JPS5995216A - Drug for external use - Google Patents
Drug for external useInfo
- Publication number
- JPS5995216A JPS5995216A JP57205859A JP20585982A JPS5995216A JP S5995216 A JPS5995216 A JP S5995216A JP 57205859 A JP57205859 A JP 57205859A JP 20585982 A JP20585982 A JP 20585982A JP S5995216 A JPS5995216 A JP S5995216A
- Authority
- JP
- Japan
- Prior art keywords
- drug
- water
- dequalinium chloride
- chloride
- cyclodextrin
- 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.)
- Pending
Links
- 229940079593 drug Drugs 0.000 title abstract description 13
- 239000003814 drug Substances 0.000 title abstract description 13
- LTNZEXKYNRNOGT-UHFFFAOYSA-N dequalinium chloride Chemical compound [Cl-].[Cl-].C1=CC=C2[N+](CCCCCCCCCC[N+]3=C4C=CC=CC4=C(N)C=C3C)=C(C)C=C(N)C2=C1 LTNZEXKYNRNOGT-UHFFFAOYSA-N 0.000 claims abstract description 24
- 229960001378 dequalinium chloride Drugs 0.000 claims abstract description 23
- 238000002360 preparation method Methods 0.000 claims abstract description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 29
- 239000003795 chemical substances by application Substances 0.000 abstract description 6
- 239000000203 mixture Substances 0.000 abstract description 6
- 229920000858 Cyclodextrin Polymers 0.000 abstract description 5
- 239000001116 FEMA 4028 Substances 0.000 abstract description 5
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 abstract description 5
- 235000011175 beta-cyclodextrine Nutrition 0.000 abstract description 5
- 229960004853 betadex Drugs 0.000 abstract description 5
- 239000006071 cream Substances 0.000 abstract description 5
- 239000007788 liquid Substances 0.000 abstract description 5
- 239000004094 surface-active agent Substances 0.000 abstract description 5
- 239000000499 gel Substances 0.000 abstract description 3
- 239000006210 lotion Substances 0.000 abstract description 2
- 210000002966 serum Anatomy 0.000 abstract description 2
- 238000013329 compounding Methods 0.000 abstract 2
- 239000000645 desinfectant Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000002779 inactivation Effects 0.000 abstract 1
- 239000000758 substrate Substances 0.000 abstract 1
- 239000008213 purified water Substances 0.000 description 15
- -1 etc.) Substances 0.000 description 8
- 239000012071 phase Substances 0.000 description 8
- 239000003921 oil Substances 0.000 description 7
- 235000019198 oils Nutrition 0.000 description 7
- 238000003756 stirring Methods 0.000 description 6
- 239000002585 base Substances 0.000 description 5
- 238000010438 heat treatment Methods 0.000 description 4
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 3
- 239000005977 Ethylene Substances 0.000 description 3
- 239000008346 aqueous phase Substances 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 3
- 229960000520 diphenhydramine Drugs 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 229930003231 vitamin Natural products 0.000 description 3
- 239000011782 vitamin Substances 0.000 description 3
- 229940088594 vitamin Drugs 0.000 description 3
- 235000013343 vitamin Nutrition 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 description 2
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 239000012190 activator Substances 0.000 description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-N ammonia Natural products N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
- 239000000739 antihistaminic agent Substances 0.000 description 2
- 229940125715 antihistaminic agent Drugs 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000003589 local anesthetic agent Substances 0.000 description 2
