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Solids in which the atoms, ions, or molecules are arranged in a definite repeating pattern are known as crystalline solids. Metals and ionic compounds typically form ordered, crystalline solids. A crystalline solid has a precise melting temperature because each atom or molecule of the same type is held in place with the same forces or energy. Amorphous solids or non-crystalline solids (or, sometimes, glasses) which lack an ordered internal structure and are randomly arranged. Substances that...
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Network covalent solids contain a three-dimensional network of covalently bonded atoms as found in the crystal structures of nonmetals like diamond, graphite, silicon, and some covalent compounds, such as silicon dioxide (sand) and silicon carbide (carborundum, the abrasive on sandpaper). Many minerals have networks of covalent bonds.
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To understand intra-specific interactions in populations, scientists measure the spatial arrangement of species individuals. This geographic arrangement is known as the species distribution or dispersion. Highly territorial species exhibit a uniform distribution pattern, in which individuals are spaced at relatively equal distances from one another. Species that are highly tied to particular resources, such as food or shelter, tend to concentrate around those resources, and thus exhibit a...
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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).
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Tailoring supersaturation from amorphous solid dispersions.

Na Li1, Lynne S Taylor1

  • 1Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, United States.

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|April 15, 2018
PubMed
Summary
This summary is machine-generated.

Poorly soluble polymers significantly impact amorphous solid dispersion (ASD) drug solubility. Drug-polymer interactions and drug loading in ASDs alter maximum achievable concentrations, crucial for formulation design.

Keywords:
Drug releaseMiscibilityPolymerSolubilityThermodynamics

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Physical Chemistry

Background:

  • The maximum drug concentration in solution is governed by the solid form's chemical potential.
  • Amorphous solids exhibit higher chemical potential than crystalline forms, potentially leading to higher transient solubility.
  • Mixing amorphous drugs with components, especially poorly soluble polymers in amorphous solid dispersions (ASDs), can alter their chemical potential and thus solubility.

Purpose of the Study:

  • To investigate the effect of poorly soluble polymers on the amorphous solubility of drugs in ASDs.
  • To understand how drug-polymer interactions and composition influence the maximum achievable drug concentration.
  • To provide insights into drug phase behavior within ASDs.

Main Methods:

  • Formulation of lopinavir-based amorphous solid dispersions (ASDs) with various model polymers.
  • Determination of lopinavir's amorphous solubility as a function of ASD composition and drug loading.
  • Characterization of drug-polymer interactions using infrared spectroscopy (IR), differential scanning calorimetry (DSC), and moisture sorption analysis.

Main Results:

  • The maximum achievable concentration (amorphous solubility) of lopinavir varied significantly with different polymers and drug loadings.
  • Stronger drug-polymer interactions correlated with altered amorphous solubility.
  • The drug weight fraction within the ASD was a critical factor influencing the maximum concentration.

Conclusions:

  • Poorly soluble polymers can modulate the amorphous solubility of drugs in ASDs.
  • Drug-polymer interactions and composition are key determinants of maximum achievable concentrations in ASDs.
  • This study enhances understanding of drug phase behavior in ASDs, particularly with pH-responsive polymers.