Quick,self-dissolving,foamable antimicrobial tablet and method of preparation thereof

Abstract

A quick, self-dissolving, foamable antimicrobial tablet and a preparation method thereof, comprising the antimicrobial ingredient, the foaming agent, the polymer and the agitating disintegrator. The antimicrobial ingredient, foaming agent and the agitating disintegrator are dispersed and encapsulated in the polymer to form a quick, self-dissolving, foamable antimicrobial tablet, the encapsulated functional ingredient can then be safely transported without the extra water content and with simple containers, causing a great reduction in transportation volume and weight.

Description

QUICK,SELF-DISSOLVING,FOAMABLE ANTIMICROBIAL TABLET AND METHOD OF PREPARATION THEREOF

[0001] This invention describes a self-dissolving, foamable antimicrobial tablet and its preparation method, allowing storage and easy transportation in solid form. Where the storage form will quickly self-dissolve when placed in water to form foamable antimicrobial solution.

[0002] Many functional chemicals exist in liquid form. These liquids often need to be diluted before final consumption and therefore, large volume of water exists in their final products. During storage and transportation of the final products, strong containers are required to prevent spillage and ensure safe transportation. The extra weight from containers and the water content causes increased fuel consumption leading to unnecessary pollution. Moreover, the containers are also often discarded at end-users, further creating wastes and landfill problems. To create a sustainable environment, container wastes must be reduced and recycled. Recent technological advances and environmental policies encourages use of decomposable materials in containers. However, it does not reduce pollution caused by extra fuel consumption during transportation.

[0003] Disintegration tablets that generate cleaning solutions exists in the market as taught by Lau(CN105662902A), and Huang and Zhang(CN110755271A). However, these tablets only use already solid or powderized cleaning agents. Their cleaning solutions also only rely on cleaning agents to remove microbes and do not contain antimicrobial properties. Therefore, limiting the role of disintegration tablets to generate cleaning solutions. This invention describes the encapsulation of liquid antimicrobials to provide a broader application of disintegration tablets to cleaning and antimicrobial products, including disinfectants and rinse-free hand foams.

[0004] The present invention describes a quick and and self-dissolving tablet where upon contact with water, will quickly and completely self-dissolve, which allows a convenient, safe, and environmentally sustainable alternative that generates desirable diluted aqueous solutions at end-use site, compared to the conventional centralized production of dilute formulations.

[0005] Details of the present invention are as follows:

[0006] A quick, self-dissolving, foamable antimicrobial tablet, comprising:

[0007] an antimicrobial ingredient in solid and / or liquid state;

[0008] a water-soluble polymer in solid state;

[0009] an agitating disintegrator;

[0010] a foaming agent;

[0011] wherein the antimicrobial ingredient, the agitation disintegrator and the foaming agent are dispersed and encapsulated in the polymer to form the water-soluble tablet in a solid state.

[0012] Furthermore, the melting point of the functional ingredient is below 120°C.

[0013] Furthermore, the melting point of the polymer is above 45°C and the solubility is less than 1000msolvent / msolute.

[0014] Furthermore, the antimicrobial ingredient is selected from following antimicrobial agents and / or solutions and / or combinations thereof: Quaternary ammonium compounds (QACs), fatty amines, and guanidine- and biguanides-containing compounds; including didecyldimethylammonium chloride (DDAC), benzalkonium chloride (BAC), tetradecyl dimethylbenzyl ammonium chloride （TDBAC），dodecyl dimethyl benzyl ammonium chloride (DDBAC), cetylpyridinium chloride (CPC), lauryl dimenthyl benzyl ammonium chloride (LDBAC), dodecylamine, oleylamine, hexadecylamine, octadecylamine, ethoxylated cocoamine, chlorhexidine, chlorhexidine digluconate, polyhexamethylene biguanide (PHMB) and polyhexamethylene guanidine (PHMG).

[0015] Furthermore, the water-soluble polymer is selected from: polyethylene glycol (PEG), polypropylene glycol (PPG), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), polyhexmethylene biguanide (PHMB), polyethylenimine (PEI) , poloxamers, and / or combinations of above.

[0016] Furthermore, the agitating disintegrator is a combination of acidic and basic salt, whereas the basic salt contains at least one carbonate ion or one bicarbonate ion.

