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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...
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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,...
Polymer Classification: Crystallinity01:21

Polymer Classification: Crystallinity

Unlike ionic or small covalent molecules, polymers do not form crystalline solids due to the diffusion limitations of their long-chain structures. However, polymers contain microscopic crystalline domains separated by amorphous domains.
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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...
Crystal Growth: Principles of Crystallization01:25

Crystal Growth: Principles of Crystallization

Crystallization is a phase transformation process in which crystals are precipitated from a supersaturated solution or formed from other sources. During crystallization, atoms or molecules arrange themselves into a well-defined, rigid crystal lattice to minimize energy.
Initiating crystallization involves manipulating the concentration of the solute and the temperature of the solution. Since crystal growth occurs when the ratio of concentration and solubility of the solute in the solvent – the...
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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...

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Synthesis and Characterization of Functionalized Metal-organic Frameworks
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Characterization and selective crystallization of famotidine polymorphs.

Jie Lu1, Xiu-Juan Wang, Xia Yang

  • 1School of Chemical and Biomedical Engineering, Nanyang Technological University, Singapore 637722. lujie@ntu.edu.sg

Journal of Pharmaceutical Sciences
|May 24, 2007
PubMed
Summary

Famotidine crystallization yields two forms, A and B. Controlling factors like concentration, solvent, and nucleation temperature are key to obtaining the desired famotidine polymorph.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Chemical Engineering

Background:

  • Famotidine exists in two polymorphic forms: stable A and metastable B.
  • Understanding famotidine polymorphism is crucial for drug formulation and efficacy.

Purpose of the Study:

  • To comprehensively characterize famotidine polymorphs A and B.
  • To investigate the influence of crystallization parameters on famotidine polymorphism.
  • To determine the conditions favoring the crystallization of specific famotidine polymorphs.

Main Methods:

  • Solid characterization of famotidine polymorphs.
  • Measurement of solubility, metastable zone width, and interfacial energy.
  • Systematic investigation of solvent, cooling rate, concentration, and nucleation temperature effects.

Main Results:

  • Polymorph crystallization is dependent on concentration, solvent, cooling rate, and nucleation temperature.
  • Polymorph B formation is favored at high concentrations.
  • In aqueous solutions, nucleation temperature is the primary determinant of polymorph formation.

Conclusions:

  • Crystallization conditions significantly impact famotidine polymorph outcome, primarily due to conformational polymorphism.
  • A "polymorphic window" for famotidine crystallization from aqueous solution was established.
  • Precise control over crystallization parameters is essential for reproducible famotidine polymorph production.