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Solid and Solution Stability and Solubility of a Crystalline Form of a Novel 15-membered Azalide Derivative

Objective

  • To determine the solid state stability (4 weeks), light stability and stability and solubility in buffers and biorelavant media of  a crystalline form of  2’-O-{3-[(7-chloro-4-quinolinyl)amino]propyl}-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A, a novel 15-membered azalide.

Four weeks solid state stability

Four weeks solution stability

 Solubility

Summary

  • Solid state stability studies for up to 4 weeks showed that a crystalline form of 1 is physically and chemically stable.
  • Stability of 1 in solutions is pH and temperature dependent, and is most stable at pH 5 to 6 and at 5 oC and 25 oC.
  • Solubility of 1 is pH dependent and is high at pH values < 6.
  • Degradation of 1 in aqueous acidic media is due to hydrolysis of the cladinose sugar.

References

  • D. Filić et al., Crystal Structure and Physicochemical Properties of Crystalline Form of 2’-O-{3-[(7-chloro-4-quinolinyl)amino]propyl}-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A
    J Pharm Sci 2011, 100, 2586-2598
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