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Title:
COMPOSITION OF VITAMIN C AND VITAMIN E WITH RIFAMPICIN FOR THE TREATMENT OF ALL INFECTED WOUNDS AND ALL DERMATOLOGICAL PROBLEMS EITHER INFECTED OR AT RISK OF BEING INFECTED
Document Type and Number:
WIPO Patent Application WO/2019/240677
Kind Code:
A2
Abstract:
The invention relates to a composition of vitamin C and vitamin E with rifampicin, which has a broad activity spectrum and may be used for any wound, cut, fistula, and fissure that are either infected or at risk of being infected, as well as for any dermatologic purulent inflammation that is either infected or at risk of being infected and is sensitive to rifampicin, without using a plurality of different antibacterial preparations.

Inventors:
BILICI NAMIK (TR)
Application Number:
PCT/TR2018/000016
Publication Date:
December 19, 2019
Filing Date:
March 06, 2018
Export Citation:
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Assignee:
BILICI NAMIK (TR)
International Classes:
B24B1/00
Attorney, Agent or Firm:
ÇAVUŞOĞLU, Ali (TR)
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Claims:
CLAIMS

1. A composition of vitamin C and vitamin E with nfampicin for all infected wounds and for the treatment of all dermatological problems that are either infected or at risk of being infected, characterized by comprising, in addition to rifempicin, vitamin C and vitamin E which shorten foe wound healing process, provides good healing of the wound, reduces the bleeding and increases the ab¾ of skin and the underlying tissues to regenerate and strengthen.

2. A composition of vitamin C and vitamin E with rifempicin for ail infected wounds and for the treatment of ail dermatological problems that are either infected or at risk of being infected according to claim 1, characterized In that foe composition is in the form of a spray.

3. A method for manufacturing the composition of vitamin C and vitamin E with rifempicin for a8 infected wounds and for foe treatment of all dermatological problems that are either infected or at risk of being infected, characterized by comprising the steps of:

• solubilizing powdered nfampicin (min. 97%) in 2 ml of water by vortexing,

• adding 100 mg of poiyvinylpyrrolidine,

• performing an ultrasonication step for 5 minutes to obtain a homogenous and well-dispersed solution,

• adding 10 mg of Udocaine hydrochloride, and then comprising the steps of,

• stirring 1 mg Disodium EDTA, 40 mg of Ascorbic acid and 20 mg of Tocopherol (tocotrienol) by vortexing for 1 minutes, followed by ultrasonication (fine separation-fragmentation by sound waves) for 5-7 minutes, • adding potassium metabisulfite, followed by mixing for 3 minutes with a mixer (vortex),

• adding potassium sorbate, followed by mixing for 10 minutes in an ultrasonic bath at room temperature, and

• adjusting pH of the liquid mixture to 5.5-6, respectively.

Description:
COMPOSITION OF VITAMIN C AND VITAMIN E WITH RfFAMPICIN FOR THE TREATMENT OF ALL INFECTED WOUNDS AND ALL DERMATOLOGICAL PROBLEMS EITHER INFECTED OR AT RISK OF BEING INFECTED

TECHNICAL FIELD

The invention relates to a composition of vitamin C and vitamin E with rifampitin, which has a broad activity spectrum and may be used for any wound, cut, fistula, and fissure that are either infected or at risk of being infected, as well as for any dermatologic purulent inflammation that is either infected or at risk of being infected and is sensitive to rifampitin, without using a plurality of different antibacterial preparations. STATE OF THE ART

Today, the treatment of superficial or deep cuts, scratches, bruises, punctures and bums, which arise from a disruption in toe skin and tissue integrity due to modem life styles, variable environmental conditions and various internal and external factors and which are caused by sharp objects, crushing materials and caustic materials; and the treatment of wounds and dermatological problems due to several reasons such as diseases or surgical therapies become important day by day.

