JPH07316075A - External preparation for skin - Google Patents

Abstract

PURPOSE:To obtain an external preparation for skin suitable for treating atopic dermatitis, supplying moisture retaining function of skin, having improved synergistic and treating effects, containing a moisture retaining component such as an amino acid (salt), etc., and an anti-inflammatory analgesic in a specific ratio. CONSTITUTION:This external preparation for skin contains (A) 20-40wt.% of one or more moisture retaining components selected from an amino acid (salt) such as lysine, a saccharide such as glucose, a polyhydric alcohol such as glycerol, a polysaccharide (salt) such as chondroitinsulfuric acid, mucin or chitin, a pyrrolidonecarboxylic acid (salt) and a phospholipid such as lecithin and (B) 0.1-10wt.% of an anti-inflammatory analgesic such as indomethacin, methyl salicylate, sodium diclofenac, triamcilonone or floctafenine.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention relates to a skin external preparation. More specifically, it relates to a skin external preparation for a skin disease associated with dryness, which contains a moisturizing component and an anti-inflammatory analgesic.

[0002]

2. Description of the Related Art In recent years, atopic dermatitis has remarkably increased with the advent of patients not only in children but also in adults as a result of changes in lifestyle, especially, dietary changes.
The onset mechanism of atopic dermatitis and its cause are said to be an overreaction of the antigen-antibody reaction, but it is not yet known in detail. Because the cause is not clear, the only treatment for atopic dermatitis is to administer anti-inflammatory analgesics transdermally to alleviate inflammation and suppress itch. However, at present, these symptomatic treatments have not been effective as expected. This is because the skin function itself is impaired by atopic dermatitis, and even if an attempt is made to suppress the inflammation, the inflammation will not subside due to a negative factor due to the deterioration of the skin function. On the other hand, it has not been known that a moisturizing component enhances its effect when used in combination with an anti-inflammatory analgesic, and no attempt has been made to add a large amount of moisturizing component to the anti-inflammatory analgesic.

[0003]

The present invention has been made in view of the above circumstances, and an object thereof is to provide a skin external preparation capable of effectively suppressing inflammation of atopic dermatitis.

[0004]

[Means for Solving the Problems] In order to solve the above problems,
The present inventors have conducted extensive research to find a drug capable of suppressing inflammation of atopic dermatitis, and as a result, of the skin functions lost by atopic dermatitis, regarding the water retention effect, a moisturizing component in an anti-inflammatory analgesic external preparation. By adding a large amount of
They found that the inflammation could be suppressed and completed the invention.

(1) External preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing 20 to 40% by weight of a moisturizing component and 0.1 to 10% by weight of an anti-inflammatory analgesic.

Here, the moisturizing component is not particularly limited as long as it is a substance having a function of maintaining moisture in the external preparation for skin, and specifically, lysine, threonine,
Amino acids such as serine, alanine and glycine and / or salts thereof, sugars such as glucose, lactose and maltose,
Examples thereof include polyhydric alcohols such as glycerin, polysaccharides such as chondroitin sulfate, mucin and chitin and / or salts thereof, pyrrolidonecarboxylic acid and / or salts thereof, and phospholipids such as lecithin. The salt is not particularly limited as long as it is physiologically acceptable, for example, hydrochloride,
Mineral salts such as nitrates and sulfates, citrates, malates,
Organic acid salts such as succinate, oxalate, sodium salt,
Examples thereof include alkali metal salts such as potassium salts, alkaline earth metal salts such as calcium salts and magnesium salts, amine salts such as ammonium salts and triethylammonium salts, and basic amino acid salts such as lysine salts and arginine salts. These may be used alone or in combination of two or more.

The preferable amount of such a moisturizing component is
It is 20 to 40% by weight. This is because atopic dermatitis generally requires a large amount of moisturizing component because its water retention capacity is significantly reduced. It may not be possible to cut it. Further, even if the amount exceeds 40% by weight, the effect reaches the ceiling and is not economical. A more preferable blending amount is 25 to 35% by weight.

