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Related Concept Videos

Antiviral Nucleoside Inhibitors01:22

Antiviral Nucleoside Inhibitors

Antiviral Nucleoside InhibitorsAntiviral nucleoside inhibitors are structural analogs of natural nucleosides that interfere with viral DNA or RNA synthesis. These compounds selectively target viral polymerases due to their resemblance to host nucleosides, thereby disrupting viral genome replication.Mechanism of Acyclovir ActionAcyclovir is a guanosine analog with a three-carbon acyclic side chain. It selectively targets herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2),...
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 Nonequivalence01:27

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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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Characteristics and Nomenclature of Copolymers

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Engineering Antiviral Agents via Surface Plasmon Resonance
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Polymorphs and hydrates of acyclovir.

Katie M Lutker1, Rosalynn Quiñones, Jiadi Xu

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

Journal of Pharmaceutical Sciences
|February 1, 2011
PubMed
Summary
This summary is machine-generated.

Researchers characterized four anhydrous forms and a new hydrate of acyclovir (ACV), an antiviral drug. This study provides new structural insights into anhydrous ACV beyond its known solvate form.

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Area of Science:

  • Crystallography
  • Solid-state chemistry
  • Pharmaceutical science

Background:

  • Acyclovir (ACV) is a widely used antiviral medication.
  • The crystal structure of the commercial ACV/water solvate is known, but anhydrous forms are less understood.

Purpose of the Study:

  • To characterize novel anhydrous forms and a new hydrate of acyclovir.
  • To investigate the structural properties and stability of different acyclovir solid forms.

Main Methods:

  • Crystallization techniques
  • Solid-state characterization (e.g., X-ray diffraction, thermal analysis)
  • Structural analysis

Main Results:

  • Four new anhydrous forms of ACV were identified and characterized.
  • A novel hydrate of ACV was discovered.
  • Two anhydrous forms are air-stable needles; a third converts to the commercial form upon hydration.
  • A high-temperature modification (anhydrous form I) was obtained by heating above 180 °C.
  • Crystal structures of anhydrous form I and the novel hydrate were determined.

Conclusions:

  • This research expands the known solid forms of acyclovir.
  • Understanding these new anhydrous and hydrate forms is crucial for ACV formulation and stability.
  • The structural data provides a foundation for future pharmaceutical development of acyclovir.