JPH05286860A - Gel ointment - Google Patents

Abstract

PURPOSE:To obtain an external preparation, excellent in pharmacodynamic effects and capable of rapidly exhibiting the effects by forming a corticosteroid and an antihistaminic agent, etc., into a gel ointment. CONSTITUTION:The objective gel ointment comprises (A) 0.001-0.3wt.% corticosteroid, e.g. dexamethasone acetate or prednisolone acetate, (B) one or two or more selected from (B1) 0.1-5wt.% local anesthetic agent, e.g. lidocaine or dibucaine hydrochloride, (B2) 0.2-2.0wt.% antihistaminic agent, e.g. diphenhydramine or chlorpheniramine maleate, (B3) 2-10wt.% antipruritic agent, e.g. crotamiton and (B4) 0.3-5wt.% antiphlogistic and analgesic agent, e.g. menthol or methyl salicylate and further >=30wt.%, especially 30-60wt.% alcohols and >=0.1wt.%, especially 0.1-2.5wt.% water-soluble polymer (e.g. a carboxyvinyl polymer).

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a gel ointment capable of extremely quickly eliminating itchiness and redness against itchiness, insect bites, eczema, urticaria and the like.

[0002]

2. Description of the Related Art Conventionally, an antihistamine agent and an antipruritic agent have been used as the main ingredients for eliminating the itchiness and redness of insect rashes, eczema, etc. Creams, ointments, gel ointments, etc. are used. By the way, since these compounded compositions do not provide a sufficient anti-inflammatory effect against skin inflammation such as eczema, a cream preparation containing a small amount of corticosteroid has been recently developed.

[0003]

However, although these corticosteroid-containing creams have excellent medicinal effects, it takes a while before the onset of the effects, and especially in the case of dermatological diseases accompanied by itch, the improvement can be achieved. Was wanted.

[0004]

Therefore, the present inventors have
Various studies have been conducted on the rapid-acting properties of topical agents that use corticosteroids and antihistamines in combination.
Surprisingly, it was found that the use of these components as a gel ointment promptly eliminates symptoms such as itchiness and redness, and completed the present invention.

That is, the present invention provides a gel ointment containing a corticosteroid and one or more selected from local anesthetics, antihistamines, antipruritics and anti-inflammatory analgesics. Is.

[0006] Examples of corticosteroids which are one of the medicinal components used in the present invention include dexamethasone acetate, prednisolone acetate, hydrocortisone acetate and the like. These may be used alone or in combination of two or more. The content of such corticosteroid is preferably 0.001 to 0.3% by weight based on the total composition.

Examples of the antihistamine used in the present invention include diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate and the like. Examples of the local anesthetic include lidocaine, lidocaine hydrochloride, dibucaine hydrochloride and the like. Examples of the anti-inflammatory analgesic include menthol, camphor, methyl salicylate, glycyrrhetinic acid and the like. Examples of the antipruritic agent include crotamiton. These antihistamines, local anesthetics, antipruritics and anti-inflammatory analgesics may be used alone or in combination of two or more kinds. The content of these components is 0.2 to 2.0% by weight of antihistamine and 0.1% of local anesthetic with respect to the total composition.
~ 5 wt%, anti-inflammatory analgesic 0.3-5 wt%, antipruritic 2
10% by weight is preferred.

[0008] Further, examples of agents that can be incorporated into the gel ointment of the present invention include peripheral circulation improving agents such as tocopherol acetate, and antibacterial agents such as chlorhexidine hydrochloride, chlorhexidine gluconate and decarinium hydrochloride.

In the present invention, a base and a gelling agent are blended with these medicinal components to give a gel ointment. Alcohols are used as the base and water-soluble polymers are used as the gelling agent. ..

As alcohols, lower alcohols such as ethanol and isopropanol are used. It is preferable to add 30% by weight or more, particularly 30 to 60% by weight, of alcohols in the total composition. As the water-soluble polymer, for example, carboxyvinyl polymer or the like is used. Such a water-soluble polymer is preferably added in an amount of 0.1% by weight or more, particularly 0.1 to 2.5% by weight based on the total composition.

