JPH0328402B2 - - Google Patents
Info
- Publication number
- JPH0328402B2 JPH0328402B2 JP1917681A JP1917681A JPH0328402B2 JP H0328402 B2 JPH0328402 B2 JP H0328402B2 JP 1917681 A JP1917681 A JP 1917681A JP 1917681 A JP1917681 A JP 1917681A JP H0328402 B2 JPH0328402 B2 JP H0328402B2
- Authority
- JP
- Japan
- Prior art keywords
- acne
- cream
- acid
- pharmaceutically acceptable
- treatment
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- 239000006071 cream Substances 0.000 claims description 13
- BDJRBEYXGGNYIS-UHFFFAOYSA-N nonanedioic acid Chemical compound OC(=O)CCCCCCCC(O)=O BDJRBEYXGGNYIS-UHFFFAOYSA-N 0.000 claims description 10
- 239000004480 active ingredient Substances 0.000 claims description 5
- 230000003255 anti-acne Effects 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 4
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 0.000 claims description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 239000006210 lotion Substances 0.000 claims description 2
- 239000002674 ointment Substances 0.000 claims description 2
- 230000000699 topical effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 206010000496 acne Diseases 0.000 description 20
- 208000002874 Acne Vulgaris Diseases 0.000 description 16
- 239000000203 mixture Substances 0.000 description 10
- CFKMVGJGLGKFKI-UHFFFAOYSA-N 4-chloro-m-cresol Chemical compound CC1=CC(O)=CC=C1Cl CFKMVGJGLGKFKI-UHFFFAOYSA-N 0.000 description 4
- 210000004907 gland Anatomy 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 206010037888 Rash pustular Diseases 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 229960002242 chlorocresol Drugs 0.000 description 2
- 150000001991 dicarboxylic acids Chemical class 0.000 description 2
- 239000012153 distilled water Substances 0.000 description 2
- TVIDDXQYHWJXFK-UHFFFAOYSA-N dodecanedioic acid Chemical compound OC(=O)CCCCCCCCCCC(O)=O TVIDDXQYHWJXFK-UHFFFAOYSA-N 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 2
- WLJVNTCWHIRURA-UHFFFAOYSA-N pimelic acid Chemical compound OC(=O)CCCCCC(O)=O WLJVNTCWHIRURA-UHFFFAOYSA-N 0.000 description 2
- 208000029561 pustule Diseases 0.000 description 2
- 229960004889 salicylic acid Drugs 0.000 description 2
- CXMXRPHRNRROMY-UHFFFAOYSA-N sebacic acid Chemical compound OC(=O)CCCCCCCCC(O)=O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 description 2
- 208000017520 skin disease Diseases 0.000 description 2
- LWBHHRRTOZQPDM-UHFFFAOYSA-N undecanedioic acid Chemical compound OC(=O)CCCCCCCCCC(O)=O LWBHHRRTOZQPDM-UHFFFAOYSA-N 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- BNIZTLSGVTUSPW-UHFFFAOYSA-N 2-dodecoxyethanamine Chemical compound CCCCCCCCCCCCOCCN BNIZTLSGVTUSPW-UHFFFAOYSA-N 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- 206010054107 Nodule Diseases 0.000 description 1
- 206010033733 Papule Diseases 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- -1 Polyoxyethylene Polymers 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 206010039509 Scab Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 206010043417 Therapeutic response unexpected Diseases 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000031513 cyst Diseases 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- SMVRDGHCVNAOIN-UHFFFAOYSA-L disodium;1-dodecoxydodecane;sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O.CCCCCCCCCCCCOCCCCCCCCCCCC SMVRDGHCVNAOIN-UHFFFAOYSA-L 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002996 emotional effect Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 125000005456 glyceride group Chemical group 0.000 description 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 1
- 210000002149 gonad Anatomy 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000007803 itching Effects 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- DXNCZXXFRKPEPY-UHFFFAOYSA-N tridecanedioic acid Chemical compound OC(=O)CCCCCCCCCCCC(O)=O DXNCZXXFRKPEPY-UHFFFAOYSA-N 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
Description
【発明の詳細な説明】 本発明は抗ニキビ外用剤に関する。[Detailed description of the invention] The present invention relates to an anti-acne external preparation.
本発明者は、先に、炭素原子７乃至１３を有す
るジカルボン酸、少なくとも１の還元性官能基を
有するその誘導体又はその製薬上許容される塩を
活性成分として含む色素過多皮膚病の治療剤を見
出した。 The present inventor has previously proposed a therapeutic agent for hyperpigmented skin diseases containing a dicarboxylic acid having 7 to 13 carbon atoms, a derivative thereof having at least one reducing functional group, or a pharmaceutically acceptable salt thereof as an active ingredient. I found it.
