Pharmaceutical formulations and methods for treating patients suffering from diseases that cause muscular hypotonia

• US 5,738,873 A
• Filed: 09/27/1996
• Issued: 04/14/1998
• Est. Priority Date: 09/27/1996
• Status: Expired due to Fees

• Current Assignee: Bleiweiss; Daniel Gustavo , Bleiweiss; Eduardo Samuel , Daniel Gustavo Bleiweiss, Eduardo Samuel Bleiweiss, Herman Bleiweiss
• Original Assignee: Daniel Gustavo Bleiweiss, Eduardo Samuel Bleiweiss, Herman Bleiweiss
• Inventors: Bleiweiss, Herman, Bleiweiss, Eduardo Samuel, Bleiweiss, Daniel Gustavo
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Benston, Jr., William E.
• Application Number:
  US08/720,354
• Time in Patent Office: 564 Days
• Field of Search: 424/464, 424/465, 514/159, 435/182
• US Class Current: 424/464
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 31/375 Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/455 Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61K 33/00 Medicinal preparations containing inorganic active ingredients
• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Formulations are provided for the treatment of patients suffering from disorders that have in common the appearance of muscular hypotonia as a symptom. These disorders include Alzheimer'"'"'s type diseases, atrophy of the brain, atrophy of the cerebellum, Fragile X syndrome, mental retardation of unknown causes, multiple anomalies in the chromosomes, deletions in one or more chromosome, and fragility in a chromosome other than the X chromosome. The formulations of the invention contain therapeutically effective amounts of gamma amino butyric acid (GABA), an anti-oxidant (such as ascorbic acid and/or vitamin E), folic acid, nicotinamide, and a lithium salt, all in a pharmaceutically acceptable excipient. Methods for the treatment of these disorders by the administration of such formulations are also provided.

Claims

1. A pharmaceutical formulation for the treatment of a disorder having muscular hypotonia as a symptom, selected from the group of an Alzheimer'"'"'s disease, atrophy of the brain, atrophy of the cerebellum, Fragile X syndrome, mental retardation of unknown causes, multiple anomalies in the chromosomes, deletion in one or more chromosome, and fragility in a chromosome other than the X chromosome, said formulation comprising non toxic quantities of the following components in a pharmaceutically acceptable excipient:

a. about 0.05 to about 200 mg of gamma amino burytic acid (GABA);

b. about 50 to about 300 mg of an antioxidant selected from the group consisting of vitamin E, ascorbic acid, and mixtures thereof;

c. about 100 to about 300 mg of folic acid;

d. about 0.05 to about 0-5 mg of a nicotinamide selected from the group consisting of nicotinamide and pharmaceutically acceptable salts thereof; and

e. about 25 to about 100 mg of a lithium salt selected from the group consisting of lithium carbonate, lithium bromide, lithium chloride, and lithium acetate.

2. The pharmaceutical formulation of claim 1 wherein said antioxidant and said nicotinamide are present as ascorbate nicotinamide.

3. The pharmaceutical formulation of claim 1 wherein said formulation is further processed into a dosage form selected from the group consisting of tablets, pills, powders, coated pills, water capsules, elixirs, suspensions, emulsions, solutions, and syrups.

4. The formulation of claim 1 wherein said excipient is selected from the group consisting of lactose, dextrose, saccharose, sorbitol, mannitol, starches, gum arabic, calcium phosphate, algins, tragacanth, gelatin, calcium silicate, micro-crystalline cellulose, polyvinylpyrrolidone, cellose, water, syrup, methyl cellulose, and mixtures of any of the forgoing.

5. The formulation of claim 1 further comprising one or more agents selected from the group consisting of lubricating, humectant, emulgent, and suspending agents.

6. The formulation of claim 1 further comprising a lubricating agent selected from the group consisting of talcum powder, magnesium stearate and mineral oil.

7. The pharmaceutical formulation of claim 1 wherein said non-toxic quantities of said components are:

a. about 100 mg of gama amino butyric acid (GABA);

b. antioxidant, comprising a mixture of about 150 mg of vitamin E and about 0.5 mg of ascorbic acid;

c. about 200 mg of folic acid;

d. about 0.1 mg of nicotinamide; and

e. about 50 mg of lithium carbonate.

8. The pharmaceutical formulation of claim 1 wherein said non-toxic quantities of said components are:

a. about 0.100 mg of gamma amino butyric acid;

b. about 200 mg of an antioxidant selected from the group of ascorbic acid, vitamin E and mixtures thereof;

c. about 200 mg of folic acid;

d. about 0.1 mg of nicotinamide; and

e. about 50 mg of lithium carbonate.

9. A method for the treatment of a patient suffering from a disorder having muscular hypotonia as a symptom, said disorder selected from the group of an Alzheimer'"'"'s disease, atrophy of the brain, atrophy of the cerebellum, Fragile X syndrome, mental retardation of unknown causes, multiple anomalies in the chromosomes, deletion in one or more chromosome, and fragility in a chromosome other than the X chromosome, said method comprising administering daily to said patient about one half (1/2) to about four (4) dosage units of the pharmaceutical formulation of claim 7.

10. The method of claim 1, wherein said therapeutically effective daily dosages are:

a. about 0.100 mg of gamma amino butyric acid;

b. about 200 mg of an antioxidant selected from the group of ascorbic acid, vitamin E and mixtures thereof;

c. about 200 mg of folic acid;

d. about 0.1 mg of nicotinamide;

e. about 50 mg of lithium carbonate.

11. A method for the treatment of a patient suffering from a disorder having muscular hypotonia as a symptom, said disorder selected from the group of an Alzheimer'"'"'s disease, atrophy of the brain, atrophy of the cerebellum, Fragile X syndrome, mental retardation of unknown causes, multiple anomalies in the chromosomes, deletion in one or more chromosome, and fragility in a chromosome other than the X chromosome, said method comprising administering to said patient therapeutically effective daily dosages of the following components:

a. about 0.05 to about 200 mg of gamma amino burytic acid (GABA);

b. about 50 to about 300 mg of an antioxidant selected from the group consisting of vitamin E, ascorbic acid, and mixtures thereof;

c. about 100 to about 300 mg of folic acid;

d. about 0.05 to about 0.5 mg of a nicotinamide selected from the group consisting of nicotinimide and pharmaceutically acceptable salts thereof;

e. about 25 to about 100 mg of a lithium salt selected from the group consisting of lithium carbonate, lithium bromide, lithium chloride, and lithium acetate.

12. A method for the treatment of a patient suffering from a disorder having muscular hypotonia as a symptom, said disorder selected from the group of an Alzheimer'"'"'s disease, atrophy of the brain, atrophy of the cerebellum, Fragile X syndrome, mental retardation of unknown causes, multiple anomalies in the chromosomes, deletion in one or more chromosome, and fragility in a chromosome other than the X chromosome said method comprising administering to said patient therapeutically effective daily dosages of the following components:

about 50 to about 400 mg of gamma amino burytic acid (GABA);

b. about 75 to about 600 mg of the antioxidant vitamin E and about 0.25 to 2.0 mg of the antioxidant ascorbic acid;

c. about 100 to about 800 mg of folic acid;

d. about 0.05 to about 0°

4 mg of nicotinamide;

e. about 25 to about 100 mg of lithium carbonate.