GB2139919A - Stable high internal phase ratio topical emulsions - Google Patents
Stable high internal phase ratio topical emulsions Download PDFInfo
- Publication number
- GB2139919A GB2139919A GB08313456A GB8313456A GB2139919A GB 2139919 A GB2139919 A GB 2139919A GB 08313456 A GB08313456 A GB 08313456A GB 8313456 A GB8313456 A GB 8313456A GB 2139919 A GB2139919 A GB 2139919A
- Authority
- GB
- United Kingdom
- Prior art keywords
- composition according
- lipoidal
- agents
- oil
- emulsions
- 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.)
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- 239000000839 emulsion Substances 0.000 title claims abstract description 35
- 230000000699 topical effect Effects 0.000 title abstract description 13
- 239000000203 mixture Substances 0.000 claims abstract description 34
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 26
- 239000003921 oil Substances 0.000 claims abstract description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 12
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims abstract description 11
- 235000019198 oils Nutrition 0.000 claims abstract description 11
- 239000000600 sorbitol Substances 0.000 claims abstract description 11
- 235000011187 glycerol Nutrition 0.000 claims abstract description 10
- 239000002480 mineral oil Substances 0.000 claims abstract description 10
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims abstract description 10
- 239000013543 active substance Substances 0.000 claims abstract description 8
- 229940049964 oleate Drugs 0.000 claims abstract description 8
- 235000010446 mineral oil Nutrition 0.000 claims abstract description 7
- 239000001257 hydrogen Substances 0.000 claims abstract description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 6
- 150000002148 esters Chemical class 0.000 claims abstract description 5
- 235000015112 vegetable and seed oil Nutrition 0.000 claims abstract description 4
- 239000008158 vegetable oil Substances 0.000 claims abstract description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims abstract description 3
- 239000006071 cream Substances 0.000 claims description 14
- 239000006210 lotion Substances 0.000 claims description 10
- 229920000223 polyglycerol Polymers 0.000 claims description 8
- 230000001681 protective effect Effects 0.000 claims description 8
- OMPJBNCRMGITSC-UHFFFAOYSA-N Benzoylperoxide Chemical compound C=1C=CC=CC=1C(=O)OOC(=O)C1=CC=CC=C1 OMPJBNCRMGITSC-UHFFFAOYSA-N 0.000 claims description 6
- 239000004342 Benzoyl peroxide Substances 0.000 claims description 5
- 235000019400 benzoyl peroxide Nutrition 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 230000001166 anti-perspirative effect Effects 0.000 claims description 4
- 239000003213 antiperspirant Substances 0.000 claims description 4
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims description 4
- 150000003431 steroids Chemical class 0.000 claims description 4
- 239000004264 Petrolatum Substances 0.000 claims description 3
- 229940066842 petrolatum Drugs 0.000 claims description 3
- 235000019271 petrolatum Nutrition 0.000 claims description 3
- 238000011282 treatment Methods 0.000 claims description 3
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010000496 acne Diseases 0.000 claims description 2
- 239000000730 antalgic agent Substances 0.000 claims description 2
- 239000000058 anti acne agent Substances 0.000 claims description 2
- 230000001139 anti-pruritic effect Effects 0.000 claims description 2
- 229940124340 antiacne agent Drugs 0.000 claims description 2
- 239000003429 antifungal agent Substances 0.000 claims description 2
- 229940121375 antifungal agent Drugs 0.000 claims description 2
- 229960005475 antiinfective agent Drugs 0.000 claims description 2
- 239000004599 antimicrobial Substances 0.000 claims description 2
- 239000003908 antipruritic agent Substances 0.000 claims description 2
- 239000007844 bleaching agent Substances 0.000 claims description 2
- 239000003974 emollient agent Substances 0.000 claims description 2
- 229960000890 hydrocortisone Drugs 0.000 claims description 2
- 229920002545 silicone oil Polymers 0.000 claims description 2
