Pharmaceutical Compositions for Intranasal Administration for the Treatment of Neurodegenerative Disorders

• US 20120322727A1
• Filed: 06/15/2012
• Published: 12/20/2012
• Est. Priority Date: 06/15/2011
• Status: Active Grant

• Current Assignee: Nerve Access Incorporated
• Original Assignee: Nerve Access Incorporated
• Inventors: Abdel Maksoud, Yaser A., Maher, Mustafa A.
• Granted Patent: US 8,987,199 B2
• Time in Patent Office: Days
• US Class Current: 514/6.5
• 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 31/47 Quinolines; Isoquinolines
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• 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

Abstract

In one embodiment of the invention, a pharmaceutical composition for intranasal administration comprises insulin, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. In another embodiment of the invention, a pharmaceutical composition for intranasal administration comprises clioquinol, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. In yet another embodiment of the invention, a pharmaceutical composition for intranasal administration comprises insulin, clioquinol, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. The pharmaceutical compositions of the invention may be used to treat or prevent a neurodegenerative disorder such as Alzheimer'"'"'s disease, stroke, Parkinson'"'"'s disease, multiple sclerosis, spinal cord injuries, and/or traumatic brain injuries and the like, in addition to other systemic and local diseases.

Claims

1. A pharmaceutical composition for intranasal administration, comprising an effective amount of insulin, dimethyl sulfoxide, and a pharmaceutically acceptable excipient.

2. The composition of claim 1, wherein the pharmaceutically acceptable excipient is selected from the group consisting of polyethylene glycol, glycerin, and phenol.

3. The composition of claim 1, wherein the composition comprises insulin, dimethyl sulfoxide, polyethylene glycol, glycerin, and phenol.

4. The composition of claim 3, comprising:

insulin present in an amount from about 400 IU/mL to about 600 IU/mL;

dimethyl sulfoxide present in an amount from about 24% (v/v) to about 36% (v/v);

polyethylene glycol present in an amount from about 1.6% (v/v) to about 2.4% (v/v);

glycerin present in an amount from about 1.2% (v/v) to about 1.8% (v/v); and

phenol present in an amount from about 0.05% (v/v) to about 0.15% (v/v).

5. The composition of claim 4, comprising about 500 IU/mL insulin, about 30% (v/v) dimethyl sulfoxide, about 2% (v/v) polyethylene glycol, about 1.5% (v/v) glycerin, and about 0.1% (v/v) phenol.

6. A method of treating a neurodegenerative disorder in a patient, comprising intranasally administering the composition of claim 1 to the patient.

7. A pharmaceutical composition for intranasal administration, comprising an effective amount of clioquinol, dimethyl sulfoxide, and a pharmaceutically acceptable excipient.

8. The composition of claim 7, wherein the pharmaceutically acceptable excipient is selected from the group consisting of polyethylene glycol, propylene glycol, glycerin, boric acid, and sodium bicarbonate.

9. The composition of claim 7, wherein the composition comprises clioquinol, dimethyl sulfoxide, polyethylene glycol, propylene glycol, glycerin, boric acid, and sodium bicarbonate.

10. The composition of claim 9, comprising:

clioquinol present in an amount from about 2.4% (w/v) to about 3.6% (w/v);

dimethyl sulfoxide present in an amount from about 34% (v/v) to about 52% (v/v);

polyethylene glycol present in an amount from about 5.4% (v/v) to about 8.0% (v/v);

propylene glycol present in an amount from about 5.4% (v/v) to about 8.0% (v/v);

glycerin present in an amount from about 21% (v/v) to about 33% (v/v);

boric acid present in an amount from about 0.13% (w/v) to about 0.21% (w/v); and

sodium bicarbonate present in an amount from about 0.24% (w/v) to about 0.36% (w/v).

11. The composition of claim 10, comprising about 3% (w/v) clioquinol, about 43% (v/v) dimethyl sulfoxide, about 6.7% (v/v) polyethylene glycol, about 6.7% (v/v) propylene glycol, about 27% (v/v) glycerin, about 0.17% (w/v) boric acid, and about 0.3% (w/v) sodium bicarbonate.

12. A method of treating a neurodegenerative disorder in a patient comprising intranasally administering the composition of claim 7 to the patient.

13. A pharmaceutical composition for intranasal administration, comprising an effective amount of insulin, clioquinol, dimethyl sulfoxide, and a pharmaceutically acceptable excipient.

14. The composition of claim 13, wherein the pharmaceutically acceptable excipient is selected from the group consisting of polyethylene glycol, propylene glycol, glycerin, phenol, boric acid, and sodium bicarbonate.

15. The composition of claim 13, wherein the composition comprises insulin, clioquinol, dimethyl sulfoxide, polyethylene glycol, propylene glycol, glycerin, phenol, boric acid, and sodium bicarbonate.

16. The composition of claim 15, comprising:

insulin present in an amount from about 400 IU/mL to about 600 IU/mL;

clioquinol present in an amount from about 2.4% (w/v) to about 3.6% (w/v);

dimethyl sulfoxide present in an amount from about 34% (v/v) to about 52% (v/v);

polyethylene glycol present in an amount from about 5.4% (v/v) to about 8.0% (v/v);

propylene glycol present in an amount from about 5.4% (v/v) to about 8.0% (v/v);

glycerin present in an amount from about 21% (v/v) to about 33% (v/v);

phenol present in an amount form about 0.05% (v/v) to about 0.15% (v/v);

boric acid present in an amount from about 0.13% (w/v) to about 0.21% (w/v); and

sodium bicarbonate present in an amount from about 0.24% (w/v) to about 0.36% (w/v).

17. The composition of claim 16, comprising about 500 IU/mL insulin, about 3% (w/v) clioquinol, about 43% (v/v) dimethyl sulfoxide, about 6.7% (v/v) polyethylene glycol, about 6.7% (v/v) propylene glycol, about 27% (v/v) glycerin, about 0.1% (v/v) phenol, about 0.17% (w/v) boric acid, and about 0.3% (w/v) sodium bicarbonate.

18. A method of treating a neurodegenerative disorder in a patient, comprising intranasally administering the composition of claim 13 to the patient.