JP2003252798A - Antibacterial gel preparation - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an antibacterial gel preparation having quick-drying property, no greasiness, good elongation and excellently smooth usability. <P>SOLUTION: This preparation is obtained by formulating an antibacterial agent, a water-soluble gelling agent, a lower alcohol, a powder causing no inactivation of antibacterial activity and oil. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an antibacterial gel preparation, and more particularly to an antibacterial gel preparation which is quick-drying and excellent in usability. The antibacterial gel preparation of the present invention,
For example, as a sterilizing and disinfecting preparation for skin, it is widely applied to skin disinfection, hand and limb disinfection, armpit odor preventive, foot odor preventive, etc. Is possible.

[0002]

2. Description of the Related Art Conventionally, a water-soluble gelling agent which forms a gel, in particular, an antibacterial gel preparation using a carboxyvinyl polymer has been used for pharmaceuticals and the like. For example, as an example of such an antibacterial gel preparation, Japanese Patent No. 2533723,
JP 2001-261550 A can be cited. Water-soluble gelling agents such as carboxyvinyl polymers used in these antibacterial gel formulations may cause "wrinkling" in which the water-soluble polymer is deposited on the fingers when rubbed with the fingers when applied to the skin surface. Are known. In particular, Japanese Patent No. 2533723 is an invention relating to a technique for preventing the occurrence of "wrinkle", and is intended to improve usability by preventing the occurrence of "wobble".

[0003]

However, in the prior art, even though the occurrence of "wrinkling" can be prevented, the use of a water-soluble gelling agent such as carboxyvinyl polymer itself which has stickiness, smoothness and poor elongation. The sexual problem could not be fundamentally solved. The present invention has been made in view of such conventional circumstances, and an object thereof is to provide an antibacterial gel preparation having excellent usability such as quick-drying, non-stickiness, good spreadability and smoothness.

[0004]

Means for Solving the Problems As a result of intensive studies for solving the above problems, the present inventors have found that in addition to an antibacterial agent, a water-soluble gelling agent and a lower alcohol, a powder that does not inactivate the antibacterial activity is obtained. It was found that an antibacterial gel preparation having no stickiness, good elongation and a smooth feeling of use can be obtained by blending the oil and the oil, and the present invention has been completed.

That is, the present invention is an antibacterial gel preparation characterized by containing an antibacterial drug, a water-soluble gelling agent, a lower alcohol, a powder that does not inactivate the antibacterial activity and an oil component.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The antibacterial drug used in the present invention is
Examples include bactericidal disinfectants or antifungal agents. Examples of the disinfectant include benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, bronopol,
Examples thereof include povidone iodine, iodine tincture, methylrosaniline chloride, cresol, ovanol 516, phenol, glutaraldehyde, acrinol, alkylaminoethylglycine hydrochloride, and isopropylmethylphenol, and one or more of these are used.

The amount of the germicidal disinfectant used in the present invention is not particularly limited, and is preferably 0.05 to 10% by mass, preferably 0.1 to 5% by mass, and particularly preferably, the total amount of the compounding agent. It is 0.2 to 3 mass%. If the amount of the bactericidal disinfectant is small, the bactericidal effect on the skin cannot be sufficiently obtained, which is not preferable. On the contrary, if the amount is large, irritation is observed from the viewpoint of safety, which is not preferable.

Examples of the antifungal agent used in the present invention include clotrimazole, tolcyclate, miconazole, bifonazole, econazole, thioconazole,
Sulconazole, isoconazole, ketoconazole, oxyconazole, fluconazole, naphthifin, butenafine, linanaphthate, itraconazole, miconazole nitrate, omoconazole nitrate, isoconazole nitrate, oxyconazole nitrate, econazole nitrate, butenafine hydrochloride, etc. Alternatively, two or more kinds are used.

The amount of the antifungal agent used in the present invention is
There is no particular limitation, and 0.3 to 8% by mass is suitable for the total amount of the compounding agent, preferably 0.5 to 5% by mass, and particularly preferably 1 to 3% by mass. A small amount of the antifungal agent is not preferable because a bactericidal effect against fungi cannot be sufficiently obtained, and conversely, a large amount causes irritation from the viewpoint of safety, which is not preferable.

