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WO2019150173A1 - Tibo (topical innovative burn ointment) - Google Patents

Tibo (topical innovative burn ointment) Download PDF

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Publication number
WO2019150173A1
WO2019150173A1 PCT/IB2018/050695 IB2018050695W WO2019150173A1 WO 2019150173 A1 WO2019150173 A1 WO 2019150173A1 IB 2018050695 W IB2018050695 W IB 2018050695W WO 2019150173 A1 WO2019150173 A1 WO 2019150173A1
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
verapamil
topical
healing
inflammation
Prior art date
Application number
PCT/IB2018/050695
Other languages
French (fr)
Inventor
Ranim SHARTOUNI
Original Assignee
Shartouni Ranim
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 Shartouni Ranim filed Critical Shartouni Ranim
Publication of WO2019150173A1 publication Critical patent/WO2019150173A1/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/44221,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7135Compounds containing heavy metals

Definitions

  • the present invention relates to the treatment of burns including ointments and other topical preparations and formulations useful for the delivery of medicaments.
  • ointment base that can be used as a vehicle for a wide variety of medicaments and with a broad range of medicament volumes and concentrations.
  • the ointment base of the present invention is prepared using a combination of commonly available ingredients identified as “generally recognized as safe” (“GRAS").
  • GRAS generally recognized as safe
  • the term “ointment base” refers to a mixture of ingredients of the final formulation other than the medicament solution which will allow the topically applicable formulations to be efficacious and have a proper time-release manner.
  • medicament solution it refers to the active agent or any other agent to be delivered dermatologically, in whatever vehicle or form used to combine it with the ointment base.
  • formulation refers to the combination of the ointment base and one or more medicament solutions to create the desired topical treatment.
  • the degree of thermal damage is characterized by the zones of coagulation, stasis and hyperaemia.
  • the zone of coagulation is where all the tissue is damaged but the pathophysiological changes in the zone of hyperaemia are spontaneously reversible.
  • the zone of stasis although not immediately destroyed, converts to necrosis during the first week after injury owing to a fatal combination of several factors.
  • the healing of a burn wound proceeds from the zone of hyperaemia and follows the same course as in a surgical wound. Modifications of the healing process are produced by the graded nature of the thermal injury and by the presence of coagulated tissue acting as a foreign body.
  • Burn wound depth is an important determinant of patient morbidity and mortality. Therefore, reduction or even the prevention of secondary burn wound progression is one goal of the acute care of burned patients.
  • Second Degree Burns They are also called superficial burns; they cause minimal skin damage. Signs and symptoms include:
  • Second Degree Burns They are also called partial thickness burns; these affect the epidermis and dermis. Signs and symptoms include:
  • Verapamil a Calcium-Channel Blocker, Improves the Wound Healing Process in Rats with Excisional Full-Thickness Skin Wounds Based on Stereological Parameters. https://www.ncbi.nlm.nih.gov/pubmed/27429235

Landscapes

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

Abstract

The treatment proposed by this invention is focusing on: - Reducing: pain, inflammation, and infection - Promoting healing process It Consists of: - Isopropyl Myristate, NF (Cosmetic Grade) 532 mL - Lidocaine 2% - Bismuth Salicylates 50 mg - Teicoplanin (Targocid) 400 mg - Verapamil HCl 4.8g Method: After irrigation of the burned area with normal saline and sterilization with povidone iodine solution, the ointment is put on a sterilized gauze and used to cover the burned area, then a dressing is made Q.O.D. (every other day). Results should begin to appear starting from one week after the initiation of the treatment, showing the following: - Safety, efficacy, and gentleness - Enhancement of tissue healing - Antimicrobial Effectiveness - Efficacy for burn related pain - Healing of inflammation - Prevention and treatment of Scars formation.

Description

TIBO
TOPICAL INNOVATIVE BURN OINTMENT
Ointment for Burns (first and second degrees burns)
The present invention relates to the treatment of burns including ointments and other topical preparations and formulations useful for the delivery of medicaments.
This provides an ointment base that can be used as a vehicle for a wide variety of medicaments and with a broad range of medicament volumes and concentrations. The ointment base of the present invention is prepared using a combination of commonly available ingredients identified as "generally recognized as safe" ("GRAS"). The term “ointment base” refers to a mixture of ingredients of the final formulation other than the medicament solution which will allow the topically applicable formulations to be efficacious and have a proper time-release manner. As for the term "medicament solution", it refers to the active agent or any other agent to be delivered dermatologically, in whatever vehicle or form used to combine it with the ointment base. Lastly, the word "formulation” refers to the combination of the ointment base and one or more medicament solutions to create the desired topical treatment.
Innovative treatment for first and second degrees burns
To give an effective management for burns, the pathophysiology of the injury must be well understood.
The degree of thermal damage is characterized by the zones of coagulation, stasis and hyperaemia.
The zone of coagulation is where all the tissue is damaged but the pathophysiological changes in the zone of hyperaemia are spontaneously reversible. The zone of stasis, although not immediately destroyed, converts to necrosis during the first week after injury owing to a fatal combination of several factors. The healing of a burn wound proceeds from the zone of hyperaemia and follows the same course as in a surgical wound. Modifications of the healing process are produced by the graded nature of the thermal injury and by the presence of coagulated tissue acting as a foreign body.
Attempts to reduce the secondary tissue loss concentrate on the zone of stasis to which the damage is considered potentially reversible. Therapeutic measures positively influencing the pathophysiological processes in a burn wound are discussed.
After a burn injury, superficial partial-thickness burn wounds may progress to deep partial-thickness or full-thickness burn wounds, if kept untreated. This phenomenon is called secondary burn wound progression or conversion. Burn wound depth is an important determinant of patient morbidity and mortality. Therefore, reduction or even the prevention of secondary burn wound progression is one goal of the acute care of burned patients.
First Degree Burns: They are also called superficial burns; they cause minimal skin damage. Signs and symptoms include:
Redness
Signs of inflammation and swelling
Pain and tenderness
Second Degree Burns: They are also called partial thickness burns; these affect the epidermis and dermis. Signs and symptoms include:
Blisters
Redness
Inflammation and swelling
Pain
Peeling skin
Treatment of burns with good healing
Prevention of any infectious complication, reduction in pain and in scar formation
Fig.1
Medical
Verapamil, a Calcium-Channel Blocker, Improves the Wound Healing Process in Rats with Excisional Full-Thickness Skin Wounds Based on Stereological Parameters. https://www.ncbi.nlm.nih.gov/pubmed/27429235
Gel ointment of verapamil for percutaneous absorption. https://www.ncbi.nlm.nih.gov/pubmed/3509338
Topical Application of a Silicone Gel Sheet with Verapamil Microparticles in a Rabbit Model of Hypertrophic Scar. https://www.ncbi.nlm.nih.gov/pubmed/26710018
Increased calcium levels alter cellular and molecular events in wound healing. https://www.ncbi.nlm.nih.gov/pubmed/2555928
[Pathophysiology of the burn wound]. https://www.ncbi.nlm.nih.gov/pubmed/4076854
Topical Antimicrobials for Burn Wound Infections https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2935806/
"Corygest" Unlisted Drugs (Mar. 1982) vol. 34, No. 3, pp. 38.

