A novel rizatriptan oral gel formulation: Bioavailability and bioequivalence

Area of Science:

• Pharmacokinetics and Drug Metabolism
• Pharmaceutical Sciences

Background:

• Rizatriptan benzoate is a widely used medication for acute migraine treatment.
• Developing novel drug delivery systems can improve patient compliance and therapeutic outcomes.

Purpose of the Study:

• To assess the relative bioavailability of a new oral gel formulation of rizatriptan benzoate compared to a standard oral lyophilisate formulation.
• To evaluate the safety and palatability of the novel oral gel formulation.

Main Methods:

• An open-label, randomized, 2-period cross-over trial was conducted in 47 healthy subjects.
• Pharmacokinetic parameters, including AUC0-tlast, AUC0-∞, and Cmax, were determined using LC-MS/MS.
• Adverse events and product palatability were assessed.

Main Results:

• The new oral gel formulation showed pharmacokinetic profiles comparable to the reference lyophilisate product.
• Point estimates for AUC0-tlast, Cmax, and AUC0-∞ were within the 80-125% bioequivalence range.
• The most common adverse events were headache and dizziness, with no severe events reported. Palatability was deemed acceptable.

Conclusions:

• The oral gel formulation of rizatriptan benzoate is bioequivalent to the marketed lyophilisate product.
• The new formulation is well-tolerated and acceptable to users, presenting a viable alternative for migraine management.