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[X-ray diffraction studies on tolbutamide solid dispersion].

X Ma1, S K Rong, Q Q Wu

  • 1Department of Pharmacy, Lanzhou Medical College.

Yao Xue Xue Bao = Acta Pharmaceutica Sinica
|January 1, 1992
PubMed
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Tolbutamide (D860) solid dispersions with urea, polyvinyl pyrrolidone (PVP), and polyethylene glycol (PEG) showed enhanced dissolution. Amorphous D860-PVP and solid solutions of D860-urea/PEG exhibited higher activity and faster drug release.

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Physical Chemistry

Background:

  • Tolbutamide (D860) is an oral hypoglycemic agent.
  • Solid dispersions can improve the dissolution rate and bioavailability of poorly soluble drugs.
  • Carrier selection is crucial for the performance of solid dispersions.

Purpose of the Study:

  • To investigate the solid-state properties of tolbutamide (D860) dispersions.
  • To correlate the physical state of D860 in various solid dispersions with their dissolution rates.
  • To evaluate the impact of different carriers (urea, PVP, PEG 6000) on D860's dissolution behavior.

Main Methods:

  • Preparation of D860 solid dispersions using urea, polyvinyl pyrrolidone (PVP), and polyethylene glycol (PEG) 6000 as carriers.

Related Experiment Videos

  • X-ray diffraction (XRD) analysis to characterize the solid-state forms (amorphous, solid solution, microcrystalline).
  • Dissolution rate studies to assess drug release profiles.

    • Main Results:

    • D860 in D860-PVP dispersion was found to be in an amorphous state, exhibiting a significantly greater dissolution rate.
    • D860-urea and D860-PEG melts formed partly miscible solid solutions and partly microcrystalline states, showing higher activity and increased dissolution rates.
    • D860-PEG coprecipitate, a physical mixture, demonstrated a slower dissolution rate compared to its melt form.
    • No changes in the crystal structure of D860 dispersions were observed during ageing tests, indicating good physical stability.

    Conclusions:

    • The amorphous state of D860 in PVP dispersions enhances its dissolution rate.
    • Solid solutions formed with urea and PEG also improve tolbutamide's dissolution characteristics.
    • Carrier selection and preparation method (melt vs. coprecipitation) significantly influence the solid-state properties and dissolution performance of D860.