WO2023084537A1

WO2023084537A1 - Molecular iodine and alcohol based formulation and its application in air sanitization/disinfection

Info

Publication number: WO2023084537A1
Application number: PCT/IN2022/050981
Authority: WO
Inventors: Anil KEJRIWAL
Original assignee: Kejriwal Anil
Priority date: 2021-11-09
Filing date: 2022-11-09
Publication date: 2023-05-19

Abstract

Disclosed herein is a pharmaceutical and/or cosmeceutical composition comprising free molecular Iodine (I2) and alcohol which act as germicide, antiseptic, and disinfectant 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 glycerol. The composition can be utilized as an aerial and surface sanitizing agent or disinfectant in pharmaceutical and cosmeceutical applications by giving a persistent disinfectant and antiseptic effect, 10 to be employed in enclosed spaces.

Description

MOLECULAR IODINE AND ALCOHOL BASED FORMULATION AND ITS APPLICATION IN AIR SANITIZATION/DISINFECTION

CROSS REFERENCE TO RELATED APPLICATIONS

This application claims the benefit of Indian Provisional Patent Application No. 202111051229 filed November 09, 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/or cosmeceutical composition comprising free molecular Iodine (I2) and alcohol which act as germicide, antiseptic, and disinfectant 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 glycerol. The composition can be utilized as an aerial and surface sanitizing agent or disinfectant in pharmaceutical and cosmeceutical applications by giving a persistent disinfectant and antiseptic effect, to be employed in enclosed spaces.

BACKGROUND OF THE INVENTION

Current technology comprises a formulation of a water-based air sanitizer consisting of a malodour absorbing compound, a solubilizer and a chelating agent for sanitizing air and reducing air malodour. Zinc ricinoleate, the malodour reducing compound, reacts with and controls osmogenes like hydrogen sulphide, mercaptan, thioether, isovaleric acid and ammonia thereby preventing the odour emissions in air. iV-alkyl aminopropyl glycine is the antimicrobial compound used in this technology which kills Gram-positive and Gram-negative bacteria, yeast and fungi, and certain viruses. The chelating agent, sodium iminodisuccinate and the solubilizer, a combination of PEG-45 palm kernel glycerides and PEG-6 capric/caprylic glycerides used, prevent the formation of precipitate. Yet another technology involves a combination of air sanitizer, soft surface sanitizer/deodorizer and hard surface disinfectant. Active ingredient used for air sanitization and soft surface deodorizer is triethylene glycol (TEG). Triethylene glycol (TEG) is known to kill certain airborne bacteria. Active ingredient for soft surface sanitization and hard surface disinfection is alkyl dimethyl benzyl ammonium saccharinate.

Zinc ricinoleate is known to cause allergic contact dermatitis in case of exposure to the eyes and does not have any bactericidal or fungicidal properties. A- alkyl aminopropyl glycine is considered as one of the hazardous ingredients leading to serious eye and skin irritation. It might also cause chemical burning of the mouth, throat and stomach in case of accidental ingestion. Triethylene glycol (TEG) is irritant to the eyes and is combustible when exposed to heat or flame. Alkyl dimethyl benzyl ammonium saccharinate does not possess the property of removal of airborne bacteria or treating malodour.

As such there is no product available in the market which provides broad spectrum antimicrobial and disinfectant properties; which is hypoallergenic, non-toxic, nonirritant and non-corrosive as well as does not form precipitates, together in a single product.

SUMMARY OF THE INVENTION

In one aspect, the present invention provides a pharmaceutical and/or cosmeceutical composition which comprises molecular iodine (I2), a lower alcohol, and glycerol, wherein the composition is stable, wherein the composition delivers free molecular iodine ranging between 450 ppm and 550 ppm, and wherein the composition is formulated for application as an aerial and surface sanitizing agent or disinfectant. In another aspect, the present invention provides a process for preparing a stable molecular iodine (I2) and a lower alcohol-based composition which delivers free molecular iodine in a range between 450 ppm and 550 ppm.

The process comprises the steps of:

(a) adding molecular iodine (I2) with a lower alcohol to obtain a solution; and

(b) adding glycerol to the solution obtained in step a).

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 and/or cosmeceutical composition which comprises molecular iodine (I2), a lower alcohol, and glycerol, wherein the composition is stable, wherein the composition delivers (only) free molecular iodine ranging between 450 ppm and 550 ppm, and wherein the composition is formulated for application as an aerial and surface sanitizing agent or disinfectant.

In one embodiment of this aspect, the present invention relates to formulations for air sanitizer, disinfectant which provides the combination of free molecular iodine and alcohol in varied compositions for a persistent antimicrobial effect. In another embodiment of this aspect, the formulations can be in aerosol form to be sprayed in enclosed space that needs to be sanitized, and/or disinfected.

