JP2005146003A - Carrier - Google Patents

Abstract

A carrier comprising an active ingredient and an activity promoting ingredient that activates a microorganism or an enzyme, wherein the active ingredient is released by the microorganism or the enzyme.
[Effects] According to the present invention, it is possible to provide a carrier having excellent initial expression, sustained release, sustainability, and action control of an active ingredient, and a composition containing the carrier.
[Selection figure] None

Description

  The present invention relates to a carrier that promotes and sustains the expression of active ingredients by the action of microorganisms or enzymes.

  The active ingredient represented by a fragrance | flavor component, a pigment | dye, a bactericidal component, a medicinal effect ingredient, etc. is desired for the sustained active expression and the active expression in arbitrary places and time. On the other hand, physical adsorption and retention of chemical affinity with the support (for example, see Patent Document 1: JP 59-175402 A), matrix structure of partition walls, porous structure, polymerization degree, etc. (For example, refer to Patent Document 2: Japanese Patent Application Laid-Open No. 63-178840) has proposed a technique in which an active ingredient is retained and the ingredient is gradually released in a natural diffusion manner. However, the reduction of supported components due to natural diffusion has always been a problem.

  A technique for controlling the diffusion by coating the surface of the support to cope with the problem of reduction of the support component due to natural diffusion has been proposed (see Patent Document 3: Japanese Patent Application Laid-Open No. 60-16914), but has excellent sustainability. However, there is a problem in the initial expression of activity when in contact with microorganisms or enzymes.

  On the other hand, as the active ingredient release control technology, the destruction and release of the carrier by physical force (for example, see Patent Document 4: Japanese Patent Laid-Open No. 52-86411), and the control by pH (for example, Patent Document 5: Japanese Patent Application Laid-Open No. 2005-86400). Sho 61-28440), controlled by salt concentration (Patent Document 6: JP 03-504968), controlled by surfactant (Patent Document 7: JP 07-506137) Etc.) have been proposed, but both require physical and chemical factors to be changed, and there are significant restrictions on the expression of activity.

  Moreover, as an active ingredient release control technique in which a biological activity is involved, a sustained release technique at the time of internal use with an indigestible component (for example, refer to Patent Document 8: Japanese Patent Laid-Open No. 04-124126) and solubility in saliva. Intraoral sustained release techniques (for example, see Patent Document 9: Japanese Patent Publication No. 56-500848) have been proposed, but all are techniques related to sustainability and have a problem in initial activity expression.

JP 59-175402 A JP-A-63-178840 Japanese Patent Laid-Open No. 60-16914 JP 52-86411 A JP-A-61-28440 Japanese translation of National Publication No. 03-504968 JP 07-506137 A JP 04-124126 A JP-T 56-500848

  The present invention has been made in view of the above circumstances, and an object of the present invention is to provide a carrier excellent in initial expression, sustained release, sustainability, and action controllability of an active ingredient, and a composition containing the carrier. And

  As a result of intensive studies to achieve the above object, the present inventor has controlled the expression of the active ingredient by causing the microorganism or enzyme to act on the support containing the active ingredient and the activity promoting ingredient that activates the microorganism or the enzyme. It has been found that this is possible, and the present invention has been made.

  That is, the active ingredient carrier of the present invention is a microorganism or enzyme produced by allowing a microorganism or enzyme present in the human body or the environment to act on a carrier in which an active ingredient and an activity promoting component that activates the microorganism or enzyme are mixed. It is surmised that the mild organic substance decomposing action possessed by this shows the sustained release action of the supported active ingredient.

Accordingly, the present invention provides [1] a carrier comprising an active ingredient and an activity promoting ingredient that activates a microorganism or an enzyme, wherein the active ingredient is released by the microorganism or the enzyme,
[2] The carrier according to [1], wherein the carrier comprises a core substance and a wall film, and the core substance contains an active ingredient.
[3] The carrier according to [1] or [2], wherein the active ingredient is one or more selected from a fragrance, a pigment, a bactericidal component and a medicinal component,
[4] Any one of [1] to [3], wherein the activity promoting component is one or more selected from divalent metal compounds, chlorides, nonionic surfactants and amphoteric surfactants. A carrier according to claim 1,
[5] A composition containing the carrier according to any one of [1] to [4] is provided.

