WO1997005858A1 - Preparation pour aerosol - Google Patents
Preparation pour aerosol Download PDFInfo
- Publication number
- WO1997005858A1 WO1997005858A1 PCT/JP1996/002124 JP9602124W WO9705858A1 WO 1997005858 A1 WO1997005858 A1 WO 1997005858A1 JP 9602124 W JP9602124 W JP 9602124W WO 9705858 A1 WO9705858 A1 WO 9705858A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- weight
- propellant
- aerosol
- fatty acid
- menthol
- Prior art date
Links
- 239000000443 aerosol Substances 0.000 title claims abstract description 19
- 238000002360 preparation method Methods 0.000 title claims abstract description 8
- 239000003380 propellant Substances 0.000 claims abstract description 13
- -1 fatty acid esters Chemical class 0.000 claims abstract description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 9
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims abstract description 8
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 8
- 229930195729 fatty acid Natural products 0.000 claims abstract description 8
- 239000000194 fatty acid Substances 0.000 claims abstract description 8
- 239000011550 stock solution Substances 0.000 claims abstract description 8
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229940041616 menthol Drugs 0.000 claims abstract description 7
- 239000004094 surface-active agent Substances 0.000 claims abstract description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 5
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims abstract description 4
- 241000723346 Cinnamomum camphora Species 0.000 claims abstract description 4
- 229960000846 camphor Drugs 0.000 claims abstract description 4
- 229930008380 camphor Natural products 0.000 claims abstract description 4
- 229920001214 Polysorbate 60 Polymers 0.000 claims abstract description 3
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 claims description 6
- 238000002156 mixing Methods 0.000 claims description 4
- 239000012046 mixed solvent Substances 0.000 claims description 2
- 238000013329 compounding Methods 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 abstract description 22
- 230000007803 itching Effects 0.000 abstract description 12
- 238000006243 chemical reaction Methods 0.000 abstract description 7
- 230000001139 anti-pruritic effect Effects 0.000 abstract description 6
- 208000006877 Insect Bites and Stings Diseases 0.000 abstract description 5
- 230000003111 delayed effect Effects 0.000 abstract description 3
- 239000011877 solvent mixture Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 description 6
- 230000000052 comparative effect Effects 0.000 description 5
- 239000007788 liquid Substances 0.000 description 5
- 235000019441 ethanol Nutrition 0.000 description 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 239000003908 antipruritic agent Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- BWMISRWJRUSYEX-SZKNIZGXSA-N terbinafine hydrochloride Chemical compound Cl.C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 BWMISRWJRUSYEX-SZKNIZGXSA-N 0.000 description 3
- 201000004647 tinea pedis Diseases 0.000 description 3
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 2
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 2
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 2
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- 229940121375 antifungal agent Drugs 0.000 description 2
- 239000003429 antifungal agent Substances 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 238000001816 cooling Methods 0.000 description 2
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 2
- NNPPMTNAJDCUHE-UHFFFAOYSA-N isobutane Chemical compound CC(C)C NNPPMTNAJDCUHE-UHFFFAOYSA-N 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 229960004194 lidocaine Drugs 0.000 description 2
- 239000003589 local anesthetic agent Substances 0.000 description 2
- 229960005015 local anesthetics Drugs 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000001587 sorbitan monostearate Substances 0.000 description 2
- 229940035048 sorbitan monostearate Drugs 0.000 description 2
- 235000011076 sorbitan monostearate Nutrition 0.000 description 2
- SPSPIUSUWPLVKD-UHFFFAOYSA-N 2,3-dibutyl-6-methylphenol Chemical compound CCCCC1=CC=C(C)C(O)=C1CCCC SPSPIUSUWPLVKD-UHFFFAOYSA-N 0.000 description 1
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical compound CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- IYLLULUTZPKQBW-UHFFFAOYSA-N Acrinol Chemical compound CC(O)C(O)=O.C1=C(N)C=CC2=C(N)C3=CC(OCC)=CC=C3N=C21 IYLLULUTZPKQBW-UHFFFAOYSA-N 0.000 description 1
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 description 1
- 241000255925 Diptera Species 0.000 description 1
