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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

Abstract

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 scarring.

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 barrier.

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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If you want to learn more about this patent, please go directly to the U.S. Patent and Trademark Office Web site to access the full patent.

 

 

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