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WO2007003204A1 - Topical formulation for the treatment of ano-rectal diseases - Google Patents

Topical formulation for the treatment of ano-rectal diseases Download PDF

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Publication number
WO2007003204A1
WO2007003204A1 PCT/EG2005/000031 EG2005000031W WO2007003204A1 WO 2007003204 A1 WO2007003204 A1 WO 2007003204A1 EG 2005000031 W EG2005000031 W EG 2005000031W WO 2007003204 A1 WO2007003204 A1 WO 2007003204A1
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
formulation
acetyl
topical pharmaceutical
ano
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/EG2005/000031
Other languages
French (fr)
Inventor
Mahmoud Timour Mohamed Radwan
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 WO2007003204A1 publication Critical patent/WO2007003204A1/en
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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/255—Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone

Definitions

  • the pharmaceutical forms of the above formula can be used in the form of cream, ointment , enema, paste.
  • Our new invention topical pharmaceutical formula made mainly from nutritional components with high safety profile with minimal side effects.
  • the new topical pharmaceutical formula used for medical treatment of hemorrhoid anal fissures, rectal fistula in the form of cream ointments, suppositories, enema, paste composed of: L- Cysteine ( from 2% to 20% ), N- Acetyl - D, L- Homocysteinethiolactone ( from 2% to 20% ), D- Panthenol ( from 1% to 10% ), Iodochlorhydroxylquin ( from 0.1% to 3% ), Lidocaine ( from 1 to 6% ), Hydrocortisone acetate ( from 0.5% to 3% ) .
  • L- Cysteine from 2% to 20%
  • N- Acetyl - D L- Homocysteinethiolactone
  • D- Panthenol from 1% to 10%
  • Iodochlorhydroxylquin from 0.1% to 3%
  • Lidocaine from 1 to 6%
  • Hydrocortisone acetate from 0.5% to 3%
  • N- Acetyl - D, L- Homocysteinethio lactone & L- Cysteine activate various essential enzymatic systems of the vital cells especially the cells whose damaged by infectious or toxic substances results in necrosis.
  • the above two amino acids have preventive curative anti necrotic action also they act as physiological carriers of sulfhydryl groups so they are of decisive importance to various intermediary processes of the metabolism and for the maintenance of redox potential. They have detoxicating influence and antiallergic influence.
  • the above two amino acids potentiat the blood circulation and relief ischemia in this area.
  • D- Panthenol have an important role in healing of tissues and is easily absorbed to make the skin and soft tissues soft , clean, moist.
  • D-Panthenol increases the absorption of the above amino acid so increase the bioavailability of the active ingredients so increases the therapeutic effect.
  • Iodochlorhydroxy quin is an antibacterial anti fungal.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The present invention refers to a topical pharmaceutical formulation in the form of a cream, a ointment, suppositories, a paste, an enema, respectively, useful for the treatment of hemorrhoids and anal fistula resp. fissures. Said formulation is composed of D-panthenol, L- cysteine, N-acetyl-D, L-homocystein thiolactone, hydrocortisone acetate, iodochlorhydroxyquin and lidocaine. The above formulation has the following pharmacological actions: It activates various essential enzymatic systems especially on the cells whose damaged. It shows a preventive curative anti-necrotic action and maintains the redox potential. The formulation has a detoxicating and anti-allergic influence. The formulation has an anti-bacterial, an anti-fungal and a local anesthetic action.

Description

A NEW PHARMACEUTICAL FORMULA FOR TREATMENT OF ANO-RECTAL DISEASES
Technical Field:
Pharmaceutical formula for medical treatment of Ano-rectal diseases this topical pharmaceutical formula used in the treatment of external and internal hemorrhoids with all degrease & treatment of low and high rectal fistula also used in the treatment of anal fissures
The pharmaceutical forms of the above formula can be used in the form of cream, ointment , enema, paste.
Background Art
The most topical pharmaceutical preparations present the market of pharmacy present now used for symptomatic relief of the anorectal diseases so this preparations contains antiallergic, antipruritic, anti-inflammatory, Vasoconstrictors, astringent, anti
Bacterial, demulcent etc.
Example .Bismuth sub Gallat 2.25% , Zinc Oxide 10.75%, Balsam Peru 1.87%, Bismuth Oxide 0.87%.
All the above chemical substances have soothing, astringent effect for treatment simple anorectal inflammations and irritations it relives hemorrhoid pain.
Our new invention topical pharmaceutical formula made mainly from nutritional components with high safety profile with minimal side effects.
Our new topical pharmaceutical formula used not only for symptomatic relive of the above anorectal diseases but also it use for complete treatment of this diseases. Disclosure of the Invention
The new topical pharmaceutical formula used for medical treatment of hemorrhoid anal fissures, rectal fistula in the form of cream ointments, suppositories, enema, paste. This formula composed of: L- Cysteine ( from 2% to 20% ), N- Acetyl - D, L- Homocysteinethiolactone ( from 2% to 20% ), D- Panthenol ( from 1% to 10% ), Iodochlorhydroxylquin ( from 0.1% to 3% ), Lidocaine ( from 1 to 6% ), Hydrocortisone acetate ( from 0.5% to 3% ) . Properties:
Our topical pharmaceutical formula affords prompt relief from unpleasant symptoms of hemorrhoid, Anal fissures, rectal fistula i.e pain smarting, itching, skin tension. The properties of each above substances in our formula:
A. N- Acetyl - D, L- Homocysteinethio lactone & L- Cysteine activate various essential enzymatic systems of the vital cells especially the cells whose damaged by infectious or toxic substances results in necrosis. So the above two amino acids have preventive curative anti necrotic action also they act as physiological carriers of sulfhydryl groups so they are of decisive importance to various intermediary processes of the metabolism and for the maintenance of redox potential. They have detoxicating influence and antiallergic influence. The above two amino acids potentiat the blood circulation and relief ischemia in this area. B. D- Panthenol have an important role in healing of tissues and is easily absorbed to make the skin and soft tissues soft , clean, moist.
Also D-Panthenol increases the absorption of the above amino acid so increase the bioavailability of the active ingredients so increases the therapeutic effect.
C. Hydrocortisone used as anti inflammatory and allergic and Antipruritic.
D. Iodochlorhydroxy quin is an antibacterial anti fungal.
E. Lidocaine is along active local anesthetic. Indications:
Treatment of external & internal hemorrhoids with different degrees & anal fissures & low and high rectral fistula also used as prophylaxis between attack to prevent recurrences. In hemorrhoidal complication like anal purities pre-operative and post-operative treatments of hemorrhoid ectomy.

