WO2006110120A1 - Produit de traitement du dysfonctionnement erectile chez l'homme - Google Patents

Produit de traitement du dysfonctionnement erectile chez l'homme Download PDF

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Publication number
WO2006110120A1
WO2006110120A1 PCT/UA2006/000021 UA2006000021W WO2006110120A1 WO 2006110120 A1 WO2006110120 A1 WO 2006110120A1 UA 2006000021 W UA2006000021 W UA 2006000021W WO 2006110120 A1 WO2006110120 A1 WO 2006110120A1
Authority
WO
WIPO (PCT)
Prior art keywords
sildenafil
erectile dysfunction
triglyconate
treatment
erection
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/UA2006/000021
Other languages
English (en)
Russian (ru)
Inventor
Victor Pavlovich Kutnyak
Vadym Alekseyevich Kozlovskiy
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of WO2006110120A1 publication Critical patent/WO2006110120A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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 invention relates to a high-quality composition for the treatment of erectile dysfunction in men.
  • State of the art
  • impotence means any pathological violation of male sexuality, for example, flaccid erection, rapid ejaculation, lack of orgasm, etc. It is clear that the causes and manifestations of impotence are very diverse and that its causal treatment should be aimed at eliminating identified lesions.
  • sildenafil citrate as such has a rather low bioavailability. So, depending on the filling of the patient’s stomach and the acidity of the gastric juice, only from 40 to 60% of the oral dose is absorbed. Since the path from the digestive tract to the bloodstream is quite long, the waiting period for an erection is rarely less than 40 minutes, which is very inconvenient.
  • the use of high (usually at least 50 mg) single doses of the active substance to compensate for these deficiencies causes many side effects in many patients, such as headache (from 17 to 30%), dyspepsia (from 17 to 20%), and impaired color perception (from 9 up to 11%) (Mosbu's CD, 2000).
  • the invention is based on the task of creating a qualitative composition by creating O based on sildenafil is a more bioavailable treatment for erectile dysfunction, which would provide a therapeutic effect even in relatively small doses.
  • sildenafil triglyconate as a means for the treatment of erectile dysfunction.
  • sildenafil triglyconate stimulates an erection when used in significantly lower doses than sildenafil citrate.
  • the attached graph shows the dilator response of the strips excised from the rat aorta to the effect of sildenafil triglyconate and sildenafil citrate.
  • sildenafil triglyconate was obtained: either from sildenafil in the form of a base — by adding gluconic acid to its aqueous-alcohol solution (at the rate of 3 moles of gluconate anions per 1 mole of sildenafil) with further evaporation of the solvents under vacuum and drying of the target product in vacuum a desiccator over dispersed calcium oxide, or either from sildenafil citrate available on the pharmaceutical market by adding an appropriate amount of sodium (or potassium) gluconate to its water-alcohol solution and zhnym stirring the reaction mixture until the precipitate of sodium citrate (or potassium). After that, the precipitate was separated by filtration, and the target product was isolated from the filtrate, as described above.
  • potassium chloride was introduced into the solution at a concentration of 10 "6 mM / L, which resulted in a reduction (spasm) of the vessel.
  • sildenafil triglyconate was introduced into the perfusion solution at a concentration of 10 " 4 mm / l and recorded relaxation of the vessel by 80% relative to the original length, which indicates a pronounced dilator effect of the agent according to the invention.
  • sildenafil citrate was introduced into the perfusion solution at a concentration of 10 " 4 mM / L and recorded relaxation of the vessel by 52% relative to the original length. This is significantly less than with sildenafil triglyconate.
  • sildenafil has long and successfully been used in direct (as a cardiotropic) and in “other” prescribing (as the basis for the treatment of erectile dysfunction). Therefore, its single introduction into the human body in a therapeutically acceptable dose can be considered practically harmless.
  • gluconate anions are included in many medicines, for example: calcium gluconate, which is widely available in pharmacies, and in an antiarrhythmic drug in the form of a mixture of potassium and magnesium gluconates, for which Russian patents Ns 2,223,759 and Ukraine N ° 72,317 are issued. , this drug is approved for clinical use in Ukraine and is available to patients under the RITMOCOR® brand name.
  • Example 1 Patient M., 55 years old, 3 years old suffered from erectile dysfunction, and therefore repeatedly sought medical help. He was diagnosed with erectile dysfunction and was recommended to take sildenafil citrate before coitus.
  • Example 2 Patient K-in, 62 years old, 5 years old suffered from erectile dysfunction. For 2 years, he took sildenafil citrate in a single dose of 0.05 g before sexual intercourse. In this case, after taking a very severe headache, requiring the use of analgesics. The patient expressed a desire to use sildenafil triglyconate tablets. Oral administration of sildenafil trigluconate tablets in a single dose of 0.025 g 10 minutes before each coitus with adequate sexual stimulation caused a sufficient erection. A side effect in the form of a headache was not observed.
  • Example 3 Patient Ks, 42 years old, 5 years old suffered from erectile dysfunction. During these 5 years I took sildenafil citrate in a single dose of 0.1 g before coition, which was possible no earlier than 40-50 minutes after taking the drug.
  • the data presented indicate a high bioavailability of sildenafil triglyconate.
  • the agent according to the invention can be used for the treatment of erectile dysfunction in the form of tablets taken peraso or predominantly sublingually (sublingually), as well as in the form of inhaled aerosols, spray, capsules, drops, injections, transdermal or urethral applications and rectal suppositories.
  • the agent according to the invention can be easily manufactured industrially and used for the effective treatment of erectile dysfunction in doses substantially lower than sildenafil citrate.
  • experimental data indicate that, depending on the concentration used, sildenafil triglyconate is more than 50% more effective than sildenafil citrate.

