JP2758405B2 - Toothpaste composition - Google Patents

Description

The present invention relates to a hydrophobic medicinal ingredient which can be applied to the oral cavity is encapsulated in microcapsules, whereby the medicinal ingredient is stably maintained in the dentifrice composition, and The present invention relates to a dentifrice composition capable of leaking from a microcapsule during use to exert its pharmacological effect.

2. Description of the Related Art Conventionally, various hydrophobic medicinal ingredients such as fat-soluble vitamins, azulene, and shikonin have been blended in dentifrice compositions. However, such a hydrophobic medicinal ingredient is liable to be inactivated by interacting with a dentifrice material in a dentifrice composition or undergoing an oxidation reaction or a photolysis reaction, so that its pharmacological effect cannot be sufficiently obtained. There is. on the other hand,
In the pharmaceutical field, preparations using microcapsules have been made for the purpose of stabilizing drugs, masking bitterness and the like, and sustained release. However, when microcapsules are used in the dentifrice composition, they not only stabilize the medicinal ingredient, but also endure the stirring share in the dentifrice manufacturing process, and do not have physical properties that can be easily disintegrated by brushing during use. The microcapsule containing a medicinal ingredient in such a microcapsule and blended in a dentifrice composition has not been known so far.

Means for Solving the Problems In view of such problems, the present inventors have surprisingly combined hydrophobic medicinal components with chain-type saturated hydrocarbons at a specific ratio during various studies, and By encapsulating them in a specific amount of a microcapsule resin film and forming microcapsules having a specific particle size distribution, the inventors have found that the above problems can be solved, and have completed the present invention.

That is, the present invention includes a hydrophobic medicinal ingredient (I) applicable to the oral cavity and a chain saturated hydrocarbon (II) which is liquid paraffin or squalane at a weight ratio of (I) / (II) ≦ 2. The present invention provides a dentifrice composition comprising one or more microcapsules.

According to the dentifrice composition of the present invention, the compounded hydrophobic medicinal ingredient does not interact with the dentifrice material, undergoes an oxidation reaction or a photolysis reaction and is not inactivated, and has a pharmacological effect when used. Are sufficiently expressed.

Thus, the microcapsules to be incorporated into the dentifrice composition of the present invention must be sufficiently impermeable to the encapsulated components so that the encapsulated components do not leak, and are applied to the oral cavity. It must not be toxic to the human body. From such a viewpoint, acrylic acid, methacrylic acid, acrylate (for example, methyl acrylate,
One or more of acrylates, methacrylates (eg, methyl methacrylate, ethyl methacrylate, etc.), vinyl acetate, vinyl chloride, vinylidene chloride, ethylene, styrene, divinylbenzene, ethylene glycol dimethacrylate, etc. And a homopolymer or copolymer formed from a monomer selected from

Examples of the hydrophobic medicinal component included in such microcapsules include vitamin A or a derivative thereof, vitamin E or a derivative thereof, β-carotene, azulene, shikonin, and the like.

Hydrophobic active ingredient (I) and chain type saturated hydrocarbon (II)
Is encapsulated in microcapsules at a weight ratio of (I) / (II) ≦ 2. When the ratio is (I) / (II)> 2, a functional group such as an ester bond existing in the hydrophobic medicinal ingredient may exert an inhibitory effect in a polymerization step for forming a microcapsule resin film. As a result, a uniform and dense resin film cannot be obtained, and the inclusion components leak out over time, causing a reduction in stability due to a reaction with the dentifrice material or the like. On the other hand, the lower limit of the ratio (I) / (II) varies depending on the type of the hydrophobic medicinal component used, and is not particularly limited, and is appropriately determined within a range in which a desired medicinal effect is exhibited.

In the present invention, 50 to 85% by weight of a hydrophobic medicinal ingredient and a chain-type saturated hydrocarbon applicable to the oral cavity are added to the total weight of the microcapsules. If the blending amount is less than 50% by weight, the thickness of the microcapsules becomes thicker, and the leakage of the encapsulated components due to the shearing share during toothpaste production can be prevented, but the leakage amount during brushing is significantly reduced, and the compounded medicinal component Cannot be fully utilized. On the other hand, the blending amount is 85
If it is more than 10% by weight, the thickness of the microcapsule becomes thin,
The disintegration of the microcapsules due to the shearing shear during toothpaste production is remarkable, and it is impossible to stabilize the encapsulated components.

