CN1204256A - 气雾剂 - Google Patents
气雾剂 Download PDFInfo
- Publication number
- CN1204256A CN1204256A CN96198984A CN96198984A CN1204256A CN 1204256 A CN1204256 A CN 1204256A CN 96198984 A CN96198984 A CN 96198984A CN 96198984 A CN96198984 A CN 96198984A CN 1204256 A CN1204256 A CN 1204256A
- Authority
- CN
- China
- Prior art keywords
- weight
- aerosol
- alcohol
- stock solution
- carbon
- 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
Links
- 239000000443 aerosol Substances 0.000 title claims abstract description 42
- 238000002360 preparation method Methods 0.000 title abstract description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 54
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 239000003380 propellant Substances 0.000 claims abstract description 5
- 239000011550 stock solution Substances 0.000 claims description 24
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 14
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 235000011389 fruit/vegetable juice Nutrition 0.000 claims description 12
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- 150000001298 alcohols Chemical class 0.000 claims description 4
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- -1 spermol Chemical compound 0.000 description 8
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 7
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- 238000002156 mixing Methods 0.000 description 4
- MCCACAIVAXEFAL-UHFFFAOYSA-N 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazole;nitric acid Chemical compound O[N+]([O-])=O.ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 MCCACAIVAXEFAL-UHFFFAOYSA-N 0.000 description 3
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- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
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- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
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- 229960005040 miconazole nitrate Drugs 0.000 description 3
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- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- ZEMPKEQAKRGZGQ-AAKVHIHISA-N 2,3-bis[[(z)-12-hydroxyoctadec-9-enoyl]oxy]propyl (z)-12-hydroxyoctadec-9-enoate Chemical class CCCCCCC(O)C\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CC(O)CCCCCC)COC(=O)CCCCCCC\C=C/CC(O)CCCCCC ZEMPKEQAKRGZGQ-AAKVHIHISA-N 0.000 description 2
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 description 2
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- 239000004166 Lanolin Substances 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