  ADVANTAGE OF THE INVENTION According to this invention, the carrier which was excellent in the initial stage expression property of an active ingredient, sustained release property, sustainability, and the effect controllability, and the composition containing this carrier can be provided.

Hereinafter, the present invention will be described in more detail.
The carrier of the present invention contains an active ingredient and an activity promoting substance that activates microorganisms or enzymes, and the active ingredient activates the microorganisms or enzymes to release an effective amount of the active ingredients. is there.

  The active ingredient of the present invention is not particularly limited as long as it exhibits actions such as chemical action, physical action, physiological action, and psychological action. Specific examples include aroma components, taste components, pigment components, physiologically active components, cleaning components, softening components, antioxidant components, antibacterial components, deodorizing components, catalytic components, medicinal components, enzymes, and the like. In this invention, these can be used individually by 1 type or in combination of 2 or more types as appropriate. In particular, it is preferable to use a fragrance, a pigment, a bactericidal component and a medicinal component.

  The blending amount of the active ingredient is preferably 0.00001% by mass, more preferably 0.0001% by mass, and particularly preferably 0.001% by mass in the total amount of the support. The upper limit is preferably 70% by mass, more preferably 50% by mass, and particularly preferably 30% by mass. If the blending amount is too small, the effect may not be exhibited. If the blending amount is too large, it may not be supported, and inconveniences such as poor controllability of activity expression may occur.

  The activity promoting component that promotes the activity of the microorganism or enzyme is appropriately selected depending on the combination with the active component. For example, calcium phosphate, magnesium phosphate, zinc phosphate, zinc acetate, magnesium acetate, magnesium sulfate, zinc sulfate, etc. Divalent metal compounds, chlorides such as sodium chloride, calcium chloride, zinc chloride, magnesium chloride, nonionic surfactants such as polyoxyethylene alkyl ethers and polyoxyethylene phosphates, carboxybetaine amphoteric surfactants, ascorbine Ascorbic acids such as sodium acid, magnesium ascorbate, and potassium ascorbate, thiamine, riboflavin, pyridoxine, cobalamin, niacin, folic acid, pantothenic acid and other vitamin B groups, cysteine, glutathione, and the like.

  The blending amount of the activity promoting component is preferably 0.0001% by mass and more preferably 0.001% by mass in the total amount of the support. The upper limit is preferably 30% by mass, more preferably 10% by mass. If it is less than 0.0001% by mass, a sufficient activity promoting effect may not be observed, and if it exceeds 30% by mass, it may be difficult to form a carrier.

  As the other components constituting the carrier, any known substance can be used. Examples of organic substances include natural polymers such as gelatins, agar, sodium alginate, starches, cyclodextrins, carrageenan, gellan gum, curdlan, pectin, and celluloses. Among these, gelatins, starches, cyclodextrins, and celluloses are preferable.

  The other components constituting the carrier are combined with inorganic substances such as silicate compounds such as sodium silicate, calcium silicate and magnesium silicate, and borate compounds such as sodium borate, calcium borate and magnesium borate. Also good. In the present invention, the organic substances can be used singly or in appropriate combination of two or more, and in combination of one or more inorganic substances.

  In addition, synthetic polymer compounds such as acrylic acid polymers such as methyl acrylate, ethyl acrylate, polymethyl methacrylate, and polyethyl methacrylate, melamine resins, polyurethane resins, and epoxy resins, which are a mixture of organic and inorganic substances, are also used. These can be used singly or in appropriate combination of two or more.

  The lower limit of the amount of other components constituting the carrier is preferably 5% by mass, more preferably 10% by mass, and particularly preferably 15% by mass in the total amount of the carrier. The upper limit is preferably 90% by mass, more preferably 85% by mass, and particularly preferably 80% by mass.