The particle size of the microcapsules used is 5 μm or less and
Each having a size of 60 μm or more is selected so as to be 10% by weight or less of the total weight of the microcapsules to be blended.
When the content of the microcapsules having a particle size of 5 μm or less is 10% by weight or more of the total weight of the microcapsules, the disintegration of the microcapsules due to the shear during brushing is reduced, and the medicinal component is not sufficiently utilized. On the other hand, if the content of the microcapsules having a particle size of 60 μm or more is 10% by weight or more of the total weight of the microcapsules, the microcapsules cannot sufficiently withstand the agitation share at the time of dentifrice production, and the contained components cannot be stabilized.

As a method for producing microcapsules to be added to the dentifrice composition of the present invention, for example, a monomer having a polymerizable unsaturated bond such as acrylic acid and styrene and a hydrophobic medicinal ingredient applicable to the oral cavity such as vitamin A and The chain-type saturated hydrocarbon and the polymerization initiator are mixed and dispersed in an aqueous medium containing an emulsifying and dispersing aid so as to form oil droplets having a desired particle size, thereby polymerizing the monomer. The particle size of the microcapsule and the amount of the included component can be adjusted by appropriately selecting the mixing ratio of the monomer component and the included component, the amount and type of the emulsification / dispersion aid, the dispersion conditions, and the like.

The components used in the base of the dentifrice composition of the present invention vary depending on the type and purpose of the composition, but usually the following components are used.

For example, as an abrasive, dicalcium phosphate 2
Hydrates and anhydrides, silica-based abrasives such as monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, titanium oxide, alumina, hydrated alumina, silica gel, colloidal silica, and anhydrous alkali metal silicate complex salt; Aluminum silicate, insoluble sodium metaphosphate, insoluble potassium metaphosphate, tertiary magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, synthetic resin, and the like.
More than seeds, usually 5 to 60% by weight based on the total amount of the dentifrice composition
Mix.

Examples of the binder include carrageenan, sodium carboxymethylcellulose, methylcellulose, hydroxyethylcellulose, cellulose derivatives such as carboxymethylhydroxyethylcellulose sodium, alkali metal alginate such as sodium alginate, propylene glycol alginate, xanthan gum, tragacanth gum, karaya gum, gum arabic gum and the like. Gums, synthetic binders such as polyvinyl alcohol, sodium polyacrylate, carboxyvinyl polymer, and polyvinylpyrrolidone; and inorganic binders such as silica gel, aluminum silica gel, veegum, and laponite. Is usually added to the dentifrice composition in an amount of 0.5 to 5% by weight.

Examples of the thickener include sorbitol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltitol, lactit, and the like. Usually, 10 to 70% by weight is added to the total amount.

As the surfactant, an alkyl group such as sodium lauryl sulfate and sodium myristyl sulfate has 8 to 18 carbon atoms.
Water-soluble salts of higher alkyl sulfates, water-soluble higher fatty acid monoglyceride monosulfates such as hydrogenated coconut oil fatty acid monoglyceride sodium sulfate, alkyl aryl sulfonates such as sodium dodecylbenzene sulfonate, higher alkyl sulfonates Higher fatty acid esters of 1,2-dihydroxypropanesulfonate, N-
Anionic activators such as substantially saturated higher fatty acid acylamides of lower aliphatic aminocarboxylic acid compounds such as sodium, potassium or ethanolamine salts of lauroyl, N-myristoyl or N-palmitoyl sarcosine; sucrose mono and dilaurate; Fatty acid esters having 12 to 18 carbon atoms such as lactose fatty acid ester, lactitol fatty acid ester, maltitol fatty acid ester, stearic acid monoglyceride,
Polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monostearate, polyoxyethylene (10,20,40,60,80,100 mol) hydrogenated castor oil, polymer of ethylene oxide and propylene oxide, and polyoxyethylene polyoxypropylene Nonionic activators such as condensation products of polyethylene oxide such as monolauryl ester with fatty acids, fatty alcohols, polyhydric alcohols and polypropylene oxide; amphoteric activators such as betaine type and amino acid type; The above is usually 0 to 5 with respect to the total amount of the dentifrice composition.
% By weight.

