Quantification of Grapiprant and Its Stability Testing under Changing Environmental Conditions

Area of Science:

• Veterinary Pharmacology
• Analytical Chemistry
• Drug Development

Background:

• Grapiprant is a selective EP4 receptor antagonist approved for canine osteoarthritis pain and inflammation.
• Its anti-inflammatory effects are documented in preclinical and clinical studies.
• Potential applications in oncological therapy are being explored.

Purpose of the Study:

• To develop and validate a thin-layer chromatography (TLC) method for grapiprant identification and quantification.
• To assess the stability of grapiprant under various conditions.
• To investigate grapiprant degradation pathways using UPLC-MS/MS.

Main Methods:

• Development of TLC separation using silica gel 60F254 plates and ethyl acetate-toluene-butylamine mobile phase.
• Method validation according to ICH guidelines, including linearity, limit of detection (146.65 µg/mL), precision, and accuracy.
• Quantification in pharmaceutical preparations and stability studies.
• Degradation product analysis using UPLC-MS/MS.

Main Results:

• Optimal TLC conditions were established for grapiprant separation.
• The validated method demonstrated linearity, sensitivity, and reliability.
• Grapiprant quantification in a pharmaceutical formulation was successful.
• Stability studies identified potential degradation pathways under stress conditions.

Conclusions:

• A validated TLC-densitometric method provides a reliable means for grapiprant analysis.
• The method is suitable for quality control and stability testing of grapiprant pharmaceutical preparations.
• Understanding grapiprant's degradation is crucial for its therapeutic application and potential new uses.