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Pulmonary and nasal deposition of ketorolac tromethamine solution (SPRIX) following intranasal administration.

Abstract

Ketorolac tromethamine is a racemic, non-steroidal, anti-inflammatory drug (NSAID). An intra-nasal (IN) formulation, SPRIX(®), is approved for the treatment of short term (up to 5 days) acute moderate to moderately severe pain. The primary objective of this study was to determine whether (99m)Tc-diethylenetriaminepenta acetic acid (DTPA) radiolabelled ketorolac tromethamine formulation (31.5 mg) was deposited in the lungs of healthy subjects (4 men and 9 women) following nasal inhalation of different intensities (gentle or vigorous sniff) and under different postural conditions (upright or semi-supine). The secondary objectives were to determine the deposition pattern of radiolabelled ketorolac solution in the nasal cavity and the clearance of the radiolabel over a 6h period post-administration. The nasal spray pump delivery device used showed a droplet size distribution with a volume mean diameter (VMD) of 50 μm and approximately 85% of the aerosol mass contained in droplets >10 μm diameter. The fraction of the dose recorded from the lung regions averaged <0.5%, and was considered to represent scattered radiation rather than true pulmonary deposition. This fraction was not affected by posture or by inhalation manoeuvre. The majority of the radiolabelled intranasal dose was deposited in the nasal cavity. The visual spread patterns within the nasal cavity were most uniform following administration in the upright position regardless of inhalation manoeuvre. Clearance from the nasal cavity was initially very rapid, with only 16-30% of the dose remaining after 10 min and 6-14% after 6 h. Retention was greatest following gentle inhalation.

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  • Publisher Full Text

    • Authors

    Bacon R, Newman S, Rankin L, Pitcairn G, Whiting R

    Institution

    Pharmaceutical Profiles Ltd., Nottingham, UK.

    Source

    International journal of pharmaceutics 431:1-2 2012 Jul 15 pg 39-44

    MeSH

    Administration, Intranasal
    Adult
    Anti-Inflammatory Agents, Non-Steroidal
    Cross-Over Studies
    Esophagus
    Female
    Humans
    Ketorolac Tromethamine
    Lung
    Male
    Middle Aged
    Nasal Cavity
    Posture
    Stomach

    Pub Type(s)

    Clinical Trial
    Journal Article
    Randomized Controlled Trial
    Research Support, Non-U.S. Gov't

    Language

    eng

    PubMed ID

    22525081