Examples of the active ingredient include allantoins, epsilon aminocaproic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme, and enzymes such as litechenzyme, and alkalis such as sodium monofluorophosphate and potassium monofluorophosphate. Metal monofluorophosphate, sodium fluoride, ammonium fluoride, fluorides such as stannous fluoride,
Examples thereof include dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acid, glycerophosphate, chlorophyll, caropeptide, water-soluble inorganic phosphate compounds, and vitamins, and one or more of these can be blended.

Furthermore, sweeteners such as saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, thaumatin, asparatylphenylalanine methyl ester, p-methoxycinnamic aldehyde, sucrose, lactose, fructose, sodium cyclamate, etc. 0 to 1% by weight, preferably 0.01 to 0.5% by weight, and more preferably p-hydroxymethylbenzoic acid, p-hydroxyethylbenzoic acid, p-hydroxypropylbenzoic acid, p-
Preservatives such as hydroxybutyl benzoic acid, sodium benzoate, lower fatty acid monoglyceride, etc., flavors such as wintergreen oil, spearmint oil, peppermint oil, sassafras oil, clove oil, eucalyptus oil, gelatin, peptone, arginine hydrochloride, albumin, casein , A whitening agent such as titanium dioxide, silicone, a dye, and other components.

The dentifrice composition of the present invention is manufactured by blending the above microcapsules in a dentifrice base prepared from the above components according to a conventional method in an amount of 0.01 to 10% by weight based on the total amount of the composition, uniformly mixing and degassing. It can be made into a usual dosage form such as toothpaste, powdered toothpaste, lubricated toothpaste, and water toothpaste. If the amount of the microcapsules is less than 0.01% by weight, the effect of the medicinal ingredient cannot be sufficiently obtained, while if it is more than 10% by weight, the stability of the dentifrice itself may be impaired.

Examples Next, the present invention will be described in more detail with reference to Examples and Comparative Examples, but the present invention is not limited to these.

Examples 1 to 8 and Test Examples 1 to 6 According to the formulations and preparation methods shown below, microcapsules containing hydrophobic medicinal ingredients and chain-type saturated hydrocarbons of various compounding ratios were prepared.

Formulation Ingredients Amount (parts by weight) Methyl methacrylate 495 Methacrylic acid 20 Hydrophobic medicinal ingredient ^* (described in Table 1) Described in Table 1 Chain-type saturated hydrocarbon ^* (described in Table 1) Described in Table 1 Diisopropylperoxy Dicarbonate 15 Colloidal silica dispersion (solid content 20% by weight) 1390 10% Diethanolamine-adipic acid condensate aqueous solution 90 Purified water 6300 *: Total amount of hydrophobic medicinal components and linear saturated hydrocarbons is always 1545% by weight Department.

Preparation Method Methyl methacrylate, methacrylic acid, a hydrophobic medicinal ingredient, a chain saturated hydrocarbon and diisopropyl peroxydicarbonate were sufficiently mixed to prepare an oil layer. Separately,
An aqueous phase formed by thoroughly mixing a mixture of purified water, a colloidal silica dispersion and a 10% aqueous solution of diethanolamine-adipic acid condensate was adjusted to pH 3.5 with hydrochloric acid.
Then, the oil phase and the aqueous phase were stirred at a high speed of 10,000 rpm for 60 seconds to disperse the oil phase in the aqueous phase, followed by purging with nitrogen.
And a polymerization reaction was carried out at 55-60 ° C. for 20 hours under stirring at 30 rpm. After completion of the reaction, the product was repeatedly filtered and washed with water using a centrifuge.
The product thus obtained is further dried in a flash dryer to obtain an average particle size of 20 μm to 25 μm comprising a methyl methacrylate / methacrylic acid copolymer film (particle size distribution is 5 μm
Hereinafter, 7% by weight, 60 μm or more and 2% by weight), and microcapsules in which the weight of the membrane resin / the weight of the included component = 25/75 were obtained.

A microcapsule-containing dentifrice composition was prepared from the thus obtained microcapsules according to the following formulation and preparation method.

Formulation Ingredient Content (% by weight) Methyl parahydroxybenzoate 0.40 Heavy calcium carbonate 42.00 Sodium carboxymethylcellulose 1.60 Sodium saccharin 0.15 Sorbit (70% aqueous solution) 28.00 Sodium lauryl sulfate 1.40 Propylene glycol 5.00 Microcapsules 1.00 Fragrance 1.00 Prepared in purified water 100 Preparation Method The above components except for microcapsules containing propylene glycol and a desired component were kneaded by a conventional method.
Next, a propylene glycol solution in which the microcapsules were dispersed was added, and the mixture was further kneaded under reduced pressure for 20 minutes to obtain a microcapsule-containing dentifrice composition.