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- 235000014113 dietary fatty acids Nutrition 0.000 description 2
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- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- IZUPBVBPLAPZRR-UHFFFAOYSA-N pentachlorophenol Chemical compound OC1=C(Cl)C(Cl)=C(Cl)C(Cl)=C1Cl IZUPBVBPLAPZRR-UHFFFAOYSA-N 0.000 description 2
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- IJDNQMDRQITEOD-UHFFFAOYSA-N sec-butylidene Natural products CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 2
- MQHLMHIZUIDKOO-OKZBNKHCSA-N (2R,6S)-2,6-dimethyl-4-[(2S)-2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl]morpholine Chemical compound C1=CC(C(C)(C)CC)=CC=C1C[C@H](C)CN1C[C@@H](C)O[C@@H](C)C1 MQHLMHIZUIDKOO-OKZBNKHCSA-N 0.000 description 1
- YCIHPQHVWDULOY-FMZCEJRJSA-N (4s,4as,5as,6s,12ar)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carboxamide;hydrochloride Chemical compound Cl.C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]4(O)C(=O)C3=C(O)C2=C1O YCIHPQHVWDULOY-FMZCEJRJSA-N 0.000 description 1
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
- 229940058015 1,3-butylene glycol Drugs 0.000 description 1
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- FRPZMMHWLSIFAZ-UHFFFAOYSA-N 10-undecenoic acid Chemical compound OC(=O)CCCCCCCCC=C FRPZMMHWLSIFAZ-UHFFFAOYSA-N 0.000 description 1
- ZJRHNNNACBPWEB-UHFFFAOYSA-N 2-[2-(dimethylamino)ethoxy]ethyl phenothiazine-10-carboxylate;hydron;chloride Chemical compound Cl.C1=CC=C2N(C(=O)OCCOCCN(C)C)C3=CC=CC=C3SC2=C1 ZJRHNNNACBPWEB-UHFFFAOYSA-N 0.000 description 1
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 1
- XMIIGOLPHOKFCH-UHFFFAOYSA-N 3-phenylpropionic acid Chemical compound OC(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-N 0.000 description 1
- PJJGZPJJTHBVMX-UHFFFAOYSA-N 5,7-Dihydroxyisoflavone Chemical compound C=1C(O)=CC(O)=C(C2=O)C=1OC=C2C1=CC=CC=C1 PJJGZPJJTHBVMX-UHFFFAOYSA-N 0.000 description 1
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 description 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- AKUJBENLRBOFTD-RPRRAYFGSA-N Dexamethasone acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COC(C)=O)(O)[C@@]1(C)C[C@@H]2O AKUJBENLRBOFTD-RPRRAYFGSA-N 0.000 description 1
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- ZRTQSJFIDWNVJW-WYMLVPIESA-N Lanoconazole Chemical compound ClC1=CC=CC=C1C(CS\1)SC/1=C(\C#N)N1C=NC=C1 ZRTQSJFIDWNVJW-WYMLVPIESA-N 0.000 description 1
