JPS60156608A - Ointment - Google Patents

Ointment

Info

Publication number
JPS60156608A
JPS60156608A JP59012696A JP1269684A JPS60156608A JP S60156608 A JPS60156608 A JP S60156608A JP 59012696 A JP59012696 A JP 59012696A JP 1269684 A JP1269684 A JP 1269684A JP S60156608 A JPS60156608 A JP S60156608A
Authority
JP
Japan
Prior art keywords
ointment
water
gentamicin sulfate
alcohol
prepared
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.)
Granted
Application number
JP59012696A
Other languages
Japanese (ja)
Other versions
JPH0219090B2 (en
Inventor
Youji Takashima
高島 雍治
Shigeo Tanaka
田中 重男
Ichiro Kawamata
川又 一郎
Hiroshi Murayama
村山 普
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Taisho Pharmaceutical Co Ltd
Original Assignee
Taisho Pharmaceutical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Taisho Pharmaceutical Co Ltd filed Critical Taisho Pharmaceutical Co Ltd
Priority to JP59012696A priority Critical patent/JPS60156608A/en
Publication of JPS60156608A publication Critical patent/JPS60156608A/en
Publication of JPH0219090B2 publication Critical patent/JPH0219090B2/ja
Granted legal-status Critical Current

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  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PURPOSE:An ointment, prepared by limiting the mixing proportion of an alcohol with water, and using a base containing a small amount of sodium pyrosulfate, containing gentamicin sulfate and adrenocortical hormone in a solution state, and effective for treating inflammatory dermatopathy, etc. CONSTITUTION:An ointment, prepared by using a mixture containing 2.0- 10.0pts.wt. preferably 3.0-7.0pts.wt. alcohol and water at 1:1-9:1 ratio, 0.1- 6.0pts.wt. surfactant, preferably a monionic surfactant, 97-75pts.wt. higher poraffinic hydrocarbon, preferably 16-40C and 0.02-0.2pts.wt., preferably 0.02- 0.o4pts.wt. sodium pyrosulfate as a base and further 0.2-5mg potency gentamicin sulfate and 0.2-5mg adrenocortical hormone, e.g. hydrocortisone or betamethasone valerate in 1g product. The amount of the water is preferably as large as possible so long as the contained adrenocortical hormone can be dissolved.

Description

【発明の詳細な説明】 本発明は軟膏に関し、更に詳しくは硫酸ゲンタマイシン
と副腎皮質ホルモンを含有する軟膏に関する。
DETAILED DESCRIPTION OF THE INVENTION The present invention relates to ointments, and more particularly to ointments containing gentamicin sulfate and corticosteroids.

炎症性皮崩疾患の治療に使用する軟膏には、。Ointments used to treat inflammatory skin disintegration diseases include:

患部に対して消炎、止痛作用を有する副腎皮質ホルモン
と患部の細菌感染を防止する抗生物質とを併用するのが
好ましく、また両者は基剤中に溶解状態で存在している
のが効果的である。
It is preferable to use adrenocortical hormones, which have anti-inflammatory and analgesic effects on the affected area, and antibiotics, which prevent bacterial infection in the affected area, in combination, and it is effective for both to be present in a dissolved state in the base. be.

しかしながら、抗生物質として硫酸ゲンタマイシンを選
定し、これと副腎皮質ホル、モンを併用する場合、硫酸
ゲンタマイシンは水には極めてよく溶解するがアルコー
ル類には溶解しないし、副腎皮質ホルモンはアルコール
類、に溶解するが水には溶解せず、アルコール類、と水
の混合比を変化させるだけでは硫酸ゲンタマイシンと副
腎皮質ホルモンとの双方を溶解することはできない。
However, when selecting gentamicin sulfate as an antibiotic and using it together with adrenal corticosteroids, gentamicin sulfate is extremely soluble in water but not in alcohol; It is soluble, but not in water, and it is not possible to dissolve both gentamicin sulfate and adrenal corticosteroid simply by changing the mixing ratio of alcohol and water.

また、硫酸ゲンタマイシンと副腎皮質ホルモンの双方を
溶解している軟膏を調製するには多量の界面活性剤を必
要とするが、多、量の界面活性剤の使用は副腎皮質ホル
モンの作用を低下させてしまう。
In addition, a large amount of surfactant is required to prepare an ointment that dissolves both gentamicin sulfate and corticosteroid, but the use of a large amount of surfactant may reduce the effect of corticosteroid. It ends up.

