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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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Cytochrome P450 (CYP450) enzymes are a superfamily of heme-containing monooxygenases that play a pivotal role in Phase I drug metabolism by catalyzing oxidation and reduction reactions.These enzymes transform lipophilic xenobiotics into more hydrophilic metabolites, facilitating subsequent Phase II conjugation and eventual excretion. The CYP450 family is classified into families (e.g., CYP1–CYP3) and subfamilies (e.g., CYP2A, CYP2C), based on amino acid sequence homology.CYP450 isoenzymes,...
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Coherent anti-Stokes Raman Scattering (CARS) Microscopy Visualizes Pharmaceutical Tablets During Dissolution
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Published on: July 4, 2014

Polymorphism in Carbamazepine Cocrystals.

William W Porter1, Sophia C Elie, Adam J Matzger

  • 1Department of Chemistry and the Macromolecular Science and Engineering Program, University of Michigan, 930 North University Avenue, Ann Arbor, Michigan 48109-1055.

Crystal Growth & Design
|September 28, 2011
PubMed
Summary
This summary is machine-generated.

Polymorphism in carbamazepine cocrystals was investigated. New polymorphs of carbamazepine-nicotinamide (CBZ-NCT) and carbamazepine-saccharin (CBZ-SAC) cocrystals were identified, revealing unique structural features.

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Area of Science:

  • Crystallography
  • Materials Science
  • Pharmaceutical Science

Background:

  • Carbamazepine (CBZ) cocrystals are widely studied for drug formulation.
  • Polymorphism significantly impacts pharmaceutical properties.
  • Understanding cocrystal polymorphs is crucial for drug development.

Purpose of the Study:

  • To investigate the polymorphism of carbamazepine-nicotinamide (CBZ-NCT) and carbamazepine-saccharin (CBZ-SAC) cocrystals.
  • To characterize novel polymorphs using advanced analytical techniques.
  • To explore the role of polymer heteronuclei in cocrystal formation.

Main Methods:

  • Cocrystal synthesis via solution growth in the presence of polymer heteronuclei.
  • Characterization using Raman spectroscopy and powder X-ray diffraction (PXRD).
  • Single-crystal X-ray diffraction for structural determination of new polymorphs.

Main Results:

  • Two polymorphs of CBZ-NCT cocrystals were identified: CBZ-NCT I and a polymer-nucleated (PN) form.
  • A new polymorph of CBZ-SAC, designated CBZ-SAC II, was discovered.
  • CBZ-SAC II crystallizes in the monoclinic space group C2/c, exhibiting a distinct heterosynthon formation between carbamazepine and saccharin.

Conclusions:

  • Carbamazepine-nicotinamide and carbamazepine-saccharin cocrystals exhibit polymorphism.
  • Polymer heteronuclei can influence the formation of specific cocrystal polymorphs.
  • The discovery of new polymorphs, particularly CBZ-SAC II with its unique heterosynthon, expands the understanding of carbamazepine cocrystal behavior.