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Related Concept Videos

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).
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The pV diagram, which is a graph of pressure versus volume of the gas under study, is helpful in describing certain aspects of the substance. When the substance behaves like an ideal gas, the ideal gas equation describes the relationship between its pressure and volume. On a pV diagram, it is common to plot an isotherm, which is a curve showing p as a function of V with the number of molecules and the temperature fixed. Then, for an ideal gas, the product of the pressure of the gas and its...
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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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Synthesizing a Gel Polymer Electrolyte for Supercapacitors, Assembling a Supercapacitor Using a Coin Cell, and Measuring Gel Electrolyte Performance
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Polymorphs of DP-VPA Solid Solutions and Their Physicochemical Properties.

Chao Hao1, Jian Jin2, Jiaying Xiong1

  • 1Department of Biomedical Engineering, Systems Biology Theme, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China.

Journal of Pharmaceutical Sciences
|April 3, 2020
PubMed
Summary

This study characterized solid forms of DP-VPA, an antiepileptic drug candidate. Form B exhibited optimal physicochemical properties, suggesting it as the preferred form for drug development.

Keywords:
DP-VPAPhysicochemical propertiesPolymorphsSolid solutions

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Area of Science:

  • Pharmaceutical Sciences
  • Solid-State Chemistry
  • Drug Development

Background:

  • Physicochemical properties of drug solid forms critically impact stability, bioavailability, and manufacturability.
  • DP-VPA, a phosphatidylcholine complex, is an antiepileptic drug candidate developed as a solid solution of DP-VPA-C16 and DP-VPA-C18.

Purpose of the Study:

  • To characterize the various solid forms (polymorphs) of DP-VPA solid solution.
  • To investigate the physicochemical properties, including hygroscopicity, thermodynamic behavior, and stability, of each polymorph.

Main Methods:

  • Characterization techniques included Powder X-ray Diffraction (PXRD), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), Attenuated Total Reflection Fourier Transform Infrared Spectroscopy (ATR-FTIR), Scanning Electron Microscopy (SEM), Dynamic Vapor Sorption (DVS), and Optical Microscopy.
  • Hygroscopicity was assessed using DVS, and stability was evaluated under varying relative humidity conditions.

Main Results:

  • DP-VPA solid solution demonstrated reduced hygroscopicity compared to DP-VPA-C16.
  • Forms A and B were relatively stable, whereas Forms A-1, B-1, C, and D were unstable under ambient humidity.
  • Milling induced a transformation of Form A into Form B.

Conclusions:

  • Form B possesses favorable physicochemical properties, including reduced hygroscopicity and relative stability.
  • Form B is identified as the potentially optimal solid form for the formulation and development of DP-VPA as an antiepileptic medication.