  As microorganisms and enzymes used in the present invention, those present in the human body, food and living environment, or those used in fermentation production, food production processing, pharmaceutical production, quasi-drug production, cosmetic production Any known one can be used.

  For example, enterobacteria such as Lactobacillus genus, Lactococcus genus, skin resident fungi such as Propionibacterium genus, Staphylococcus genus, industrial microorganisms such as Saccharomyces genus and Bacillus genus, enzymes include protease, peptidase, amylase, Cellulase, pullulanase, pectinase, lipase, esterase, oxidase and the like can be mentioned, but are not limited thereto. As a microorganism or an enzyme, these can be used individually by 1 type or in combination of 2 or more types as appropriate.

  The combination of the activity promoting component and the microorganism or enzyme is preferably a divalent metal compound and a resident skin bacterium, chloride and amylase, a nonionic surfactant and cellulase, or a divalent metal compound and pretease.

The particle size of the carrier is not particularly limited and may be appropriately selected depending on the intended purpose. The lower limit is preferably 2 μm, more preferably 50 μm. The upper limit is preferably 3000 μm,
More preferably, it is 2500 μm. If the particle size of the carrier is less than 2 μm, it may be difficult to prepare the carrier and may aggregate during production. If it exceeds 3000 μm, it will be difficult to uniformly disperse in the preparation, and the appearance and feel May get worse.

  The particle diameter of the carrier can be confirmed with an optical microscope observation, a particle size distribution measuring instrument, a sieve, etc. In the present invention, the average particle diameter of 2 to 50 μm is the average of 50 to 500 μm as observed with an optical microscope. The particle size was measured using LDSA-1400A (manufactured by Tohnichi Computer Applications Co., Ltd.), and the average particle size of 500 to 3000 μm was measured using a sieve.

  The carrier of the present invention is preferably a microcapsule in which the carrier is composed of a core substance and a wall film, and the core substance contains an active ingredient. The core substance contains an active ingredient, but may contain an activity promoting ingredient, and it is preferable that the wall membrane contains an activity promoting ingredient from the viewpoint of promoting the release of the active ingredient. In the case of microcapsules, the core material is released by breaking the wall membrane with microorganisms or enzymes. When the activity promoting component is contained in the wall membrane, the activity promoting component in the wall membrane increases the activity of the microorganism or enzyme by contacting with the microorganism or the enzyme, and promotes the decomposition of the wall membrane to promote the activity of the core substance. Ingredients are released.

  As long as the effects of the present invention are not hindered, the core substance of the present invention can be appropriately mixed with the following components other than the above active ingredients. For example, in the case of organic substances, oils, alcohols, hydrocarbons, organic acids, fatty acids, anionic surfactants, nonionic surfactants and amphoteric surfactants other than activity promoting components, polyols, silicone compounds and the like can be mentioned. Examples of inorganic substances include silicate compounds such as metal oxides and zeolites. Among these, it is preferable to blend an oil, a silicone compound, and polyols.

  As a component constituting the wall film containing the core substance, other components constituting the carrier, such as a polymer compound, can be used, and an activity promoting component may be included.

  The microcapsule may have a single-core structure as the core material, or may have a multi-core structure encapsulated in the wall film in a state where a large number of fine particles made of the core material are dispersed.

  The ratio of the core material to the wall film is not particularly limited, but it is usually preferable that the core material: wall film = 10: 90 to 95: 5, particularly 15:85 to 90:10 in terms of mass ratio. It is. If the ratio of the core substance is too large, it may be difficult to hold it in the carrier, and if it is too small, it may be difficult to release the core substance.

  The average particle diameter of the core material particles of the present invention is not particularly limited, but the lower limit is preferably 0.01 μm, more preferably 0.1 μm. The upper limit is preferably 2995 μm, more preferably 2990 μm. If the particle size of the core substance is too large, the support may be broken when the support is blended into the composition, and the core substance may not be retained. If it is too small, the effect when the core substance is released is weak. There is a case. The measuring method of the particle diameter can be confirmed by optical microscope observation, particle size distribution measuring instrument, sieve, etc. In the present invention, the average particle diameter of 2-50 μm is the average particle diameter of 50-500 μm. The diameter was measured using LDSA-1400A (manufactured by Tohnichi Computer Applications Co., Ltd.), and the average particle size of 500 to 3000 μm was measured using a sieve.

