Pharmacokinetics and Safety of Ketorolac Following Single Intranasal and Intramuscular Administration in Healthy Volunteers

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Abstract
Ketorolac was administered to 15 healthy volunteers in a phase 1, single‐dose, crossover, randomized study. Subjects received open‐label randomized 15‐ and 30‐mg intramuscular (IM) ketorolac and blinded randomized 15‐ and 30‐mg intranasal (IN) ketorolac. The IN ketorolac was well tolerated; the only nasal symptoms were some instances of mild irritation. The IN ketorolac was rapidly and well absorbed (median tmax, 0.50–0.75 hours), and the half‐life was approximately 5 to 6 hours, values that were similar to those following IM administration. Relative bioavailability of IN compared to IM administration at the same doses was approximately 67% to 75%. Dose proportionality was noted between the 15‐ and 30‐mg IN and IM dose levels. Thus, IN ketorolac offers a therapeutic alternative to IM administration and may provide benefits in the clinical setting.

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