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

In another embodiment of this aspect, the pharmaceutical and/or cosmeceutical composition comprises: (a) molecular iodine in a range between 450 ppm and 550 ppm;

(b) a lower alcohol selected from ethanol, isopropyl alcohol, or mixtures thereof; and

(c) glycerol.

In another embodiment of this aspect, the pharmaceutical and/or cosmeceutical composition comprises:

(a) molecular iodine in a range between 2000 ppm and 3000 ppm;

(c) glycerol, wherein the composition is required to be used post dilution in an aqueous medium, preferably water, in the ratio of 1:5 (one part of the said composition in five parts of the aqueous medium). The said composition will provide a final delivery of 450 to 550 ppm of molecular iodine and 15% to 25% of the lower alcohol upon dilution.

(a) molecular iodine in a range between 2000 ppm and 3000 ppm;

(b) ethanol, isopropyl alcohol, or mixtures thereof in a range between 85% to 95% v/v of the total concentration of the composition; and

(c) glycerol in a range between 15% and 25% v/v of the total concentration of the composition, wherein the composition is required to be used post dilution in an aqueous medium, preferably water, in the ratio of 1:5 (one part of the said composition in five parts of the aqueous medium). The said composition will provide a final delivery of 450 to 550 ppm of molecular iodine and 15% to 25% of the lower alcohol upon dilution. In another embodiment of this aspect, the pharmaceutical and/or cosmeceutical comprises:

(a) molecular iodine in a range between 450 ppm and 550 ppm;

(b) ethanol in a range between 75% to 95% v/v of the total concentration of the composition; and

(c) glycerol in a range between 15% and 25% v/v of the total concentration of the composition.

The said composition can be used without any dilution.

In yet another embodiment of this aspect, the pharmaceutical and/or cosmeceutical composition act as the aerial sanitizer/disinfectant that provides a persistent broadspectrum antimicrobial effect against a wide range of microorganisms. Molecular iodine (I2), the active ingredient in the above-mentioned compositions, has been shown to be effective against both gram-negative and gram-positive bacteria, yeasts, and some viruses.

In yet another embodiment of this aspect, the pharmaceutical and/or cosmeceutical composition consisting of isopropyl alcohol (IPA) may have its application in enclosed spaces such as rooms, office spaces, etc. While the formulation consisting of ethanol may have its application in enclosed spaces such as public conveyance vehicles. The said pharmaceutical and/or cosmeceutical compositions might serve as an active sanitizer/disinfectant against the bioaerosols present in enclosed spaces. The pharmaceutical and/or cosmeceutical composition of this invention might leave no odor post the application.

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 was according to the requirements of the end product as an aerial sanitizer/disinfectant. In another aspect, the present invention provides a process for preparing a stable molecular iodine (I2) and a lower alcohol-based composition which delivers free molecular iodine in a range between 450 ppm and 550 ppm which comprises the steps of:

(a) adding molecular iodine (I2) with a lower alcohol; and

(b) adding glycerol to the solution obtained in step a).

In one embodiment of this aspect, the lower alcohol can be ethanol, isopropanol or mixtures thereof.

In another embodiment of this aspect, the steps a) and b) further comprises mixing thoroughly to obtain a solution.

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

(a) adding molecular iodine in a range between 2000 ppm and 3000 ppm or 2 % to 3% w/v with an alcohol selected from ethanol or isopropanol in a range between 85% to 95% v/v of the total concentration of the composition;

(b) adding glycerol in a range between 15% and 25% v/v of the total concentration of the composition;

(c) diluting the mixture in an aqueous medium in the ratio of 1:5 (one part of the said composition in five parts of the aqueous medium), wherein upon dilution the composition delivers free molecular iodine in a range between 450 ppm and 550 ppm.

In another embodiment, the steps a) and b) further comprises mixing thoroughly to obtain a solution. In another embodiment, the step b) further comprises stirring for about 10 minutes to about 15 minutes using a magnetic stirrer at 500 rotations per minute (rpm). In yet another embodiment, the process comprises:

(a) adding molecular iodine in a range between 450 ppm and 550 ppm or 0.45% to 0.55% w/v with ethanol in a range between 75% to 95% v/v of the total concentration of the composition;

(b) adding glycerol in a range between 15% and 25% v/v of the total concentration of the composition.

In another embodiment, the steps a) and b) further comprises mixing thoroughly to obtain a solution. In another embodiment, the step b) further comprises stirring for about 15 minutes to about 20 minutes using a magnetic stirrer at 500 rotations per minute (rpm).

Stability and Test Data:

The results of the test samples are provided in the below tables: Concentration of molecular iodine in the Sample: approx. 500 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 molecular 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 -mentioned examples was obtained as a stock solution with Iodine maintained at 1 mg/ml (w/v) concentration. (For a to be prepared, required amounts of iodine was measured and added according to the final concentrations required in the formulation being prepared).