  The method for supporting the active ingredient in the carrier is not particularly limited, but can be obtained by mixing and molding the active ingredient and the activity promoting ingredient. For example, it can be efficiently prepared by the microencapsulation method shown below. Specifically, the active ingredient can be encapsulated by a microencapsulation method such as a phase separation method, an orifice method, a liquid curing method, a spray cooling method, or the like, but is not limited thereto.

  The phase separation method is a water-containing state in which an active ingredient is dispersed in an aqueous phase containing a carrier component and the particle size is adjusted, and then the carrier in the aqueous phase is phase-separated by pH or inorganic salt and adsorbed on the active ingredient. This is a method for obtaining a carrier.

  The in-liquid curing method is a method in which an aqueous phase containing a carrier component in which an active ingredient is dispersed in a dispersion medium such as fat or oil is dispersed to adjust the particle diameter, and then the aqueous phase is cooled and solidified, and then the dispersion medium is separated and removed. In this way, a water-containing carrier is obtained.

  In the orifice method, an aqueous phase containing a carrier component in which an active ingredient is dispersed is dropped into a dispersion medium such as fats and oils, and the aqueous phase is cooled and solidified. How to get.

  The spray cooling method is a method for obtaining a water-containing carrier by spraying an aqueous phase containing a carrier component in which an active ingredient is dispersed, cooling and solidifying the aqueous phase, and collecting the aqueous phase.

  In the present invention, the phase separation method and the spray cooling method are particularly preferable.

  The composition of the present invention is a composition containing the carrier. The carrier of the present invention is applied to skin, hair, oral cavity, etc., for example, cream, hand cream, milky lotion, lotion, soap, hand soap, body soap, antiperspirant, athlete's foot drug, acne treatment agent, Skin preparations such as disinfectants, whitening agents, patches, packs, eye drops, shampoos, rinses, treatments, tonics, hair restorers, hair gels, hair waxes, hair creams, hair foams, hair sprays, hair waters It can be applied to oral compositions such as a preparation, a toothpaste, a mouthwash, and a gingival massage cream.

  In addition, the carrier of the present invention can be applied to clothing compositions, kitchen compositions, residential compositions, and the like, such as clothes detergents, clothes detergent pretreatment agents, athletic shoe detergents, softeners, bleaching agents. , Rinse agent, water repellent, anti-static agent, dish detergent, vegetable detergent, range detergent, automatic dishwasher detergent, toilet detergent, bathroom tub detergent, window detergent, furniture / floor / tatami mat It can be applied to detergents, indoor fragrance deodorants, air conditioner cleaning deodorants, and the like. Furthermore, the carrier of the present invention can be applied to all functional foods including foods for specified health use, nutritional functional foods and the like.

  In this case, the composition of the present invention can be prepared by a conventional method using known blending components according to the type, dosage form, etc. of the preparation. For example, surfactants, oils, alcohols, moisturizers, thickeners, preservatives, chelating agents, pH adjusters, fragrances, pigments, UV absorbers / scatterers, vitamins, water, etc. can do. The optional component is not limited to these. Moreover, in addition to the said active ingredient, the deodorant, preservative, antioxidant, etc. which are generally used can be mix | blended with the composition of this invention together.

The present invention is expected to be able to control the site of activity expression by the location of the microorganism or enzyme to be combined, such as on the skin or in the oral cavity. Furthermore, high safety can be expected for a living body by using a carrier, a working microorganism, or an enzyme derived from a living body or food.
Therefore, the carrier of the present invention can be used for various uses such as pharmaceuticals, quasi drugs, cosmetics, foods, and detergents.

  EXAMPLES Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, unless otherwise specified, “%” indicates mass%, and the ratio indicates mass ratio.