- 229960005015 local anesthetics Drugs 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 229940105132 myristate Drugs 0.000 description 2
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 2
- 239000002244 precipitate Substances 0.000 description 2
- 229940032094 squalane Drugs 0.000 description 2
- TUNFSRHWOTWDNC-UHFFFAOYSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 2
- 239000005526 vasoconstrictor agent Substances 0.000 description 2
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- 240000006766 Cornus mas Species 0.000 description 1
- 241000270288 Gekko Species 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 241001441724 Tetraodontidae Species 0.000 description 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 description 1
- MECHNRXZTMCUDQ-UHFFFAOYSA-N Vitamin D2 Natural products C1CCC2(C)C(C(C)C=CC(C)C(C)C)CCC2C1=CC=C1CC(O)CCC1=C MECHNRXZTMCUDQ-UHFFFAOYSA-N 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 239000003899 bactericide agent Substances 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000003245 coal Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960002061 ergocalciferol Drugs 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 229960005016 naphazoline Drugs 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000001892 vitamin D2 Nutrition 0.000 description 1
- MECHNRXZTMCUDQ-RKHKHRCZSA-N vitamin D2 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)/C=C/[C@H](C)C(C)C)=C\C=C1\C[C@@H](O)CCC1=C MECHNRXZTMCUDQ-RKHKHRCZSA-N 0.000 description 1
- 239000011653 vitamin D2 Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
不発ＩＪ、］は外用剤に関し、更に詳しくは塩化テノノ
リニウムとβ−７クロデキストリンとを基剤に配合して
なる殺菌性外用剤である。DETAILED DESCRIPTION OF THE INVENTION [Dufu IJ] relates to an external preparation, and more specifically, it is a bactericidal external preparation containing tenonorinium chloride and β-7 clodextrin as a base.
塩化デカリニウム〔１，１′−デカメチレンビス（４−
アミンギナルジニウム クロリド）。Dequalinium chloride [1,1'-decamethylenebis(4-
amineginaldinium chloride).
Ｃ３０Ｈ４０Ｃ／１ｐＮ４．分子量５２７６０〕は血清
によって不活化されにりく、安定性も良好な優れた殺菌
剤であるか、油相成分に殆ど溶解せず、大量の岑＋ｆ＋
ｉ活性剤の使用なくしては水にも溶解しにくいのてその
［製剤化が困難であり、寸た折角製剤化しても保存中に
基剤から析出しやすい欠点があった。C30H40C/1pN4. [Molecular weight 52,760] is an excellent bactericidal agent that is not easily inactivated by serum and has good stability.
Without the use of an activator, it is difficult to formulate a formulation because it is difficult to dissolve in water, and even if it is made into a formulation, it has the disadvantage that it tends to precipitate from the base during storage.
本発明者は、これらの欠点を解消すべく鋭意研究の結果
、β−７クロテキストリ／を配合することにより塩化デ
カＩＪ ニウムを多量に含み、且つ保存安定性のすぐれ
た外用剤を容易に得ることに成功し、本発明を完成した
。As a result of intensive research in order to eliminate these drawbacks, the present inventors have found that by incorporating β-7 clotextry, it is possible to easily create an external preparation that contains a large amount of decaIJnium chloride and has excellent storage stability. The present invention was successfully completed.
本発明の外用剤は、０１〜０８重量％の塩化デカリニウ
ムと０１〜１００重量％のβ−シクロテキストリンとを
基剤に配合してなる外用剤である。The external preparation of the present invention is an external preparation prepared by blending 01 to 08% by weight of dequalinium chloride and 01 to 100% by weight of β-cyclotextrin into a base.
ここにおいて、外用剤は液剤、ローンヨン剤。Here, external preparations include liquid preparations and lawn-on preparations.
ゲル剤、クリーム剤などの各種剤型を含み、剤型の種類
に適した基剤を用いる。It includes various dosage forms such as gels and creams, and a base suitable for the type of dosage form is used.
基剤は水と水相成分、捷たけ水と水相成分と油相成分と
の混合物からなる。The base consists of a mixture of water, aqueous phase components, strained water, aqueous phase components, and oil phase components.
