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Related Experiment Videos

Solubilization and preformulation of carbendazim.

Nina Ni1, Tapan Sanghvi, Samuel Yalkowsky

  • 1College of Pharmacy, The University of Arizona, Tucson, AZ 85721, USA. na@pharmacy.arizona.edu

International Journal of Pharmaceutics
|September 3, 2002
PubMed
Summary

Investigating carbendazim solubility, researchers found that acidic conditions (pH 2) significantly enhance drug solubility by 250-fold, especially with complexants. Basic conditions (pH 7) showed minimal solubility improvements with additives.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Physical Chemistry

Background:

  • Carbendazim is a widely used fungicide with poor aqueous solubility.
  • Enhancing carbendazim solubility is crucial for developing effective pharmaceutical formulations.
  • Understanding the impact of pH and excipients on carbendazim solubility is key for formulation development.

Purpose of the Study:

  • To investigate the solubilization of carbendazim using pH modification in combination with cosolvents, surfactants, and complexants.
  • To determine the optimal conditions for maximizing carbendazim solubility for oral formulations.

Main Methods:

  • Solubility studies were conducted across a range of pH values (pH 2 and pH 7).
  • The effects of cosolvents, nonionic surfactants, and complexants on carbendazim solubility were evaluated.

Related Experiment Videos

  • Stability of a proposed oral formulation at pH 2 was assessed upon dilution with water and Seven Up.

    • Main Results:

    • Carbendazim solubility increased by 250-fold at pH 2 compared to pH 7 (6.11 ± 0.45 μg/ml).
    • Cosolvents and nonionic surfactants showed limited efficacy at pH 2, while complexants significantly enhanced solubility.
    • The proposed oral formulation at pH 2 remained stable in Seven Up and water but precipitated in pH 7 buffer at 1:10 dilution.

    Conclusions:

    • Acidic conditions (pH 2) are highly effective in solubilizing carbendazim, particularly when combined with complexants.
    • The choice of excipient is critical and depends on the pH of the formulation.
    • A carbendazim formulation at pH 2 shows promising stability for oral administration.