Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-04-19
2002-08-13
Krass, Frederick (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S969000
Reexamination Certificate
active
06433003
ABSTRACT:
BACKGROUND OF THE INVENTION.
1. Field of the Invention
This invention is directed to methods for treating hyperhidrosis in mammals. Specifically, the methods of this invention involve the topical administration of an effective amount of a glycopyrrolate compound to a mammal suffering from hyperhidrosis.
REFERENCES
The following publications, patent applications and patents are cited in this application:
1. Riolo et al.,
South Med J.
83:1138-1143 (1990)
2. Glogau R. G.
Cermatol. Surg.
24:817-94 (1998)
3. Schnider et al.,
Br. J. Dermatol.
136:548-52 (1997)
4. Atkin et al., “Treatment of diabetic gustatory sweating with topical glycopyrrolate cream”
Diabetic Medicine
13:493-494 (1996)
5. Shaw et al., “A randomized controlled trial of topical glycopyrrolate, the first specific treatment for diabetic gustatory sweating”
Diabetologia
40:299-301 (1997)
6. May et al., “Frey's Syndrome: Treatment with topical glycopyrrolate”
Head
&
Neck
(January/February 1989) p.85-89
7. Col. Leonard L. Hays, “The Frey syndrome: A review and double blind evaluation of the topical use of a new anticholinergic agent”
The Laryngoscope
88:1976 (1978)
8.
Remington's Pharmaceutical Sciences
, Mace Publishing Company Philadelphia Pa. 17
th
ed. (1985)
9. U.S. Pat. No. 5,525,347, Kellner et al.
10. U.S. Pat. No. 2,956,062, Lunsford et al.
11. Hays et al., “The Frey syndrome: a simple, effective treatment”
Otolaryngol Head Neck Surg.
90:419-425 (1982)
All of the above publications, patent applications and patents are herein incorporated by reference in their entirety to the same extent as if each individual publication or patent was specifically and individually indicated to be incorporated by reference in its entirety.
2. State of the Art
Hyperhidrosis is an idiopathic pathological condition characterized by excessive, uncontrollable sweating beyond that required to cool the body. Disturbance of the central nervous system has been associated with this condition. It affects approximately one out of every one hundred people. Hyperhidrosis not only may result in intense social embarrassment, but also may even interfere with a person's occupation.
It most often involves one or several areas, especially the hands, axillae, feet or face, although it can even involve the whole body. Palmar hyperhidrosis is the most common form. Antiperspirants are generally ineffective in treating this form of perspiration. Oral medications are occasionally beneficial, but may have side effects. As a result, many persons with hyperhidrosis have resorted to a surgical procedure, endoscopic thoracic sympathectomy (1). Although the surgery affords permanent benefit in some 40% to 90% of affected individuals, it is invasive, requires general anesthesia and is not without potential side effects. As many as 50% of persons who have undergone thoracic sympathectomy develop compensatory and annoying sweating of the trunk or thighs.
More recently, botulinum A neurotoxin (BOTOX) which blocks the action on sweat glands of acetylcholine that is released by the autonomic nerves, has proven effective in hyperhidrosis. Minute amounts of BOTOX injected into the palms or axillae of affected individuals results in statistically significant benefit (2,3). The effect lasts for several months but requires repeat injections.
A non-invasive, convenient and effective treatment with few side effects would be a welcome alternative for treating hyperhidrosis.
Topical glycopyrrolate has been used previously to treat gustatory sweating associated with diabetic autonomic neuropathy (4, 5) In this disorder, sweating that often is profuse, begins soon after the patient ingests food, starting on the forehead and then involving the face, scalp and neck. A solution of glycopyrrolate was applied to the face of the patient which prevented the gustatory sweating.
Similarly, glycopyrrolate has also been used previously to treat gustatory sweating associated with Frey's syndrome which may develop after parotidectomy (11, 6, 7). Frey's syndrome is believed to result from the aberrant reinnervation of the sweat glands of the face by the severed parotid parasympathetic nerve fibers.
In both diabetic gustatory sweating and Frey's syndrome, the profuse facial sweating is induced by the specific stimulus of eating. Moreover, the sweating in each is a consequence of a distinct neuropathological process. In contrast, hyperhidrosis occurs spontaneously without a specific stimulus.
Glycopyrrolate administered with iontophoresis has been used to treat hyperhidrosis(8). In this case 0.1% of glycopyrrolate was administered topically to the skin and then the area of application was subjected to iontophoresis. For some patients, this treatment regime reduced the hyperhidrosis for up to 4 weeks. However, the patients needed to attend at the physicians office for the treatment and the treatment was associated with side effects such as abdominal discomfort and this treatment was not effective for all patients.
This invention is directed in part to the discovery that the daily topical application of a 0.25% to 6% glycopyrrolate compound to a mammal overcomes many of the prior problems in treating hyperhidrosis. Additionally, it provides advantages heretofore not achieved by conventional treatments for hyperhidrosis. For example, the glycopyrrolate compound to be applied does not have the side effects associated with Botox treatments or iontophoresis.
SUMMARY OF THE INVENTION
This invention is directed to methods for treating hyperhidrosis by the topical application of a composition comprising from about 0.25 to 6% by weight of a glycopyrrolate compound to a mammal.
This invention is directed to a method for alleviating hyperhidrosis in a mammal, which method comprises the steps of identifying a mammal susceptible to hyperhidrosis; and topically administering to the skin of said mammal a composition comprising from about 0.25% to 6% by weight of a glycopyrrolate compound. Preferably, the glycopyrrolate compound has formula I:
wherein X
−
is a pharmaceutically acceptable counter ion salt.
This invention is also directed to a method for alleviating hyperhidrosis in a mammal, which method comprises the steps of identifying a mammal susceptible to hyperhidrosis; and topically administering to said mammal a pharmaceutical composition comprising from about 0.25 to 6% by weight of a glycopyrrolate compound and a pharmaceutically acceptable excipient. Preferably the glycopyrrolate compound has formula I:
wherein X
−
is a pharmaceutically acceptable counter ion salt.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
This invention is directed to methods for treating hyperhidrosis in a mammal by the topical application of a glycopyrrolate compound to a mammal.
Definitions
As used herein, the following terms have the following meanings;
The term “glycopyrrolate compound” means a compound of the formula:
wherein X
−
is a pharmaceutically acceptable counter ion salt.
The term “glycopyrrolate compound” also refers to analogues of glycopyrrolate capable of inhibiting hyperhidrosis wherein the chemical structure has been modified so as to introduce, modify and/or remove one or more functionalities of the structure. For example, such modification can result in the removal of an OH functionality, the introduction of an amine functionality, the introduction of a halo functionality, and the like. In so far as the glycopyrrolate analogues are capable of inhibiting hyperhidrosis they are encompassed by the definition of “glycopyrrolate compound”.
Hyperhidrosis is a condition commonly known and understood by the average consumer who lacks any medical skill. It is an idiopathic condition characterized by excessive, uncontrollable perspiration beyond that required to cool the body.
The term “mammal” includes, without being limiting, such mammals as mice, rats, ovines, bovines and humans. Preferably the mammal is a human.
The term “therapeutically effective amount” means that amount of a drug or pharmaceutical agent that will elicit the biologica
Bobrove Arthur M.
Urman Jeffrey D.
Burns Doane Swecker & Mathis L.L.P.
Krass Frederick
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