- 229960001422 aluminium chlorohydrate Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- LVYZJEPLMYTTGH-UHFFFAOYSA-H dialuminum chloride pentahydroxide dihydrate Chemical compound [Cl-].[Al+3].[OH-].[OH-].[Al+3].[OH-].[OH-].[OH-].O.O LVYZJEPLMYTTGH-UHFFFAOYSA-H 0.000 claims 1
- 238000002360 preparation method Methods 0.000 abstract description 8
- ASKIVFGGGGIGKH-UHFFFAOYSA-N 2,3-dihydroxypropyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OCC(O)CO ASKIVFGGGGIGKH-UHFFFAOYSA-N 0.000 abstract description 6
- 239000000872 buffer Substances 0.000 abstract description 3
- 239000003086 colorant Substances 0.000 abstract description 3
- 239000000796 flavoring agent Substances 0.000 abstract description 3
- 235000019634 flavors Nutrition 0.000 abstract description 3
- 239000004606 Fillers/Extenders Substances 0.000 abstract description 2
- 235000020374 simple syrup Nutrition 0.000 abstract description 2
- 239000007787 solid Substances 0.000 abstract description 2
- 235000010356 sorbitol Nutrition 0.000 abstract description 2
- 239000003085 diluting agent Substances 0.000 abstract 1
- 229910052500 inorganic mineral Inorganic materials 0.000 abstract 1
- 239000000047 product Substances 0.000 description 8
- 239000004615 ingredient Substances 0.000 description 7
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 6
- 239000008367 deionised water Substances 0.000 description 6
- 229910021641 deionized water Inorganic materials 0.000 description 6
- UKHVLWKBNNSRRR-ODZAUARKSA-M dowicil 200 Chemical compound [Cl-].C1N(C2)CN3CN2C[N+]1(C\C=C/Cl)C3 UKHVLWKBNNSRRR-ODZAUARKSA-M 0.000 description 5
- 239000004200 microcrystalline wax Substances 0.000 description 5
- 235000019808 microcrystalline wax Nutrition 0.000 description 5
- 240000006497 Dianthus caryophyllus Species 0.000 description 4
- 235000009355 Dianthus caryophyllus Nutrition 0.000 description 4
- 239000012530 fluid Substances 0.000 description 4
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
- 229920001296 polysiloxane Polymers 0.000 description 4
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 4
- 229960005274 benzocaine Drugs 0.000 description 3
- 239000002537 cosmetic Substances 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- -1 fatty acid esters Chemical class 0.000 description 3
- 239000003205 fragrance Substances 0.000 description 3
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 239000005642 Oleic acid Substances 0.000 description 2
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000003925 fat Substances 0.000 description 2
- 235000019197 fats Nutrition 0.000 description 2
- 150000004665 fatty acids Chemical class 0.000 description 2
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
- 229960002216 methylparaben Drugs 0.000 description 2
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 2
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 2
- 229960003415 propylparaben Drugs 0.000 description 2
- 239000001993 wax Substances 0.000 description 2
- FFJCNSLCJOQHKM-CLFAGFIQSA-N (z)-1-[(z)-octadec-9-enoxy]octadec-9-ene Chemical compound CCCCCCCC\C=C/CCCCCCCCOCCCCCCCC\C=C/CCCCCCCC FFJCNSLCJOQHKM-CLFAGFIQSA-N 0.000 description 1
- 241001133760 Acoelorraphe Species 0.000 description 1
- 235000017060 Arachis glabrata Nutrition 0.000 description 1
- 244000105624 Arachis hypogaea Species 0.000 description 1
- 235000010777 Arachis hypogaea Nutrition 0.000 description 1
- 235000018262 Arachis monticola Nutrition 0.000 description 1
- 240000002791 Brassica napus Species 0.000 description 1
- 235000004977 Brassica sinapistrum Nutrition 0.000 description 1
- 244000020518 Carthamus tinctorius Species 0.000 description 1
- 235000003255 Carthamus tinctorius Nutrition 0.000 description 1
- 244000060011 Cocos nucifera Species 0.000 description 1
- 235000013162 Cocos nucifera Nutrition 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
- 244000068988 Glycine max Species 0.000 description 1
- 235000010469 Glycine max Nutrition 0.000 description 1
- 244000020551 Helianthus annuus Species 0.000 description 1
- 235000003222 Helianthus annuus Nutrition 0.000 description 1
- 240000007817 Olea europaea Species 0.000 description 1
- 244000000231 Sesamum indicum Species 0.000 description 1
