WO2001028541A2 - Composition comprising sildenafil and l-arginine - Google Patents
Composition comprising sildenafil and l-arginine Download PDFInfo
- Publication number
- WO2001028541A2 WO2001028541A2 PCT/IL2000/000622 IL0000622W WO0128541A2 WO 2001028541 A2 WO2001028541 A2 WO 2001028541A2 IL 0000622 W IL0000622 W IL 0000622W WO 0128541 A2 WO0128541 A2 WO 0128541A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- sildenafil
- arginine
- composition
- treatment
- erectile dysfunction
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
Definitions
- the present invention relates to a Sildenafil preparation having an extended activity.
- the filling of the cavernous sinusoidal spaces is a tightly regulated process depending not merely on the inflow of penile arterial blood but also on the relaxation of the vascular smooth muscle cells of these sinusoidal spaces. This relaxation process is largely mediated by the local release of nitric oxide, i.e. of NO.
- Sildenafil is a type 5-CGMP phosphodiesterase inhibitor which has been approved for the treatment of erectile dysfunction of various etiologies of men.
- the preparation is administered orally usually about one hour prior to the intended intercourse and is effective for about 4 hours post-ingestion . It has been shown that doses of 25 -100 g are both efficacious and safe.
- Sildenafil-amplified erection depends on sexual arousal and neural transmission to the penis and subsides post-coitally .
- Sildenafil-assisted erection frees individuals from the embarassement of unwanted or protracted erection generated often by the use of alternative means such as of intravenous injection of vasoactive drugs or of external vacuum pumps.
- L-Arginine has a synergistic effect on the activity of Sildenafil in the treatment of erectile dysfunction.
- the present invention thus consists in a synergistic composition for the treatment of erectile dysfunction comprising suitable amounts of Sildenafil and of L-Arginine.
- the amounts of Sildenafil should be advantageously 25 - 100 mg and that of L-Arginine 0.5 - 1.5 g.
- composition according to the present invention may be in the form of oral dosage forms as tablets, coated tablets, dispersible tablets, effervescent tablets, capsules, granules, suspensions, solutions, etc. These compositions may be prepared common known techniques by common known techniques . Said compositions may contain in addition to the active ingredients excipients such as carriers, disentegrants , lubricants, stabilizers, flavoring agents, solvents, etc.
- composition according to the present invention may comprise both active ingredients in one dosage form or may be in two separate dosage forms. Both separate dosage forms, if present, should be administered together or within short intervals, preferably starting with the L-Arginine dosage form.
- the preferred composition comprises 100 mg of Sildenafil and 1 g of L-Arginine.
- the present invention also consists in the use of a syner- gistic composition comprising Sildenafil and L-Arginine for the treatment of erectile dysfunction.
- the present invention also consists in a method for the treatment of erectile dysfunction by administering a composition comprising Sildenafil and L-Arginine.
- Example 1 The people treated in the following Examples were treated also with certain amounts of L-Arginine. However there was shown no a low activity.
- Example 1 The people treated in the following Examples were treated also with certain amounts of L-Arginine. However there was shown no a low activity.
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Gynecology & Obstetrics (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
Claims
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU76826/00A AU7682600A (en) | 1999-10-19 | 2000-10-05 | Sildenafil preparation |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IL13246099A IL132460A0 (en) | 1999-10-19 | 1999-10-19 | Sildenafil preparation |
IL132460 | 1999-10-19 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2001028541A2 true WO2001028541A2 (en) | 2001-04-26 |
WO2001028541A3 WO2001028541A3 (en) | 2002-03-14 |
Family
ID=11073348
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IL2000/000622 WO2001028541A2 (en) | 1999-10-19 | 2000-10-05 | Composition comprising sildenafil and l-arginine |
Country Status (3)
Country | Link |
---|---|
AU (1) | AU7682600A (en) |
IL (1) | IL132460A0 (en) |
WO (1) | WO2001028541A2 (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005018620A2 (en) * | 2003-08-26 | 2005-03-03 | Cell Center Cologne Gmbh | Use of nitric oxide synthase (nos) cofactor for the treatment of sexual dysfunction |
WO2023152500A1 (en) * | 2022-02-09 | 2023-08-17 | Future Pharmtech Inc. | Combination of compounds for treating vascular diseases comprising pde5 inhibitor, arginine and n-acetylcysteine |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5958926A (en) * | 1996-11-01 | 1999-09-28 | Nitromed, Inc. | Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses |
WO1999051252A1 (en) * | 1998-04-03 | 1999-10-14 | The Daily Wellness Company | Compositions comprising l-arginine, ginseng and gingko biloba for enhancing blood circulation |
WO2000000212A1 (en) * | 1998-06-26 | 2000-01-06 | Nutracorp Scientific, Inc. | Promoting nitric oxide and cyclic gmp activity |
-
1999
- 1999-10-19 IL IL13246099A patent/IL132460A0/en unknown
-
2000
- 2000-10-05 WO PCT/IL2000/000622 patent/WO2001028541A2/en active Application Filing
- 2000-10-05 AU AU76826/00A patent/AU7682600A/en not_active Abandoned
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5958926A (en) * | 1996-11-01 | 1999-09-28 | Nitromed, Inc. | Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses |
WO1999051252A1 (en) * | 1998-04-03 | 1999-10-14 | The Daily Wellness Company | Compositions comprising l-arginine, ginseng and gingko biloba for enhancing blood circulation |
WO2000000212A1 (en) * | 1998-06-26 | 2000-01-06 | Nutracorp Scientific, Inc. | Promoting nitric oxide and cyclic gmp activity |
Non-Patent Citations (1)
Title |
---|
WALLACE, ARTHUR W. ET AL: "Interaction of L-arginine and phosphodiesterase inhibitors in vasodilatio of the porcine internal mammary artery" ANESTH. ANALG. (BALTIMORE) (2000), 90(4), 840-846 , 2000, XP001023695 * |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005018620A2 (en) * | 2003-08-26 | 2005-03-03 | Cell Center Cologne Gmbh | Use of nitric oxide synthase (nos) cofactor for the treatment of sexual dysfunction |
WO2005018620A3 (en) * | 2003-08-26 | 2005-07-28 | Cell Ct Cologne Gmbh | Use of nitric oxide synthase (nos) cofactor for the treatment of sexual dysfunction |
WO2023152500A1 (en) * | 2022-02-09 | 2023-08-17 | Future Pharmtech Inc. | Combination of compounds for treating vascular diseases comprising pde5 inhibitor, arginine and n-acetylcysteine |
Also Published As
Publication number | Publication date |
---|---|
IL132460A0 (en) | 2001-03-19 |
WO2001028541A3 (en) | 2002-03-14 |
AU7682600A (en) | 2001-04-30 |
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