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Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
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Studies on Aspirin Crystals Generated by a Modified Vapor Diffusion Method.

Amit Mittal1, Deepak Malhotra1, Preeti Jain1

  • 1Lovely School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi, G.T. Road (NH-1), Phagwara, Jalandhar, Punjab, India, 144411.

AAPS Pharmscitech
|January 6, 2016
PubMed
Summary
This summary is machine-generated.

A modified vapor diffusion method rapidly forms aspirin crystals in 12 hours, significantly faster than traditional techniques. Characterization confirmed identical internal structures but altered crystal habits, suggesting potential for polymorph screening.

Keywords:
aspirincrystal habitcrystallizationscanning electron microscopyvapor diffusion

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Area of Science:

  • Crystallization Science
  • Pharmaceutical Technology
  • Solid-State Chemistry

Background:

  • Understanding drug crystal formation is crucial for pharmaceutical development.
  • Classical vapor diffusion methods for crystal generation are time-consuming.
  • Aspirin (ASP-I) serves as a model drug for investigating crystallization parameters.

Purpose of the Study:

  • To investigate the influence of non-solvents (diethylether, dichloromethane) on aspirin crystal formation using a modified vapor diffusion method.
  • To characterize and compare aspirin crystals (ASP-II, ASP-III) generated by the modified method with unprocessed aspirin (ASP-I).
  • To evaluate the efficiency of the modified vapor diffusion method for rapid drug crystal generation and polymorph screening.

Main Methods:

  • Modified vapor diffusion technique utilizing diethylether and dichloromethane as non-solvents.
  • Analytical characterization employing Fourier transform-infrared spectroscopy (FT-IR), X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC), and Scanning Electron Microscopy (SEM).
  • Comparison of generated crystals (ASP-II, ASP-III) with the unprocessed model drug (ASP-I).

Main Results:

  • The modified method successfully generated aspirin crystals (ASP-II, ASP-III) within 12 hours, a significant improvement over the 15-day classical method.
  • FT-IR analysis confirmed identical internal structures for ASP-I, ASP-II, and ASP-III.
  • XRD, DSC, and SEM revealed modifications in crystal habit (platy for ASP-II, needle for ASP-III) and size, without altering the internal polymorphic structure.
  • Slow dissolution rates of generated crystals indicated the formation of the stable polymorph I.

Conclusions:

  • The modified vapor diffusion method is a rapid and efficient technique for generating drug crystals.
  • This method allows for the modification of crystal habit and size without changing the internal drug structure.
  • The technique holds potential for routine screening and securing various polymorphic forms of other drug entities.