Next, the results of testing the homogeneity of the formed microcapsule membrane by measuring the daily change of the amount of the encapsulated component in the microcapsule blended in the obtained dentifrice composition are shown. The test method and evaluation were performed as follows.

Daily change test of the amount of components contained in microcapsules Immediately after production and after standing for 3 months at a temperature of 40 ° C and a humidity of 75%, 1 g of microcapsule-containing toothpaste was precisely weighed, and each was dispersed in 10 ml of purified water. And then acetone
20 ml was added and shaken for 10 minutes. Then, the mixture was centrifuged at 5000 rpm for 10 minutes, and the supernatant was placed in a volumetric flask. To the sediment, 30 ml of acetone was further added, shaken for 10 minutes, and centrifuged again at 5000 rpm for 10 minutes to collect the supernatant.
The above operation was repeated once again, the supernatant was separated, combined with the above supernatant, and adjusted to 100 ml with acetone. The two kinds of samples thus obtained were filtered through a 0.45 μm liquid chromatography disk, and the hydrophobic medicinal component and the residual amount were quantified by high performance liquid chromatography (hereinafter referred to as HPLC) by a conventional method. Then, the residual amount (%) after three months was calculated, with the residual amount immediately after production as 100, and evaluated as follows.

:: Residual rate after 3 months passed 90% or more ×: Residual rate after 3 months passed less than 90% The results are shown in Table 1.

As is apparent from Table 1, microcapsules consisting of a homogeneous and dense resin film can be obtained only when the blending ratio of the hydrophobic medicinal component and the chain saturated hydrocarbon is 2 or less.

Examples 9 to 13 and Comparative Examples 7 to 9 Methyl methacrylate /
Using methacrylic acid (weight ratio 2: 1) and vitamin E nicotinate / liquid paraffin (weight ratio 1: 1) as components included in the microcapsules in the mixing ratio shown in Table 2,
Average particle diameter containing desired components according to the above method 20 to
25 μm (particle size distribution is 5 μm or less 5% by weight, 60 μm or less 5
% By weight) microcapsules were prepared. This was added to the dentifrice base of the above formulation, and a microcapsule-containing dentifrice composition was similarly obtained.

Next, with respect to the obtained dentifrice composition, the leakage amount of the encapsulated components from the microcapsules immediately after production and immediately after brushing a panel with the dentifrice was measured. The measurement method and evaluation were performed as follows.

Measurement of leakage of encapsulated components immediately after production of microcapsule-containing dentifrice composition 1 g of microcapsule-containing dentifrice immediately after production
A 30% sodium lauryl sulfate solution was added, and the mixture was shaken for 10 minutes. Then, the mixture was centrifuged at 5000 rpm for 10 minutes, and the supernatant was placed in a volumetric flask. Regarding the sedimentation, the above operation was further repeated twice. The supernatants obtained by the three extractions are combined, and 100 ml of a 2% sodium lauryl sulfate solution is added.
And filtered through a 0.45 μm liquid chromatography disk. The prepared sample was measured by HPLC, and the amount of encapsulated components leaked from the microcapsules was quantified. Next, an extraction operation with acetone was performed according to the above-mentioned Example, and the total amount of vitamin E nicotinate and liquid paraffin immediately after the production of the dentifrice was similarly quantified by HPLC. Then, assuming the total amount of vitamin E nicotinate and liquid paraffin immediately after production of the toothpaste as 100, the leakage rate (%) of the encapsulated components from the microcapsules immediately after production, that is, the leakage rate (%) of vitamin E nicotinate and liquid paraffin, was calculated based on the following criteria. Was evaluated.