The anti-inflammatory analgesic which is another essential component of the external preparation for skin of the present invention is not particularly limited as long as it is a commonly used anti-inflammatory analgesic, but specifically, indomethacin and salicylic acid. Methyl, diclofenac sodium, flufenamic acid, bufexamac, ibuprofen, zaltoprofen, naproxen, flurbiprofen, phlorobiprofen acetyl, fenbufen, mefenamic acid, piroxicam, ampyroicum,
Tenoxicam, felbinac, tocoretinate, hydrocortisone, prednisolone, methylprednisolone,
Betamethasone, dexamethasone, triamsilonone, triamsilonone acetonide, flumethasone, fluocinonide, beclomethasone, fluocinolone, fluoxycortide, mometasone, clobetasone, clobetasol, prednisolone valerate acetate, propionate hydrocortisone, amphenacuronin, oxapronine, oxapronine. Is mentioned. These anti-inflammatory analgesics may be used alone or in combination of two or more. The suitable compounding amount of such an anti-inflammatory analgesic varies depending on the type of the anti-inflammatory analgesic, but is approximately 0.1 to 10% by weight.
Is. This is because if it is less than 0.1%, the anti-inflammatory and analgesic action cannot be expected, and if it exceeds 10% by weight, the action will reach the ceiling. A more preferable compounding amount is 1 to 5% by weight, which has a clear anti-inflammatory and analgesic effect and has a large effect on the concentration.

The external preparation for skin of the present invention contains various optional components necessary for formulation into a dosage form, in addition to such a moisturizing component and an anti-inflammatory analgesic. The optional component is not particularly limited as long as it is usually used for external preparations for skin, for example,
Hydrocarbons such as liquid paraffin and petrolatum, esters such as jojoba oil and gayleu, triglycerides such as olive oil and beef tallow, higher alcohols such as cetanol and stearyl alcohol, stearic acid and palmitic acid. Higher fatty acids, stearic acid monoglyceride, polyoxyethylene hydrogenated castor oil, sorbitan monostearate, nonionic surfactants such as polyoxyethylene sorbitan monostearate, sodium lauryl sulfate, anionic surfactants such as sodium alkylsulfosuccinate, Cationic surfactants such as alkyl ammonium salts, amphoteric surfactants such as alkyl betaines, preservatives such as parabens, UV absorbers such as aminobenzoic acid derivatives, tocopherols, antioxidants such as butylhydroxytoluene, fragrances, pH adjusting agents such as acids salts.

The external preparation for skin of the present invention is obtained by formulating such components by a conventional method, and the dosage form is not particularly limited. Examples of dosage forms include lotions, creams, gels, emulsions, ointments and the like.

(2) Action of the external preparation for skin of the present invention The external preparation for skin of the present invention compensates for the skin function impaired by inflammation by the action of the moisturizing component and suppresses the inflammation by the action of the anti-inflammatory analgesic. Administration of conventional anti-inflammatory and analgesic external preparations such as atopic dermatitis has the effect of remarkably improving the symptoms of dermatitis, for which little improvement in symptoms can be expected.

In order to obtain such effects of the external preparation for skin of the present invention, the external preparation for skin of the present invention may be applied uniformly to the affected area in which inflammation is occurring and its vicinity several times a day. .

[0013]

The present invention will be described in more detail with reference to the following examples, but it goes without saying that the present invention is not limited to these examples. The numerical values in the formulation examples are parts by weight.

Example 1. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Bufexamac 1 (B) Propylene glycol 5 Glycerin 25 Methylparaben 0.3 Water 18.6

Example 2. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Indomethacin 1 (B) Propylene glycol 5 Glycerin 15 Maltose 6 Methylparaben 0.3 Water 22.6

Embodiment 3. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Bufexamac 1 (B) Propylene glycol 5 Glycerin 20 l-Threonine 3 Methylparaben 0.3 Water 25.6

Embodiment 4. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Tenoxicam 1 (B) Propylene glycol 5 Glycerin 20 Sodium chondroitin sulfate 2 Methylparaben 0.3 Water 21.6

Example 5. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Ibuprofen 1 (B) Propylene glycol 5 Glycerin 25 Sodium pyrrolidonecarboxylate 3 Methylparaben 0.3 Water 15.6

Example 6. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 15 Egg yolk lecithin 5 Butylparaben 0.1 Indomethacin 1 (B) Propylene glycol 5 Glycerin 25 Methylparaben 0.3 Water 18.6

Example 7. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 10 Soybean lecithin 5 Butylparaben 0.1 Indomethacin 1 (B) Propylene glycol 5 Glycerin 25 Glycine 3 Pyrrolidonecarboxylic acid triethanolamine 2 Methylparaben 0.3 Water 18.6

Example 8. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 10 Butylparaben 0.1 Indomethacin 1 (B) Propylene glycol 5 Glycerin 17 Serine 3 Methylparaben 0.3 Water 33.6

Example 9. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Indomethacin 1 (B) Propylene glycol 5 Glycerin 20 Chitin 1 Methylparaben 0.3 Water 22.6

Example 10. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Lecithin 5 Butylparaben 0.1 Indomethacin 1 (B) Propylene glycol 5 Glycerin 15 Methylparaben 0.3 Water 23.6