本発明者は、ここに、上記した組成物が座瘡の
処置の抗ニキビ皮膚外用剤の活性成分は全炭素数
（カルボキシル基の炭素も含む）が７乃至１３で
あるａ，ω−飽和脂肪族ジカルボン酸又はその製
薬上許容される塩であり、予期せざる治療効果を
示すことを見出した。本発明において、より好ま
しいジカルボン酸はピメリン酸、ゼベリン酸、ア
ゼライン酸、セバシン酸、１，９−ノナンジカル
ボン酸、１，10−デカンジカルボン酸及び、１，
11−ウンデカンジカルボン酸である。その誘導体
としてはナトリウム塩等の製薬上許容される塩が
ある。 The present inventor hereby provides that the active ingredient of the anti-acne skin external preparation for the treatment of acne in the composition described above is an a,ω-saturated fat having a total carbon number of 7 to 13 (including carbons in the carboxyl group). dicarboxylic acids or pharmaceutically acceptable salts thereof, and have been found to exhibit unexpected therapeutic effects. In the present invention, more preferred dicarboxylic acids are pimelic acid, xeveric acid, azelaic acid, sebacic acid, 1,9-nonanedicarboxylic acid, 1,10-decanedicarboxylic acid and 1,
11-undecanedicarboxylic acid. Derivatives thereof include pharmaceutically acceptable salts such as sodium salts.
知られるように、座瘡（ニキビ）は主に顔面
（及び肩や胸）の皮膚を冒す膚病であり、吹出物
や面皰やのうほうを生じ、皮膚腺の感染によつて
起こる。この座瘡は主に12，13から20才の若者に
多く発生する。座瘡の最初の原因は、ある腺、特
に性腺（これは10代はじめに特に活発でしばしば
不安定になる）及び成長に関する腺の活動の一時
的異常にある。小腺のバランスと正常な働きを狂
わす感情の変化もまた座瘡を生ずる原因となる。 As is known, acne is a skin disease that primarily affects the skin of the face (and shoulders and chest), causing pimples, comedones, and cysts, and is caused by infection of the skin glands. This acne mainly occurs in young people between the ages of 12 and 13 to 20. The initial cause of acne lies in temporary abnormalities in the activity of certain glands, especially the gonads (which are especially active and often unstable in the early teens) and growth glands. Emotional changes that disrupt the balance and normal functioning of the glands can also cause acne.
本発明の抗ニキビ皮膚外用剤はクリーム、軟膏
又はローシヨンとして用いられる。活性成分は、
公知の処方に従つて、ガレン式調剤で通常用いら
れる周知の製薬上許容されるビヒクルと混合され
る。 The anti-acne skin external preparation of the present invention is used as a cream, ointment or lotion. The active ingredient is
It is mixed according to known formulations with well-known pharmaceutically acceptable vehicles commonly used in galenic formulations.
以下の実施例１〜３は座瘡治療に用いられるク
リーム組成物の一例であり、本発明を制限するも
のではない。 Examples 1 to 3 below are examples of cream compositions used for acne treatment and are not intended to limit the invention.
実施例 １ 次の組成のクリームを調製した。Example 1 A cream with the following composition was prepared.
重量％
アゼライン酸 15.0
クロロクレゾール 0.1
二酸化チタン 1.0
サリチル酸 2.0
グリセロールモノステアレート 2.0
セチルアルコール 3.0
Tween80 5.0
ラウリルエーテル硫酸ナトリウム 10.0
ラウリルエーテル硫酸エタノールアミン 1.0
オリーブ油 2.0
ビタミンＣ 1.0
蒸留水 残部（100％まで）
このクリーム組成物を中位の座瘡（面皰、膿
疱、丘疹、小節）を有する20〜24才の10人の女性
に１日２回２ケ月間適用した。これらのうち３例
はあご部に慢性の月経前期の座瘡の影響がみられ
た。しかしさらに２ケ月間処置をつづけると、す
べての患者の座瘡は消滅した。 Weight% Azelaic acid 15.0 Chlorocresol 0.1 Titanium dioxide 1.0 Salicylic acid 2.0 Glycerol monostearate 2.0 Cetyl alcohol 3.0 Tween80 5.0 Sodium lauryl ether sulfate 10.0 Ethanolamine lauryl ether sulfate 1.0 Olive oil 2.0 Vitamin C 1.0 Distilled water Balance (up to 100%) This cream composition The product was applied twice a day for 2 months to 10 women aged 20-24 years with moderate acne (comedones, pustules, papules, nodules). In three of these cases, the chin area was affected by chronic premenstrual acne. However, after continuing treatment for two more months, all patients' acne disappeared.
上記クリーム組成物中のクロロクレゾール及び
サリチル酸を欠いたクリーム組成物を用いて同様
な処置を続けることにより、ほぼ同様な結果が得
られた。すなわち、20〜24才の中程度のニキビ症
状の女性10人に１日２回クリームを適用すること
により、２〜４ケ月の間に全員完治した。 Substantially similar results were obtained by continuing a similar treatment using a cream composition lacking the chlorocresol and salicylic acid in the cream composition described above. That is, by applying the cream twice a day to 10 women aged 20 to 24 with moderate acne symptoms, all of them were completely cured within 2 to 4 months.