Examples of the water-soluble gelling agent used in the present invention include carboxyvinyl polymer, hydroxypropylcellulose, polyvinylpyrrolidone, silica gel and the like, and if necessary, one kind or two or more kinds may be used in combination. . Of these, carboxyvinyl polymer is particularly preferable.

The amount of the water-soluble gelling agent used in the present invention is preferably 0.2 to 7% by mass, and more preferably 0.
It is 5 to 5 mass%, particularly preferably 1 to 3 mass%. If the amount of the water-soluble gelling agent is small, it is not preferable because the viscosity of the system cannot be obtained.

The lower alcohol used in the present invention is, for example, ethanol, propanol, isopropanol,
Denatured ethanol and the like can be mentioned, and if necessary, one kind or two or more kinds can be used in combination. Particularly preferred among these are ethanol and denatured ethanol.

The amount of the lower alcohol used in the present invention is preferably 16% by mass or more, preferably 30% by mass or more, and particularly preferably 60% by mass or more. When the amount of the lower alcohol is small, it is not preferable because the quick-drying property cannot be obtained in terms of usability, and when the amount of the lower alcohol is large, the antibacterial action is also preferable.

The powder which does not inactivate the antibacterial activity used in the present invention is, for example, starch such as corn starch, potato starch, rice starch, wheat starch, crystalline cellulose, synthetic aluminum silicate, nylon powder, polyethylene powder, One type or two or more types selected from latex powder and the like are used. Of these, starches,
Crystalline cellulose and nylon powder are preferable, and starches are particularly preferable.

The amount of the powder used in the present invention which does not inactivate one or more antibacterial activities is preferably 2 to 40% by mass, preferably 5 to 20% by mass, particularly preferably 8 to It is 15% by mass. If the amount of the powder that does not inactivate the antibacterial activity is small, it is not preferable because the effect of improving the stickiness of the system cannot be sufficiently obtained, and if it is large, the usability is impaired and the system becomes powdery, which is not preferable.

Further, the powder which does not inactivate the antibacterial activity used in the present invention has a mass ratio of (powder which does not inactivate the antibacterial activity) / (water soluble gelling agent) to the water-soluble gelling agent. And used in a ratio of 2/1 to 150/1, preferably,
5/1 to 50/1, more preferably 8/1 to 20 /
Used in a ratio of 1. If the amount of powder that does not inactivate the antibacterial activity is less than that of the water-soluble gelling agent, it is difficult to obtain the improvement of stickiness, which is not preferable. If the amount of powder is too large, the powder remains excessively on the skin, resulting in poor usability. Not preferable.

The oil used in the present invention is, for example, glycerin triisooctanoate, cetyl isooctanoate, diethyl sebacate, dibutyl sebacate, diisopropyl adipate, isopropyl myristate, myristyl myristate, ethyl oleate, decyl oleate,
One selected from crotamiton, triethyl citrate, glycerin tricaprate, triacetin, isopropyl linoleate, isostearic acid, stearic acid, oleic acid, palmitic acid, isopropyl palmitate, cetyl palmitate, stearyl alcohol, myristyl alcohol, cetanol, ceresin, etc. Alternatively, two or more kinds are used. Of these, glyceryl triisooctanoate, cetyl isooctanoate and isopropyl myristate are preferable, and glyceryl triisooctanoate is particularly preferable.

The amount of oil used in the present invention is 0.
2 to 20 mass% is suitable, and preferably 0.5 to 10
%, Particularly preferably 1 to 5% by weight. If the amount of the oil component is small, it is not preferable because the effect of improving the smoothness of the system cannot be sufficiently obtained, and if it is large, the usability is impaired and the system becomes oily, which is not preferable.

Further, in the oil component used in the present invention, the oil component / water-soluble gelling agent is used in a mass ratio of 1/5 to 30/1 with respect to the water-soluble gelling agent, and preferably, 1
/ 2 to 15/1, more preferably 2/1 to 10/1
Used in the ratio of. If the oil content is too small with respect to the water-soluble gelling agent, it is difficult to obtain improvement in elongation and smoothness, which is not preferable, and if it is too large, stickiness due to the oil content is produced and usability deteriorates, which is not preferable.