Example 11. Formulation example A cream was prepared based on the formulation shown below. That is, components A and B were heated and dissolved at 80 ° C., B was gradually added to A and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Indomethacin 1 (B) Propylene glycol 5 Glycerin 20 Glucose 2 1-Alanine 3 Methylparaben 0.3 Water 18.6

Example 12 Conductance Measurement The effects of the creams of Examples 1 to 11 and the creams of the following comparative examples on the conductance on the skin, which is an index of the skin moisturizing function, were examined. That is, after applying the cream, after quietly spending 1 hour in a thermostatic chamber at 25 ° C., the skin conductance was measured with a skin surface hydrometer (IBS Co., SKIKON-200). The results are shown in Table 1. From this, it is understood that the external preparation for skin of the present invention improves the moisturizing function of the skin. (Comparative Example) A cream was prepared based on the following formulation. That is, A and B components are heated and melted at 80 ° C.
Was gradually added and cooled to obtain a cream. (A) Microcrystalline wax 20 Polyoxyethylene (20) Stearyl 5 Cetanol 5 Squalane 20 Butylparaben 0.1 Bufexamac 1 (B) Propylene glycol 5 Glycerin 10 Methylparaben 0.3 Water 33.6

[0026]

[Table 1]

Example 13 Usage test: 13 patients with atopic dermatitis and 7 voluntarily 7 groups A and 6
The group A is divided into the group B, and the group A is treated with the cream of Example 1 for the first week and then left uncoated for the next week to eliminate the effect of the cream of Example 1 and continue for the next week. I got it using the cream of the comparative example. Further, the other group B was treated with the cream of the comparative example for the first week and left uncoated for the next week to eliminate the influence of the cream of the comparative example, and for the following week, the cream of the example 1 was continued. I got it using. After that, a questionnaire was asked to determine which cream is more effective in suppressing atopic dermatitis. The results are shown in Table 2. From this, the cream of the present invention is superior in the effect of suppressing atopic dermatitis than the cream of the comparative example regardless of the time of use, and the combination of a moisturizing component and an anti-inflammatory analgesic is effective against atopic dermatitis. I understand things.

[0028]

[Table 2]

[0029]

The external preparation for skin of the present invention supplements the moisturizing function of the skin and suppresses inflammation by the antiphlogistic / analgesic agent, so that acetogenic dermatitis can be effectively suppressed.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI Technical indication location A61K 31/045 9455-4C 31/18 9455-4C 31/19 9455-4C 31/195 9455-4C 31/38 31/405 31/42 31/47 31/54 31/57 31/60 31/70 31/725 45/00 AAH ABE AGZ // (A61K 31/18 31: 045) (A61K 31/18 31 : 195) (A61K 31/19 31: 045) (A61K 31/405 31:70) (A61K 31/54 31: 725)

Claims (7)

[Claims] 1. An external preparation for skin comprising 20 to 40% by weight of one or more moisturizing components selected from the following Group A and 0.1 to 10% by weight of an anti-inflammatory analgesic. (A) Amino acid and / or salt thereof, saccharide, polyhydric alcohol, polysaccharide and / or salt thereof, pyrrolidonecarboxylic acid and / or salt thereof, phospholipid 2. The amino acid is one or more selected from lysine, threonine, serine, alanine and glycine.
The external preparation for skin according to claim 1. 3. The external preparation for skin according to claim 1, wherein the saccharide is one or more selected from glucose, lactose and maltose. 4. The external preparation for skin according to claim 1, wherein the polyhydric alcohol is glycerin. 5. The polysaccharide is chondroitin sulfate, mucin,
The external preparation for skin according to claim 1, which is chitin. 6. The method according to claim 1, wherein the phospholipid is lecithin.
The external preparation for skin according to 5. 7. The external preparation for skin according to claim 1, wherein the anti-inflammatory analgesic is one or more selected from the following group B. (B) indomethacin, methyl salicylate, diclofenac sodium, flufenamic acid, bufexamac, ibuprofen, zaltoprofen, naproxen, flurbiprofen, phlorobiprofen acetyl, fenbufen, mefenamic acid, piroxicam, ampiricicum, tenoxicam, felbinac, tocolectinate, Hydrocortisone, prednisolone, methylprednisolone, betamethasone, dexamethasone, triamsilonone, triamsilonone acetonide, flumethasone, fluocinonide, beclomethasone, fluocinolone, fluoxycortide, mometasone, clobetasone,
Clobetasol, valeric acid prednisolone acetate, hydrocortisone butyrate propionate, ampenac sodium,
Oxaprozin, Floctaphenin