Composition and method of use in treating sexual dysfunction using cGMP-specific phosphodiesterase type 5 inhibitors

• US 6,338,862 B1
• Filed: 03/26/2001
• Issued: 01/15/2002
• Est. Priority Date: 03/26/2001
• Status: Expired due to Term

• Current Assignee: Noven Pharmaceuticals Inc (Hisamitsu Pharmaceutical Company Incorporated), PBN Pharma LLC
• Original Assignee: Noven Pharmaceuticals Inc (Hisamitsu Pharmaceutical Company Incorporated)
• Inventors: Niazi, Sarfaraz K
• Primary Examiner(s): Tate, Christopher R.
• Assistant Examiner(s): WINSTON, RANDALL O
• Application Number:
  US09/681,362
• Time in Patent Office: 295 Days
• Field of Search: 424/728, 424/725, 514/565
• US Class Current: 424/728
• 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 31/4415 Pyridoxine, i.e. Vitamin B6 pyridoxal phosphate A61K31/675
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/714 Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
• CPC Class Codes: A61K 36/258 Panax (ginseng)
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The inhibitors of cyclic guanosine monophosphate (cGMP) phosphodiesterases type 5 (cGMP-PDE5) such as sildenafil citrate (Viagra®) act by increasing the level of cGMP in sexual organs to produce enhanced blood flow and an erectile response of sexual organs. Though sildenafil citrate is a specific inhibitor of cGMP-PDE5, its effects on other body organs produce many side effects including fatalities. Described here is a method of combining cGMP-PDE5 inhibitors with natural sources of nutrients that instantly enhance the levels of endogenous cGMP and thus reduce the therapeutic dose and therefore the side effects of cGMP-PDE5 inhibitors. We have discovered that if sildenafil citrate, as a prototype of cGMP-PDE5, is combined with L-arginine, ginseng, vitamin B6, vitamin B12, and folic acid, all natural and safe ingredients, the dose requirements for sildenafil citrate can be reduced substantially. The specific composition described here assists in the action of sildenafil primarily by increasing the production of cGMP through modulation of nitric oxide pathway (L-arginine→nitric oxide→cGMP) and secondarily by having its own effect on improving blood circulation to sexual organs.

Claims

1. A composition for treating sexual dysfunction comprising effective amounts of an inhibitor of cGMP-specific phosphodiesterase type 5 enzyme, a natural amino acid, ginseng, vitamin B6, vitamin B12 and folic acid.

2. The composition as in claim 1 wherein each of the component of the composition is administered in a separate dosage form.

3. The composition as in claim 1 wherein the inhibitor of cGMP specific phosphodiestrase type 5 is sildenafil citrate or any of its other salt forms.

4. The composition as in claim 1 wherein the natural amino acid is L-arginine.

5. The composition as in claim 1 wherein the natural amino acid is present in the dose range of 100 to 1000 mg.

6. The composition as in claim 1 wherein vitamin B6 is present in the dose range of 50 to 250 mg.

7. The composition as in claim 1 wherein vitamin B12 is present in the dose range of 0.5 to 1.0 mg.

8. The composition as in claim 1 wherein folic acid is present in the dose range of 0.4 to 10 mg.

9. The composition as in claim 1 wherein ginseng represents extract of Ginseng Panax.

10. The composition as in claim 1 wherein ginseng is present in the dose range of 50 to 200 mg.

11. The composition as in claim 1 which consists of: