Pharmacokinetics of a new subcutaneous diclofenac formulation administered to three body sites: Quadriceps, gluteus, and abdomen

摘要

Objective: To assess the relative bioavailability of a new subcutaneous (SC) diclofenac hydroxypropyl β-cyclodextrin (HPβCD) formulation administered to three body sites: quadriceps, gluteus, and abdomen. Materials and methods: This was a pilot, single-dose, randomized, three-way crossover relative bioavailability study. A total of 12 healthy subjects received a single SC injection of diclofenac HPβCD 50 mg/1 mL in the quadriceps, gluteus, or abdomen. Results: The AUC was comparable after SC diclofenac HPβCD in the quadriceps, gluteus, and abdomen. The Cmax was comparable after SC administration in the quadriceps or abdomen, and ~ 17% higher in the gluteus. The absorption was rapid (30 minutes) after administration of the treatment at any site. The treatment was well tolerated. Conclusions: The relative bioavailability of SC diclofenac HPβCD was comparable when administered to the quadriceps, gluteus, and abdomen. The new diclofenac formulation can therefore be administered subcutaneously to any of these sites without clinically significant differences. A further adequately powered study would be necessary to reveal any differences among injection sites in terms of peak plasma concentration.