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- 229930182555 Penicillin Natural products 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- CRKGMGQUHDNAPB-UHFFFAOYSA-N Sulconazole nitrate Chemical compound O[N+]([O-])=O.C1=CC(Cl)=CC=C1CSC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 CRKGMGQUHDNAPB-UHFFFAOYSA-N 0.000 description 1
- 208000002474 Tinea Diseases 0.000 description 1
- 241000130764 Tinea Species 0.000 description 1
- IJCWFDPJFXGQBN-RYNSOKOISA-N [(2R)-2-[(2R,3R,4S)-4-hydroxy-3-octadecanoyloxyoxolan-2-yl]-2-octadecanoyloxyethyl] octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCCCCCCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCCCCCCCCCCCC IJCWFDPJFXGQBN-RYNSOKOISA-N 0.000 description 1
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- 230000000844 anti-bacterial effect Effects 0.000 description 1
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- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 229960000686 benzalkonium chloride Drugs 0.000 description 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 1
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- 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
- 229960004022 clotrimazole Drugs 0.000 description 1
- VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 description 1
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- CIKWKGFPFXJVGW-UHFFFAOYSA-N ethacridine Chemical compound C1=C(N)C=CC2=C(N)C3=CC(OCC)=CC=C3N=C21 CIKWKGFPFXJVGW-UHFFFAOYSA-N 0.000 description 1
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- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
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- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 229960002389 glycol salicylate Drugs 0.000 description 1
- IDWJWYPAJJDASX-GKXBZDASSA-N hachimycin Chemical compound O1C(=O)CC(=O)CC(O)CC(O)CCCC(O)CC(O)CC(O2)(O)CC(O)C(C(O)=O)C2CC(OC2C(C(N)C(O)C(C)O2)O)\C=C/C=C\C=C\C=C/C=C\C=C\C=C\C(C)C1C(C)CCC(O)CC(=O)C1=CC=C(N)C=C1 IDWJWYPAJJDASX-GKXBZDASSA-N 0.000 description 1
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- SBUJHOSQTJFQJX-NOAMYHISSA-N kanamycin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N SBUJHOSQTJFQJX-NOAMYHISSA-N 0.000 description 1
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- 229930182823 kanamycin A Natural products 0.000 description 1
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- 239000003921 oil Substances 0.000 description 1
- 229960003483 oxiconazole Drugs 0.000 description 1
- QRJJEGAJXVEBNE-MOHJPFBDSA-N oxiconazole Chemical compound ClC1=CC(Cl)=CC=C1CO\N=C(C=1C(=CC(Cl)=CC=1)Cl)\CN1C=NC=C1 QRJJEGAJXVEBNE-MOHJPFBDSA-N 0.000 description 1