従って、従来は硫酸ゲンタマイシンと副腎皮質ホルモン
のいずれを為または双方を結晶のまま基剤中に分散して
軟膏を調製することが多かった。
Therefore, in the past, ointments were often prepared by dispersing either or both of gentamicin sulfate and adrenocortical hormone in a base in the form of crystals.

本発明者らは、これら従来品の欠点を解消すべぐ鋭意研
究した結果、アルコール類と水の割合をある範囲に限定
t、少量のピ・硫酸ナトリウムを配合することによシ硫
ぼゲンタマイシンと副腎皮質ホルモンの双方を溶解状態
で含有し、炎症性皮膚疾患などの治療に有効な軟膏を調
製することに成功し、本発明を完成した。
As a result of intensive research to eliminate these drawbacks of conventional products, the inventors of the present invention found that by limiting the ratio of alcohol and water to a certain range and adding a small amount of sodium sulfate, gentamicin The present invention has been completed by successfully preparing an ointment that contains both adrenal cortical hormones in a dissolved state and is effective in treating inflammatory skin diseases.

本発明は、アルコール類と水を1:1〜9:1の割合で
2.0〜10.0重量部、界面活性剤を0.1重量部か
らなる混合物を基剤とし、製品12中にmfゲンタマイ
シン0.2〜5〜力価と副腎皮質ホルモン02〜5■を
含有させることを特徴とする軟膏である。
The present invention is based on a mixture of alcohol and water in a ratio of 1:1 to 9:1, consisting of 2.0 to 10.0 parts by weight and 0.1 part by weight of a surfactant. This ointment is characterized by containing mf gentamicin in a titer of 0.2 to 5 and adrenocortical hormone 02 to 5.

ここにおいて、副腎皮質ホルモンとは、ヒドロコルチゾ
ン、酪酸ヒドロコルチゾン、酪[フロピオン酸ヒドロコ
ルチゾン、吉草ばベタメタシン。
Here, adrenocortical hormones include hydrocortisone, hydrocortisone butyrate, hydrocortisone butypropionate, and betamethacin.

グレードニジロン、酢酸デキサメタシン、フルオシノ″
A7″′トート・ トリア”ジノ°7アセト=ドなどの
、水にほとんど溶解しない副腎皮質ホルモンをいう。
Grade Nigiron, Dexamethacin Acetate, Fluocino''
Refers to adrenal cortical hormones that are hardly soluble in water, such as A7'''totria'' dino°7 acetate.

アルコール類トは、エタノール、インプロパノ、−ル、
フロパノール、ベンジルアルコールナトの一価のアルコ
ール、フロピレンゲリコール、エチレンクリコール、グ
リセリン、ブタンジオール。
Alcohols include ethanol, inpropanol,
Furopanol, benzyl alcohol, monohydric alcohol, furopylene gelicol, ethylene glycol, glycerin, butanediol.

ヘキサトリオール、プロピレン〆す、コールカーボネー
トなどの多価アルコールおよびその訪樽体をいう。
Refers to polyhydric alcohols such as hexatriol, propylene alcohol, and coal carbonate, and their derivatives.

界面活性剤とは、油性軟膏の調製に利用することができ
る界面活性剤であればよいが、就中、ポリオキシエチレ
ンソルビタン脂肪酸エステル、ンルビタン脂肪酸エステ
ル、グリセリン脂肪酸エステル、プロピレングリコール
脂肪酸エステルなどで代表される非イオン性界面活性剤
〔たとえば、ニラコールTSIO,ニラコールso i
 o、ニラコールMGE+ 、 ニラコールPMS (
いずれも商品名1日本ザーファクタント工業株式会社製
)〕を使用することが好ましい。
The surfactant may be any surfactant that can be used in the preparation of oil-based ointments, and representative examples include polyoxyethylene sorbitan fatty acid ester, nrubitan fatty acid ester, glycerin fatty acid ester, propylene glycol fatty acid ester, etc. nonionic surfactants [e.g., niracol TSIO, niracol so i
o, Niracol MGE+, Niracol PMS (
In both cases, it is preferable to use product name 1 (manufactured by Nippon Surfactant Industries Co., Ltd.).