本発明の外用剤においては、塩化デカリニウムを０１〜
０８重量％、好ましくは０２〜０７重量％：β−７クロ
テキストリンを０１〜１ Ｄ、 ０重量％、好ましくは
４０〜７０重量％、水板外の水相成分と油相成分と界面
活性剤とをあわせて８０〜２００重量％、好捷しくけ１
０〜１４重量％、必要に応じて局所麻酔剤、抗ヒスタミ
ン剤、血管収縮剤、ビタミン剤なとの薬剤の適当量を配
合し、剤４１；１．Ｉに応じて水を適正量配合する。In the external preparation of the present invention, dequalinium chloride is
08% by weight, preferably 02-07% by weight: β-7 crotextrin in 01-1D, 0% by weight, preferably 40-70% by weight, aqueous phase components and oil phase components outside the water plate and surface activity. 80-200% by weight together with the agent, 1
0 to 14% by weight, and appropriate amounts of drugs such as local anesthetics, antihistamines, vasoconstrictors, vitamins, etc. are blended as necessary, and Agent 41; 1. Add appropriate amount of water according to I.
水相成分としては、水、多価アルコール類（たトエば、
グロピレングリコール、グリセリン、ポリエチレングリ
コール、ノルビトールなど）、油相成分としては、油脂
類（たとえば、ゴマ油、犬スλ油なと）、ロウ類（たと
えば、ミツロウ、ラノリンなど）高級炭化水素類（たと
えば、流動パランイノ、スクワラン、パラフィンなど）
、高級アレ
級脂肪酸エステル類（たとえば、ミリスチン酸イノプロ
ピル、ミリスチン酸オクチルドデンルなど）：界ｄ＋ｊ
活性剤としてはポリオキンエチレンソルビタン脂肪酸エ
ステル、ソルビタン脂肪酸エステル。Water phase components include water, polyhydric alcohols
glopylene glycol, glycerin, polyethylene glycol, norbitol, etc.), oil phase components include oils and fats (e.g., sesame oil, dogwood oil, etc.), waxes (e.g., beeswax, lanolin, etc.), higher hydrocarbons (e.g., , liquid paran-ino, squalane, paraffin, etc.)
, higher arealic fatty acid esters (e.g., inopropyl myristate, octyldodenyl myristate, etc.): d+j
The activator is polyquine ethylene sorbitan fatty acid ester, sorbitan fatty acid ester.
ボリオギシエチレン高級アルコールエステルなど。Boriogyshiethylene higher alcohol ester, etc.
局所麻酔剤としては／ブカインなど、抗ヒスタミン剤と
してはジフェンヒドラミンなど、血管収縮剤としてはナ
ファゾリンなど：ビタミン剤としてはビタミンＡ、ビタ
ミンＤ２．ビタミンＥなどを用いることができる。Local anesthetics include bucaine, antihistamines include diphenhydramine, vasoconstrictors include naphazoline, and vitamins include vitamin A, vitamin D2, etc. Vitamin E etc. can be used.
本発明の外用剤は、たとえば次の方法によって製造する
ことができる。The external preparation of the present invention can be produced, for example, by the following method.
（液 剤）
加温下に精製水にβ−７クロデキストｌ）ンを溶解した
後、これに更に塩化デカリニウムおよび必要に応じてそ
の他の′水溶性薬剤を溶解し、これを３０℃壕で急冷す
る。(Liquid) After dissolving β-7 clodextone in purified water under heating, dequalinium chloride and other water-soluble drugs as necessary are further dissolved therein, and the solution is rapidly cooled in a trench at 30°C. do.
（ロー／ワン剤）
加温下に精製水にβ−７クロデキストリンを溶解した後
、更に塩化デカリニウムおよび必要に応じてその他の水
溶性薬剤を溶解した。これを、あらかじめ加温下に水相
成分、油相成分、界面活性剤および油溶性薬剤を混合し
た液に加えて、十分攪拌しながら、６０℃まで急冷する
。(Row/One formulation) After β-7 clodextrin was dissolved in purified water under heating, dequalinium chloride and other water-soluble drugs were further dissolved as needed. This is added to a solution in which a water phase component, an oil phase component, a surfactant, and an oil-soluble drug are mixed in advance while being heated, and the mixture is rapidly cooled to 60° C. while thoroughly stirring.
