Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-02-05
2002-08-13
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06432972
ABSTRACT:
BACKGROUND OF THE INVENTION
This invention relates to the use of desloratadine for the preparation of a medicament for treating and/or preventing congestion associated with allergic and inflammatory conditions, such as allergic rhinitis.
Desloratadine, disclosed in U.S. Pat. No. 4,659,716, is a non-sedating antihistamine useful for treating allergic reactions in animals including humans. U.S. Pat. No. 5,695,997 discloses pharmaceutical compositions containing desloratadine and methods of using desloratadine for treating and preventing disease states, e.g., allergic rhinitis.
Nasal congestion/stuffiness is a chronic symptom in patents with allergic disorders such as allergic rhinitis. However, currently available antihistamines have not been effective in treating nasal congestion/stuffiness associated with allergic disorders. Congestion associated with allergic rhinitis has been treated by the administration of combination products containing an antihistamine and the decongestant pseudoephedrine. For example, the Claritin D12 and D24 commercial products are combinations of loratadine and pseudoephredrine and the “Allegra-D” commercial product is a combination of fexofenadine and pseudoephedrine. See, Physicians Desk Reference 2000.
However, the administration of pseudoephedrine may cause unwanted side effects. Side effects associated with pseudoephedrine include insomnia, dizziness, weakness, tremor or arrhythmia. These and other unwanted side effects may cause patients suffering from congestion associated with allergic disorders to avoid or discontinue treatment with pseudoephedrine-containing products.
There is a need for a clinically effective therapy to treat or prevent such congestion associated with allergic and inflammatory conditions of the airway passages in a human with a non-sedating antihistamine which does not provide the potential adverse side effects that may be experienced with products containing pseudoephedrine. That is, there is a need for a non-sedating antihistamine that provides decongestant effect to reduce the amount of, or eliminate the need for, an additional decongestant such as pseudoephedrine.
SUMMARY OF THE INVENTION
The present invention provides a method of treating and/or preventing congestion associated with allergic and inflammatory conditions of the airway passages in a human, which comprises administering an amount of desloratadine effective for such treating and/or preventing. The present invention also provides a method of treating and/or preventing congestion associated with seasonal or perennial allergic rhinitis in a human which comprises administering an amount of desloratadine effective for such treating and/or preventing. The present invention further provides a method of treating and/or preventing congestion associated with allergic and inflammatory condition comprising administering desloratadine in combination with a reduced amount of one or more supplemental decongestants, such as pseudoephedrine.
DETAILED DESCRIPTION OF INVENTION
The phrase “allergic and inflammatory conditions of the airway passages” means those allergic and inflammatory conditions and symptoms found and in the upper and lower airway passages from the nose to the lungs. Typical allergic and inflammatory conditions or upper and lower airway passages include seasonal and perennial allergic rhinitis, non-allergic rhinitis, asthma including allergic and non-allergic asthma, sinusitis, and colds.
The term “congestion” means obstruction, stuffiness or blockage of the upper and/or lower airway passages from the nose to the lungs, including nasal congestion.
The amount of desloratadine effective for treating or preventing congestion associated with allergic and inflammatory conditions of the airway passages will vary with the age, sex, body weight and severity of the allergic and inflammatory condition of the patient. Typically, the amount of desloratadine effective for treating or preventing such allergic and inflammatory conditions is in the range of about 2.5 mg/day to about 45 mg/day, preferably about 2.5 mg/day to about 20 mg/day, or about 5.0 mg/day to about 15 mg/day, or about 5.0 mg/day to about 10 mg/day, more preferably about 5.0 mg/day to about 7.5 mg/day, and most preferably about 5.0 mg/day in single or divided doses, or a single dose of 5.0 mg/day.
U.S. Pat. No. 4,659,716 discloses methods of making desloratadine, pharmaceutical compositions containing it and methods of using desloratadine and pharmaceutical compositions containing it to treat allergic reaction in mammals. U.S. Pat. No. 5,595,997 discloses pharmaceutical compositions containing desloratadine and methods of using desloratadine for treating and preventing various disease states, e.g., allergic rhinitis. Desloratadine is available from Schering Corporation, Kenilworth, N.J.
The pharmaceutical compositions of desloratadine can be adapted for any mode of administration e.g., for oral, parenteral, e.g., subcutaneous (“SC”), intramuscular (“IM”), intravenous (“IV)” and intraperitoneal (“IP”), topical or vaginal administration or by inhalation (orally or intranasally). Preferably desloratadine is administered orally.
Such pharmaceutical compositions may be formulated by combining desloratadine or an equivalent amount of a pharmaceutically acceptable salt thereof with a suitable, inert, pharmaceutically acceptable carrier or diluent that may be either solid or liquid. Desloratadine may be converted into the pharmaceutically acceptable acid addition salts by admixing it with an equivalent amount of a pharmaceutically acceptable acid. Typically suitable pharmaceutically acceptable acids include the mineral acids, e.g., HNO
3
, H
2
SO
4
, H
3
PO
4
, HCl, HBr, organic acids, including, but not limited to, acetic, trifluoroacetic, propionic, lactic, maleic, succinic, tartaric, glucuronic and citric acids as well as alkyl or arylsulfonic acids, such as p-toluenesulfonic acid, 2-naphthalenesulfonic acid, or methanesulfonic acid. The preferred pharmaceutically acceptable salts are trifluoroacetate, tosylate, mesylate, and chloride. Desloratadine is more stable as the free base than as an acid addition salt and the use of the desloratadine free base in pharmaceutical compositions of the present invention is more preferred.
Solid form preparations include powders, tablets, dispersible granules, capsules, cachets and suppositories. The powders and tablets may be comprised of from about 5 to about 95 percent active ingredient. Suitable solid carriers are known in the art, e.g. magnesium carbonate, magnesium stearate, talc, sugar or lactose. Tablets, powders, cachets and capsules can be used as solid dosage forms suitable for oral administration. Examples of pharmaceutically acceptable carriers and methods of manufacture for various compositions may be found in A. Gennaro (ed.), Remington's Pharmaceutical Sciences, 18th Edition, (1990), Mack Publishing Co., Easton, Pa.
Liquid form preparations include solutions, suspensions and emulsions. As an example may be mentioned water or water-propylene glycol solutions for parenteral injection. Solid form preparations may be converted into liquid preparations shortly before use for either oral or administration. Parenteral forms to be injected intravenously, intramuscularly or subcutaneously are usually in the form of sterile solutions and may contain tonicity agents (salts or glucose), and buffers. Opacifiers may be included in oral solutions, suspensions and emulsions. Liquid form preparations may also include solutions for intranasal administration.
Aerosol preparations suitable for inhalation may include solutions and solids in powder form, which may be in combination with a pharmaceutically acceptable carrier, such as an inert compressed gas, e.g., nitrogen.
Also included are solid form preparations which are intended to be converted, shortly before use, to liquid form preparations for either oral or parenteral administration. Such liquid forms include solutions, suspensions and emulsions.
The compounds of the invention may also be deliverable transdermally.
Lorber Richard R.
Salmun Luis M.
Hoffman Thomas D.
Jarvis William R. A.
Kim Vickie
Schering Corporation
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