In producing the gel ointment of the present invention, a pH adjusting agent, a stabilizer, water and the like can be added, if necessary.

The gel ointment of the present invention is a mixture of the above components,
It can be produced by a conventional method.

[0013]

EXAMPLES The present invention will now be described in detail with reference to examples, but the present invention is not limited thereto.

Example 1 A gel ointment having the following composition was prepared. (Composition) (wt%) dexamethasone acetate 0.025 crotamiton 5.0 dibucaine hydrochloride 0.3 diphenhydramine hydrochloride 1.0 dl-camphor 3.0 l-menthol 3.5 carboxyvinyl polymer 1.2 diisopropanolamine 0.34 Denatured 99 degree ethanol 38.0 Purified water Balance total 100.0

Test Example 1 Effect of Histamine on Enhancement of Vascular Permeability (Method) The gel ointment of the present invention obtained in Example 1 or a comparative product of 30 mg / cm ³ (total 240 mg / rat) was applied to the back of a rat for 4 hours. After that, 3 μg / 0.1 ml of histamine was intradermally administered to the drug application site. Evans blue 50 mg / kg (5 ml / kg) was intravenously injected 5 minutes before histamine administration, skin was collected 30 minutes after histamine administration, and the amount of leaked pigment was measured by Katayama et al. (Microbiol. Immunol., 22) .
(2) , 89 to 101 (1978). The comparative product used was a cream containing the following medicinal components. Comparative product 1 (% by weight) Prednisolone acetate 0.125 Lidocaine hydrochloride 3.0 Chlorpheniramine maleate 1.0 l-menthol 0.5 dl-camphor 0.5 Methyl salicylate 2.0 Chlorhexidine hydrochloride 0.2 Comparative product 2 (Wt%) hydrocortisone acetate 0.25 crotamiton 10.0 glycyrrhetinic acid 0.5 tocopherol acetate 0.5 Comparative product 3 (wt%) prednisolone acetate 0.25 crotamiton 10.0 dibucaine hydrochloride 0.3 diphenhydramine hydrochloride 1.0 l -Menthol 3.5 dl-camphor 3.0 (Results) As shown in Table 1, the gel ointment of the present invention rapidly exhibited the effect, and was the most excellent in the comparison after 30 minutes.

[0016]

[Table 1]

Test Example 2 Inhibitory effect on PCA reaction (Method) Anti-ovalbumin (OV) diluted on rat back
A) Rat serum was intradermally administered and passively sensitized. 44
Inventive gel ointment of Example 1 or comparative products 1-33 after time
0 mg / cm ³ (total 240 mg / rat) was applied to the serum administration site, and 4 hours later, 10 mg / kg of the antigen OVA was intravenously injected together with 50 mg / kg of Evans blue, and 30 minutes later, the skin was collected and the amount of leaked pigment Was measured by the method of Katayama et al. (Results) As shown in Table 2, the gel ointment of the present invention rapidly exhibited efficacy and was superior to any of the comparative products.

[0018]

[Table 2]

Further, the gel ointment of the present invention has an excellent effect of suppressing inflammation in the affected area and lowering skin temperature, that is, a cooling effect, and exhibits the maximum cooling effect as compared with any of Comparative Products 1 to 3. Was the shortest.

[0020]

The gel ointment of the present invention can be used to treat itch, eczema, dermatitis, sores, heat rashes, rashes, mosquitoes, insect bites, urticaria and the like very quickly.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁵ Identification code Internal reference number FI Technical display area A61K 45/00 AEM // (A61K 31/575 45:00)

Claims (2)

[Claims] 1. A gel ointment containing a corticosteroid and one or more selected from a local anesthetic, an antihistamine, an antipruritic and an anti-inflammatory analgesic. 2. The gel ointment according to claim 1, which contains 30% by weight or more of alcohols as a base and 0.1% by weight or more of a water-soluble polymer as a gelling agent.