JP3054758B2 - Trauma composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a wound composition for disinfecting and protecting wounds such as wounds, abrasions and burns caused by external insults on skin or mucous membranes. More particularly, it relates to a wound dressing composition containing a bactericide, alum and a thickener.

[0002] According to the composition, it is possible to sterilize and protect a damaged skin such as a wound, abrasion, burn or pressure sore, and to significantly prevent suppuration caused by infecting the affected part with bacteria. Furthermore, the composition of the present invention can protect and dry the affected area moistened by the exudation of blood or lymph due to the astringent action thereof, and can provide early repair and healing of the trauma affected area.

[0003]

2. Description of the Related Art Disinfectants have conventionally been used to disinfect wounds such as wounds or abrasions and to prevent suppuration due to bacterial infection. Since many of these disinfectants have a low viscosity, there has been a problem that the efficacy of the disinfectant does not last for a long time because the disinfectant runs down or adheres to clothes or the like. For this reason,
A combination of a bactericide and a thickener allows the bactericidal agent to stay at the application site for a long period of time to maintain the bactericidal effect.

[0004] Guanidine-based germicides such as chlorhexidine, which are widely used as wound germicides, exhibit an antibacterial effect widely on Gram-positive bacteria and Gram-negative bacteria, and can be used in other germicides such as quaternary ammonium, phenyl or iodine preparations. It is known to exhibit a stronger bactericidal effect than bactericides.

However, in the case of the guanidine fungicide,
If a thickening agent is added to make the bactericidal effect persistent, there is a problem that the bactericidal effect is considerably reduced.

[0006] In addition, some conventional wound medicines have only a bactericidal effect or only a convergence effect. However, these are not suitable for protecting wounds, preventing infection and early healing effect. Not enough.

[0007] Therefore, there is a need for an external preparation which can simultaneously realize a disinfecting treatment, an astringent / hemostatic treatment, and an anti-suppuration treatment, and further, an external preparation which does not discolor the affected part after treatment and is transparent and has no noticeable wound. It is a fact.

[0008]

DISCLOSURE OF THE INVENTION The present invention relates to a trauma composition containing a guanidine fungicide as a fungicide, which can be retained in an affected part without reducing the bactericidal effect.
An object of the present invention is to provide a composition for trauma having a convergence effect. Further, the present invention provides a composition for trauma which can significantly prevent purulence of an affected part due to bacterial infection such as Pseudomonas aeruginosa, further promote hemostasis and desiccation of the affected part, and can quickly repair and heal the wound. The purpose is to provide.

[0009]

Means for Solving the Problems In the development of a composition for wounds and abrasions, the present inventors have found that if a thickening agent is added to a guanidine fungicide, the effect of retaining the fungicidal composition in the affected area is improved. A problem has been encountered that the sterilization effect is significantly reduced. In order to solve this problem, we have been conducting intensive research.By adding alum to a mixed composition of a guanidine fungicide and a thickener, the reduction of the germicidal effect of the guanidine fungicide is significantly suppressed. And
In addition, the present inventors have found that the composition exhibits various excellent properties as a composition for treating wounds due to the astringent action of alum and the retention effect of the sterilizing composition by the thickener. The composition further comprises:
The present invention has been completed by confirming that it has the desirable characteristics as an external preparation such that the affected part is transparent without coloring the wound and the wound is not noticeable.

That is, the present invention is a trauma composition comprising any one of the following embodiments.

(1) A composition for wounds comprising a guanidine fungicide, alum and a thickener.

(2) The wound dressing composition according to the above (1), wherein the guanidine fungicide is at least one selected from chlorhexidine hydrochloride and chlorhexidine gluconate.

(3) The wound dressing according to the above (1) or (2), wherein the thickener is at least one selected from the group consisting of cellulose, acrylic acid and alginic acid. Composition.

(4) Per 100% by weight of the composition, 0.1 to 0.2% by weight of a guanidine fungicide and 10% of alum are used.
The composition for trauma according to any one of the above (1) to (3), which comprises about 90% by weight and 0.1 to 5% by weight of a thickener.

[0015]

BEST MODE FOR CARRYING OUT THE INVENTION The fungicide to be used in the present invention is not particularly limited as long as it is a guanidine fungicide. Usually, an acid salt of chlorhexidine, for example, chlorhexidine dihydrochloride or its digluconate, ie, chlorhexidine hydrochloride. Or chlorhexidine gluconate.