[Preparation Example 1]
Perfume-carrying methylcellulose microcapsule-1
The fragrance | flavor 1 described in following Tables 8-18 was prepared by the phase-separation method using 150 mass parts, polyoxyethylene oleyl ether (HLB13.6) 10 mass parts, and methylcellulose 19.5 mass parts as an active ingredient. The mass ratio of polyoxyethylene oleyl ether to methylcellulose in the prepared fragrance carrier is 1:39.

[Preparation Comparative Example 1]
Fragrance-carrying methylcellulose microcapsule-2
The fragrance | flavor 1 described in following Tables 8-18 was prepared by the phase-separation method using 150 mass parts and 20 mass parts of methylcellulose as an active ingredient.

[Preparation Example 2]
Mulberry extract supported hardened gelatin film microcapsule-1
Mulberry extract in which mulberry root bark ethanol extract solid was dissolved in isopropyl myristate was used as an active ingredient. 30 parts by mass of the active ingredient to which 300 mM of the activity promoting ingredient calcium phosphate was added was encapsulated by a phase separation method using 5 parts by mass of gelatin and 1 part by mass of pectin. Then, it hardened | cured with 0.1 mass part of glutaraldehyde.

[Preparation Comparative Example 2]
Mulberry extract supported hardened gelatin film microcapsule-2
Using a mulberry extract obtained by dissolving a solid extract of mulberry root bark ethanol in isopropyl myristate as an active ingredient, 30 parts by mass of the above-mentioned active ingredient not containing an activity promoting ingredient calcium phosphate is phase-separated using 5 parts by mass of gelatin and 1 part by mass of pectin. Encapsulated by law. Then, it hardened | cured with 0.1 mass part of glutaraldehyde.

[Preparation Example 3]
Perfume-carrying methyl esterified starch-1
100 parts by mass of perfume 3 listed in Tables 19 to 26, 295 parts by mass of methyl esterified starch, and 5 parts by mass of calcium chloride dihydrate were mixed and molded.

[Preparation Comparative Example 3]
Perfume-carrying methyl esterified starch-2
100 parts by mass of perfume 3 described in Tables 19 to 26 and 300 parts by mass of methyl esterified starch were mixed and molded.

[Example 1, Comparative Example 1]
Hair cream blended with a fragrance carrier A hair cream having the composition shown in Table 1 was prepared according to a conventional method, and the strength of the scent when applied to the hair was evaluated. Evaluation was performed by 5 subjects from 1 hour to 48 hours after application based on the following evaluation criteria. The results are also shown in Table 1.

<Evaluation criteria>
++: Feels fragrance strongly ＋: Feels fragrance ±: Feels fragrance slightly −: Does not feel fragrance

＊１ プロモイスＳＩＬＫ７００ＩＧ（（株）成和化成製）
＊２ カルボポール１３４２（グッドリッチ社製）

* 1 Promois SILK700IG (manufactured by Seiwa Kasei Co., Ltd.)
* 2 Carbopol 1342 (Goodrich)

  From the results shown in Table 1, it was confirmed that the carrier of the present invention (Example 1) has higher scent early development and sustainability than Comparative Example 1.

[Example 2, Comparative Example 2]
Aerosol-type antiperspirant formulated with a deodorant component carrier composition An aerosol-type antiperspirant having the composition shown in Table 2 was prepared based on a conventional method. The deodorizing effect of body odor generated by oxidation when the obtained aerosol type antiperspirant was applied to the armpit was evaluated. Evaluation was performed by 5 subjects from 1 hour to 6 hours after application based on the following evaluation criteria. The results are also shown in Table 2.

<Evaluation criteria>
++: Feels odor strongly ＋: Feels odor ±: Feels odor slightly −: Does not feel odor

  From the results shown in Table 2, it was confirmed that the carrier of the present invention (Example 2) had a quicker deodorizing effect and higher sustainability than Comparative Example 2.

