ODOR

CROSS REFERENCE TO RELATED APPLICATIONS

This application claims the benefit of Indian Provisional Patent Application No. 202111044007 filed September 28, 2021, which is incorporated herein by reference for all purposes in its entirety.

FIELD OF THE INVENTION

The present invention relates to a pharmaceutical and cosmeceutical composition comprising molecular Iodine (I2) and an alcohol which act as germicide and antiseptic, to kill a wide range of microorganisms including bacteria, fungi, and to some extent viruses, and also a process for its preparation. The composition further comprises propanediol, and inert excipients. The composition can be utilized as a topical antimicrobial, skin antiseptic, and body odor remover which may provide long lasting body freshness.

BACKGROUND OF THE INVENTION

At present, there are innumerable antiperspirants and deodorants available in the market, in the form of sprays, deodorant sticks and roll-ons to provide relief from the odor produced from axillary sweating. A few products provide full body cleansing benefits to a consumer. Such products include a soap, a liquid free medicated and antimicrobial skin cleansing lotion consisting of cetyl alcohol, propylene glycol, sodium lauryl sulphate, stearyl alcohol, polysorbate 20. Methyl hydroxy benzoate is also available in the market which provides non-drying and non-irritant cleansing while keeping the skin moisturized as well as maintains the pH of the skin. Chlorhexidine gluconate (CHG) present in certain formulations has antiseptic properties. Most of the antiperspirant and deodorant formulations contain active ingredients such as astringent metallic salts, generally, aluminium salts (aluminum chlorohydrate, aluminum chloride, aluminum sesquichlorohydrate, aluminum-zirconium hydroxy chloride), silver citrate, alcohols, 2,4,4'- trichloro-2 '-hydroxy diphenyl ether (Triclosan), benzethonium chloride, benzalkonium chloride, polyhexamethylene biguanides, triethyl citrate, 2-amino-2-methyl- 1 -propanol (AMP), cetyl- trimethylammomium bromide, cetyl pyridinium chloride, farnesol (3,7,l l-trimethyl-2,6,10- dodecatrien-l-ol). Aluminium salts are known to reduce sweating by plugging sweat glands and act as natural antimicrobial agents thereby reducing foul sweat odor. Silver citrate has antimicrobial properties and is effective against gram positive and gram negative bacteria, yeasts and moulds. It is also a deodorizing agent and masks unpleasant body odor. Triclosan has both antimicrobial properties that slow down the growth of the microorganisms. Benzethonium chloride acts as a skin disinfectant and has surfactant, antiseptic and broad spectrum antimicrobial properties. Benzalkonium chloride is used in many cosmetic properties for its antimicrobial, conditioning, foaming and cleansing properties. Poly hexamethylene biguanide is an antimicrobial agent that is used as a disinfectant and antiseptic agent in many topical formulations. It is known to reduce foul body odour. Triethyl citrate is derived from natural substances that inhibit esterase-based metabolism of sweat components that are responsible for unpleasant body odour. Cetyltrimethylammonium bromide and cetyl pyridinium chloride are quaternary ammonium salts having biocidal, antistatic and surface cleansing properties. Farnesol acts as a deodorizing, antimicrobial agent that has specific activity for gram-negative bacteria responsible for malodor.

Active ingredients that are generally used may have detrimental effects on the health of consumers upon prolonged use. Subchronic use of cetyl alcohol is associated with features of exfoliative dermatitis. Polyethylene glycol is mildly irritating to the eyes. Sodium lauryl sulphate might be absorbed into the body via skin and also cause skin redness. Stearyl alcohol causes skin and eye irritation upon prolonged exposure. Methyl hydroxy benzoate has been reported to cause contact dermatitis in a few people upon cutaneous exposure. Some reports suggest that aluminium salts may cause skin irritation, itching and allergic reactions. It is also suspected that aluminium salts may be responsible for development of neurodegenerative disorders such as Alzheimer’s disease and breast cancer. Silver citrate is moderately toxic and on prolonged use may cause permanent skin discoloration. Silver released from the compound may accumulate in the tissue and lead to argyria. Studies of triclosan suggest that it is readily absorbed into human skin and its traces get accumulated in tissues and fluids which causes endocrine disrupting properties and poses a great risk to early embryonic development and cellular homeostasis. FDA also reported that triclosan might lead to the development of antibiotic resistance. Benzethonium chloride causes itching, skin irritation and severe allergic reactions and hypersensitivity. Poly hexamethylene biguanide may cause systemic toxicity, AMP causes severe skin irritation and farnesol is a skin allergen. CHG may cause severe skin irritation, rashes and hives and triethanolamine lauryl sulphate is responsible for severe skin irritation upon prolonged exposure and is not recommended for chronic use.