[0017] Furthermore, the acidic salt is monoprotic or diprotic acidic salts selected from: ascorbic acid, lactic acid, sodium dihydrogen phosphate, potassium dihydrogen phosphate, tartaric acid, malic acid, fumaric acid and cinnamic acid.

[0018] Furthermore, the foaming agent is a cationic surfactant, nonionic surfactant and amphoteric surfactant.

[0019] The invention also aims at providing a method of preparation of the said encapsulation system quickly and easily as follows:

[0020] A method of preparation of the quick and self-dissolving antimicrobial tablet, wherein the antimicrobial ingredient and foaming agent are set in a liquid state and the polymer is melted, after which the antimicrobial ingredient and foaming agent are dispersed into the melted polymer, forming a dispersed mixture that subsequently cools and solidifies to form an encapsulated structure, and then is granularized into encapsulated granules, which are combined with the agitating disintegrator and molded into a self-dissolving encapsulated tablet.

[0021] A method of preparation of the quick and self-dissolving antimicrobial tablet, wherein the functional ingredient and foaming agent are set in a liquid state and the polymer is melted, after which the functional ingredient and foaming agent are dispersed into the melted polymer, forming a dispersed mixture that subsequently cools and solidifies to form an encapsulated structure; the encapsulated structure is melted and mixed with the agitating disintegrator, then cooled and molded into a self-dissolving encapsulated tablet.

[0022] Furthermore, the mixture of the antimicrobial ingredient, the foaming agent and the melted polymer is dispersed by sonication.

[0023] This invention provides a solution to reducing waste and pollution by encapsulating functional liquids in their concentrated form and then further converting into solid form, such as tablets. The encapsulated liquid can then be safely transported without the extra water content and with simple containers, causing a great reduction in transportation volume and weight. Upon placing into water, the solid encapsulation can then be self-dissolved at low temperature without the need of any extra agitation from end-user. The tablets are completely dissolvable, leaving no residue and no solid wastes. The dissolved solution is then also readily available for final consumption by end-user.

[0024] The invention is further illustrated in the accompanying drawings as follows.Fig.1

[0025] shows the process of the preparation of quick and self-dissolving encapsulated antimicrobial and foaming agent.Fig.2

[0026] shows the preparation of a quick, self-dissolving, foamable antimicrobial tablet from granulated form in the first embodiment.Fig.3

[0027] shows the preparation of a quick, self-dissolving, foamable antimicrobial tablet from single-solid form in the second embodiment.Fig.4

[0028] shows the optical images of a tablet.Fig.5

[0029] shows an enlarged view of position A in.

[0030] The invention describes an encapsulation antimicrobial ingredient and foaming agent in tablet form where upon contact with water, will completely self-dissolve without the need of any external agitation. It allows a convenient, safe, and environmentally sustainable alternative that generates foamable antimicrobial liquid at end-use site, compared to the conventional centralized production of dilute formulations. It is achieved by first encapsulating the ingredients in concentrated form into molten soluble polymer, followed by incorporating agitating disintegrators. The final system is mouldable and can be moulded into spheres, cubes, or any irregular tablet shape. The invention aims at an environmental friendly and completely dissolvable encapsulation of non-aqueous liquids or highly concentrated aqueous solutions at room temperature. The encapsulated liquids can then be stored and transferred in any solid form, such as cube, tablet, and powder, asandshown.

[0031] Liquids that can be encapsulated include chemicals with melting points below 120°C, solutions where chemicals is / are dissolved in solvents with no more than 90% water, and / or mixtures of liquids of from above. The liquids to be encapsulated will be referred as antimicrobial ingredient and foaming agent. Examples of antimicrobial agents solutions includes the following and / or combinations thereof: Quaternary ammonium compounds (QACs), fatty amines, and guanidine- and biguanides-containing compounds; including didecyldimethylammonium chloride (DDAC), benzalkonium chloride (BAC), tetradecyl dimethylbenzyl ammonium chloride （TDBAC），dodecyl dimethyl benzyl ammonium chloride (DDBAC), cetylpyridinium chloride (CPC), lauryl dimenthyl benzyl ammonium chloride (LDBAC), dodecylamine, oleylamine, hexadecylamine, octadecylamine, ethoxylated cocoamine, chlorhexidine, chlorhexidine digluconate, polyhexamethylene biguanide (PHMB) and polyhexamethylene guanidine (PHMG).