- 150000002960 penicillins Chemical class 0.000 description 1
- 230000002688 persistence Effects 0.000 description 1
- 229960002702 piroxicam Drugs 0.000 description 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
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- 230000032361 posttranscriptional gene silencing Effects 0.000 description 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
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- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 description 1
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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
- A61K9/122—Foams; Dry foams
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/046—Aerosols; Foams
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/24—Thermal properties
- A61K2800/244—Endothermic; Cooling; Cooling sensation
Abstract
一种气雾剂,其组成为一种含有C1－3醇和C12以上醇的基液以及一种含有液化气的喷射剂,而且能给出凝固成冰果汁状的喷出物。在生产该制剂时,可以掺入对水不稳定的组分,无需任何复杂的乳化程序。它有持久的冷却效果。因此,它能有效地迅速缓解由挫伤、扭伤、肌肉疲劳等引起的疼痛,或由足癣、虫咬等引起的骚痒。
Description
技术领域
本发明涉及一种喷射时喷出物在喷射部凝固成冰果汁状、冷却效果高的气雾剂。
背景技术
为了使挫伤、扭伤、肌肉疲劳等引起的疼痛或足癣、虫咬等引起的发痒迅速镇定下来，使患部冷却的做法是有效的。以往对这些症状往往使用以雾状喷出的气雾剂。然而，由于以雾状喷出的气雾剂对皮肤的冷却效果没有持续性，因而喷出物不能达到使患部的疼痛、发痒持久镇定的效果。作为解决这一缺点的办法，WO 90／11068号公报说明书、特开平4-103526号公报等公开了喷射物能形成冰果汁状泡沫凝胶的气雾剂。但是，先有技术上已知的气雾剂制造时需要使原液加温、乳化来配制这样复杂的操作，制造效率低下，是成问题的。
此外，先有技术上已知的。喷射物凝固成冰果汁状的气雾剂，由于是通过使配合的水冷冻达到持久冷却效果的，因而必须有水的配合，使得在水中不稳定的药剂或亲油性高的药剂难以配合。
发明公开
为了解决上述问题，本发明者等人反复进行深入研究的结果，发现由低级醇、高级醇和液化气配合而成的气雾剂制造时不需要乳化操作，而且喷射时喷出物凝固成冰果汁状，因而有持久的冷却效果，从而完成本发明。
即，本发明是由含有1～3个碳的低级醇和12个碳以上的高级醇的原液以及含有液化气的喷射剂组成的、喷射物凝固成冰果汁状的气雾剂。
先有技术上已知的、喷出物会凝固的气雾剂，全都是借助于使配合的水冷冻而使喷出物凝固的，但本发明的气雾剂不一定必须有水的配合，其特征在于在全新的条件下使喷出物凝固。
本发明的气雾剂，是使被液化气的气化热冷却的高级醇连同低级醇一起凝固而变成冰果汁状的。
本发明中1～3个碳的低级醇，系指直链状或支链状的醇，具体地可以列举甲醇、乙醇、改性乙醇、丙醇、异丙醇等，但尤其好的可以列举乙醇。低级醇的配合量，较好的是制剂总量的0．3～65％(重量)、更好的是1．5～50％(重量)、最好的是15～35％(重量)。低级醇的配合量若不足0．3％(重量)则原液与喷射剂难以均匀混合，而若超过65％(重量)则由于喷射剂量相对减少而变得没有冷感。
本发明中12个碳以上的高级醇系指直链状或支链状的醇，是必须能与其它配合成分混合而成为均一体系者。具体地说，可以列举月桂醇、鲸蜡醇、硬脂醇、鲸蜡硬脂醇(cetostearyl alcohol)、山萮醇、羊毛脂醇、氢化羊毛脂醇等的纯品或混合物，尤其好的可以列举硬脂醇或鲸蜡醇。
高级醇的配合量，较好的是制剂总量的0．005～14％(重量)、更好的是0．015～10％(重量)、最好的是0．5～5％(重量)。高级醇的配合量若不足0．005％(重量)则喷出物难以凝固，因而持续冷感变弱。而若超过14％(重量)则高级醇难以溶解，因而制造变得繁杂。
高级醇若不能被低级醇和液化气完全溶解而成为均一体系，就不能达到本发明的效果。因此，高级醇溶解不充分时也可以配合其它溶剂、溶解助剂(聚氧乙烯烷基醚、聚氧乙烯氢化蓖麻油、己二酸二异丙酯、肉豆蔻酸异丙酯、1，3-丁二醇、丙二醇、聚乙二醇、甘油、乳酸、氢氧化钠等)等。
液化气只要是在通常气雾剂中可以作为喷射剂使用的即可，但较好的可以列举二甲醚、正丁烷、异丁烷、丙烷、液化石油气等的纯品或混合物。液化气的配合量较好的是制剂总量的30～95％(重量)、更好的是50～85％(重量)。液化气的配合量若不足30％(重量)则气雾剂的冷感降低，对疼痛、骚痒的镇定效果变弱。而液化剂的配合量若超过95％(重量)，则气雾剂的喷射性状就成为雾状，难以达到持久的冷却效果。
本发明的气雾剂若考虑把凝固成冰果汁状的条件区分为气雾剂原液和液化气，则1～3个碳的低级醇在原液中的配比必须在6％(重量)以上，12个碳以上的高级醇在原液中的配比必须在1％(重量)以上，相对于原液1重量份而言，液化气的量必须是0．5～20重量份。