In addition to the antibacterial drug, the antibacterial gel preparation of the present invention may contain a drug. The drug used in the present invention is not particularly limited as long as it is used as an antibacterial gel preparation. For example, as drugs, anti-inflammatory agents such as glycyrrhetinic acid, dipotassium glycyrrhizinate, and monoammonium glycyrrhizinate, vitamin E
Examples include blood circulation promoters such as acetate and wound healing agents such as allantoin.

In addition to the above components, the antibacterial gel preparation of the present invention may further contain a surfactant, a wetting agent, a cooling agent, an antioxidant, a chelating agent, an absorption promoter, a fragrance, a coloring agent, etc. It can be blended within a range that does not impair the effects of the present invention. In particular, it is preferable to add a surfactant among them in order to stably add an oil component. The surfactant used in the present invention is preferably a hydrophilic surfactant.
Further, among hydrophilic surfactants, nonionic surfactants are particularly preferable, and examples thereof include polyoxyethylene hydrogenated castor oil, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene sorbitan fatty acid ester, propylene glycol fatty acid ester. One or more selected from polyglycerin fatty acid ester and the like are used.

[0022]

EXAMPLES Next, the present invention will be described in more detail by showing Examples and Comparative Examples of the antibacterial gel preparation of the present invention, but these do not limit the present invention in any way. In the following examples, "%" indicates "mass%" unless otherwise specified, and the numerical values in the composition table also indicate mass%.

The method for producing each composition is not particularly limited, but can be prepared using, for example, a stirring mixer such as a homomixer or a dispermixer.

Examples 1 to 3 and Comparative Examples 1 to 6 Antibacterial gel preparations having the compositions shown in Tables 1 and 2 were prepared by the following method, and the antibacterial activity and usability of the obtained antibacterial gel preparations were evaluated. In Examples, formulations were prepared in which corn starch was used as a powder that did not inactivate the antibacterial activity, and glycerin triisooctanoate was used as an oil component. In Comparative Examples, formulations were prepared without these powders and oil components.

(Production Method of Example) Benzalkonium chloride, diisopropanol, glycerin triisooctanoate and concentrated glycerin were added to 95% ethanol and dissolved, and then carboxyvinyl polymer was added to purified water and mixed with stirring. The antibacterial gel preparation of the present invention was obtained by adding corn starch to the system and mixing with stirring.

(Production Method of Comparative Example) Each antibacterial gel preparation was obtained according to the production method of Example.

Next, in order to investigate the usability of the antibacterial gel preparation of the present invention, the tests in Examples 1 to 3 and Comparative Examples 1 to 6 were carried out. Regarding usability, stickiness, elongation, and smoothness were evaluated, and the following criteria were used for evaluation.

(Stickiness) ○: Not sticky △: Almost no stickiness ×: Sticky (Stretch) ○: Good growth Δ: Slightly good growth X: poor growth (Smoothness) ○: Smooth △: Slightly smooth ×: squeaky

The antibacterial activity was evaluated by the presence or absence of a growth inhibition zone for bacteria. Staphylococcus epidermidis IFO376, a skin-resident bacterium
2) was used as the test strain. The outline of the test is as follows: 0.1 ml of the inoculum solution (1,000,000 conidia / ml) was dropped on the SCD agar medium and the whole surface of the medium was evenly coated.
The formulations of Examples and Comparative Examples were prepared on paper discs at 0.
An amount of 05 g was weighed out, uniformly applied, and allowed to stand in a medium inoculated with the bacterium. After culturing this at 30 ° C. for 48 hours, it was evaluated whether or not a growth inhibition zone of bacteria was formed by each sample, and the following criteria were used for evaluation. (Evaluation criteria of antibacterial activity) ○: No inactivation of antibacterial activity is observed. X: Inactivation of antibacterial activity was observed.

The test results are shown in Tables 1 and 2. As can be seen from these results, it was confirmed that the antibacterial gel preparation according to the present invention had markedly improved usability as compared with the preparation of Comparative Example. Regarding the antibacterial activity, inactivation of the antibacterial activity was not observed in the antibacterial gel preparation of the present invention.