EXAMPLE 1:

A 50 ml solution was made containing molecular iodine at a concentration of 2500 ppm.

Iodine solution (1.25 ml) from the stock solution was added to isopropyl alcohol (IPA) (46.25 ml) or ethanol (46.25 ml) and mixed thoroughly by shaking manually till iodine solution was completely dissolved. Glycerol (2.5ml) was added to the solution and mixed for 10 minutes to 15 minutes using a magnetic stirrer at 500 rpm to make sure that glycerol was dissolved thoroughly.

This concentrated form was diluted in distilled water in the ratio of 1:5 (one part of the formulation in five parts of distilled water). The final delivery of molecular iodine was approximately 500 ppm upon dilution.

Iodine content was stable in the formulation at the different time intervals. The formulation was observed to be stable with respect to its colour, consistency, and stability at all the time intervals.

EXAMPLE 2:

A 100 ml solution was made up containing molecular iodine at a concentration of 500 ppm.

Iodine solution (0.5 ml) from the stock solution was added to ethanol (94.5ml) and mixed thoroughly till complete dissolution. To this solution, glycerol (5 ml) was added and stirred for 15 minutes to 20 minutes using a magnetic stirrer at 500 ppm until it was properly dissolved in the solution. (This composition is to be used as is provided without any dilution).

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.

Claims

CLAIMS I claim:

1. A pharmaceutical and/or cosmeceutical composition which comprises molecular iodine (I2), a lower alcohol, and glycerol, wherein the composition is stable, wherein the composition delivers (only) free molecular iodine ranging between 450 ppm and 550 ppm, and wherein the composition is formulated for application as an aerial and surface sanitizing agent or disinfectant.

2. The composition as claimed in claim 1, wherein the composition is in aerosol form.

3. The composition as claimed in claim 2, wherein aerosol form can be sprayed in enclosed space that needs to be sanitized, and/or disinfected.

4. The composition as claimed in claim 1, wherein the lower alcohol is ethanol, isopropanol, or mixtures thereof.

5. The composition as claimed in claim 1, wherein the composition comprises:

(a) molecular iodine in a range between 450 ppm and 550 ppm;

(c) glycerol.

6. The composition as claimed in claim 1, wherein the composition comprises:

(a) molecular iodine in a range between 2000 ppm and 3000 ppm;

(c) glycerol, wherein the composition is required to be used post dilution in an aqueous medium, in the ratio of 1:5, and wherein composition will provide a final delivery of 450 to 550 ppm of molecular iodine and 15% to 25% of the lower alcohol upon dilution.

7. The composition as claimed in claim 6, wherein the aqueous medium is water.

8. The composition as claimed in claim 6, the lower alcohol selected from ethanol, isopropyl alcohol, or mixtures thereof is in a range between 85% to 95% v/v of the total concentration of the composition; and glycerol is in a range between 15% and 25% v/v of the total concentration of the composition.

9. The composition as claimed in claim 1, wherein the composition comprises:

(a) molecular iodine in a range between 450 ppm and 550 ppm;

(c) glycerol in a range between 15% and 25% v/v of the total concentration of the composition. wherein the composition is used without any dilution.

10. The composition as claimed in claim 1, wherein the composition serves as an active sanitizer or disinfectant against the bioaerosols present in enclosed spaces.

11. The cosmeceutical composition as claimed in claim 1, wherein the composition is stable for at least 24 months at room temperature.

12. The cosmeceutical composition as claimed in claim 1, wherein the composition is stable for at least 180 days.

13. A process for preparing a stable molecular iodine (I2) and a lower alcohol-based composition which delivers free molecular iodine in a range between 450 ppm and 550 ppm which comprises the steps of:

(a) adding molecular iodine (I2) with a lower alcohol; and 15

(b) adding glycerol to the solution obtained in step a).

14. The process as claimed in claim 13, wherein the lower alcohol is ethanol, isopropanol or mixtures thereof.

15. The process as claimed in claim 14, wherein the steps a) and b) further comprises mixing thoroughly to obtain a solution.

16. The process as claimed in claim 13, wherein the process comprises the steps of:

17. The process as claimed in claim 16, wherein the aqueous medium is water.

18. The process as claimed in claim 16, wherein the steps a) and b) further comprises mixing thoroughly to obtain a solution.

19. The process as claimed in claim 16, wherein the step b) further comprises stirring for about 10 minutes to about 15 minutes using a magnetic stirrer at 500 rotations per minute (rpm). 16

20. The process as claimed in claim 13, wherein the process comprises the steps of:

21. The process as claimed in claim 20, wherein the steps a) and b) further comprises mixing thoroughly to obtain a solution.

22. The process as claimed in claim 20, wherein the step b) further comprises stirring for about 15 minutes to about 20 minutes using a magnetic stirrer at 500 rotations per minute (rpm).