[Example 3]
Toilet detergent blended with a fragrance carrier A toilet detergent having the composition shown in Table 3 was prepared according to a conventional method. Using the obtained toilet detergent, the fragrance was evaluated by the following method. The results are also shown in Table 3.

  Apply an aqueous amylase solution (containing 0.5% by mass of Duramil 60T (Amorase manufactured by Novo Nordisk)) uniformly to the toilet bowl in a Western style flush toilet, thoroughly dry the water and adsorb amylase, and then use 20 mL of toilet detergent. The strength of the scent when the inside of the toilet bowl was washed using was evaluated. The evaluation of fragrance was evaluated by sensory evaluation by three specialist panels until 1 day, 3 days and 7 days after washing based on the following evaluation criteria.

<Evaluation criteria>
++: Feels fragrance strongly ＋: Feels fragrance ±: Feels fragrance slightly −: Does not feel fragrance

＊１：ケルザンＴ：メルク社製（Ｍｗ＝約２００万）

* 1: Kelzan T: manufactured by Merck & Co. (Mw = about 2 million)

  From the results of Table 3, it was confirmed that the carrier of the present invention (Example 3) had higher scent early expression and sustainability than Comparative Example 3.

[Examples 4 to 9]
Hereinafter, the formulation example which mix | blended the active ingredient support body composition of this invention is shown.
Each was prepared based on the conventional method of preparation.

＊１：活性成分をグルコン酸クロルヘキシジン、活性促進成分として塩化マグネシウムを用いた以外は調製実施例２と同様に調製した。
＊２：香料１に、ジブチルヒドロキシトルエンを０．００１％添加したもの。

* 1: Prepared in the same manner as in Preparation Example 2 except that chlorhexidine gluconate was used as the active ingredient and magnesium chloride was used as the activity promoting ingredient.
* 2: Perfume 1 with 0.001% dibutylhydroxytoluene added.

＊１：活性成分をイソプロピルメチルフェノール、活性促進成分として塩化ナトリウムを用いた以外は調製実施例３と同様に調製した。
＊２：香料１に、ジブチルヒドロキシトルエンを０．００１％添加したもの。

* 1: Prepared in the same manner as in Preparation Example 3 except that isopropylmethylphenol was used as the active ingredient and sodium chloride was used as the activity promoting ingredient.
* 2: Perfume 1 with 0.001% dibutylhydroxytoluene added.

＊１：活性成分をスペアミントオイル、活性促進成分としてリン酸カルシウムを用いた以外は調製実施例２と同様に調製した。
＊２：特願２００２−１０４２４０号の香料２に、ジブチルヒドロキシトルエンを０．００１％添加したもの。

* 1: Prepared in the same manner as in Preparation Example 2 except that spearmint oil was used as the active ingredient and calcium phosphate was used as the activity promoting ingredient.
* 2: A product obtained by adding 0.001% of dibutylhydroxytoluene to fragrance 2 of Japanese Patent Application No. 2002-104240.

＊１：ＫＦ６０１２（信越化学工業（株）製）
＊２：活性成分を香料１、活性促進成分として塩化カルシウム二水和物を用いた以外は調製実施例３と同様に調製した。

* 1: KF6012 (manufactured by Shin-Etsu Chemical Co., Ltd.)
* 2: Prepared in the same manner as in Preparation Example 3 except that the active ingredient was perfume 1 and calcium chloride dihydrate was used as the activity promoting ingredient.

Claims (5)

  A carrier comprising an active ingredient and an activity promoting component that activates a microorganism or an enzyme, wherein the active ingredient is released by the microorganism or the enzyme.   2. The carrier according to claim 1, wherein the carrier comprises a core substance and a wall film, and the core substance contains an active ingredient.   The carrier according to claim 1 or 2, wherein the active ingredient is one or more selected from a fragrance, a pigment, a bactericidal component and a medicinal component.   The activity promoting component is one or more selected from divalent metal compounds, chlorides, nonionic surfactants and amphoteric surfactants, according to any one of claims 1 to 3. Carrier. The composition containing the support body of any one of Claims 1-4.