Among these active ingredients, none provides long lasting, safe and persistent full body protection benefits to the consumer on long term use. As such there is no product available in the market that can get rid of unpleasant body odor, provide a cleansing action as well as give instant, long-lasting full body protection with the best safety index against microbes, together in a single product.

SUMMARY OF THE INVENTION

In one aspect, the present invention provides a pharmaceutical or a cosmeceutical composition which comprises molecular iodine (I2), an alcohol, and propanediol wherein the composition is stable, and wherein the composition delivers free molecular iodine ranging between 200 ppm and 300 ppm.

In another aspect, the present invention provides a process for preparing a stable molecular iodine (I2) and alcohol based formulation which delivers free molecular iodine in a range between 200 ppm and 300 ppm. The process comprises the steps of:

(a) dissolving molecular iodine in an alcohol to obtain a solution;

(b) adding propanediol,

(c) adding glycerol; and

(d) optionally adding one or more fragrance substances.

DETAILED DESCRIPTION OF THE INVENTION

The term “molecular iodine” refers to diatomic iodine, which is represented by the chemical symbol I2. Molecular iodine is also referred to as “elemental iodine” when in the solid state.

In one aspect, the present invention provides a pharmaceutical or a cosmeceutical composition which comprises molecular iodine (I2), an alcohol, and propanediol wherein the composition is stable, and wherein the composition delivers free molecular iodine ranging between 200 ppm and 300 ppm.

In one embodiment of this aspect, the alcohol can be a lower alcohol.

In another embodiment of this aspect, the lower alcohol can be ethanol or isopropanol.

In another embodiment of this aspect, the composition further comprises glycerol.

In another embodiment of this aspect, the propanediol is 1,3 -propanediol.

In another embodiment of this aspect, propylene glycol may be used in place of propanediol in the composition.

In another embodiment of this aspect, the cosmeceutical composition comprises:

(a) molecular iodine in a range between 200 ppm and 300 ppm or 0.20% to 0.30% w/v;

(b) ethanol or isopropanol;

(c) propanediol;

(d) glycerol; (e) optionally, one or more fragrance substances.

In yet another embodiment of this aspect, the cosmeceutical composition comprises:

(a) molecular iodine in a range between 200 ppm and 300 ppm or 0.20% to 0.30% w/v;

(b) ethanol or isopropanol in a range between 45% to 55% v/v of the total concentration of the composition;

(c) propanediol in a range between 35% to 45% v/v of the total concentration of the composition;

(d) glycerol in a range between 5% and 15% v/v of the total concentration of the composition;

(e) optionally, a fragrance in a range between 0.1% to 0.5% v/v of the total concentration of the composition.

In yet another embodiment of this aspect, the fragrance can be selected from aqua kiss, lavender, tempting, invincible, or a mixture thereof.

In yet another embodiment of this aspect, the composition can be topically applied on the entire body of a human.

In yet another embodiment of this aspect, the composition can be in a liquid form to be sprayed onto the body of a human, thereby eliminating the need to be applied as a deodorant stick.