Claims

1 - A new topical pharmaceutical formula composition with ranges of concentration of each component: L-Cysteine ( from 2% to 20%), N-acetyl - D5L- Homocysteine thiolactone (from 2% to 20%) , D-Panthenol (from 1% to 10%), Hydrocortisone acetate (from 0.5% to 3%), Iodochlorohydroxyqin (from 0.1% to 3%), Lidocaine (from 1% to 6%).
2- As in number (1 ) the use of the upper topical pharmaceutical formula the uses for treatment of external and internal hemorrhoids with deferent degrees & the treatment of low and high rectal fistula & in the treatment of anal fissures.
3- As in number (1 ) the new topical use of L-Cystein & N-Acetyl - D5L- Homocysteinethiolactone in concentration ranges (from 2% to 20% ) in anorectal area.
4- As in number (1) the use of upper pharmaceutical formula in the form of cream, ointment, suppositories, enema, paste.
PCT/EG2005/000031 2005-07-06 2005-09-25 Topical formulation for the treatment of ano-rectal diseases Ceased WO2007003204A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EG2005070314 2005-07-06
EG2005070314 2005-07-06

Publications (1)

Publication Number Publication Date
WO2007003204A1 true WO2007003204A1 (en) 2007-01-11

Family

ID=37604093

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EG2005/000031 Ceased WO2007003204A1 (en) 2005-07-06 2005-09-25 Topical formulation for the treatment of ano-rectal diseases

Country Status (1)

Country Link
WO (1) WO2007003204A1 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105939719A (en) * 2013-10-30 2016-09-14 格摩丹有限责任公司 Agent in suppository form for treatment of haemorrhoids, proctitis and other inflammatory proctological disorders
US11865207B2 (en) 2018-04-25 2024-01-09 Ferring B.V. Topical pharmaceutical composition for treatment of anal fissures and hemorrhoids

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0692833A (en) * 1991-12-27 1994-04-05 Shiseido Co Ltd Skin external agent
US20050090553A1 (en) * 1992-06-30 2005-04-28 Shapiro Howard K. Compositions and method for treatment of chronic inflammatory diseases

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0692833A (en) * 1991-12-27 1994-04-05 Shiseido Co Ltd Skin external agent
US20050090553A1 (en) * 1992-06-30 2005-04-28 Shapiro Howard K. Compositions and method for treatment of chronic inflammatory diseases

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DATABASE MEDLINE [online] MARIGLIANO F.: "Results in using the combination corticosteroid and iodochlorhydroxyquinoline in proctology", XP003006625, Database accession no. (NLM4242960) *
DATABASE MEDLINE [online] NEIGER A. ET AL.: "The symptomatic therapy of hemorrhoids and anal eczema - a report of experiences from proctology practice", XP003006626, Database accession no. (NLM2392628) *
HOSPITAL, vol. 72, no. 5, November 1967 (1967-11-01), pages 1551 - 1554 *
SCHWEIZERISCHE RUNDSCHAU FUER MEDIZIN, vol. 79, no. 31-32, 2 August 1990 (1990-08-02), pages 918 - 920 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105939719A (en) * 2013-10-30 2016-09-14 格摩丹有限责任公司 Agent in suppository form for treatment of haemorrhoids, proctitis and other inflammatory proctological disorders
US20160271080A1 (en) * 2013-10-30 2016-09-22 Obschestvo S Ogranichennoi Otvetstvennostyu "Gemodan" Agent in suppository form for the treatment of haemorrhoids, proctitis and other inflammatory proctological disorders
EP3064210A4 (en) * 2013-10-30 2017-07-12 Obschestvo S Ogranichennoi Otvetstvennostyu "Gemodan" Agent in suppository form for the treatment of haemorrhoids, proctitis and other inflammatory proctological disorders
US11865207B2 (en) 2018-04-25 2024-01-09 Ferring B.V. Topical pharmaceutical composition for treatment of anal fissures and hemorrhoids

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