The alum used in the present invention includes:
General _{^{formula: M I 2 SO 4 M III}} 2 (SO 4) 3 · 24H 2 O, or M ^I M
^III (SO ₄₎ in ₂ · 12H ₂ O [Formula, M ^I represents a monovalent cation, M ^III represents a trivalent metal ion. Or a double salt thereof, or an anhydrous salt obtained by removing water of crystallization from the above salt.

Here, as the monovalent cation, for example, T
l ⁺ , Cs ⁺ , Rb ⁺ , K ⁺ , Na ⁺ , Li ⁺ , Ag ⁺ , NH ₄
⁺ , Alkyl ammonium ions and the like. Examples of the trivalent metal ions include, for example, Al ³⁺ , Ti ³⁺ ,
V ³⁺ , Cr ³⁺ , Mn ³⁺ , Fe ³⁺ , Co ³⁺ , Fe ³⁺ , Ga
³⁺ , In ³⁺ , Ir ³⁺ , Rh ^{3+ and the} like.

More specifically, potassium aluminum sulfate [Al ₂ (SO ₄ ) ₃ · K ₂ SO ₄ · 24H ₂ O or AlK (SO ₄ ) ₂ · 12H ₂ O: K alum], sodium aluminum sulfate [Al ₂ (SO ₄ ) ₃
Na ₂ SO ₄ · 24H ₂ O or AlNa (SO ₄ ) ₂ · 12H ₂ O: Na alum], aluminum cesium sulfate (Cs alum),
Examples thereof include ammonium ammonium sulfate (ammonium alum), sodium iron sulfate (iron sodium alum) and the like, preferably potassium aluminum sulfate, and usually aluminum potassium sulfate [AlK (SO ₄ ) ₂・ 12H ₂ O].
Those containing 5% or more are used.

The thickener used in the present invention is not particularly limited as long as it exhibits viscosity and exerts a thickening effect by an appropriate treatment. For example, thickeners in the fields of cosmetics, foods, pharmaceuticals, etc. Agents used as thickeners, dispersants, suspending agents, emulsifiers, gelling agents, binders, and the like can be widely mentioned. Specific examples include alginic acid-based, acrylic acid-based, and cellulose-based thickeners.

Although there is no particular limitation as long as it is a thickener belonging to these systems, usually, specific examples of the alginic acid-based thickener include alginic acid salts or esters, and more specifically, Examples include sodium alginate and propylene glycol alginate.

As the acrylic acid-based thickener, an acidic high molecular compound which is a copolymer of acrylic acid and a small amount of allyl sucrose or the like, specifically, carboxyvinyl polymer or polyacrylamide is used. Is exemplified.

Further, examples of the thickener belonging to the cellulosic type include water-soluble cellulose derivatives such as hydroxyalkyl ether or carboxyalkyl ether of cellulose or salts thereof. Here, the alkyl group includes a lower alkyl group having 1 to 5 carbon atoms. More specifically, examples of the hydroxyalkyl ether of cellulose include hydroxymethyl cellulose, hydroxyethyl cellulose and hydroxypropyl cellulose, and examples of the carboxyalkyl ether of cellulose include carboxymethyl cellulose. Examples of the salt include an alkali metal salt such as sodium or potassium, and preferably a sodium or potassium salt of carboxymethylcellulose.

The thickener is appropriately selected and employed from the above-mentioned various thickeners according to the kind of the disinfectant to be blended, the application place or application of the composition of the present invention, etc., and preferably, alginic acid is used. Sodium and polyacrylamide. These can be used alone or in combination of two or more.

The above-mentioned guanidine fungicide, alum and thickener may be those which are currently commercially available or will be available in the future.

The composition of the present invention is not particularly limited as long as it contains the above-mentioned three components. Usually, a guanidine fungicide is used in an amount of 0.1% per 100% by weight of the composition. 0.2% by weight, alum 10-9
It is preferable to contain 0% by weight and 0.1 to 5% by weight of a thickener. A more preferable mixing ratio is 0.1 to 0.2% by weight of the guanidine fungicide, 20 to 80% by weight of the alum, and 0.2 to 4% by weight of the thickener, and more preferably, the guanidine fungicide. Agent is 0.1 ~
0.2% by weight, alum 40-70% by weight and thickener 0.2-3% by weight.