[0032] Encapsulant used are soluble polymers with melting points above 45°C with solubility of less than 1000msolvent / msolute. Where msolventis the mass of solvent required to dissolve one unit of mass of solute (msolute). Examples include polyethylene glycol (PEG), polypropylene glycol (PPG), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP) , polyhexmethylene biguanide (PHMB), polyethylenimine (PEI) and poloxamers.

[0033] The invention is of a fast self-dissolving antimicrobial tablet which forms an antimicrobial liquid that foams when used in accompanied with a foam dispenser. The dissolved antimicrobial solution, accompanied with a foam dispenser, can also be used as a foaming hand sanitizer.

[0034] Antimicrobial materials are delicate chemicals which can quickly react with target-site of microbes such as microbial membrane, resulting in the termination of these microbes or their inability to further infect humans. However, the high-activity of these antimicrobials also resulted in their incompatibility with many chemicals. In this described specific application of the invention, the antimicrobial ingredient, the encapsulation polymer, and the disintegrating agitator are specifically designed to overcome this problem. Moreover, the dissolved solution is further able to have foaming properties, allowing a more efficient and thorough application of disinfection on surfaces, including hands.

[0035] The composition of the fast self-dissolving antimicrobial tablet includes, at least one antimicrobial ingredient, at least one polymer encapsulant, at least two agitators, and at least one foaming agent. The foaming agent can also act as the sole antimicrobial agent within the composition.

[0036] The antimicrobial ingredient are chemicals or solutions with antimicrobial properties with no more than 90% water content. Quaternary ammonium compounds (QACs), fatty amines, and guanidine- and biguanides-containing compounds; including didecyldimethylammonium chloride (DDAC), benzalkonium chloride (BAC), tetradecyl dimethylbenzyl ammonium chloride （TDBAC），dodecyl dimethyl benzyl ammonium chloride (DDBAC), cetylpyridinium chloride (CPC), lauryl dimenthyl benzyl ammonium chloride (LDBAC), dodecylamine, oleylamine, hexadecylamine, octadecylamine, ethoxylated cocoamine, chlorhexidine, chlorhexidine, digluconate, polyhexamethylene biguanide (PHMB) and polyhexamethylene guanidine (PHMG)..

[0037] Encapsulant is any soluble polymer with melting points above 45°C with solubility of less than 1000msolvent / msolute. Examples include polyethylene glycol (PEG), polypropylene glycol (PPG), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), polyhexmethylene biguanide (PHMB), polyethylenimine (PEI) and poloxamers.

[0038] Foaming agent is any cationic surfactant, non-ionic surfactant or amphoteric surfactant, such as cocamidopropyl betaine (CAPB), decyl glucoside, didecyldimethylammonium chloride (DDAC), disodium cocoamphodiacetate, lauryl gucoside, polyquaternium-7 and sodium cocoyl isethionate (SCI). In this invention, the foaming agent is preferably didecyldimethylammonium chloride (DDAC).

[0039] Agitating disintegrators are a combination of acidic and basic salt, whereas the basic salt contains at least one carbonate ion or one bicarbonate ion. Upon dissolving in water, these salts react to release carbon dioxide, thereby creating an uplifting force that agitates the solution. Due to cationic nature of the antimicrobial agent and foaming agent, the acidic salt must be monoprotic or diprotic acidic salts, such as ascorbic acid, lactic acid, sodium dihydrogen phosphate, potassium dihydrogen phosphate, tartaric acid, malic acid, fumaric acid and cinnamic acid. Triprotic acidic salts, such as citric acid is excluded from the specified application as the resultant trianion will attract, tangle up and precipitate with the antimicrobial ingredients and foaming agents within the composition.