実施例 ２
実施例１に示したと同じクリームを１日２回程
度の異なる尋常性座瘡の10例（16〜25才の男性６
人，女性４人）の処置に用いた。膿疱は速か（１
〜２日）に乾燥し、小節は直ちに平らになり炎症
反応は消え、４〜６日後にかさぶたができた。２
ケ月間処置すると、すべての患者が治つた。この
治療は抗生物質による通常の治療に耐性がない重
症の座瘡の患者に特に有効である。Example 2 The same cream shown in Example 1 was administered to 10 different cases of acne vulgaris (6 males aged 16 to 25) about twice a day.
It was used in the treatment of 4 women. Is the pustule fast? (1)
The nodule immediately flattened, the inflammatory reaction disappeared, and a scab formed after 4-6 days. 2
After several months of treatment, all patients were cured. This treatment is particularly effective for patients with severe acne that is not resistant to conventional treatment with antibiotics.
実施例 ３
実施例１に記載したクリームを１日２回、閉じ
た面皰で主に表わされる非炎症性座瘡を有する15
〜18才の３人の女性に適用した。クリームを適用
後３〜４ケ月で患者の治療は完了した。Example 3 Applying the cream described in Example 1 twice a day to patients with non-inflammatory acne manifested primarily by closed comedones.
It was applied to three women aged ~18 years. The patient's treatment was completed 3-4 months after applying the cream.
本発明の抗ニキビ皮膚外用剤を用いる治療で
は、治療の初期及び治療の過程で、患者は一時の
かゆみと炎症を感じ、皮膚はわずかに赤くうろこ
状になる。 In the treatment using the anti-acne skin topical preparation of the present invention, the patient feels temporary itching and inflammation, and the skin becomes slightly red and scaly at the beginning and during the course of the treatment.
実施例 ４
ニキビ（acne vulgaris）を有する25人の患者
（女性13人、男性12人）を次なる組成のクリーム
で処置した。Example 4 Twenty-five patients (13 women, 12 men) with acne (acne vulgaris) were treated with a cream of the following composition.
アゼライン酸 20.0％
脂肪酸のポリオキシエチレンエステル 5.0％
グリセリドとワツクスの混合物 7.0％
セテアリールオクタネート
（cetearyloctanate） 3.0％
グリセロール 1.5％
プロピレングリコール 12.5％
安息香酸（保存剤） 6.2％
蒸留水 50.8％
100％
１日に２回適用処置することにより、２〜４ケ
月の間にすべての患者のニキビがなおるという優
れた作用効果を示した。 Azelaic acid 20.0% Polyoxyethylene ester of fatty acids 5.0% Glyceride and wax mixture 7.0% Cetearyloctanate 3.0% Glycerol 1.5% Propylene glycol 12.5% Benzoic acid (preservative) 6.2% Distilled water 50.8% 100% 1 By applying the treatment twice a day, all patients' acne was cured within 2 to 4 months, showing excellent efficacy.
クリームの活性成分としてアゼライン酸を他の
酸で置きかえて用いることができることはいうま
でもない。 It goes without saying that other acids can be used in place of azelaic acid as the active ingredient in the cream.
Claims (1)
ａ，ω−飽和脂肪族ジカルボン酸又はその製薬上
許容される塩を製薬上許容される担体中に含むこ
とを特徴とする抗ニキビ皮膚外用剤。 ２ 製薬上許容される担体が、クリーム、軟膏又
はローシヨン状である特許請求の範囲第１項記載
の治療剤。 ３ ジカルボン酸がアゼライン酸である特許請求
の範囲第１項記載の治療剤。[Scope of Claims] 1. It is characterized by containing an a,ω-saturated aliphatic dicarboxylic acid having a total carbon number of 7 to 13 or a pharmaceutically acceptable salt thereof as an active ingredient in a pharmaceutically acceptable carrier. Anti-acne skin topical preparation. 2. The therapeutic agent according to claim 1, wherein the pharmaceutically acceptable carrier is in the form of a cream, ointment, or lotion. 3. The therapeutic agent according to claim 1, wherein the dicarboxylic acid is azelaic acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1917681A JPS57134416A (en) | 1981-02-13 | 1981-02-13 | Acne treatment and therapeutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1917681A JPS57134416A (en) | 1981-02-13 | 1981-02-13 | Acne treatment and therapeutical composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS57134416A JPS57134416A (en) | 1982-08-19 |
| JPH0328402B2 true JPH0328402B2 (en) | 1991-04-19 |
Family
ID=11992035
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1917681A Granted JPS57134416A (en) | 1981-02-13 | 1981-02-13 | Acne treatment and therapeutical composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS57134416A (en) |
-
1981
- 1981-02-13 JP JP1917681A patent/JPS57134416A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS57134416A (en) | 1982-08-19 |
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