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Related Concept Videos

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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...
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

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,...
Factors Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
Pharmaceutical Equivalents01:26

Pharmaceutical Equivalents

As defined by regulatory standards, pharmaceutical equivalents require generic drug products to have identical dosage forms and chemically identical active pharmaceutical ingredients (APIs). They must adhere to compendial or applicable standards for potency, content uniformity, disintegration times, and dissolution rates. In the case of modified-release dosage forms, variations in drug content are permissible as long as the delivered amount remains consistent with the innovator drug product.

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Structural characterization and comparative analysis of polymorphic forms of psilocin (4-hy-droxy-<i>N</i>,<i>N</i>-di-methyl-tryptamine).

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Pharmaceutical Cocrystals and Their Physicochemical Properties.

Nate Schultheiss1, Ann Newman

  • 1SSCI, Inc., A Division of Aptuit, West Lafayette, Indiana, and Seventh Street Development Group, Lafayette, Indiana.

Crystal Growth & Design
|June 9, 2009
PubMed
Summary

This review covers advances in pharmaceutical cocrystals over the past decade. These cocrystals improve drug properties, bridging crystal engineering and pharmaceutical sciences.

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Published on: July 4, 2016

Area of Science:

  • Pharmaceutical sciences
  • Crystal engineering
  • Materials science

Background:

  • Pharmaceutical cocrystals are solid forms of a drug with a second molecule.
  • Cocrystal formation can significantly alter physicochemical properties of active pharmaceutical ingredients.
  • Advances in understanding intermolecular interactions have driven cocrystal development.

Purpose of the Study:

  • To review the progress in pharmaceutical cocrystal technology over the last 10 years.
  • To highlight improvements in physical and chemical properties achieved through cocrystal formation.
  • To foster integration between crystal engineering and pharmaceutical sciences.

Main Methods:

  • Literature review of research published in the last decade.
  • Analysis of studies focusing on cocrystal design and characterization.
  • Discussion of property enhancements reported in various cocrystal systems.

Main Results:

  • Significant improvements in solubility, dissolution rate, and bioavailability have been demonstrated.
  • Enhanced chemical stability and mechanical properties are frequently observed.
  • Successful examples span diverse therapeutic areas, showcasing broad applicability.

Conclusions:

  • Pharmaceutical cocrystals represent a powerful strategy for drug property enhancement.
  • Continued interdisciplinary collaboration is crucial for advancing the field.
  • Cocrystal technology holds substantial promise for future drug development.