本发明的气雾剂可以通过使低级醇与高级醇溶解而成为均一体系，必要时进一步配合不破坏均一体系的其它成分，由此得到的原液连同液化气一起灌装到气雾剂容器中来制造。作为气雾剂容器，可以用通常使用的金属制或塑料制的容器。从冷却效果的持久性观点来看，作为不破坏均一体系的其它成分，若配合适量的水则更好。若原液中配合了水，则配合量可以在原液总量的90％(重量)以下，但从制剂设计的容易性观点来看，在原液中的配合量较好在20～60％(重量)。
本发明的气雾剂，为了增进患部的镇痛、止痒效果，可以在不损害本发明效果的限度内配合消炎镇痛剂(消炎痛，水杨酸甲酯，水杨酸乙二醇酯，酮苯丙酸，氟联苯丙酸，吡罗昔康，双氯芬酸，布洛芬，甲灭酸，乙酸氟美松等)，止痒剂(克罗他米通、鱼石脂，mochthamol，麝香草脑酸等)，抗真菌剂(盐酸阿莫罗芬，十一烯酸，五氯苯酚，克霉唑，癣退，曲古霉素，双氯苯咪唑硝酸盐，lanoconazole，硝酸硫康唑，oxyconazole硝酸盐，联苯苄唑等)，抗组胺剂(苯海拉明，盐酸苯海拉明，盐酸氮异丙嗪等)，局部麻醉剂(利多卡因，盐酸狄布卡因等)，抗菌剂(碘化钾，葡糖酸洗必泰，利凡诺，氯化苯甲烃铵等)，抗化脓性疾患剂(青霉素类、盐酸四环素，新霉素，卡那霉素等)，清凉剂(1-薄荷脑，樟脑，薄荷油等)等药效成分。药效成分的配合量因成分而异，较好的是制剂总量的0．001～10％(重量)。
本发明的气雾剂必要时也可以在不损害本发明效果的限度内配合抗氧剂(二丁基羟基甲苯等)，经皮吸收促进剂(甘油脂肪酸酯，油脂类，脂肪族羧酸酯，烟酸酯，azone，烷二醇脂肪酸酯等)，香料、染料等气雾剂中通常使用的添加剂。
产业上利用的可能性
按照本发明制造时不需要繁杂的乳化操作，且具有与先有技术产品同样的冷却效果，使其喷出物能凝固成冰果汁状的气雾剂的提供成为可能。
发明的最佳实施形态
以下用实施例和试验例更详细地说明本发明。
实施例1
硬脂醇4．76重量份与乙醇28．53重量份混合、搅拌，配制成均匀溶解的原液。这种原液灌装到耐压容器中，装上阀门，然后灌装丙烷0．07重量份、正丁烷1．93份、异丁烷0．93重量份和二甲醚63．78重量份。装上喷雾用喷嘴，就制成了气雾剂。
实施例2
消炎痛(抗炎吲哚酸)0．31重量份、己二酸二异丙酯4．11重量份、聚氧乙烯烷基醚1．23重量份、变性乙醇16．47重量份、精制水13．39重量份和鲸蜡醇1．23重量份混合、搅拌、均匀溶解，调制成原液。把该原液灌装到耐压容器中，装上阀门，再灌装二甲醚63．26重量份。装上喷雾用喷嘴，就得到了气雾剂。
实施例3
双氯苯咪唑硝酸盐0．35重量份、己二酸二异丙酯1．76重量份、肉豆蔻酸异丙酯1．05重量份、甘油0．70重量份、变性乙醇15．80重量份、精制水8．74重量份、硬脂醇0．53重量份、鲸蜡醇0．53重量份、聚氧乙烯烷基醚0．70重量份和聚氧乙烯氢化蓖麻油0．35重量份混合、搅拌、均匀溶解，调制成原液。把该原液灌装到耐压容器中，装上阀门，再灌装二甲醚69．49重量份，装上喷雾用喷嘴，就得到了气雾剂。
比较例1
用实施例1的硬脂醇改变成乙醇的处方，按照与实施例1同样的方法，得到了气雾剂。
比较例2
用实施例2的聚氧乙烯烷基醚改变成变性乙醇、鲸蜡醇改变成精制水的处方，按照与实施例2同样的方法，得到了比较用的气雾剂。
比较例3
双氯苯咪唑硝酸盐0．36重量份、己二酸二异丙酯1．79重量份、肉豆蔻酸异丙酯1．07重量份、甘油0．71重量份、变性乙醇17．06重量份和精制水8．27重量份混合、搅拌、均匀溶解，调制成原液。把该原液灌装到耐压容器中，装上阀门，再灌装二甲醚70．74重量份。装上喷雾用喷嘴，得到了比较用的气雾剂。
比较例4(制造时需要乳化作业的气雾剂)
消炎痛(抗炎吲哚酸)0．31重量份、己二酸二异丙酯4．07重量份、聚氧乙烯脱水山梨醇单硬脂酸酯1．22重量份、聚氧乙烯脱水山梨醇三硬脂酸酯0．81重量份和脱水山梨醇单硬脂酸酯1．22重量份加温、熔融后，添加温精制水15．94重量份，充分混合。进一步边搅拌边冷却后，加入变性乙醇14．23重量份，均匀分散，调制成原液。该原液灌装到耐压容器中，装上阀门，再灌装二甲醚62．20重量份。装上喷雾用喷嘴，制成气雾剂。
试验例1
在设定于33℃的恒温水槽上，放置一块用胶带固定了热电偶传感器的薄板，对热电偶传感器分别喷涂3秒钟实施例1～3和比较例1～4的气雾剂。确认喷出物的性状，测定热电偶传感器显示值随时间的变化。结果列于表1中。
表1
| 样品 | 乳化操作 | 冰果汁状物 | 热电偶传感器的温度变化(℃) | |||||||
| 喷射前 | 15秒 | 30秒 | 45秒 | 60秒 | 90秒 | 120秒 | 180秒 | |||
| 实施例1实施例2实施例3比较例1比较例2比较例3比较例4 | 不要不要不要不要不要不要要 | 形成形成形成未形成未形成未形成形成 | 33.533.533.233.333.333.433.3 | 18.414.815.030.933.022.015.8 | 20.815.314.731.930.531.915.5 | 21.518.815.632.032.532.118.9 | 23.523.520.232.432.932.423.0 | 24.626.122.932.633.032.931.2 | 30.729.331.633.233.333.031.2 | 33.031.532.933.233.233.333.0 |
实施例1～3和比较例4的喷出物形成了冰果汁状固形物，但比较例1～3不形成冰果汁状固形物。而且，即使在热电偶传感器的温度变化方面，比较例1～3也在喷射30秒后就达到30℃以上，45秒后就回到差不多原来的温度，相对而言，发现实施例1～3和比较例4有持久的冷却效果。
Claims (6)
1．喷出物能凝固成冰果汁状的气雾剂，其组成为含有1～3个碳的低级醇和12个碳以上的高级醇的原液，以及含有液化气的喷射剂。
2．权利要求1所述的气雾剂，其中，1～3个碳的低级醇是总量的0．3～65％(重量)，12个碳以上的高级醇是总量的0．005～14％(重量)，且液化气是30～95％(重量)。