（ゲル化剤）
加温下に精製水にβ−シクロデキスｌ−’Ｊンを溶解し
た後、これに塩化デカリニウムおよび必要に応じてその
他の水溶性薬剤を溶解し、３０℃まで急冷する。これに
油相成分を徐々に加えて十分に攪拌した後、アンモニヤ
水またはその他のアルカリで中オ］１する１、
（クリーム剤）
加も’ｌｌ’ｌ下に精製水にβ−／クロテキストリンを
溶解した後、塩化デカリニウムおよび必要に応じてその
他の水溶性薬剤を加えて溶解する。これを、あらかじめ
加温下に油相成分、界面活性剤および油溶性薬剤を溶解
した液に加えて十分に攪拌しなから３Ｄ’Ｃ寸で急冷す
る。(Gelling agent) After dissolving β-cyclodextrin in purified water while heating, dequalinium chloride and other water-soluble drugs as necessary are dissolved therein, and the solution is rapidly cooled to 30°C. After gradually adding the oil phase components and stirring thoroughly, add β-/chlorotext to purified water with aqueous ammonia or other alkali (cream agent). After the phosphorus is dissolved, dequalinium chloride and other water-soluble agents as needed are added and dissolved. This is added to a solution in which an oil phase component, a surfactant, and an oil-soluble drug have been dissolved in advance while being heated, thoroughly stirred, and then rapidly cooled to 3D'C dimensions.
本発明においては、β−７クロテキストリンを配合する
ことにより、塩化デカリニウムの水に対する＃ＥＴ解性
を飛躍的に増大し、これが外用剤の塩化デカリニウムの
含有量を増大させている。In the present invention, by blending β-7 crotextrin, the #ET dissolubility of dequalinium chloride in water is dramatically increased, which increases the content of dequalinium chloride in the external preparation.
すなわち、塩化デカリニウムの水に対する溶解量は、β
−７クロテキストリンの配合量が０１重−１□ｉ％未満
てはβ−７クロデキストｌ）ンを未配合の場合と大ノψ
なく、β−ンクロデキストリンの配合量が０１〜１００
重量％ではβ−／クロデキストリンを未配合の場合の１
１〜５倍量である。In other words, the amount of dequalinium chloride dissolved in water is β
If the amount of -7 clodextrin is less than 01wt-1□i%, it is different from the case without β-7 clodextrin.
No, the amount of β-ncrodextrin is 01 to 100.
In terms of weight%, it is 1 when β-/clodextrin is not added.
1 to 5 times the amount.
しかしながら、β−／クロデキストリンの配合量を増や
して１００重量％を超えさせても、塩化デカリニウムの
水に対する溶解量はβ−ンクロテキストｌ）ンを１００
重量％配合した場合と大差がないばかりか、これを冷所
に保存すると析出物を生じるなどの不都合が生じる。However, even if the blended amount of β-/chlodextrin is increased to exceed 100% by weight, the amount of dequalinium chloride dissolved in water is 100% by weight.
Not only is there not much difference from the case where it is mixed by weight%, but there are also disadvantages such as the formation of precipitates if this is stored in a cold place.
以上の如く、本発明の外用剤は、β−／クロテキストリ
ンの配合にょシ界面活性剤の使用量を減じながらも塩化
デカリニウムの含有量を増大させてその治療効果を高め
るとともにその保存安定性を著しく向上させた。As described above, the external preparation of the present invention increases the content of dequalinium chloride while reducing the amount of surfactant used by combining β-/clotextrin, thereby increasing its therapeutic effect and improving its storage stability. significantly improved.
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
２５℃において、β−ンクロテキストリンを精製水に配
合した場合と配合しない場合、これらに対する塩化デカ
リニウムの溶解量はどのように変化するかを調−・た３
゜
その結果を第１表に示す。Test Example 1 At 25°C, we investigated how the amount of dequalinium chloride dissolved in purified water changes when β-encrotextrin is added to purified water and when it is not added.
