Combination of sedating and non sedating antihistamines

Second generation antihistamines were developed in the 1980s and are much less sedating than first-generation antihistamines.They act on histamine-1 receptors in the periphery and are unlikely to penetrate the brain, so are less likely to cause side effects or interact with drugs. While aspirin and acetaminophen have been utilized in these previous compositions, it has not been heretofore proposed to use any of the newer non-steroidal anti-inflammatory drugs (i.e., excluding aspirin, acetaminophen and phenacetin) in the preparation of advantageous cough/cold pharmaceutical compositions.

Interactions with other drugs are more common with first-generation antihistamines compared with second-generation antihistamines.

For example, the antipyretic effectiveness of ibuprofen in comparison to aspirin and to acetaminophen has been studied. In the first study, 17 adult patients with fever of 100° F. In the patients with upper respiratory tract infections antipyretic effect from both treatments began approximately one hour after dosing.

More specifically, the applicants herein have found that certain non-steroidal anti-inflammatory agents are ideally suited for use in cough/cold formulations by reason of their enhanced analgesic anti-inflammatory and antipyretic activity and low incidence of untoward side effects, particularly at the optimum dosages provided for in the present invention, compared to aspirin or acetaminophen. et al, "Antipyretic Activity of Ibuprofen (Brufen)", J. Physicians, India (1973) 9-584 describes the results of two randomized, double-blind, parallel studies comparing the antipyretic efficacy of ibuprofen to that of aspirin. Once peak temperature was reached as indicated by cessation of rigors, each patient received either ibuprofen 400 mg (5 patients) or aspirin 600 mg (6 patients).

It is a further object of the present invention to provide methods for the symptomatic relief of cough, cold, cold-like and flu symptoms and the discomfort, pain, headache, fever and general malaise associated therewith, by the administration of preselected dosages of the pharmaceutical compositions of the present invention.

It is, therefore, a primary object of the present invention to provide pharmaceutical compositions of matter comprising an analgesically effective amount of a non-steroidal anti-inflammatory drug in combination with a non-sedating antihistamine, and optionally one or more active components selected from a decongestant, cough suppressant, expectorant and, further optionally including pharmaceutically acceptable carriers therefor.

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