In yet another embodiment of this aspect, the composition can be applied uniformly throughout the body of a human in spray form without any of it getting accumulated at a single region on the body. Molecular iodine (I2) as an active ingredient with ethanol or isopropanol as an antiseptic and antibacterial disinfectant along with propanediol as a moisturizer and cleanser provides a persistent antiseptic effect along with a broad spectrum antimicrobial activity against a wide range of bacteria, fungi and some viruses. There is no known evidence of bacteria developing resistance against molecular iodine. Molecular iodine (I2), the active ingredient in the composition, is an active broad spectrum antibacterial and antifungal agent which acts as an effective antimicrobial against the infection-causing and odor-causing bacteria that might grow due to sweat, in particular, alter the activity of odor-causing bacteria, Staphylococcus hominis, Staphylococcus epidermidis and Cutibacterium avidum helping to get rid of the foul odor from the body.

The composition may help in preventing armpit blackening occurring due to growth and secretions of the staphylococcal species, owing to the broad spectrum antimicrobial and antiseptic action of the free molecular iodine and ethanol or isopropanol working synergistically. The formulation may rapidly kill all the vegetative forms of bacteria that might colonize one’s body due to exposure to pollutants and dirt in different environmental conditions.

The humectants propanediol and glycerol used in the composition help in moisturizing the regions of application. Propanediol possess emollient and deep cleansing properties which acts as a moisturizer and provides cleansing action, respectively. It can help to remove dirt and oil from the skin thereby helping to attain a clean and fresh body free from any odor. The composition also gives a non- greasy feel owing to the lightweight texture of propanediol.

The composition can be ideal for use for all skin types without any anaphylactic reactions. This composition can keep the skin properly hydrated and moisturized with no significant transdermal toxicity.

The composition can be used for body cleansing of people who have undergone surgeries thereby eliminating the need for sponge baths in healthcare settings. The composition can also be useful for patients who are on bed-rest and may get back sores due to longer duration on a bed.

The composition can have an application of its use in the colder geographical regions where bathing regularly is difficult due to the cold temperatures. The composition can also have an application in areas of water scarcity such as drought hit areas. The composition can have an application among people who frequently go for trekking, camping, long rides.

The composition can act as an antiperspirant, keeping one fresh, clean and fragrant. It can act as a personal hygiene deodorant which will show its effect persisting for a longer duration of time owing to the persistent antimicrobial activity of molecular iodine working synergistically with the other components of the composition. The composition can provide a persistent antimicrobial activity along with full body cleansing and freshness.

In yet another embodiment of this aspect, the composition is stable for at least 24 months at room temperature. In yet another preferred embodiment, the composition is stable for at least 24 months at room temperature when stored in a closed container at room temperature. In yet another preferred embodiment, the composition is stable for at least 180 days, and no phase separation was observed in the composition.

In another aspect, the present invention provides a process for preparing a stable molecular iodine (I2) and alcohol based formulation which delivers free molecular iodine in a range between 200 ppm and 300 ppm which comprises the steps of:

(a) dissolving molecular iodine in a alcohol to obtain a solution;

(b) adding propanediol,

(c) adding glycerol; and

(d) optionally adding one or more fragrance substances.

In one embodiment of this aspect, the process can be carried out at room temperature.

In another embodiment of this aspect, the alcohol can be a lower alcohol.

In another embodiment of this aspect, the lower alcohol can be ethanol or isopropanol.

In another embodiment of this aspect, step b) further comprises constant stirring. In another embodiment of this aspect, step c) further comprises stirring using a magnetic stirrer at 500 rotations per minute (rpm).

In another embodiment of this aspect, the fragrance can aqua kiss, lavender, tempting, invincible, or a mixture thereof.

In yet another embodiment of this aspect, the process comprises:

(a) dissolving molecular iodine in a range between 200 ppm and 300 ppm or 0.20% to 0.30% w/v in an alcohol selected from ethanol or isopropanol in a range between 45% to 55% v/v of the total concentration of the composition to obtain a solution;

(b) adding propanediol in a range between 35% to 45% v/v of the total concentration of the composition,

(c) adding glycerol in a range between 5% and 15% v/v of the total concentration of the composition; and

(d) optionally adding one or more fragrance substances in a range between 0.1% to 0.5% v/v of the total concentration of the composition.

Stability and Test Data:

The results of the test samples are provided in the below tables:

Concentration of molecular iodine in the Sample: approx. 250 PPM

Sample Quantity: 50 ml*5

Table 1 provides the stability of the sample in its appearance, colour and odour. No major change was observed and the formulation was observed to be stable.