There is a certain natural process tar the healing of dermatological p roblems and wounds to be occurred on the skin which defines a border between the inner and outer environments of an individual, has an important role for reflecting various feelings and reactions, is the biggest organ of the body and is the first line of defense. In some cases, the health perception and the quality of life of an individual are affected negatively when said dermatological problems and wounds heal late, are not closed or are exposed to an infection. Various infections may be developed in said dermatological problems and wounds depending on the type of the wound, hygiene of the environment and the immune system of the individual. These infections may be caused by bacteria, viruses and fungi. The most prominent characteristics of said infections are redness aid swelling around the wound, degeneration around the tissue, and in an advanced stage, necrosis in the surrounding tissue layer,

Wound and skin infections develop when the tissues are invaded by one or more microorganisms. These infections lead to an inflammatiph aid tissue damage by triggering the immune system of the body, and also may slow down the healing process. Although many infections are restricted to a small area such as an infected scratch or hair follicle and heal spontaneously, the infection may worsen and spread to long distances and/or deep tissues if it is not treated. Certain infections may spread to other organs and lead to septicemia.

In the present invention, rifampicin is used in the treatment of severe bacterid infections in mammals, especially in humans, wherein rifampicin is a semi- synthetic antibiotic obtained from microorganisms as for marry other antibacterial. Rifampicin is a semi-synthetic derivative of "rifampicin B" which is known to be produced by actinomycetes referred as first Streptomyces mediterranei, then Nocardia mediterranei and today, Amycolatopsis mediterranei.

Rifampirin is a semi-synthetic bactericidal (which kills the bacteria completely) antibiotic which can be used orally. It inhibits DNA-dependent RNA polymerase in sensitive bacteria it is particularly effective on bacteria! RNA, However, this type of effect is not seen on mammals, including humans. Thus, it only kills viable microorganisms in living organisms and does not damage the cells of the living organism. There is no finding in the literature about cross-resistance to rifampitin. It is effective on many kinds of bacteria, including Mycobacterium. Marty penicillinase produdng/non-penici!tinase producing bacterial strains and beta lactam resistant staphylococcus are sensitive to rifampicin. It is used for a number of severe infections such as severe staphylococcus infections such as tuberculosis, leprosy and methidllrn-resistant staphylococcus, meningococcus. Haemophilus influenza and bruseilosis. In addition to its parenteral and enteral use, it is also used for wound dressing after stitching by physicians (especially surgeons) in the operation rooms. For this type of use, ampoules are broken aid poured onto the surgical wound, thereby providing an antibacterial protection to prevent post-operative infections. It is also used in the treatment of infected wounds, treatment of persistent vaginitis and decubitus wounds. This is intended for creating a serious antibacterial activity against the risk of post-operative infection and protecting the epidermal activity from microorganisms, for important injuries. Rifampicin is a commonly used antibacterial product in order to accelerate cicatrization and to avoid infections as it is capable of adhering, penetrating, drying in a short time, and restricting the wound. ft has a bactericidal effect (which kilts the bacteria completely) for particularly MRSA (methicillin resistant Staph, aureus): mycobacterium species: other streptococcus species, particularly Str. Pneumoniae ; Neisseria menmgiditis and N. gonorrhoeae, Haermphyius influenzae , Clostridium difficile, brucella species, legioneiia. Chlamydia. It is effective for Enterobacteriaceae family and Pseudomonas spp. as long as it is not used frequently and for a long time. Said microorganisms are qualified and their eradication is extremely difficult, Indeed the activity spectrum of rifampicin is broader. Its efficacy for many gram (*} and gram (-) microorganisms has been found in the literature. Multiple drug use is required as the current antibacterial preparations are each not effective atone. Rifampicin avoids multiple drug use and can be used alone. Skin thinning, skin peeling and subsequently infection are not prevented on the pressure points of the body weight of each individual who has to stay in bed for an extended period of time, particularly chronic bedridden elderly patients. Drugs that are currently used in the treatment are in multiple combinations.

In the current drugs used for wounds and surgical wounds, there is no antibacterial drug in which vitamin C and vitamin E are combined, which shorten the wound healing process, provides good healing of the wound, reduces the bleeding and increases the ability of skin and the underlying tissues to regenerate and strengthen.

Drug substance of rifampicin is administered intramuscularly and intravenously in the form of ampoule, tablet and capsule, and orally in the form of tablet-capsule as an antibacterial. In use, a uniform distribution is provided by breaking and pouring the ampoules onto the wound. As a uniform distribution of drug on every site of the wound is not provided, spread ing/dispersing with a hand is required, which has been already done.

