A self-dissolving encapsulation system, a method of preparation and a self-dissolving tablet thereof

Abstract

A self-dissolving encapsulation system, a preparation method and a self-dissolving tablet thereof, comprising the functional ingredient and the polymer, the functional ingredient is dispersed and encapsulated in the polymer to form the water-soluble encapsulation system in a solid state, 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

A SELF-DISSOLVING ENCAPSULATION SYSTEM, A METHOD OF PREPARATION AND A SELF-DISSOLVING TABLET THEREOF

[0001] This invention describes a self-dissolving encapsulation system and a preparation method, allowing storage and easy transportation in solid form. Where the storage form will quickly self-dissolve when placed in water.

[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] The present invention describes a self-dissolving encapsulation system where upon contact with water, will 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.

[0004] Details of the present invention are as follow:

[0005] A self-dissolving encapsulation system, comprising:

[0006] a functional ingredient in solid and / or liquid state;

[0007] a water-soluble polymer in solid state;

[0008] wherein the functional ingredient is dispersed and encapsulated in the polymer to form the water-soluble encapsulation system in a solid state.

[0009] Furthermore, the melting point of the functional ingredient is below 120°C.

[0010] Furthermore, the melting point of the polymer is above 45°C and the solubility is less than 1000msolvent / msolute.

[0011] Furthermore, the solid encapsulation system is granularized into encapsulated granules.

[0012] Furthermore, the functional 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).

[0013] Furthermore, the functional ingredient is essential oils, solvents, fragrances, herbal extracts, aroma therapy blends, microbial suspensions, nutrient broths and probiotics.

[0014] 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.

[0015] The invention also aims at providing a method of preparation of the said encapsulation system quickly and easily as follows:

[0016] A method of preparation of the encapsulation system, the functional ingredient is set in a liquid state and the polymer is melted, after which the functional ingredient is dispersed into the melted polymer, forming a dispersed mixture that subsequently cools and solidifies into a solid state.

[0017] Furthermore, the mixture of the functional ingredient and the melted polymer is dispersed by sonication.

[0018] And the invention further provides A self-dissolving tablet prepared by the above preparation method as follow:

[0019] An agitating disintegrator is provided; the functional ingredient and the agitation disintegrator are dispersed and encapsulated in the polymer to form the water-soluble tablet in a solid state; 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.

[0020] An agitating disintegrator is provided; the water-soluble encapsulation system is granularized into encapsulated granules, mixed with the agitating disintegrator and molded into a self-dissolving encapsulated tablet; 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.

[0021] 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.

[0022] The invention is further illustrated in the accompanying drawings as follows.Fig.1

[0023] shows the process of the preparation of self-dissolving encapsulation system.Fig.2

[0024] shows the preparation of self-dissolving tablet from granulated encapsulated system in the first embodiment.Fig.3

[0025] shows the preparation of a self-dissolving tablet from encapsulated system in the second embodiment.Fig.4

[0026] shows the optical images of a solidified encapsulate.Fig.5

[0027] shows an enlarged view of position A in.

[0028] The invention describes an encapsulation system 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 desirable diluted aqueous solutions at end-use site, compared to the conventional centralized production of dilute formulations. It is achieved by first encapsulating the desirable liquid 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. Depending on the encapsulated functional ingredient, the liquid-encapsulated solids can be used as aroma-releasing tablets, or after suspending in water to self-dissolve into detergents, disinfectants, pest repellents, colloidal aromatic solutions, probiotic solutions and microbial culture.

[0029] Liquids that can be encapsulated include chemicals with melting points below 120°C, solutions where chemicals are dissolved in solvents with no more than 90% water, and / or mixtures of liquids of from above. The ingredient to be encapsulated will be referred as functional ingredient. Examples of functional ingredients include (a) essential oils such as agarwood oil, benzoin oil, bergamot oil, cajuput oil, cananga oil, chamomile oil, cedar oil, china rose oil, cinnamon bark oil, citron oil, citronella oil, clove oil, eucalyptus oil, fennel oil, geranium oil, ginger oil, grapefruit oil, green tea oil, helichrysum oil, jasmine oil, kaffir lime oil, lavender oil, lemon oil, lemongrass oil, lime oil, marjoram oil, mugwort oil, musk oil, myrrh oil, neem oil, neroli oil, nutmeg oil, olliumxanthorrhiza oil, orange oil, origanum oil, orris oil, palmarosa oil, patchouli oil, peppermint oil, petitgrain oil, rose oil, rosemary oil, rosewood oil, sandalwood oil, tea tree oil, thyme oil, verbena oil, vetiver oil and combinations thereof; (b) solvents such as water, ethanol, carrier oils, glycerol; (c) fragrances and perfumes that combines essential oils, solvents, and aromatic compounds; (d) liquids with dissolved polymers or chemicals, such as polyethylene glycol (PEG) solutions, polypropylene glycol (PPG) solutions, polyhexmethylene biguanide (PHMB) solutions, poloxamer solutions, sodium lauryl sulphate solutions, cocamidopropyl betaine solutions, sodium chlorite solutions, hypochlorite solutions, picaridin solution, N,N-diethyl-m-toluamide solution; (e) liquid suspensions such as herbal extracts, aroma therapy blends，microbial suspensions, nutrient broths and probiotics, etc; and (f) antimicrobial agents such as 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).