゜The results are shown in Table 1.
試験例 ２
２５℃において、界面活性剤ポリオキ／エチレンノルビ
クンモノステアレート〔二、コール゛ｒＳ１０（［月光
ケミカルズ社製）〕を精製水に配合した場合と配合しな
い場合、および更にβ−シクロデキストリンを配合した
場合、これらに対する塩化デカリニウムの溶解量がどの
ように変化するかを調べた。Test Example 2 At 25°C, the surfactant polyoxy/ethylene norbiqune monostearate [2, Coal rS10 (manufactured by Gekko Chemicals Co., Ltd.)] was blended with purified water, and when it was not blended, and also when β-cyclodextrin was blended. We investigated how the amount of dequalinium chloride dissolved in these substances changes when these are added.
その結果を第２表に示す。The results are shown in Table 2.
第 ２ 表
試験例 ６
検体Ａ（β−７クロデキストリン不配合、塩化デカリニ
ウム０１５重量％配合、残余は精製水の液剤。実施例１
に準じて調製。）、検体Ｂ（実施例１で調製した液剤）
および検体Ｃ（実施例４で調整したクリーム剤）につい
て５℃および室温における保存安定性を調べた。Table 2 Test Example 6 Specimen A (liquid formulation without β-7 clodextrin, with 15% by weight of dequalinium chloride, the remainder being purified water. Example 1
Prepared according to. ), Sample B (liquid prepared in Example 1)
The storage stability of Sample C (cream preparation prepared in Example 4) at 5° C. and room temperature was investigated.
その結果を第５表に示す。The results are shown in Table 5.
註） Ｑ 析出物なし、′Ｘ＝やや析出物あり、Ｘ：析
出物あシ実施例 １
７０〜８０℃に加温して精製水８００ｚにβ−シクロテ
キストリン５０７を溶解し、これに更に塩化デカリニウ
ム０．５９を加えて溶解した後、３０℃まで急冷し、最
後に精製水を加えて全量を１００． Ｏｆとし、薬剤を
調製した。Note) Q: No precipitate, 'X = Slightly precipitated, After adding and dissolving 0.59% of dequalinium chloride, it was rapidly cooled to 30°C, and finally purified water was added to bring the total amount to 100%. Of, and the drug was prepared.
実施例 ２
７０〜８０℃に加温して精製水７０．０ ！ｉ′にβ−
７クロテキストリン１００７を溶解し、これに更に塩化
デカリニウム０フグを加えて溶解した。この溶液を、あ
らかじめ７０〜８０℃に加温して溶解したジフェンヒド
ラミン１０？、スクワラン３０？、ポリオキシエチレン
ンルビクンモノオレエート４０２およびノルビタンモノ
オレエート１．０９から々る浴液に加え、十分に攪拌し
た後、３０℃まで急冷し、最後に精製水を加えて全量を
ｉ ｏ ｏ、 ｏ ｙとし、ローション剤を調製した。Example 2 Purified water heated to 70-80°C 70.0! β- to i′
7 Clotextrin 1007 was dissolved, and dequalinium chloride 0 pufferfish was further added thereto and dissolved. This solution was preheated to 70-80°C and dissolved in 10% diphenhydramine. , Squalane 30? , polyoxyethylene rubicune monooleate 402 and norbitan monooleate 1.09 were added to the bath solution, stirred thoroughly, and rapidly cooled to 30°C.Finally, purified water was added to adjust the total amount to io o, o y, and a lotion was prepared.
′ノニ〃龜例 ろ
７０〜８０℃に加温して精製水８００７にβ−／クロテ
キストリン４，０７を溶解し、とれに更に塩化デカリニ
ウムロ２７を加えて溶解した後、３０℃寸で急冷した。Example: Dissolve β-/clotextrin 4,07 in purified water 8007 heated to 70-80°C, add dequalinium chloride 27 to the solution, dissolve, and then rapidly cool at 30°C. did.
