Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
1995-05-31
2001-02-27
Moezie, Minna (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C514S423000, C514S850000
Reexamination Certificate
active
06194460
ABSTRACT:
BACKGROUND OF THE INVENTION
Angiotensin converting enzyme (ACE) inhibitors are widely used in the treatment of hypertension, congestive heart failure, acute myocardial infarction and diabetic nephropathy. One of the side effects that is often observed in patients who are taking ACE inhibitors is a persistent, dry cough that is refractory to most commonly prescribed cough suppressants. The cough is sometimes so severe that therapy with the ACE inhibitor must be discontinued.
Even those patients who respond to conventional cough suppressants are subject to the disadvantages associated with long term use of opiates and other non-opiate cough suppressants.
In the prior art, baclofen has been described as a GABA
&bgr;
agonist which has antitussive effects. Br. J. Pharmacol.(1993)110, 491-495) These effects have been demonstrated by counting the number of coughs elicited during a 4 minute or 30 minute period against capsaicin challenge by subcutaneous administration or by inhalation when baclofen and other antitussives were administered.
The present invention provides a method of suppressing the cough that is observed in patients, who are being maintained on an ACE inhibitor, which comprises the coadministration of baclofen with the ACE inhibitor. Based on the published literature, it was surprising and unexpected that no substantial antitussive effect, which could be attributed to the coadministration of baclofen with the ACE inhibitor, is observed until about three days after the initiation of baclofen therapy.
SUMMARY OF THE INVENTION
The present invention is directed to the coadministration of an amount of baclofen which is effective to suppress the cough of a patient who is afflicted with a cough that is induced by the administration of an ACE inhibitor. The usual dose of baclofen, for the treatment of cough associated with the administration of ACE inhibitors, is from 10 to 30 mg daily p.o. which is given in two to four divided doses. Higher doses may be used, if required in specific circumstances.
The invention also comprises a novel pharmaceutical composition which comprises a therapeutically effective amount of an ACE inhibitor in combination with an amount of baclofen which is effective to suppress the cough which is caused by the administration of the therapeutic dose of an ACE inhibitor.
Generally the composition will contain the usual therapeutic dose of the ACE inhibitor and from 2 to 10 mg of baclofen per oral dosage unit such as a tablet or capsule. If desired, the composition may be formulated as an extended or sustained release dosage formulation which contains a dose of baclofen which is based on the inclusion of a portion of the daily dose of baclofen which would be required over the time period during which the specific type of dosage form will release the ACE inhibitor.
Specific examples of the ACE inhibitors include enalapril, captopril, lisinopril, fosinopril, benazepril, quinapril, alacepril, cilazapril, delapril, enalaprilat, moveltopril, perindopril and ramipril. Persistent dry coughing has been observed as side effect in patients who are treated with these drugs.
The composition of the ACE inhibitor and the baclofen may be prepared using conventional excipients and binders which are well known in the art. For example a tablet may be made which contains 25 mg of captopril, 5 mg of baclofen, microcrystalline cellulose, corn starch, lactose and stearic acid. Other formulations may be prepared using techniques which are disclosed in Remington's Pharmaceutical Sciences, 1985 Ed., Mack Pub. Co., Easton, Pa. which is incorporated by reference.
REFERENCES:
patent: 5006560 (1991-04-01), Kreutner et al.
Bolser et al, Br.J. Pharmacol. (1994),113, 1344-1348.
Bolser et al, Br.J. Pharmacol. (1993) 110, 491-495.
Houston et al., British Journal of Pharmacology, Proceedings Supplement, vol. 112, May 1994, 264p.
Hedman & Costigan ,P.C.
Moezie Minna
Montefiore Medical Center
Wang S.
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