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-UHFFFAOYSA-N 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 244000088401 Pyrus pyrifolia Species 0.000 description 1
- 235000001630 Pyrus pyrifolia var culta Nutrition 0.000 description 1
- 206010040914 Skin reaction Diseases 0.000 description 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- LPQOADBMXVRBNX-UHFFFAOYSA-N ac1ldcw0 Chemical compound Cl.C1CN(C)CCN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN3CCSC1=C32 LPQOADBMXVRBNX-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- WNLRTRBMVRJNCN-UHFFFAOYSA-L adipate(2-) Chemical compound [O-]C(=O)CCCCC([O-])=O WNLRTRBMVRJNCN-UHFFFAOYSA-L 0.000 description 1
- 229960000458 allantoin Drugs 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 1
- 229960003333 chlorhexidine gluconate Drugs 0.000 description 1
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 description 1
- 229940046978 chlorpheniramine maleate Drugs 0.000 description 1
- IVHBBMHQKZBJEU-UHFFFAOYSA-N cinchocaine hydrochloride Chemical compound [Cl-].C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCC[NH+](CC)CC)=C21 IVHBBMHQKZBJEU-UHFFFAOYSA-N 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- DNTGGZPQPQTDQF-XBXARRHUSA-N crotamiton Chemical compound C/C=C/C(=O)N(CC)C1=CC=CC=C1C DNTGGZPQPQTDQF-XBXARRHUSA-N 0.000 description 1
- 229960003338 crotamiton Drugs 0.000 description 1
- 229940045574 dibucaine hydrochloride Drugs 0.000 description 1
- 229960000520 diphenhydramine Drugs 0.000 description 1
- 229960000525 diphenhydramine hydrochloride Drugs 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960003720 enoxolone Drugs 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 201000006747 infectious mononucleosis Diseases 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000001282 iso-butane Substances 0.000 description 1
- 229960003517 isothipendyl Drugs 0.000 description 1
- OQJBSDFFQWMKBQ-UHFFFAOYSA-N isothipendyl Chemical compound C1=CN=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 OQJBSDFFQWMKBQ-UHFFFAOYSA-N 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 239000001294 propane Substances 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 231100000430 skin reaction Toxicity 0.000 description 1
- 230000035483 skin reaction Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K31/125—Camphor; Nuclear substituted derivatives thereof
Definitions
- the present invention relates to an azosol agent having an excellent antipruritic effect on itching caused by insect bites, athlete's foot and the like.
- the skin reactions caused by insect bites include itching and redness.
- the delayed response itching can be controlled by application of drugs such as common ointments containing local anesthetics and antipruritics.
- An object of the present invention is to provide a preparation having an excellent antipruritic effect on itch of immediate reaction due to insect bites and itch of athlete's foot. Disclosure of the invention
- the present invention is an aerosol comprising a stock solution and a propellant obtained by mixing the following components (A) to (C) with a mixed solvent of water and a lower alcohol.
- Polyoxyethylene sorbitan fatty acid esters used in the present invention and The surfactant selected from the group consisting of sorbitan fatty acid esters is a paste or semi-solid at room temperature at the time of preparation of the stock solution.
- Sorbitan monostearate, polyoxyethylene (20) Sorbinane tristearate and a mixture of sorbitan monostearate are preferred. The amount of these compounds is 0.5 to 8% by weight, preferably 0.5 to 4% by weight.
- the solvent is a mixture of water and a lower alcohol, and preferably has a weight ratio in the range of 30:70 to 70:30.
- a liquefied gas is used as the propellant, and dimethyl ether, n-butane, isobutane, propane or a mixture thereof can be used as the liquefied gas.
- a propellant containing dimethyl ether of 80% by weight or more is preferable.
- the mixing amount of the propellant is 40 to 80% by weight, preferably 50 to 70% by weight of the whole preparation.
- the aerosol of the present invention includes components normally contained in antipruritic agents and antifungal agents, for example, antipruritic agents (crotamiton, dictamol, mokuyumol, thymolic acid, etc.), antifungal agents (tolnaftetol, nitric acid, etc.).
- the aerosol of the present invention is prepared by heating, mixing and stirring components other than the propellant to dissolve or evenly disperse the component to prepare a liquid, and then filling the liquid with the propellant in an aerosol container.