Measurement of Leakage Amount of Encapsulated Components Immediately After Brushing with Microcapsule-Containing Toothpaste Composition 1 g of microcapsule-containing toothpaste was precisely weighed, taken on a toothbrush, and brushed for 1 minute by a panelist. Then, the dentifrice in the oral cavity and on the toothbrush was thoroughly washed with 30 ml of a 2% aqueous sodium lauryl sulfate solution. After shaking the washing solution for 10 minutes, centrifuged at 5000 rpm for 10 minutes,
The supernatant was taken into a volumetric flask. For sedimentation, the same operation was repeated twice using a 2% aqueous sodium lauryl sulfate solution. The obtained supernatants were combined, adjusted to 100 ml with a 2% aqueous sodium lauryl sulfate solution, and filtered through a 0.45 μm liquid chromatography disk. The sample thus prepared was measured by HPLC, and the amount of contained components leaked from the microcapsules by brushing was quantified. Next, the leakage rate (%) of the included components by brushing was calculated with the total amount of the included components immediately after the production, that is, the total amount of vitamin E nicotinate and liquid paraffin as 100, and evaluated based on the following criteria.

：: Leakage rate immediately after production is 10% or less, and leakage rate immediately after brushing is 90% or more. ×: Leakage rate immediately after production is 10% or more and / or leakage rate immediately after brushing is 90% or less. Shown in

As is clear from Table 2, suitable microcapsules that can withstand the share during manufacture and can be broken down by the share during brushing only when the total weight of the encapsulated components is 50 to 85% by weight of the weight of the microcapsule membrane. Can be obtained.

Examples 14 to 16 and Comparative Examples 10 to 12 Methyl methacrylate / methacrylic acid (2: 1 by weight) as a microcapsule membrane component and vitamin E / liquid paraffin (1: 1 by weight) as a component included in a microcapsule were used. : 75, and microcapsules having a particle size distribution shown in Table 3 were prepared according to the method described above. This was added to the dentifrice base of the above formulation, and a microcapsule-containing dentifrice composition was similarly obtained.

Next, with respect to the obtained dentifrice composition, the leakage amount of the encapsulated components from the microcapsules immediately after the production and immediately after brushing the panel with the dentifrice was measured, and the leakage rate was calculated in the same manner. The measurement method and evaluation were performed as described above.

 Table 3 shows the results.

As is clear from Table 3, the microcapsules having a particle size distribution of not more than 5 μm and not less than 60 μm have a particle size distribution of not more than 10% by weight of the total weight of the microcapsules, respectively. Suitable microcapsules that can withstand and break down due to shear during brushing can be obtained.

Example 14 Methyl methacrylate / microcapsule membrane component
Methacrylic acid (weight ratio 2: 1) and shikonin / squalane (40: 6 weight ratio)
0) was used in a mixing ratio of 25:75 to prepare microcapsules having an average particle size of 25 μm (the particle size distribution is 3% by weight or less and 5 μm or more and 2% by weight or more) according to the above method. Using the microcapsules containing the desired components thus obtained, a microcapsule-containing toothpaste was prepared according to the following method according to the following formulation.

Formulation Composition Blended amount (% by weight) Precipitated silica 20.0 Sodium carboxymethylcellulose 1.4 Titanium oxide 0.5 Sorbit (70% aqueous solution) 60.0 Sodium lauryl sulfate 1.5 Sodium saccharin 0.2 Propylene glycol 5.0 Microcapsules 1.5 Prepared in purified water 100 Example 15 Microcapsule membrane Methyl methacrylate /
Vinyl acetate (weight ratio 4: 1) and vitamin E nicotinate / liquid paraffin (weight ratio 30:70) as an inclusion component
0: Used in a mixing ratio of 80, an average particle size of 20 according to the method described above.
Microcapsules of μm (particle size distribution is 4% by weight of 5 μm or less, 3% by weight of 60 μm or less) were prepared. Using the microcapsules containing the desired components thus obtained, a microcapsule-containing toothpaste was prepared according to the following method according to the following formulation.

Formulation Ingredient Blending amount (% by weight) Precipitable silica 20.0 Sodium carboxymethylcellulose 1.4 Titanium oxide 0.5 Sorbit (70% aqueous solution) 60.0 Sodium lauryl sulfate 1.5 Sodium saccharin 0.2 Propylene glycol 5.0 Microcapsules 1.0 Prepared in purified water 100 Example 16 Microcapsule membrane Average particle size according to the above-mentioned method using methyl acrylate / methyl methacrylate (weight ratio 2: 1) as a component and β-carotene / squalane (weight ratio 50:50) as an inclusion component in a mixing ratio of 30:70. Microcapsules having a particle size of 23 μm (the particle size distribution is 6% by weight of 5 μm or less and 2% by weight of 60 μm or more) were prepared. A microcapsule-containing toothpaste was prepared according to the following method using the microcapsules containing the desired components thus obtained and according to the following method.

