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Characterization and In vivo Evaluation of Polymorphic Valnemulin Hydrogen Fumarate
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Aims:
In the present study, a valnemulin hydrogen fumarate prodrug was characterized,
its stability was compared with valnemulin hydrochloride, and the efficacy was evaluated in Actinobacillus
pleuropneumoniae-induced pneumonia in mice.
Method:
Optical microscopy, X-ray powder diffraction, infrared spectroscopy, and hydrogen nuclear
magnetic resonance spectroscopy were used to study the physical and chemical properties of
the prodrug. The thermal stability was investigated in comparison with valnemulin hydrochloride
to improve the preparation process of valnemulin hydrogen fumarate soluble powder and maximize
its drug effect. Additionally, the efficacy of valnemulin hydrogen fumarate was evaluated in
a challenge-treatment trial in mice using an in vitro antimicrobial susceptibility test.
Results:
The valnemulin hydrogen fumarate had high crystallinity. After light irradiation for 20
days, valnemulin hydrogen fumarate did not degrade, whereas valnemulin hydrochloride did. These
results showed that the valnemulin hydrogen fumarate was stable. At the same dose in drinking
water, the valnemulin hydrogen fumarate was more effective than the reference drug (tiamulin
fumarate) in an Actinobacillus pleuropneumoniae challenge-treatment trial.
Conclusion:
Valnemulin hydrogen fumarate shows excellent potential for application as a veterinary
drug.
Bentham Science Publishers Ltd.
Title: Characterization and In vivo Evaluation of Polymorphic Valnemulin Hydrogen Fumarate
Description:
Aims:
In the present study, a valnemulin hydrogen fumarate prodrug was characterized,
its stability was compared with valnemulin hydrochloride, and the efficacy was evaluated in Actinobacillus
pleuropneumoniae-induced pneumonia in mice.
Method:
Optical microscopy, X-ray powder diffraction, infrared spectroscopy, and hydrogen nuclear
magnetic resonance spectroscopy were used to study the physical and chemical properties of
the prodrug.
The thermal stability was investigated in comparison with valnemulin hydrochloride
to improve the preparation process of valnemulin hydrogen fumarate soluble powder and maximize
its drug effect.
Additionally, the efficacy of valnemulin hydrogen fumarate was evaluated in
a challenge-treatment trial in mice using an in vitro antimicrobial susceptibility test.
Results:
The valnemulin hydrogen fumarate had high crystallinity.
After light irradiation for 20
days, valnemulin hydrogen fumarate did not degrade, whereas valnemulin hydrochloride did.
These
results showed that the valnemulin hydrogen fumarate was stable.
At the same dose in drinking
water, the valnemulin hydrogen fumarate was more effective than the reference drug (tiamulin
fumarate) in an Actinobacillus pleuropneumoniae challenge-treatment trial.
Conclusion:
Valnemulin hydrogen fumarate shows excellent potential for application as a veterinary
drug.
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