Claims (6)

  1. What is claimed is the following:
  2. A method of stimulating cellular production or release of growth factors, comprising: administering a preparation containing a bismuth compound in a topical dosage form.
  3. The said topical dosage form is selected from a group of options consisting of ointments, gels, creams, solutions, suspensions, emulsions, dressings, and aerosols. The bismuth compound is applied in an occlusive barrier to promote wound healing, or in a non-occlusive barrier to allow wound drainage, and to treating skin redness and erythema.
  4. Teicoplanin is used for its antimicrobial efficacy.
  5. Lidocaine gel is a local anesthetic agent.
  6. Verapamil, a calcium channel blocker which, selected from the group consisting of verapamil, nifedipine, diltiazem, amalodipine, felodipine, isradipine, nicardipine, nimodipine, nisoldipine, bepridil and mixtures thereof, is a non-invasive transdermal carrier agent, is used topically to improve wound healing by enhancing fibroblast proliferation, collagen bundle synthesis, and revascularization in skin injuries, preventing scar formation and treating existing scars as well.
PCT/IB2018/050695 2018-02-01 2018-02-05 Tibo (topical innovative burn ointment) WO2019150173A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CYPCT/CY2018/111997 2018-02-01
CY2018111997 2018-02-01

Publications (1)

Publication Number Publication Date
WO2019150173A1 true WO2019150173A1 (en) 2019-08-08

Family

ID=61226623

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2018/050695 WO2019150173A1 (en) 2018-02-01 2018-02-05 Tibo (topical innovative burn ointment)

Country Status (1)

Country Link
WO (1) WO2019150173A1 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6426085B1 (en) * 1994-05-02 2002-07-30 Josman Laboratories Inc. Use of bismuth-containing compounds in topical oral dosage forms for the treatment of halitosis
US20150335704A1 (en) * 2014-05-23 2015-11-26 Imprimis Pharmaceuticals, Inc. Pharmaceutical compositions comprising gels and methods for fabricating thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6426085B1 (en) * 1994-05-02 2002-07-30 Josman Laboratories Inc. Use of bismuth-containing compounds in topical oral dosage forms for the treatment of halitosis
US20150335704A1 (en) * 2014-05-23 2015-11-26 Imprimis Pharmaceuticals, Inc. Pharmaceutical compositions comprising gels and methods for fabricating thereof

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
"Corygest", UNLISTED DRUGS, vol. 34, no. 3, March 1982 (1982-03-01), pages 38
ARHANA CHATTOPADHYAY ET AL: "An Inexpensive Bismuth-Petrolatum Dressing for Treatment of Burns :", PLASTIC AND RECONSTRUCTIVE SURGERY GLOBAL OPEN, vol. 4, no. 6, 1 June 2016 (2016-06-01), pages e737, XP055510003, ISSN: 2169-7574, DOI: 10.1097/GOX.0000000000000741 *
DONNA MAXWELL: "Topical 2% lidocaine gel versus placebo in burn wound debridement pain - Donna Maxwell, J O'brien, G Sparkes, Dh Lalonde, 1996", 1 January 1996 (1996-01-01), XP055510032, Retrieved from the Internet <URL:http://journals.sagepub.com/doi/10.1177/229255039600400210> [retrieved on 20180926] *
J. A. STEER ET AL: "Teicoplanin versus flucloxacillin in the treatment of infection following burns", JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY., vol. 39, no. 3, 1 March 1997 (1997-03-01), GB, pages 383 - 392, XP055510106, ISSN: 0305-7453, DOI: 10.1093/jac/39.3.383 *
RU WANG ET AL: "Role of verapamil in preventing and treating hypertrophic scars and keloids : Verapamil therapy for hypertrophic scars and keloids", INTERNATIONAL WOUND JOURNAL, vol. 13, no. 4, 12 May 2015 (2015-05-12), UK, pages 461 - 468, XP055510017, ISSN: 1742-4801, DOI: 10.1111/iwj.12455 *

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