- 235000003434 Sesamum indicum Nutrition 0.000 description 1
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 description 1
- 240000008042 Zea mays Species 0.000 description 1
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 description 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000001464 adherent effect Effects 0.000 description 1
- 229940009840 aluminum chlorhydrate Drugs 0.000 description 1
- 235000021120 animal protein Nutrition 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 238000010923 batch production Methods 0.000 description 1
- YOUGRGFIHBUKRS-UHFFFAOYSA-N benzyl(trimethyl)azanium Chemical compound C[N+](C)(C)CC1=CC=CC=C1 YOUGRGFIHBUKRS-UHFFFAOYSA-N 0.000 description 1
- 239000003054 catalyst Substances 0.000 description 1
- 239000007795 chemical reaction product Substances 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 238000010924 continuous production Methods 0.000 description 1
- 235000005822 corn Nutrition 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000008014 freezing Effects 0.000 description 1
- 238000007710 freezing Methods 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 235000020232 peanut Nutrition 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 238000005191 phase separation Methods 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000010296 thiabendazole Nutrition 0.000 description 1
- WJCNZQLZVWNLKY-UHFFFAOYSA-N thiabendazole Chemical compound S1C=NC(C=2NC3=CC=CC=C3N=2)=C1 WJCNZQLZVWNLKY-UHFFFAOYSA-N 0.000 description 1
- 229940044134 tresaderm Drugs 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
- C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
- C09K23/00—Use of substances as emulsifying, wetting, dispersing, or foam-producing agents
- C09K23/34—Higher-molecular-weight carboxylic acid esters
-
- 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
-
- 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
- A61K8/06—Emulsions
-
- 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
- A61K8/06—Emulsions
- A61K8/064—Water-in-oil emulsions, e.g. Water-in-silicone emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/37—Esters of carboxylic acids
- A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/38—Percompounds, e.g. peracids
-
- 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
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
-
- C—CHEMISTRY; METALLURGY
- C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
- C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
- C09K23/00—Use of substances as emulsifying, wetting, dispersing, or foam-producing agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q15/00—Anti-perspirants or body deodorants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
Abstract
Delivery systems for topical preparations which are commercially stable. The emulsions are water-in-oil in which the water phase comprises at least 70% of the emulsion by volume, or similar emulsions with glycerol, sorbitol or sugar syrup as the disperse phase. The emulsifier is a non-ionic oil soluble straight or branched chain ester or combination thereof composition having at least two hydrogen bonding sites per molecule, e.g. polyglyceryl oleate or glycerol monoisostearate. The disperse phase may include active agents, suspended solids, emulsions, extenders, diluents, colours, flavours, or buffers; the oil may be a mineral or vegetable oil.
Description
SPECIFICATION
Stable high internal phase ratio topical emulsions
The present invention is directed to topical preparation systems which are high internal phase water-in-oil
emulsions. Specifically, the invention is concerned with high internal phase water-in-oil emulsions which are
commercially stable.
It has been found advantageous to formulate topical preparations in high internal phase ratio water-in-oil
systems. Topical preparations include cosmetic and/or pharmaceutical products which are applied to
external skin areas. By incorporating active agents desirable for topical use in high internal phase ratio
water-in-oil emulsions, a number of advantages are obtained. Such advantages include the obtaining of an
oil adherent system utilising high concentrations of oil.