Landscapes

  • 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention concerne l'utilisation de trigluconate sildénafile comme produit de traitement du dysfonctionnement érectile chez l'homme.
PCT/UA2006/000021 2005-04-15 2006-04-12 Produit de traitement du dysfonctionnement erectile chez l'homme Ceased WO2006110120A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
UAA200503574 2005-04-15
UAA200503574A UA84688C2 (uk) 2005-04-15 2005-04-15 Засіб для лікування еректильної дисфункції

Publications (1)

Publication Number Publication Date
WO2006110120A1 true WO2006110120A1 (fr) 2006-10-19

Family

ID=37087314

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/UA2006/000021 Ceased WO2006110120A1 (fr) 2005-04-15 2006-04-12 Produit de traitement du dysfonctionnement erectile chez l'homme

Country Status (2)

Country Link
UA (1) UA84688C2 (fr)
WO (1) WO2006110120A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0463756A1 (fr) * 1990-06-20 1992-01-02 Pfizer Limited Pyrazolopyrimidones comme agents antiangineux
RU2130776C1 (ru) * 1993-06-09 1999-05-27 Пфайзер Рисерч Энд Дивелопмент Компани Н.В./С.А. Пиразолпиримидиноны для лечения импотенции

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0463756A1 (fr) * 1990-06-20 1992-01-02 Pfizer Limited Pyrazolopyrimidones comme agents antiangineux
RU2130776C1 (ru) * 1993-06-09 1999-05-27 Пфайзер Рисерч Энд Дивелопмент Компани Н.В./С.А. Пиразолпиримидиноны для лечения импотенции

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
DATABASE MEDLINE [online] DEVECI S. ET AL.: "Sublingual sildenafil in the treatment of erectile dysfunction: faster onset of action with less dose", Database accession no. (15509203) *
DATABASE MEDLINE [online] DOGGRELL S.A.: "Comparison of clinica trials with sildenafil, vardenafil and tadalafil in erectile dysfunction", Database accession no. (15709885) *
EXPERT OPIN. PHARMACOTHER., vol. 6, no. 1, January 2005 (2005-01-01), pages 75 - 84 *
INT. J. UROL., vol. 11, no. 1, November 2004 (2004-11-01), pages 989 - 992 *
MIKHAILOV I.B.: "Natolnaya kniga po klinicheskoi farmakologii S-Pb", FOLIANT, 2001, pages 591 - 592 *
REGISTR LEKARSTVENNYKH SREDSTV ROSSII. ENTSIKLOPEDIYA LEKARSTV M., 2000, pages: 788 - 789 *

Also Published As

Publication number Publication date
UA84688C2 (uk) 2008-11-25

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