DETAILED DESCRIPTION OF THE INVENTION

The present invention relates to a composition of vitamin C and vitamin E with rifampitin, which has a broad activity spectrum, for all infected wounds and for foe treatment of all dermatological problems that are either infected or at risk of being infected in order to eliminate foe above-mentioned drawbacks and to provide novel advantages in foe relevant technical field.

In foe detailed description, the preferred alternatives of the composition of vitamin C and vitamin E with rifampicin for the infected wounds of foe invention and for the treatment of all dermatological problems that are either infected or at risk of being infected are described only for better understanding the subject matter without limitation.

The object of foe invention is to both provide a fast wound healing and an increase in the wound tensile strength (effect of vitamin C) with a protective- stimulative effect for foe open tissue, and to provide an activity that is known to be epifoeihdng, cicatrizant and protective and is used (vitamin E), by adding vitamin C and vitamin E to rifampicin which is a semi-synthetic antibiotic obtained from microorganisms for any wound, cut, fistula, and fissure that are either infected or at risk of being infected, as well as for any dermatologic purulent inflammation that is either infected or at risk of being infected and is sensitive to rifampicin. In the case of skin thinning, skin peeling and subsequently infection on the pressure points Of the body weight of each individual Who has tb stay in bed for an extended period of time, particularly chronic bedridden elderly patients, for the treatment of such wounds foe composition of vitamin C and vitamin E with rifampicin may be used alone due to its cicatrizant, antioxidant, epithelizing and collagen-stimulating activity as well as its antibacterial and protective activity, instead of multiple drug combinations currently used in the treatment.

As vitamin C and vitamin E is not present in the current liquid preparations used as an antibiotic in the wound treatment, it is not possible to make use of the activities of these vitamins. The composition of vitamin C and vitamin E with rifampicin according to the invention may be effectively used alone, instead of an antiseptic + antibiotic composition used in the field hospitals. By adding vitamin C and vitamin E to rifampicin:

Vitamin C: Vitamin C is of vital importance due to its other therapeutic effects on skin and wound, particularly stimulation of collagen and supporting of collagen production.

Vitamin E: It is of vital importance for platelet aggregation (adhesion) and epithelium regeneration, as well as its epithelizing (skin-forming) and antioxidant activity.

The composition of foe invention may be used in veterinary medicine for the same purposes. Another object of the invention is to provide a uniform distribution on the corresponding area and an equal distribution on the intended region by non- pressure spraying the composition from a distance of 3-20 cm together with vitamin C- and vitamin E-containing spray form of antibacterial drug substance of rifampicin which is administered intramuscularly arid intravenously in the form of ampoule, tablet and capsule, and orally in foe form of tablet-capsule , but has no dermatological spray form. Thus, spreading/dispersing with a hand is avoided as an equal drug distribution on every region of foe wound is provided. The spray form is easy and simple to use.

In addition of the spray form of the composition according to foe invention, it may also be prepared in foe form of foam and gel by developing individual and measured techniques for combat soldiers. Again it may be applied onto the wound by impregnating into a suitable material asTTS (transderma! therapeutic system).

"This formulation is only for spray.

In-Vitro Preparation of Composition of Vitamin C and Vitamin E with Rifampicin in a volume of 5 mi: * powdered rifampicin (min. 97%) is solubilized in 2 mi of water by vortexing,

• 100 mg of poiyvtnylpyrrolid ' tne is added,

• an ultrasonication step is performed for 5 minutes to obtain a homogenous and well-dispersed solution,

* 10 mg of Udocaine hydrochloride is added.

Then;

• 1 mg Disodium EDTA, 40 mg of Ascorbic acid and 20 mg of Tocopherol (tocotnenol) are stirred by vortexing for 1 minutes, followed by ultrasonication (fine separation-fragmentation by sound waves) for 5- 7 minutes,

• potassium metebisutfite is added, followed by mixing for 3 minutes with a mixer (vortex),

• potassium sorbate is added, followed by mixing for 10 minutes in an ultrasonic bath at room temperature,

• pH of the liquid mixture is adjusted to 5.5-6,

• the mixture is filled into colored glass vials of 5 ml with a spray pump.

• Drugs of 10, 30, 50, 100, 250 and 500 ml may be prepared with the ratios being constant.

• Drug is filled into dark colored glass vials sterilized by gamma irradiation (<25 kGy ) and then is sterilized in the same manner.

• Drug may be manufactured as a mass production under contract manufacturers having GMP conditions.