[0040] Referring to, to prepare for the fast self-dissolving antimicrobial tablet, polymer encapsulant is first molten and mixed with the antimicrobial agent and foaming agent. The mixture is further homogenized by sonication to form colloid. The colloid is then allowed to cool and solidify for encapsulation. The solidified colloid is then crushed by blending or grinding to form encapsulated granules. Agitators are then mixed thoroughly with the granulated capsules. The resultant mixture is then compressed by tablet press to form the final tablets, asshown. An alternate method, if the solidified colloid is not crushed, it is brought back to melt by heating, followed by addition of the agitators, forming a liquid-solid slurry. The slurry is then quickly transferred into desirable moulds and cooled, forming the final tablet, asshown.

[0041] Example 1

[0042] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.5ml of 80% DDAC is added into the molten polymers under stirring, followed by sonication, foaming a DDAC-Polymer colloid. After cooled, the solidified colloid is then blended into granules, followed by mixing 1.5g sodium bicarbonate and 3g lactic acid. The mixture is then tablet pressed into a solid tablet.

[0043] Example 2

[0044] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.1ml of 20% PHMB is added into the molten polymers under stirring, followed by sonication, foaming a PHMB-Polymer colloid. After cooled, the solidified colloid is then blended into granules, followed by mixing 1.5g sodium bicarbonate and 3g ascorbic acid. The mixture is then tablet pressed into a solid tablet.

Claims

A quick, self-dissolving, foamable antimicrobial tablet, comprising:an antimicrobial ingredient in solid and / or liquid state;a water-soluble polymer in solid state;an agitating disintegrator;a foaming agent;wherein the antimicrobial ingredient, the agitation disintegrator and the foaming agent are dispersed and encapsulated in the polymer to form the water-soluble tablet in a solid state.The quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the melting point of the antimicrobial ingredient is below 120°C.The quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the melting point of the polymer is above 45°C and the solubility is less than 1000msolvent / msolute.The quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the antimicrobial ingredient is selected from following antimicrobial agents and / or solutions and / or combinations thereof: Quaternary ammonium compounds (QACs), fatty amines, and guanidine- and biguanides-containing compounds; including didecyldimethylammonium chloride (DDAC), benzalkonium chloride (BAC), tetradecyl dimethylbenzyl ammonium chloride （TDBAC），dodecyl dimethyl benzyl ammonium chloride (DDBAC), cetylpyridinium chloride (CPC), lauryl dimenthyl benzyl ammonium chloride (LDBAC), dodecylamine, oleylamine, hexadecylamine, octadecylamine, ethoxylated cocoamine, chlorhexidine, chlorhexidine digluconate, polyhexamethylene biguanide (PHMB) and polyhexamethylene guanidine (PHMG).The quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the water-soluble polymer is selected from: polyethylene glycol (PEG), polypropylene glycol (PPG), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), polyhexmethylene biguanide (PHMB), polyethylenimine (PEI), poloxamers, and / or combinations of above.The quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the agitating disintegrator is a combination of acidic and basic salt, whereas the basic salt contains at least one carbonate ion or one bicarbonate ion.The quick, self-dissolving, foamable antimicrobial tablet of claim 6, wherein the acidic salt is monoprotic or diprotic acidic salts selected from: ascorbic acid, lactic acid, sodium dihydrogen phosphate, potassium dihydrogen phosphate, tartaric acid, malic acid, fumaric acid and cinnamic acid.The quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the foaming agent is a cationic surfactant, nonionic surfactant and amphoteric surfactant.A method of preparation of the quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the antimicrobial ingredient and foaming agent are set in a liquid state and the polymer is melted, after which the antimicrobial ingredient and foaming agent are dispersed into the melted polymer, forming a dispersed mixture that subsequently cools and solidifies to form an encapsulated structure, and then is granularized into encapsulated granules, which are combined with the agitating disintegrator and molded into a self-dissolving encapsulated tablet.A method of preparation of the quick, self-dissolving, foamable antimicrobial tablet of claim 1, wherein the antimicrobial ingredient and foaming agent are set in a liquid state and the polymer is melted, after which the antimicrobial ingredient and foaming agent are dispersed into the melted polymer, forming a dispersed mixture that subsequently cools and solidifies to form an encapsulated structure; the encapsulated structure is melted and mixed with the agitating disintegrator, then cooled and molded into a self-dissolving encapsulated tablet.The method of preparation of claim 9 or claim 10, wherein the mixture of the antimicrobial ingredient, the foaming agent, and the melted polymer is dispersed by sonication.

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