A method of preparing a water-in-oil high internal phase ratio topical emulsion is described in UK Patent
1,415,528 which is incorporated by reference herein. The emulsions disclosed in the patent do not display
commercial stability. That is, they fail to remain emulsified for more than five freeze-thaw cycles. A
freeze-thaw cycle is defined as the freezing of a sample of an emulsion at -10"C for 24 hours and then allowing it to thaw at room temperature, 22"C for 24 hours. Freeze-thaw cycles simulate conditions which
may be encountered during transportation and/or storage of a product. For an emulsion to be commercially
acceptable, it must survive at least five freeze-thaw cycles.
As discussed above, it has been possible to formulate water-in-oil high internal phase ratio topical
emulsions which demonstrate limited non-commercial stability. The most commonly used emulsifier in
these formulations is POE(2) oleyl ether which is oleic acid that has been oxyalkylated with two moles of
ethylene oxide.
The present invention is advantageous in that it provides a non-lipoidal media in lipoidal media high
internal phase ratio emulsion which is stable for extended periods, even at elevated temperatures. Further,
the invention is advantageous since it provides a non-lipoidal media in lipoidal media high internal phase
ratio emulsion which does not break or leak after five freeze-thaw cycles and remains on the skin for
extended periods while being cosmetically acceptable.
The present invention provides topical compositions which comprises non-lipoidal media in lipoidal
media emulsions containing non-ionic oil soluble straight or branched chain ester emulsifiers having at least
two hydrogen bonding sites per molecule.
The present invention is directed to topical preparations incorporated into delivery systems which exhibit
commercial stability. That is they do not show phase separation or leaking of the internal phase after at least
five freeze-thaw cycles. It has been discovered that this stability is attributable to the selection of a certain
class of emulsifiers to form the emulsions. Also, the present invention is directed to preparations which do
not wash off as easily as prior art preparations which are cosmetically acceptable since they do not feel
waxy.
The emulsions of the invention are comprised of lipoidal and non-lipoidal phases. The non-lipoidal phase
comprises at least 70%, and preferably at least 75% of the emulsion and is the internal phase. This phase
may comprise either water, glycerine, sorbitol, sugar syrups or combinations thereof. The internal phase
may be multi-phasic and may be a solution, suspension, emulsion or combination thereof, and it may
contain a portion of an active agent. Also, the internal phase may contain suspended solids, emulsions,
extenders and dilutants, as well as colours, flavours and buffers.
The external phase is comprised of lipoidal media such as mineral oils or vegetable oils. The phase is the
continuous phase of the systems. The term lipoidal pertains to any of a group of organic compounds
comprising the neutral fats, fatty acids, waxes, steroids, petrolatum, phosphatides, fatty acid esters and
mineral oils having the following common properties: insoluble in water, soluble in alcohol, ether,
chloroform or other fat solvents, and which exhibit a greasy feel.Examples of oils suitable for use in these
delivery systems are mineral oils with viscosities of 6.7 to 68.7 centistokes, preferably 6.7 to 42 centistokes,
and vegetable oils illustrated by coconut, palm kernel, cocoa butter, cottenseed, peanut, olive, palm,
sunflower, seed, sesame, corn safflower, rape seed, soybean and fractionated liquid triglycerides of short
chain (naturally derived) fatty acids. This external phase may also contain colours, flavours and buffers.
The systems may contain an independent active agent. Such an active agent may be any one of those
which are approved for or used as topical applications in the treatment and/or prophylaxis of any disease
diagnostic purposes, or cosmetic effect. Potential agents are normally well known due to their common
usage and include silicone oil, aluminium chlorhydrate, benzoyl peroxide and steroids.The topical
preprations of the invention have numerous uses, such as suntan lotions, moisturising creams, rub-down
emulsions, cleansing baby oil emulsions, wax cream, petrolatum creams, hair care creams, tooth polish,
acne cream, tresaderm cream, hydrocortisone cream, antiperspirant, protective lotions, anti-inflammatory,
including steroids and non-steroidal agents, analgesic agents, anti-fungal agents, anti-infective agents,
emollients, agents for the treatment of psoriasis, anti-pruritics, and anti-acne agents, and bleaching agents.
