report. The four polymorphs were crystallized from solution under different conditions. All polymorphs differ in the degree of conjugation of the two aromatic rings and thus are of conformational polymorphism. Three of the four modifications have more than one conformer in the asymmetric unit. Due to the difference in conformation, all polymorphs display distinctive colors as well as different hydrogen-bonding arrangements. Phase behaviors of the four forms were studied by differential scanning calorimetry and hot-stage microscopy, indicating that metastable forms underwent phase transition to the stable one initiated by mechanical perturbation in solution or assisted by heating in the solid state. As such, this polymorphic system exhibits polychromism, conformational isomorphism, thermochromism, and mechanochromism. It may be valuable for further solid-state structure-property relationship studies.

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Crystalline Polymorphism of Organic Compounds

Cited by 113 publications

References 114 publications

Polymorph Impact on the Bioavailability and Stability of Poorly Soluble Drugs

Polymorph Impact on the Bioavailability and Stability of Poorly Soluble Drugs

Conformational Polymorphism on Imatinib Mesylate: Grinding Effects

Polymorphism and Phase Behaviors of 2-(Phenylamino)nicotinic Acid

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