[0031]

[Table 1]

[0032]

[Table 2]

Next, further examples will be shown in order to make the external preparation for skin of the present invention more specific. Of course, these do not limit the present invention in any way. And these manufacturing methods are based on Example 1.

[0034] Example 4 (bactericidal disinfectant)   (Prescription) Compounding amount (%) Chlorhexidine gluconate 0.2 Carboxy vinyl polymer 0.5 Hydroxypropyl cellulose 0.08 Polyvinylpyrrolidone 0.5 Isopropanol 50.0 95% ethanol 17.4 Glycerin triisooctanoate 0.5 Corn starch 5.0 Polyoxyethylene (60 mol) hydrogenated castor oil 0.1 Disopropanolamine 0.67 EDTA-2Na 0.05 Purified water residue              Total 100.00

[0035]

[0036] Example 6 (antifungal agent)   (Prescription) Compounding amount (%) Miconazole nitrate 2.0 Carboxy vinyl polymer 0.7 Diisopropanol 0.9 Cetyl isooctanoate 2.5 Isopropyl myristate 2.0 Polyvinylpyrrolidone (Plasdone K-90) 0.5 Nylon powder 10.0 Polyethylene glycol (Macrogol 400) 4.0 Purified water 18.5 95% denatured ethanol residual              100.0 in total

[0037]

EFFECTS OF THE INVENTION The antibacterial gel preparation of the present invention has a quick-drying property and is excellent in usability as compared with the conventional preparations, has no stickiness, has good elongation, is smooth and has a feeling of discomfort during use. It is not stimulating. In addition, the antibacterial gel preparation of the present invention does not show inactivation of antibacterial activity.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 47/32 A61K 47/32 47/34 47/34 47/36 47/36 47/38 47/38 A61P 17/00 101 A61P 17/00 101 31/00 31/00 31/04 31/04 31/10 31/10 // A61K 31/14 A61K 31/14 31/155 31/155 31/4174 31/4174 ( 72) Inventor Yukari Tsutsumi 2-12-1, Fukuura, Kanazawa-ku, Yokohama-shi, Kanagawa F-term (reference) within the Shiseido Research Center (Hakkei Kanazawa) 4C076 AA09 BB31 CC31 DD27 DD29 DD34 DD37 DD38 DD41 DD42 DD45 DD46 DD47 DD49 DD50 DD51 EE03 EE09 EE13 EE16 EE23 EE26 EE31 EE32 EE38 EE52 FF16 FF17 FF35 FF36 FF43 FF63 4C086 AA01 AA02 BC38 MA03 MA05 MA28 MA63 NA20 ZA90 ZB32.

Claims (6)

[Claims] 1. An antibacterial gel preparation comprising an antibacterial agent, a water-soluble gelling agent, a lower alcohol, a powder that does not inactivate the antibacterial activity, and an oil component. 2. The antibacterial gel preparation according to claim 1, wherein the antibacterial drug is a germicidal disinfectant or an antifungal agent. 3. A powder which does not inactivate the antibacterial activity is corn starch, potato starch, rice starch,
2. The antibacterial gel preparation according to claim 1, which is one or more selected from wheat starch, crystalline cellulose, synthetic aluminum silicate, nylon powder, polyethylene powder and latex powder. 4. The oil component is glycerin triisooctanoate,
Cetyl isooctanoate, diethyl sebacate, dibutyl sebacate, diisopropyl adipate, isopropyl myristate, myristyl myristate, ethyl oleate, decyl oleate, crotamiton, triethyl citrate, glycerin tricaprate, triacetin, isopropyl linoleate, isostearic acid The antibacterial gel according to claim 1, which is one or more selected from stearic acid, oleic acid, palmitic acid, isopropyl palmitate, cetyl palmitate, stearyl alcohol, myristyl alcohol, cetanol and ceresin. Formulation. 5. The powder which does not inactivate the antibacterial activity is (powder which does not inactivate the antibacterial activity) / water-soluble gelling agent.
(Water-soluble gelling agent) = Used in the range of 2/1 to 150/1 (mass ratio), the antibacterial gel preparation according to claim 1. 6. The oil content is used in the range of (oil content) / (water-soluble gelling agent) = 1/5 to 30/1 (mass ratio) with respect to the water-soluble gelling agent. The antibacterial gel preparation according to claim 1.