It has been found that cosmetic grade emulsifiers which are non-ionic oil soluble straight or branched
chain esters and have at least two hydrogen bonding sites per molecule produce the stable emulsions of the
invention. Examples of such emulsifiers are polyglycerol oleate and glycerol monoisostearate. Polyglycerol oleate is produced by heating glycerol under a vacuum using a basic catalyst such as sodium acetate. A polyglycerol chain is formed which is then esterified with oleic acid. The product is partially dispersible in water having a hydrophilic-lipophilic balance (HLB) of approximately four. The glycerol monoisostearate is made by esterifying glycerine with isostearic acid. This material has flocculant-like properties when in contact with water caused by the incorporation of water into it.
As previously noted, it is believed that the two aforementioned emulsifiers form emulsions which are more stable than those of the prior art due to their being straight or branched chain esters, non-ionic, oil soluble and having at least two hydrogen bonding sites per molecule. Emulsions utilising these emulsifiers are able to withstand at least five freeze-thaw cycles. Emulsifiers which have cyclic rings and/or do not have at least two hydrogen bonding sites per molecule are ineffective in producing commercially stable emulsions.
The following Examples illustrate the principles of the invention:
Method ofpreparation: The active agent, and ingredients of the internal phase were mixed together at room temperature. The ingredients of the external phase were mixed together in a one-gallon vessel. The internal phase composition was slowly added to the external phase composition as the two phases were mixed together with a split disc stirrer at low shear until the desired viscosity was obtained.
The products described here may be prepared by continuous or batch processes. As in preparing conventional emulsions, shear force is applied to the system components by use of a homogeniser, mill, mixer, agitator, impingement surfaces, ultra-sound, shaking or vibration. Unlike conventional emulsions, the mixing gear should be at low levels in order to prevent destruction of the system by imparting excess energy. Temperature is not usually a critical factor in the preparation of the systems. The temperatures utilised will be dependent upon the final end product desired.
The products described here may be prepared by mixing the internal with the external phase in a planetary-type mixer. Another manner of preparing the system is by the use of a continuous mixer which comprises multiple impellers. The external phase is first introduced into the continuous mixer until it reaches the level of the lowest impeller in the mixing chamber. The two phases are then simultaneously introduced through the bottom of the mixer in proper proportion as its impeller or impellers rotate to apply a shear to the components. The finished product emerges through the top of the mixer. The actual speed of the impeller or impellers will vary depending upon the product produced as will the rate of flow of the two phase streams.
Protective Lotion 1
(Initial Viscosity = 50K-lOOK CPS)
Ingredients %wt.lwt.
internal Phase
Deionized Water 79.15
Sorbitol 70% Sln 8.0
Dowicil 200 0.1
Silicone Fluid 200,100 CS 1.0
External Phase
Carnation Mineral Oil 8.0
Microcrystalline Wax 0.5
Polyglycerol Oleate 3.25
Protective Lotion 2
(Initial Viscosity = 60K-150K CPS)
ingredients %wt.lwt.
Internal Phase
Deionized Water 73.8982
Sorbitol 70% Sln 8.0
Dowicil 200 0.1
Silicone Fluid 200,100 CS 1.0
External Phase
Polyglycerol Oleate 3.25
Microcrystalline Wax 0.5
Fragrance 0.1
Red Dye #3 .0018
Carnation Mineral Oil 8.0
Active Phase
TiO2 .15
Talc 5.0
Protective Lotion 3
(Initial Viscosity = 250K-450K CPS)
Ingredients %wt.lwt Internal Phase
Deionized Water 75.19
Sorbitol 70% Sln 8.0
Dowicil 200 0.1
Methylparaben 0.14
Silicone Fluid 200, 100 CS 5.0
External Phase
Microcrystalline Wax 0.5
Gloria Mineral Oil 5.0
Glycerol Monoisosterate 3.0
Polyglycerol Oleate 3.0
Propylparaben 0.03
Fragrance 0.025
Benzocaine 10%
(Initial Viscosity = lOOK-400K CPS)
Ingredients %wt./wt.