Formulation Ingredient Blending amount (% by weight) Precipitable silica 20.0 Sodium carboxymethylcellulose 1.4 Titanium oxide 0.5 Sorbit (70% aqueous solution) 60.0 Sodium lauryl sulfate 1.5 Saccharin sodium 0.2 Propylene glycol 5.0 Microcapsules 2.0 Prepared in purified water 100 Example 17 Microcapsule membrane Methyl methacrylate /
Methacrylic acid (2: 1 weight ratio) and Siconon / Squalane (40: 6 weight ratio)
0) in a mixing ratio of 25:75, and an average particle size of 25 μm (particle size distribution is 5 μm or less, 3% by weight, 60 μm
(The above is 2% by weight).
Using the microcapsules containing the desired components thus obtained, a microcapsule-containing powder toothpaste was prepared according to the following method according to the following formulation.

Formulation Ingredients Blended amount (% by weight) Dibasic calcium phosphate dihydrate 50.0 Calcium carbonate 30.0 Glycerin 10.0 Sodium lauryl sulfate 1.5 Saccharin sodium 0.1 l-Menthol 1.0 Microcapsules 1.5 Carboxymethylcellulose sodium 0.5 Prepared in purified water 100 Example 18 Microcapsule membrane Methyl methacrylate /
Vinyl acetate (weight ratio 4: 1) and vitamin E nicotinate / liquid paraffin (weight ratio 30:70) as an inclusion component
0: Used in a mixing ratio of 80, an average particle size of 20 according to the method described above.
Microcapsules having a particle size distribution of 5 μm or less (4% by weight, 60 μm or more and 3% by weight) were prepared. Using the microcapsules containing the desired component thus obtained, a microcapsule-mixed toothpaste was prepared according to the above-mentioned method by the following formulation.

Formulation Ingredients Blended amount (% by weight) Calcium carbonate 70.0 Glycerin 10.0 Sorbite solution (70%) 8.0 Sodium carboxymethyl cellulose 1.0 Stevioside 0.1 Sodium lauryl sulfate 1.5 Microcapsules 1.0 Fragrance 1.0 Prepared in purified water 100 Example 19 Acrylic acid as a microcapsule membrane component Methyl / methyl methacrylate (weight ratio 2: 1) and β-carotene / squalane (weight ratio 50:50) as an inclusion component in a mixing ratio of 30:70 were used, and the average particle size was 23 μm (average particle size) according to the above method. The microcapsules having a diameter of 5 μm or less and 6% by weight and 60 μm or more and 2% by weight) were prepared. Using the microcapsules containing the desired components thus obtained, a microcapsule-containing water dentifrice was prepared according to the following method using the following formulation.

Prescription Ingredients Blending amount (% by weight) Glycerin 35.0 Carrageenan 1.0 Sodium lauryl sulfate 1.0 Coupling sugar 2.0 Flavor 0.8 Microcapsules 2.0 Prepared in purified water 100 Effect of the invention As described above, according to the dentifrice composition of the present invention, unstable The medicinal component can be stably incorporated into the composition for a long period of time, and the medicinal effect can be sufficiently exhibited at the time of use.

──────────────────────────────────────────────────続 き Continuation of the front page (72) Hiroshi Sando, 2-3-1, Shibukawa-cho, Yao-shi, Osaka Matsumoto Yushi Pharmaceutical Co., Ltd. (56) References JP-A-63-264513 (JP, A) JP-A-55-102436 (JP, A) JP-A-61-254245 (JP, A) (58) Fields investigated (Int. Cl. ⁶ , DB name) A61K 7/16-7/28

Claims (2)

(57) [Claims] (1) A hydrophobic medicinal ingredient (I) applicable to the oral cavity.
A dentifrice composition characterized by comprising one or more microcapsules containing a chain saturated hydrocarbon (II) which is liquid paraffin or squalane at a weight ratio of (I) / (II) ≦ 2. 2. The microcapsules, wherein the total weight of the hydrophobic medicinal component and the chain saturated hydrocarbon is 50 to 85% by weight of the total weight of the microcapsules, and the microcapsules having a particle size of 5 μm or less and 60 μm or more, respectively. The dentifrice composition according to claim 1, further comprising microcapsules having a particle size distribution of 10% by weight or less of the total weight of the microcapsules.