3．权利要求1所述的气雾剂，其中，1～3个碳的低级醇占6％(重量)以上，12个碳以上的高级醇占1％(重量)以上，相对于原液1重量份而言，液化气为0．5～20重量份。
4．权利要求1～3中任何一项所述的气雾剂，其中低级醇是乙醇。
5．权利要求1～4中任何一项所述的气雾剂，其中高级醇是硬脂醇和鲸蜡醇中至少一种。
6．权利要求1～5中任何一项所述的气雾剂，其中水的配合量是原液的20～60％(重量)。
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| JP325335/95 | 1995-12-14 |
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| CN01119505A Division CN1326730A (zh) | 1995-12-14 | 2001-05-22 | 气雾剂 |
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| CN01119505A Pending CN1326730A (zh) | 1995-12-14 | 2001-05-22 | 气雾剂 |
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| WO2008112661A2 (en) | 2007-03-09 | 2008-09-18 | Alexza Pharmaceuticals, Inc. | Heating unit for use in a drug delivery device |
| US8636982B2 (en) | 2007-08-07 | 2014-01-28 | Foamix Ltd. | Wax foamable vehicle and pharmaceutical compositions thereof |
| US9439857B2 (en) | 2007-11-30 | 2016-09-13 | Foamix Pharmaceuticals Ltd. | Foam containing benzoyl peroxide |
| WO2009090495A2 (en) | 2007-12-07 | 2009-07-23 | Foamix Ltd. | Oil and liquid silicone foamable carriers and formulations |
| CA2760186C (en) | 2009-04-28 | 2019-10-29 | Foamix Ltd. | Foamable vehicle and pharmaceutical compositions comprising aprotic polar solvents and uses thereof |
| CA2769625C (en) | 2009-07-29 | 2017-04-11 | Foamix Ltd. | Non surfactant hydro-alcoholic foamable compositions, breakable foams and their uses |
| CA2769677A1 (en) | 2009-07-29 | 2011-02-03 | Foamix Ltd. | Non surface active agent non polymeric agent hydro-alcoholic foamable compositions, breakable foams and their uses |
| US9849142B2 (en) | 2009-10-02 | 2017-12-26 | Foamix Pharmaceuticals Ltd. | Methods for accelerated return of skin integrity and for the treatment of impetigo |
| CA2776366C (en) | 2009-10-02 | 2017-07-18 | Foamix Ltd. | Surfactant-free water-free foamable compositions, breakable foams and gels and their uses |
| AT513312A1 (de) * | 2012-08-17 | 2014-03-15 | Gebro Holding Gmbh | Antiseptische Zusammensetzung |
| US10398641B2 (en) | 2016-09-08 | 2019-09-03 | Foamix Pharmaceuticals Ltd. | Compositions and methods for treating rosacea and acne |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3584115A (en) * | 1968-05-31 | 1971-06-08 | Arthur Ira Gebhart | Method of applying visible aerosol compositions |
| DE3311700A1 (de) * | 1983-03-30 | 1984-10-04 | Bayer Ag | Antimykotische mittel mit hoher wirkstoff-freisetzung in form von loesung und spray |
| US4495169A (en) * | 1983-08-22 | 1985-01-22 | Basf Wyandotte Corporation | Aerosol gel shaving cream |