高級パラフィン系炭化水素とは、軽質流動パラフィン+
 a動パラフィン、白色ワセリン、パラフィン、セレシ
ンなどの、炭素数が16〜40程度のパラフィン系炭化
水素をいう二 本発明の軟膏は、前記の組成の範囲内において硫酸ゲン
タマイシンと副腎皮質ホルモンの双方を溶解状態で含有
し、薬効発現の改善が認められるが、特に好ましい組成
は、基剤がアルコール類と水を合わせて30〜ZO重量
部(そのうち水0.5〜3.0重量部)、界面活性剤0
5〜2.5重量部。
High paraffin hydrocarbons include light liquid paraffin +
The ointment of the present invention is made of paraffinic hydrocarbons having about 16 to 40 carbon atoms, such as a-motor paraffin, white petrolatum, paraffin, and ceresin. When contained in a dissolved state, improvement in the expression of medicinal efficacy has been observed, but a particularly preferred composition is that the base contains 30 to 30 parts by weight of ZO (including 0.5 to 3.0 parts by weight of water) including the alcohol and water, and the interface Activator 0
5-2.5 parts by weight.

高級パラフィン系炭化水素800〜95.0重量部。800 to 95.0 parts by weight of higher paraffinic hydrocarbon.

ピロ亜硫酸ナトリウム002〜0.04重量部からなり
、硫酸ゲンタマイシン0.2〜5■力価と副腎皮質ホル
モン0.2〜5 yyが製品1f中に含有されているも
のである。
The product 1f contains 0.2 to 0.04 parts by weight of sodium pyrosulfite, a titer of gentamicin sulfate of 0.2 to 5 yy, and a titer of 0.2 to 5 yy of adrenocortical hormone.

なお、アルコール類と水との割合は前記のとおが可能な
限シ水の配合量は多□い程よい。
Note that the ratio of alcohol to water is as high as possible, and the larger the amount of water, the better.

また、ピロ亜硫叡ナトリウムは、前記の範囲内で、配合
する水の量に応じて適宜増減して配合することができる
が、0.02重量部以下の配合では硫酸ゲンタマイシン
の溶解性を高める作用が低く、0.2重量部を超える配
合ではそれ自体の溶解が不可能となる。
In addition, sodium pyrosulfite can be blended within the above range, increasing or decreasing as appropriate depending on the amount of water to be blended, but if it is blended at 0.02 parts by weight or less, it increases the solubility of gentamicin sulfate. Its effectiveness is low, and if it exceeds 0.2 parts by weight, it cannot be dissolved by itself.

本発明の軟膏は、たとえば次のようにして調製すること
ができる。
The ointment of the present invention can be prepared, for example, as follows.

すなわち、副腎皮質ホルモンを加温下にアルコール類に
溶解し、これをあらかじめ加温、融解した高級パラフィ
ン系炭化水素と界面活性剤の混液に加えて加温下に攪拌
混合する。この混合物に、別途に調製した硫酸ゲンタマ
イシンとピロ亜硫酸ナトリウムの水溶液を加えて攪拌し
ながら冷却して本発明の軟膏を調製することができる。
That is, adrenal cortical hormone is dissolved in alcohol under heating, and this is added to a mixture of higher paraffinic hydrocarbon and surfactant that has been heated and melted in advance, and the mixture is stirred and mixed under heating. The ointment of the present invention can be prepared by adding a separately prepared aqueous solution of gentamicin sulfate and sodium pyrosulfite to this mixture and cooling it while stirring.

硫酸ゲンタマイシンとピロ亜硫酸ナトリウムの水溶液を
副腎皮質ホルモンのアルコール類溶液に添加することも
できるが、この場合には硫酸ゲンタマイシンと副腎皮質
ホルモンが一時的に析出す水溶液を混溶することか望ま
しい。
An aqueous solution of gentamicin sulfate and sodium pyrosulfite can be added to an alcoholic solution of adrenocortical hormone, but in this case, it is preferable to mix gentamicin sulfate and an aqueous solution in which adrenocortical hormone is temporarily precipitated.

本発明の軟膏は、硫酸ゲンタマイシンと副腎皮質ホルモ
ンの双方を溶解状態で含有するので、これら薬物の放出
性がよく、湿疹、皮膚炎、伝染性膿痴疹、化膿性皮疹を
伴った尋常性座癒、熱傷などの治療に極めて有効である
Since the ointment of the present invention contains both gentamicin sulfate and adrenocortical hormone in a dissolved state, it has good release properties and is effective for treating eczema, dermatitis, impetigo contagiosum, and acne vulgaris accompanied by purulent eruption. It is extremely effective in healing and treating burns.

以下、試験例と実施例を挙げて本発明を具体的に説明す
る。
The present invention will be specifically explained below with reference to Test Examples and Examples.

