Product characteristics and pharmacokinetics of intranasal ipratropium bromide.
The in vivo absorption potential of ipratropium bromide nasal spray was evaluated in studies involving healthy volunteers (0.03%, 0.06%, and 0.12% dosage strengths) and patients with perennial rhinitis (0.03% and 0.06%) and the common cold (0.06%). The dose used was two sprays per nostril, corresponding to a total dose of 84 micrograms, 168 micrograms, and 336 micrograms for the three dosage strengths. These studies indicate that 10% or less of active drug is absorbed systemically after nasal administration based on the amount of unchanged drug excreted in urine in a 24-hour interval. In most instances, the plasma drug concentrations were undetectable. In none of these studies did plasma ipratropium concentrations reach a level where systemic anticholinergic effects are known to occur.
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Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Conn. 06877-0368, USA.
Fireman
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Grossman
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Wecker
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MacGregor
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D000042:Absorption; D000284:Administration, Oral; D003139:Common Cold / Q000188:drug therapy / Q000378:metabolism*; D018592:Cross-Over Studies; D004311:Double-Blind Method; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D007275:Injections, Intravenous; D009241:Ipratropium / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008297:Male; D009297:Nasal Mucosa / Q000187:drug effects / Q000378:metabolism*; D009330:Nebulizers and Vaporizers; D011680:Pupil / Q000187:drug effects; D012221:Rhinitis, Allergic, Perennial / Q000188:drug therapy / Q000378:metabolism*
D009241:Ipratropium