Title:  Injection viral treatment

United States Patent:  6,172,053

Appl. No.:  395290

The present invention relates to a therapeutic composition and formulation for the treatment of viral diseases such as, Dengue fever and influenza. More particularly, to therapeutic preparation comprising substantially water soluble, local anesthetic of the ester type, procaine hydrochloride and a water soluble glucocorticoid, dexamethasone sodium phosphate.

DETAILED DESCRIPTION OF THE INVENTION

The present invention is useful for the effective treatment of viral infections. The viral treatment is prepared from USP approved drugs and has broad application in the treatment of several viral infections, namely AIDS, Dengue fever, influenza, common colds, herpes, mumps, measles, viral hepatitis, conjunctivitis, chickenpox and rabies.

The invention includes a formulation of procaine hydrochloride, USP, combined with dexamethasone sodium phosphate, USP. By itself, procaine hydrochloride is a local anesthetic that blocks the conduction of nerve impulses. It is readily absorbed following parenteral administration and is directly biotransformed in the bloodstream being hydrolyzed by plasma cholinesterase to para-aminobenzoic acid and diethylaminoethanol within one and one half hours from the time of administration. Procaine hydrochloride is the ester of diethylaminoethanol and para-aminobenzoic acid and is related chemically and pharmacologically to ester type local anesthetics. The chemical name of procaine hydrochloride is benzoic acid 4-amino, 2-diethly(amino)ethyl ester monohydrochloride. Dexamethasone sodium phosphate is a water-soluble inorganic ester of dexamethasone. Dexamethasone sodium phosphate, by itself, is used to treat endocrine disorders, rheumatic disorders, collagen diseases, dermatologic diseases, allergic states, ophthalmic diseases, gastrointestinal diseases, respiratory diseases, hematologic disorders, neoplastic diseases and edematous states. Dexamethasone sodium phosphate has the chemical name 9-fluoro-11.beta.,17,21-trihydroxy-16.varies.-methylpregna- 1,4-diene-3,20-dione 21-(dihydrogen phosphate) disodium salt. It comes as a surprise that procaine hydrochloride and dexamethasone sodium phosphate, when used together, can have a positive effect on the treatment of viral diseases. It is known that certain esters like procaine hydrochloride can act synergistically with esters of dexamethasone to prolong procaine hydrochloride anesthetic activity.

Procaine hydrochloride injection is available as a sterile solution in a concentration of 2% (20 mg of procaine hydrochloride in 1 ml solution). Dexamethasone sodium phosphate is available as a sterile solution in a concentration of 0.4% (4 mg of dexamethasone sodium phosphate in 1 ml solution).

The present invention includes a formulation comprising a mixture of procaine hydrochloride and dexamethasone sodium phosphate which is injected intramuscularly at certain dosages and regulated dosing intervals depending on the disease type, patient's severity of condition, age, body build and response to treatment. The following dosage schedule provides an indication of average doses and dosing intervals for adults and children:

For AIDS, Dengue fever and influenza treatment, adult patients can receive an intramuscular injection of around 30 mg of procaine hydrochloride in 1.5 ml of a 20 mg/ml solution mixed with around 2 mg of dexamethasone sodium phosphate in 0.5 ml of a 4 mg/ml solution. The total volume of 2 ml comprising the two compound formulation is aseptically transferred into a sterile 2 milliliter syringe. After the ingredients are gently mixed, the formulation containing syringe is ready for injection. In children, the average dosages are reduce to around 15 mg of procaine hydrochloride in 0.75 ml of a 20 mg/ml solution mixed with around 1 mg of dexamethasone sodium phosphate in 0.25 ml of a 4 mg/mi solution. The total volume of 1 ml comprising the two compound formulation is aseptically transferred to a 1 ml sterile syringe and mixed as described above.

One having ordinary skill in the art will readily recognize that the above ratios and concentrations may be varied and the effect or results may be readily gaged without departing from the spirit and scope of the present invention. Depending on a patient's disease type, severity of condition, age, body build and response to treatment, 5 mg to 40 mg of procaine hydrochloride can be mixed with 1 mg to 4 mg of dexamethasone sodium phosphate per intramuscular injection in order to achieve successful treatment. If the administration of procaine hydrochloride and dexamethasone sodium phosphate in tablet form is contemplated, the dosage amounts for each drug would increase since drug absorption into the circulatory system would occur during drug passage through the gastrointestinal tract whereas drug delivery by intramuscular injection allows for direct drug absorption into the circulatory system. In tablet form, the amount of procaine hydrochloride can be present in a range of about 350 mg to 600 mg and the amount of dexamethasone sodium phosphate can be present in a range of about 25 mg to 40 mg depending on a patient's disease type, severity of condition, age, body build and response to treatment.

For patient treatment, in general, dosing intervals are as follows:

For AIDS treatment, one 2 ml compilation for adults or one 1 ml compilation for children can be injected intramuscularly two times a day having an interval of two hours or more between injections. After a series of daily injections for nine to twelve consecutive days, then two injections per day can be given once a week. Subsequent treatment is determined by laboratory tests for the presence of helper T-cell lymphocytes with CD4 receptors that are susceptible to the HIV envelope glycoprotein gp120. A normal CD4 blood concentration is about 700-1000 cells per cubic millimeter of blood. As the CD4 cell count decreases, the risk of opportunistic viral, bacterial, fungal and parasitic infections increase. Patient dosages can be adjusted depending on the CD4 count and the patient response to treatment.

For Dengue fever, the 2 ml compilation for adults or the 1 ml compilation for children can be injected intramuscularly two times a day having an interval of two hours or more for three to five consecutive days.

For influenza, the 2 ml compilation for adults or the 1 ml compilation for children can be injected intramuscularly two times a day having an interval of two hours or more for one to two days.

All three viral treatments must be accompanied by supplemental oral rehydration fluids. For a severely ill patient, the dosage interval time can be reduced to one and one half hour.

The above average doses and dosing intervals describe a manner and method of making and using the invention and sets forth the best mode contemplated by the inventor for carrying out his invention but is not to be construed as limiting. For example, commercially available formulations of procaine hydrochloride and dexamethasone sodium phosphate may be used provided the amounts of these formulations generally follow the guidelines as set forth within this patent specification. The specification of U.S. Pat. No. 5,492,901 is hereby incorporated by reference noting the following differences: The present invention compilation ingredients are similar except epinephrine (as the hydrochloride) 1:50,000 is omitted. Also, in the present invention the compilation is delivered intramuscularly in different dosage amounts and on a different dosage schedule. Further, the present invention compilation has a surprisingly different use. In the present invention, the compilation treats viral diseases whereas in U.S. Pat. No. 5,492,901 the compilation treats venomous toxin diseases.

Claim 1 of 8 Claims

I claim:

1. A method of treatment for human virus diseases in individuals infected with Dengue fever virus or influenza virus comprising administering to said individuals a liquid mixture of procaine hydrochloride and dexamethasone sodium phosphate.

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