Table 1

Table 2 provides the Spectrum Study (Anti-microbial Activity) Efficacy Test.

Table 2

Table 3 provides the Patch Test which was conducted in subjects. No skin irritation was found.

Table 3

Table 4 provides the Iodine Content of the sample at different intervals.

Table 4

While the present invention has been described in terms of its specific aspect, certain modifications and equivalents will be apparent to those skilled in the art and are intended to be included within the scope of the present invention.

In the following section, the aspect is described by way of examples to illustrate the processes of the invention. However, these do not limit the scope of the present invention. Several variants of these examples would be evident to persons ordinarily skilled in the art.

EXAMPLES

The base solution/concentrate of Iodine used in all the below examples was obtained as a stock solution with Iodine maintained at 1 mg/ml (w/v) concentration. (For a formulation to be prepared, required amount of iodine was measured and added according to the final concentration required in the formulation being prepared).

A 100 ml solution was made up to be used as a scalp care lotion with Iodine concentration maintained at 250 ppm using the following components/ingredients in the below -mentioned concentrations. Iodine (0.25ml) from the stock solution was added to ethanol (58.25 ml) and mixed thoroughly to obtain a solution. To this solution, propanediol (36 ml) was added with constant stirring. After mixing the solution thoroughly, glycerol (5 ml) was added and mixed using a magnetic stirrer at 500 rpm. After complete mixing, aqua kiss fragrance (0.5 ml) was added and mixed to obtain the final product.

The resulting formulation was at the required consistency as well as sprayable. The stability of the formulation was observed at following time intervals: 3rd day, 7th day and 15th day to check for stability with Iodine, consistency and colour change. Iodine appeared to be stable in the formulation at the different time intervals. The formulation had a moisturising effect with no irritation or inflammation upon application on human skin. Furthermore, the formulation was observed to be stable with respect to its colour, consistency, sprayability and stability at all the time intervals as mentioned above.

The foregoing description of the specific embodiments so fully reveals the general nature of the embodiments herein that others can, by applying current knowledge, readily modify and/or adapt for various applications such specific embodiments without departing from the generic concept, and, therefore, such adaptations and modifications should and are intended to be comprehended within the meaning and range of equivalents of the disclosed embodiments. It is to be understood that the phraseology or terminology employed herein is for the purpose of description and not of limitation. Therefore, while the embodiments herein have been described in terms of preferred embodiments, those skilled in the art will recognize that the embodiments herein can be practiced with modification within the spirit and scope of the embodiments as described herein.

Throughout this specification the word “comprise”, or variations such as “comprises” or “comprising”, will be understood to imply the inclusion of a stated element, integer or step, or group of elements, integers or steps, but not the exclusion of any other element, integer or step, or group of elements, integers or steps. The use of the expression “at least” or “at least one” suggests the use of one or more elements or ingredients or quantities, as the use may be in the embodiment of the disclosure to achieve one or more of the desired objects or results.

Any discussion of documents, acts, materials, devices, articles or the like that has been included in this specification is solely for the purpose of providing a context for the disclosure. It is not to be taken as an admission that any or all of these matters form a part of the prior art base or were common general knowledge in the field relevant to the disclosure as it existed anywhere before the priority date of this application.

The numerical values mentioned for the various physical parameters, dimensions or quantities are only approximations and it is envisaged that the values higher/lower than the numerical values assigned to the parameters, dimensions or quantities fall within the scope of the disclosure, unless there is a statement in the specification specific to the contrary.

While considerable emphasis has been placed herein on the components and component parts of the preferred embodiments, it will be appreciated that many embodiments can be made and that many changes can be made in the preferred embodiments without departing from the principles of the disclosure. These and other changes in the preferred embodiment as well as other embodiments of the disclosure will be apparent to those skilled in the art from the disclosure herein, whereby it is to be distinctly understood that the foregoing descriptive matter is to be interpreted merely as illustrative of the disclosure and not as a limitation.