- FIGS. 1 and 2 The results are shown in FIGS. 1 and 2 as the average value of five subjects. It can be seen that the aerosol preparations of the present invention prepared in Examples 2 and 3 had a itch score peak of 1 or less, that is, almost no itching and were in a state, and that an effective itching inhibitory effect was obtained for consumers. Was. BRIEF DESCRIPTION OF THE FIGURES
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Dispersion Chemistry (AREA)
- Medicinal Preparation (AREA)
Abstract
La présente invention concerne une préparation caractérisée par une bonne efficacité antiprurigineuse à la réaction immédiate résultant d'une morsure d'insecte de même que pour le prurit de réaction secondaire. La préparation pour aérosol est constituée d'une solution de principe à trois composants (A, B, C) dans des solvants en mélange, à savoir de l'eau, un alcool inférieur et un propulseur. Le premier composant (A) est un ou plusieurs agents tensioactifs appartenant au groupe des esters d'acides gras de polyoxyéthylène sorbitane et des esters d'acides gras de sorbitane. Le deuxième composant (B) est du menthol en proportion massique de 0,5 % à 8 %. Et le troisième composant C est du camphre à raison de 1 à 0,5 parties massiques pour une partie massique de menthol.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU65319/96A AU6531996A (en) | 1995-08-10 | 1996-07-29 | Aerosol preparation |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP20479995 | 1995-08-10 | ||
| JP7/204799 | 1995-08-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1997005858A1 true WO1997005858A1 (fr) | 1997-02-20 |
Family
ID=16496560
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/JP1996/002124 WO1997005858A1 (fr) | 1995-08-10 | 1996-07-29 | Preparation pour aerosol |
Country Status (2)
| Country | Link |
|---|---|
| AU (1) | AU6531996A (fr) |
| WO (1) | WO1997005858A1 (fr) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6231835B1 (en) | 1997-06-13 | 2001-05-15 | Taisho Pharmaceutical Co., Ltd. | Aerosol preparation for skin cooling |
| US20180228862A1 (en) * | 2016-07-08 | 2018-08-16 | Weon Ju KIM | Composition for neutralizing venom from venomous insects |
| CN113444583A (zh) * | 2021-06-25 | 2021-09-28 | 山东新华莎罗雅生物技术有限公司 | 医用除胶剂及其制备方法 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS56135414A (en) * | 1980-03-27 | 1981-10-22 | Hisamitsu Pharmaceut Co Inc | Aerosol type antiphlogistic and analgesic |
| JPS63258405A (ja) * | 1987-04-13 | 1988-10-25 | Osaka Eyazoole Kogyo Kk | エアゾ−ル式外用塗布剤 |
| JPH02101010A (ja) * | 1988-10-07 | 1990-04-12 | Kashiwa Kagaku Kogyo:Kk | 人体皮膚散布薬剤 |
| JPH04103526A (ja) * | 1990-08-21 | 1992-04-06 | Taisho Pharmaceut Co Ltd | 皮膚冷却エアゾール剤 |
-
1996
- 1996-07-29 AU AU65319/96A patent/AU6531996A/en not_active Abandoned
- 1996-07-29 WO PCT/JP1996/002124 patent/WO1997005858A1/fr active Application Filing
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS56135414A (en) * | 1980-03-27 | 1981-10-22 | Hisamitsu Pharmaceut Co Inc | Aerosol type antiphlogistic and analgesic |
| JPS63258405A (ja) * | 1987-04-13 | 1988-10-25 | Osaka Eyazoole Kogyo Kk | エアゾ−ル式外用塗布剤 |
| JPH02101010A (ja) * | 1988-10-07 | 1990-04-12 | Kashiwa Kagaku Kogyo:Kk | 人体皮膚散布薬剤 |
| JPH04103526A (ja) * | 1990-08-21 | 1992-04-06 | Taisho Pharmaceut Co Ltd | 皮膚冷却エアゾール剤 |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6231835B1 (en) | 1997-06-13 | 2001-05-15 | Taisho Pharmaceutical Co., Ltd. | Aerosol preparation for skin cooling |
| US20180228862A1 (en) * | 2016-07-08 | 2018-08-16 | Weon Ju KIM | Composition for neutralizing venom from venomous insects |
| CN113444583A (zh) * | 2021-06-25 | 2021-09-28 | 山东新华莎罗雅生物技术有限公司 | 医用除胶剂及其制备方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU6531996A (en) | 1997-03-05 |
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