| EP0160051B1 (en) * | 1983-10-24 | 1992-01-08 | Lockley Services Pty. Ltd. | Foamable biocide composition |
| US4588581A (en) * | 1984-11-16 | 1986-05-13 | Basf Corporation | Methods and compositions for intravaginal contraception |
| US5143717A (en) * | 1987-12-30 | 1992-09-01 | Code Blue Medical Corporation | Burn foam and delivery system |
| JP2960445B2 (ja) * | 1988-12-28 | 1999-10-06 | 株式会社大阪造船所 | エアゾール用組成物 |
| ATE152908T1 (de) * | 1989-03-17 | 1997-05-15 | Taisho Pharmaceutical Co Ltd | Aerosolzusammensetzung zur äusserlichen verwendung |
| US5209921A (en) * | 1989-05-19 | 1993-05-11 | Beecham Group Plc | Aerosol compositions |
| KR950002879B1 (ko) * | 1989-07-28 | 1995-03-28 | 히사미쯔세이야꾸 가부시기가이샤 | 거품상 에어로솔제제 |
| JP3038837B2 (ja) * | 1990-08-21 | 2000-05-08 | 大正製薬株式会社 | 皮膚冷却エアゾール剤 |
| CN1106259A (zh) * | 1994-02-05 | 1995-08-09 | 日东制药株式会社 | 含有作为有效成分的丙酸类非类固醇性药物的新颖消炎镇痛外用凝胶制剂 |
-
1996
- 1996-12-12 EP EP96941849A patent/EP0870497B1/en not_active Expired - Lifetime
- 1996-12-12 WO PCT/JP1996/003631 patent/WO1997021426A1/ja active IP Right Grant
- 1996-12-12 NZ NZ330679A patent/NZ330679A/xx unknown
- 1996-12-12 KR KR10-1998-0704462A patent/KR100450861B1/ko not_active IP Right Cessation
- 1996-12-12 ES ES96941849T patent/ES2217334T3/es not_active Expired - Lifetime
- 1996-12-12 AU AU11103/97A patent/AU705038B2/en not_active Ceased
- 1996-12-12 DE DE69632148T patent/DE69632148T2/de not_active Expired - Fee Related
- 1996-12-12 DK DK96941849T patent/DK0870497T3/da active
- 1996-12-12 US US09/091,101 patent/US6133327A/en not_active Expired - Fee Related
- 1996-12-12 AT AT96941849T patent/ATE263546T1/de not_active IP Right Cessation
- 1996-12-12 CN CN96198984A patent/CN1084613C/zh not_active Expired - Fee Related
-
2001
- 2001-05-22 CN CN01119505A patent/CN1326730A/zh active Pending
-
2002
- 2002-03-11 HK HK02101844.4A patent/HK1040370A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR19990072131A (ko) | 1999-09-27 |
| KR100450861B1 (ko) | 2005-03-16 |
| AU705038B2 (en) | 1999-05-13 |
| CN1084613C (zh) | 2002-05-15 |
| ATE263546T1 (de) | 2004-04-15 |
| CN1326730A (zh) | 2001-12-19 |
| NZ330679A (en) | 2000-03-27 |
| WO1997021426A1 (fr) | 1997-06-19 |
| DK0870497T3 (da) | 2004-05-24 |
| EP0870497A4 (en) | 1999-03-10 |
| HK1040370A1 (zh) | 2002-06-07 |
| ES2217334T3 (es) | 2004-11-01 |
| AU1110397A (en) | 1997-07-03 |
| DE69632148D1 (de) | 2004-05-13 |
| EP0870497A1 (en) | 1998-10-14 |
| US6133327A (en) | 2000-10-17 |
| EP0870497B1 (en) | 2004-04-07 |
| DE69632148T2 (de) | 2005-03-17 |
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