The composition of the present invention may contain optional components in addition to the above components as long as the effects of the present invention are not impaired. Examples of the optional component include carriers, bases, and various additives used in pharmaceuticals such as external preparations. Specific examples include carriers such as distilled water for injection and physiological saline, and hydrophilic petrolatum and the like. Emulsion bases, bases for ointments such as fats and oils, waxes, etc., stabilizers, preservatives, dissolution aids, emulsifiers,
Examples thereof include additives such as a suspending agent and a soothing agent.

The composition of the present invention can be used for damaged skin or mucous membranes caused by external invasion such as physical action or chemical action, specifically wounds such as cuts, lacerations and bruises, abrasions, burns and pressure ulcers. It is used as an external preparation for the wound affected area. Therefore, the composition of the present invention is not particularly limited to that aspect, and all aspects generally used for external preparations are widely adopted, and can be prepared into an appropriate dosage form according to the application place or use. As a dosage form,
Specific examples include liquids, suspensions, emulsions, lotions, ointments, creams, sprays, foams, patches, plasters, and the like, and preferably ointments and creams.

Since the composition for wounds of the present invention has an excellent bactericidal action, it can significantly disinfect and disinfect skin wounds such as wounds, abrasions, burns or pressure ulcers, as well as astringent / hemostatic action and drug retention action. The composition protects and infects the affected area by infiltration due to the exudation of blood or lymph, thereby promoting early repair and early healing of the affected area.

[0029] Pseudomonas aeruginosa ( Pseu
domonas aeruginosa ) is abundant and these are the causes of suppuration of the wound. Bacteria targeted by the trauma composition of the present invention are not particularly limited, and can be broadly targeted against Pseudomonas aeruginosa, but are particularly excellent in bactericidal action against Pseudomonas aeruginosa causing suppuration of the wound as described above. Therefore, it is extremely useful as an agent for preventing suppuration. further,
Since the composition of the present invention is transparent after application and application, it also has a characteristic that the affected area is inconspicuous and is preferable as an external preparation.

[0030]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Examples and Experimental Examples, but the present invention is not limited to the Examples and the like. In addition,% described below means% by weight unless otherwise specified.

Example 1 Chlorhexidine hydrochloride, alum (containing 99.5% of aluminum potassium sulfate: manufactured by Daimei Chemical Co., Ltd.), sodium alginate and polyacrylamide were dissolved in purified water, and 0.2% of chlorhexidine hydrochloride and alum were dissolved. 6
A trauma composition (ointment) of the present invention containing 5%, a total of 2.75% of sodium alginate and polyacrylamide was prepared.

Example 2 A wound composition of the present invention was prepared in the same manner as in Example 1, except that the amount of alum was adjusted to be in the range of 5 to 95%.

EXPERIMENTAL EXAMPLE 1 0.1% of Pseudomonas aeruginosa (KPB36) prepared according to the formulation described in Example 1 for Pseudomonas aeruginosa.
Alternatively, the bactericidal effect of the trauma composition (ointment) of the present invention containing 0.2% of chlorhexidine hydrochloride was examined.

As a composition for comparison, (1) 0.
1% or 0.2% chlorhexidine hydrochloride suspension (solvent: purified water), (2) 65% alum aqueous solution (solvent:
Purified water), (3) 0.1% or 0.2% chlorhexidine hydrochloride and 2.75% thickener (polyacrylamide +
Similarly, the bactericidal effect against Pseudomonas aeruginosa was examined using an ointment containing sodium alginate).

<Experimental method> The bactericidal effect of each composition was examined by the following method.

1. Prepare a stock solution of bacteria (1 × 10 ⁸ cells).

2. Inoculate the bacterial stock solution at 100 μl per 10 ml of each test composition and mix well.

3. For each mixing / reaction time (up to 180 minutes)
Then, 50 µl was collected from the sample of 2 above and 5 ml of 7
% Polysorbate 80 in physiological saline solution to stop the reaction.

4. The reaction-stopped sample was placed on a SCDLP agar plate medium (1 liter of purified water, 1 peptone per liter of purified water).
5 g, polypeptone S 5 g, sodium chloride 5 g, agar 15 g, lecithin 1 g, polysorbate 807 g) and culture at 30 ° C. overnight.

