Title: Treatment of lupus erythematosus
United States Patent: 6,537,968
Issued: March 25, 2003
Inventors: Lezdey; Darren (Indian Rocks Beach, FL); Lezdey;
Jarett (Indian Rocks Beach, FL)
Assignee: Alphamed Pharmaceuticals Corp (Clearwater, FL)
Appl. No.: 624442
Filed: July 24, 2000
The present invention provides for the treatment of an individual
suffering from lupus erythematosus utilizing a serine protease inhibitor.
The treatment includes the use of a corticosteroid that is administered
separately or in combination. The serine proteases preferred are alpha
1-antitrypsin, secretory leucocyte protease inhibitor, alpha 2-macroglobulin
or mixtures thereof.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
In accordance with one embodiment of the invention, there is provided a
method for the treatment of individuals suffering from lupus erythematosus
or symptoms thereof by the administration of a serine protease inhibitor.
The method consists of the administration of an effective therapeutic
amount of a protease inhibitor selected from the group consisting of alpha
1-antitrypsin, secretory leucocyte, protease inhibitor, alpha
2-macroglobulin or mixtures thereof, and analogs or derivatives thereof in
a suitable pharmaceutical carrier.
Accordingly, a composition containing about 0.5 to 10 mg. of protease
inhibitor is in a suitable pharmaceutical vehicle is used in the
treatment. Generally, for topical use, about 1 to 5 mg. of the protease
inhibitor has been effective to treat the eruption and to prevent
Preferably, about 1 to 5 mg of the protease inhibitor in its natural,
transgenic or recombinant form is placed into a composition for topical
application such as a cream, gel, ointment or the like. A corticosteroid
may be included in the treating composition. The treatment provides
immediate relief of pain since the kinins and kallikreins can be
controlled. The patient can be treated daily until the lesions are reduced
and under normal bodily control. In severe cases, oral corticosteroids may
be utilized. The composition may also include penetrating agents such as
hyaluronic acid, insulin, liposome, or the like, as well as L-arginine or
the arginine containing amino acids. The penetrants may be used in an
amount of about 0.5 to 2% by weight of composition. Hyaluronic acid also
aids in wound healing.
Systemic lupus erythematosus may also be treated by weekly infusion of 200
mg of the serine protease inhibitor in a 2% saline solution or by oral
dosages daily of the inhibitor in a carrier which transgresses the gastric
It has been found that the incorporation of L-arginine or an arginine
containing amino acid having up to ten carbon atoms helps in the
penetration of the drug into the skin. The arginine also attracts hormones
to the site to help in wound healing.
Serine protease inhibitors have been found to play a major role in the
direct inactivation of the mediators of inflammation. The almost immediate
disappearance of pain indicates that there can be a control of the kinins
as well. A cocktail of serine protease inhibitors, their analogs, salts or
derivatives, appears to provide the quickest healing when used in
combination with a corticosteroid.
The drug can be administered topically in unit dosage form containing
about 1 to 5 mg per day depending on the severity of the disease. The use
of controlled release substances, for example, liposomes, diketopyperazine
microparticles as disclosed by U.S. Pat. Nos. 5,620,708 and 5,503,852
which are herein incorporated by reference, or an occlusive bandage, are
especially effective. One topical composition formed with a vasoline type
carrier, such as, AQUAPHOR has been found to be effective.
The inflammatory condition of the joints can be treated by injection at
the site of inflammation or by infusion of the drug. Generally, about
200-400 mg of the protease inhibitors can be administered daily by
injection or infusion depending on the severity of the disease.
It is understood that the different components used in the treatment of
the diseases can be administered in a single unit dose or separately
depending upon the patient and the severity of the disease. In most cases,
where the patient is a child, the use of a steroid should be avoided.
The corticosteroids which can be used in the treatment of the diseases
include triamcinolone acetonide, fluroandrenolide, prednisone,
beclomethasone valerate, amcinolone, dexamethasone, betamethasone valerate,
halocinonide, clocortolone and hydrocortisone valerate.
Claim 1 of 12 Claims
What is claimed is:
1. A method for treating an individual suffering from the disease lupus
erythematous which comprises administering to the patient a
therapeutically effective amount of a composition containing a protease
inhibitor selected from the group consisting of alpha 1-antitrypsin,
secretory leucocyte protease inhibitor and alpha 2-macroglobulin in a
suitable pharmaceutically acceptable carrier, thereby reducing
inflammation, rashes or lesions.
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