試験例1 第1表の処方によシ後記実施例1に準じて軟膏を調製し
て検体A’、B、C!、D、Eとし、調製直後と室温で
1t月保存後硫酸ゲンタマイシンと吉草酸ベタメタシン
の結晶の析出の有無を観察した。
Test Example 1 Samples A', B, and C were prepared by preparing ointment according to the recipe in Table 1 and following Example 1 below. , D, and E, and the presence or absence of precipitation of crystals of gentamicin sulfate and betamethacin valerate was observed immediately after preparation and after storage for 1 ton at room temperature.

その結果を第2表に示す。The results are shown in Table 2.

プロピレングリコールと精製水の割合を種々変化させて
みたが、硫酸ゲンタマイシンと吉草酸ベタメタシンの双
方を同時に溶解することはできなかった。
Although we tried varying the ratio of propylene glycol and purified water, we were unable to dissolve both gentamicin sulfate and betamethacin valerate at the same time.

第2表 薬物の溶解性 註) X:析出物を認めた。Table 2 Drug solubility Note) X: Precipitates were observed.

○:析出物を認めなかった。○: No precipitate was observed.

*:@製置後に硫酸ゲンタ1イク/の樹脂状の析出物を
視認した。
*: @Resinous precipitates of Gentaic sulfate were visually observed after manufacture.

肴肴:室温1ケ月保存後の偏光顕微鏡観察によシ吉草酸
ベタメタシンの結晶の析出を認めた。
Appetizer: After storage at room temperature for 1 month, observation using a polarizing microscope revealed that crystals of betamethacin valerate were precipitated.

試験例2 第3表の処方により後記実施例1に準じて軟膏を調製し
て検体F、G、H,I、Jとし、調製直後と室温で1t
月保存後硫酸ゲンタマイシンと吉草酸ベタメタシンの結
晶の析出の有無を観察した。
Test Example 2 Samples F, G, H, I, and J were prepared by preparing ointment according to Example 1 described below according to the formulation in Table 3, and 1 ton was prepared immediately after preparation and at room temperature.
After storage for months, the presence or absence of precipitation of crystals of gentamicin sulfate and betamethacin valerate was observed.

その結果を第4表に示す。The results are shown in Table 4.

註) ×、析出物を認めた。Note) x: Precipitates were observed.

○:析出物を認めなかった0 チ:調製直後に硫酸ゲンタマイシンの樹脂状の析出物を
視認した。
○: No precipitate was observed 0 H: Resin-like precipitate of gentamicin sulfate was visually observed immediately after preparation.

実施例1 白色ワセリン 92.7グ、ニラコールTS10 0.
1t、ニラコールPMS2.Ofを加温融解して油相成
分Aを調製した。
Example 1 White petrolatum 92.7g, Niracol TS10 0.
1t, Niracol PMS2. Oil phase component A was prepared by heating and melting Of.

次に加温下に吉草酸ベタメタシン o、irをプロピレ
ングリコール 4.Ovに溶解し、これを油相成分Aに
加えて攪拌した。これに、硫酸ゲンタマ亜 イシン0.1タカ価とピロ声酸ナトリウム0.031を
精製水1tに溶解した溶液を加えて撹拌して十分に分散
させた後、更に攪拌しながら冷却して軟膏100fを得
た。
Next, add betamethacin valerate o, ir to propylene glycol while heating.4. This was added to oil phase component A and stirred. To this, a solution of 0.1 taka value of gentamasinous sulfate and 0.031 sodium pyrovoate dissolved in 1 t of purified water was added and stirred to sufficiently disperse the mixture, and then cooled with further stirring to make an ointment of 100 f. I got it.

この軟膏は硫酸ゲンタマイシンまたは吉草酸ベタメタシ
ンの結晶もしくは析出物が認められなかった0 実施例2 酪酸プロピオン酸ヒドロコルチゾン 012硫酸ケンタ
マインン 017力価 プロピレングリコール 4.02 精製水 1.02 ニノコール8010 0.51i’ 流動パラフイン 10.Or 計 100.Or 実施例1に準じて上記配合の軟膏を調製した。
No crystals or precipitates of gentamicin sulfate or betamethacin valerate were observed in this ointment.Example 2 Hydrocortisone butyrate propionate 012 Kentamine sulfate 017 Potency propylene glycol 4.02 Purified water 1.02 Ninocol 8010 0.51i' Fluidity Parafine 10. Or total 100. Or An ointment having the above formulation was prepared according to Example 1.