5. Count the number of colonies appearing on the plate medium.

The results are shown in FIG. 1 (chlorhexidine hydrochloride 0.1
%) And FIG. 2 (using 0.2% of chlorhexidine hydrochloride). In the figure, the vertical axis indicates the number of colonies, and the horizontal axis indicates the mixing / reaction time (minute) between the composition and the bacteria. Further, in the respective line graphs in the figure, -x- indicates the composition for wounds of the present invention (chlorhexidine hydrochloride + alum + thickener),-■-indicates chlorhexidine hydrochloride (control sample (1)), and-▲-indicates alum ( Control sample (2)) and-◆ -chlorhexidine hydrochloride + thickener (control sample (3)) are shown.

As is evident from the results, when a thickener is added to chlorhexidine hydrochloride, the bactericidal effect of chlorhexidine hydrochloride is remarkably reduced. However, when alum is added thereto, the bactericidal action is restored, and the reduction of the bactericidal effect by the addition of the thickener can be significantly suppressed. Therefore, the composition of the present invention has an astringent and hemostatic action by alum,
In addition, the composition is a trauma composition having an excellent bactericidal effect, in addition to having the composition stay in an affected area and exhibiting a continuous bactericidal effect. In particular, the composition of the present invention is useful as a suppuration inhibitor since it has an excellent bactericidal effect against Pseudomonas aeruginosa.

Similar results were obtained when a similar experiment was performed using chlorhexidine gluconate instead of chlorhexidine hydrochloride.

EXPERIMENTAL EXAMPLE 2 Relationship between Alum Blending Amount and Feeling of Use A wound composition prepared in Example 2 (0.2% chlorhexidine hydrochloride, 5-95% alum, 2.75% sodium alginate + polyacrylic acid) (Containing amide) was used to investigate the relationship between the amount of alum and the feeling of use.

Specifically, 1 ml of each composition was applied to the face, hands and feet of 40 voluntarily selected volunteers, and the applied composition was rough, sticky, and adherent. , Hemostatic power, and transparency of the applied affected area were evaluated on a five-point scale of "good, moderately good, normal, slightly poor, and bad". Table 1 shows the results. In the table, ○,
Δ and × are based on the following standards.

：: Both “bad” and “slightly bad” are 0%.

Δ: “bad” is 40% or less, or “slightly bad” is 40
% Or less ×: “bad” is 40% or more or “slightly bad” is 40
%that's all

[0048]

[Table 1]

From these results, it can be seen that the trauma composition of the present invention can reduce the tactile discomfort such as roughness and stickiness by adding alum, and furthermore, the adhesiveness and hemostasis of the bactericidal composition. It can be seen that the power is improved.

[Brief description of the drawings]

FIG. 1 shows the bactericidal effect of the trauma composition of the present invention containing 0.1% chlorhexidine hydrochloride (ointment: indicated by -x- in the figure) on Pseudomonas aeruginosa, by using a chlorhexidine hydrochloride suspension (-■ in the figure). It is a figure which compared with each comparative control composition of alum aqueous solution (indicated by-in the figure), chlorhexidine hydrochloride + thickener (ointment: indicated by-in the figure). The vertical axis is the number of colonies, and the horizontal axis is the mixture of bacteria and each composition.
The reaction time (min) is shown.

FIG. 2 shows the bactericidal effect of the trauma composition of the present invention containing 0.2% of chlorhexidine hydrochloride (ointment: indicated by -x- in the figure) on Pseudomonas aeruginosa. It is a figure which compared with each comparative control composition of alum aqueous solution (indicated by-in the figure), chlorhexidine hydrochloride + thickener (ointment: indicated by-in the figure). The vertical axis is the number of colonies, and the horizontal axis is the mixture of bacteria and each composition.
The reaction time (min) is shown.

Continued on the front page (51) Int.Cl. ⁷ identification code FI A61P 31/02 A61P 31/02 (58) Investigated field (Int.Cl. ⁷ , DB name) A61K 33/06 A61K 31/155 A61K 47 / 30

Claims (4)

(57) [Claims] 1. A composition for trauma comprising a guanidine fungicide, alum and a thickener. 2. The composition for wounds according to claim 1, wherein the guanidine fungicide is at least one selected from chlorhexidine hydrochloride and chlorhexidine gluconate. 3. The wound dressing composition according to claim 1, wherein the thickener is at least one selected from the group consisting of cellulose, acrylic acid and alginic acid. 4. A guanidine fungicide of 0.1 to 0.2% by weight and alum of 10 to 9% by weight per 100% by weight of the composition.
The wound dressing composition according to any one of claims 1 to 3, comprising 0% by weight and 0.1 to 5% by weight of a thickener.