[0030] 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.

[0031] Referring to, the first stage of self-dissolving liquid encapsulation system consists of encapsulating the functional ingredient. Soluble polymers were first melted into liquid form by heating. At this stage, compatible polymers, such as polypropylene glycol (PPG) to PEG, poloxamer 403 to poloxamer 407, can be added to facilitate melting (as heat conductor) and encapsulation (as surfactant). When molten, functional ingredient is added under vigorous stirring. The functional ingredient is then further dispersed by sonication. The mixture is then cooled and removed from mould forming an encapsulated solid. The solid can then be further broken down into granules by physical means such as blending or grinding.

[0032] Referring toand, in the second stage of preparation of self-dissolving liquid encapsulation system, agitating disintegrators are introduced into the encapsulated functional ingredient from first stage. 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.

[0033] Depending on the state of the encapsulated functional ingredient, different approach is used to introduce the agitators into the encapsulation.

[0034] If the encapsulation is granulated form, the agitators are first mixed thoroughly with the granulated capsules, followed by compressing by tablet press to form the final tablet. If the encapsulation is a single-solid form, the encapsulation is first heated to melt. While molten, the agitators are then added and mixed, forming a liquid-solid slurry. The slurry is then quickly transferred into desirable moulds and cooled, forming the final tablet.

[0035] 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.

[0036] To prepare for the self-dissolving tablet, polymer encapsulant is first molten and mixed with the functional ingredient. 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. 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.

[0037] Example 1

[0038] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.1ml clove oil is added into the molten polymers under stirring, followed by sonication. The solution is transferred to mould and cooled.

[0039] Example 2

[0040] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.06ml China Rose oil and 0.03ml orris oil is added into the molten polymers under stirring, followed by sonication. The solution is transferred to mould and cooled.

[0041] Example 3

[0042] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.1ml fragrance liquid is added into the molten polymers under stirring, followed by sonication. The solution is transferred to mould and cooled.

[0043] Example 4

[0044] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.1g herbal extract is added into the molten polymers under stirring, followed by sonication. The solution is transferred to mould and cooled.

[0045] Example 5

[0046] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. then cool down to 50°C , 0.1ml Escherichia coli suspensions with 10g / L PEG is added into the molten polymers under stirring then the solution is transferred to mould immediately and cooled.

[0047] Example 6

[0048] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.06ml China Rose oil and 0.03ml orris oil is added into the molten polymers under stirring, followed by sonication. After cooled, the solidified encapsulation is then blended into granules, followed by mixing 1.5g sodium bicarbonate and 3g citric acid. The mixture is then tablet pressed into a solid tablet.

[0049] Example 7

[0050] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.1ml fragrance liquid is added into the molten polymers under stirring, followed by sonication. After cooled, the solidified encapsulation is then blended into granules, followed by mixing 1.5g sodium bicarbonate and 3g citric acid. The mixture is then tablet pressed into a solid tablet.

[0051] Example 8

[0052] A mixture of 4.6g PEG and 1g PPG is heated up to 100°C. 0.1g herbal extract is added into the molten polymers under stirring, followed by sonication. After cooled, the solidified encapsulation is then blended into granules, followed by mixing 1.5g sodium bicarbonate and 3g citric acid. The mixture is then tablet pressed into a solid tablet.

[0053] Example 9

[0054] 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.

Claims

A self-dissolving encapsulation system, comprising:a functional ingredient in solid and / or liquid state;a water-soluble polymer in solid state;wherein the functional ingredient is dispersed and encapsulated in the polymer to form the water-soluble encapsulation system in a solid state.The encapsulation system of claim 1, wherein the melting point of the functional ingredient is below 120°C.The encapsulation system of claim 1, wherein the melting point of the polymer is above 45°C and the solubility is less than 1000msolvent / msolute.The encapsulation system of claim 1, wherein the solid encapsulation system is granularized into encapsulated granules.The encapsulation system of claim 1, wherein the functional 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 encapsulation system of claim 1, wherein the functional ingredient is essential oils, solvents, fragrances, herbal extracts, aroma therapy blends, microbial suspensions, nutrient broths and probiotics.The encapsulation system 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.A method of preparation of the encapsulation system of claim 1, wherein the functional ingredient is set in a liquid state and the polymer is melted, after which the functional ingredient is dispersed into the melted polymer, forming a dispersed mixture that subsequently cools and solidifies into a solid state.The method of preparation of the encapsulation system of claim 8, wherein the mixture of the functional ingredient and the melted polymer is dispersed by sonication.A self-dissolving tablet prepared by the preparation method of claim 1, wherein,an agitating disintegrator is provided;the functional ingredient and the agitation disintegrator are dispersed and encapsulated in the polymer to form the water-soluble tablet in a solid state;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.A self-dissolving tablet prepared by the preparation method of claim 1, wherein,an agitating disintegrator is provided;the water-soluble encapsulation system is granularized into encapsulated granules, mixed with the agitating disintegrator and molded into a self-dissolving encapsulated tablet;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.

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