この溶液にカルホキ／ビニルポリマー１５７を徐々に加
えて十分に撹拌し／こ後、アンモニヤ水４０７を加えて
中和し、ノυ後に精製水を加えて全量を１００．０ ？
とし、よく攪拌してゲル剤を調製した。Gradually add Calhoki/Vinyl Polymer 157 to this solution and stir thoroughly. After that, add aqueous ammonia 407 to neutralize it, and then add purified water to bring the total volume to 100.0?
A gel was prepared by stirring thoroughly.
実施例 ４
７０〜８０℃に加温して精製水７０７にβ−／クロデキ
ストす７５０７を溶解し、これに更に塩化デカリニウム
０３７を溶解した。この溶液を、あらかじめ７０〜８０
℃に加温して溶解した一／ブカイノ０１７．ジフェンヒ
ドラミン１０ハ ビタミンＥ０．５ｉ？、 セトステ
アリルアルコール４．Ｄｉ？、軽質流動パラフィン６０
７．ポリオギ／・エチレンソルビクンモノステアレート
６５９およびノルビタンモノステプレート１０？からな
る溶液に加え、十分に攪拌した後、３０℃寸で急冷し、
最後に精製水を加えて全量を１０００７とし、よく攪拌
してクリーム剤を調製した３゜特許出願人 大正製薬
株式会社
代理人 弁理士 北 川 富 造−１（Example 4 β-/Clodext 7507 was dissolved in purified water 707 heated to 70 to 80°C, and dequalinium chloride 037 was further dissolved therein. Add this solution to 70 to 80 ml in advance.
1/Bukaino 017 dissolved by heating to ℃. Diphenhydramine 10ha Vitamin E0.5i? , cetostearyl alcohol4. Di? , light liquid paraffin 60
7. Poliogi/Ethylene sorbicun monostearate 659 and norbitan monostearate 10? Add to the solution consisting of, stir thoroughly, and then rapidly cool at 30 ° C.
Finally, purified water was added to make the total volume 10007, and the cream was prepared by stirring well.Patent applicant Taisho Pharmaceutical Co., Ltd. Agent Patent attorney Tomizo Kitagawa-1 (
Claims (1)
０重量％のβ−シクロテキストリンとを基剤に配合して
なる外用剤。1) 01-08% by weight of dequalinium chloride and 01-10
An external preparation containing 0% by weight of β-cyclotextrin as a base.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP57205859A JPS5995216A (en) | 1982-11-24 | 1982-11-24 | Drug for external use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP57205859A JPS5995216A (en) | 1982-11-24 | 1982-11-24 | Drug for external use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS5995216A true JPS5995216A (en) | 1984-06-01 |
Family
ID=16513891
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP57205859A Pending JPS5995216A (en) | 1982-11-24 | 1982-11-24 | Drug for external use |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5995216A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024031162A1 (en) * | 2022-08-08 | 2024-02-15 | DA SILVA, Tasso Pereira | Sporicidal antimicrobial compositions and uses thereof |
| WO2024105648A1 (en) * | 2022-11-17 | 2024-05-23 | Silva Renata Moises Iwamizu | Antiviral composition containing inclusion compounds with cyclodextrins as activity modulators and antiseptic actives and uses thereof |
-
1982
- 1982-11-24 JP JP57205859A patent/JPS5995216A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024031162A1 (en) * | 2022-08-08 | 2024-02-15 | DA SILVA, Tasso Pereira | Sporicidal antimicrobial compositions and uses thereof |
| WO2024105648A1 (en) * | 2022-11-17 | 2024-05-23 | Silva Renata Moises Iwamizu | Antiviral composition containing inclusion compounds with cyclodextrins as activity modulators and antiseptic actives and uses thereof |
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