この軟膏は酪酸プロピオン酸ヒドロコルチゾンiたは硫
ばゲンタマイシンの結晶もしくは析出物・が認められな
かった、 実施例3 フルオシノロンアセトニド 0.025f硫酸ゲンタマ
イシン 022力価 プロピレングリコール 7. Or 精製水 302 ピロ亜硫酸ナトリウム 0.22 二ノコ一ルMGS 5.07 計 100.Or 実施例1に準じて上記配合の軟膏を調製した。
No crystals or precipitates of hydrocortisone butyrate propionate or gentamicin sulfate were observed in this ointment. Example 3 Fluocinolone acetonide 0.025f Gentamicin sulfate 022 titer Propylene glycol Or Purified water 302 Sodium pyrosulfite 0.22 Ninokoil MGS 5.07 Total 100. Or An ointment having the above formulation was prepared according to Example 1.

この軟膏はフルオシノロンアセトニドまたは硫酸ゲンタ
マイシンの結晶もしくは析出物が認められなかった。
No crystals or precipitates of fluocinolone acetonide or gentamicin sulfate were observed in this ointment.

実施例4 酪酸ヒドロコルチゾン 0.21 硫酸ゲンタマイシン 0.12力価 プロピレングリコール 5.02 精製水 16ロ2 ピロ亜硫酸ナトリウム 0.04 r = 、:7−ルPMB 3.Of パラフィン 5.02 計 100.Of 実施例1に準じて上記配合の軟膏を調製した。Example 4 Hydrocortisone butyrate 0.21 Gentamicin sulfate 0.12 titer Propylene glycol 5.02 Purified water 16 ro 2 Sodium pyrosulfite 0.04 r =, :7-ru PMB 3. Of Paraffin 5.02 Total 100. Of An ointment having the above formulation was prepared according to Example 1.

この軟膏は硫酸ゲンタマイシンまたは酪酸プロピオンば
ヒドロコルチゾンの結晶もしくは析出物が認められなか
った。
No crystals or precipitates of gentamicin sulfate or propion butyrate or hydrocortisone were observed in this ointment.

特許出願人 大正製薬株式会社 代理人 弁理士 北 川 富 造Patent applicant: Taisho Pharmaceutical Co., Ltd. Agent Patent Attorney Tomizo Kitagawa

Claims (1)

【特許請求の範囲】[Claims] (1) アルコール類と水を1:1〜9°1の割合で2
0〜10.0重量部、界面活性剤を01〜6.0′重量
部、高級パラフィン系炭化水素を97〜75重量部、ピ
a亜硫・酸ナトリウムを0.02〜0.2重量部からな
る混合物を基剤とし、製品12中に硫酸ゲンタマイシン
02〜5 my力価と副腎皮質ホルモン0.2〜5 m
gを含有させることを特徴とする軟膏。
(1) Alcohol and water in a ratio of 1:1 to 9°1
0 to 10.0 parts by weight, 01 to 6.0 parts by weight of surfactant, 97 to 75 parts by weight of higher paraffinic hydrocarbon, and 0.02 to 0.2 parts by weight of sodium pia sulfite. The product 12 is based on a mixture consisting of gentamicin sulfate 02-5 my titer and corticosteroid 0.2-5 m
An ointment characterized by containing g.
JP59012696A 1984-01-26 1984-01-26 Ointment Granted JPS60156608A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP59012696A JPS60156608A (en) 1984-01-26 1984-01-26 Ointment

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP59012696A JPS60156608A (en) 1984-01-26 1984-01-26 Ointment

Publications (2)

Publication Number Publication Date
JPS60156608A true JPS60156608A (en) 1985-08-16
JPH0219090B2 JPH0219090B2 (en) 1990-04-27

Family

ID=11812542

Family Applications (1)

Application Number Title Priority Date Filing Date
JP59012696A Granted JPS60156608A (en) 1984-01-26 1984-01-26 Ointment

Country Status (1)

Country Link
JP (1) JPS60156608A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0217141A2 (en) * 1985-09-28 1987-04-08 Beiersdorf Aktiengesellschaft W/O creams containing 17-propionate-21-acetate
EP0217146A2 (en) * 1985-09-28 1987-04-08 Beiersdorf Aktiengesellschaft W/O creams containing hydrocortisone diesters

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0922261A (en) * 1995-07-06 1997-01-21 Shigeru Sugiura Optical fiber display containing movable type solar battery built in

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0217141A2 (en) * 1985-09-28 1987-04-08 Beiersdorf Aktiengesellschaft W/O creams containing 17-propionate-21-acetate
EP0217146A2 (en) * 1985-09-28 1987-04-08 Beiersdorf Aktiengesellschaft W/O creams containing hydrocortisone diesters

Also Published As

Publication number Publication date
JPH0219090B2 (en) 1990-04-27

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