Internal Phase
Deionized Water 69.3
Glycerine 8.0
Benzyl Trimethyl Ammonium
Hydrolyzed Animal Protein 1.0
Methylparaben 0.15
Propylparaben 0.05
Silicone Fluid 200,100 CS 1.0
External Phase
Carnation Mineral Oil 7.0
Polyglycerol Oleate 3.0
Microcrystalline Wax 0.5
Active Phase
Benzocaine 10.0
Antiperspirant Roll-On
(Initial Viscosity = 28K CPS-50K CPS)
Ingredients %wt.lwt Internal Phase
Deionized Water 38.5
Sorbitol 70% Sln 5.0
Aluminum Chlorhydrate 50% Sln 40.0
Dowicil 200 0.1
External Phase
LMO 7F40 11.0
Isopar C 1.0
Glycerol Monoisosterate 4.0
Fragrance 0.3
Benzoyl Peroxide 5%
(Initial Viscosity = 200K-350K CPS)
Ingredients %wt.lwt Internal Phase
Deionized Water 74.6
Microcrystalline Wax 8.0
Dowicil 200 0.1
CMC 7HF 0.2
Benzoyl Peroxide (Lucidol 70) 7.1
External Phase
Carnation Mineral Oil 5.0
Glycerol Monoisosterate 5.0
Each of the above compositions was subjected to a series of freeze-thaw cycles. The Table following summarises the results.
Average Minimum NumberofFreeze- Composition Thaw Cyc/es Prior to Breaking
Protective Lotion 1 10
Protective Lotion 2 10
Protective Lotion 3 10 Benzocaine 10% 10
Antiperspirant Roll-On 10
Benzoyl Peroxide 5% 10
The above compositions correspond to the compositions contained in the Examples of this patent. A Table summarising the freeze-thaw stability of the products disclosed in the UK Patent 1,415,528 are summarised below. The products were prepared with both 5% and 8% sorbitol concentrations to insure that sorbitol did not effect stability.
Average Minimum Number of Freeze
Example Thaw Cycles Prior to Breaking
11 0 11 Sorbitol) 0 12 0
13 0
16 1 16(8% Sorbitol) 1
20 1
21 2
23 0
24 5
26 5
As is apparent from the above results, the compositions of the prior art fail to achieve more than five freeze-thaw cycles. This compares with the compositions of the present invention which display stabilty through ten cycles.
Claims (24)
1. Atopical composition which comprises non-lipoidal media in a lipoidal media emulsion in which the non-lipoidal phase is at least 70% of the emulsion, the lipoidal phase contains non-ionic oil soluble straight or branched chain ester, or combinations thereof, emulsifier having at least two hydrogen bonding sites per molecule.
2. A composition according to claim 1, in which the non-lipoidal media comprises at least 75% of the emulsion.
3. A composition according to claim 1 or claim 2, in which the lipoidal media comprises vegetable oil.
4. A composition according to claim 1 or claim 2, in which the lipoidal media comprises mineral oil.
5. A composition according to any preceding claim, in which the non-lipoidal media is selected from water, glycerine and sorbitol.
6. A composition according to any preceding claim, in which the emulsifier comprises polyglycerol oleate.
7. A composition according to any of claims 1 to 5, in which the emulsifier comprises glycerol monoisosterate.
8. A composition according to any preceding claim including an independent active agent.
9. A composition according to claim 8, in which the independent active agent is selected from silicone oil, aluminium chlorohydrate, benzoyl peroxide and steroids.
10. A composition according to any preceding claim including an agent selected from anti-inflammatory agents, analgesic agents, anti-fungal agents, anti-infective agents, emollients, agents for the treatment of psoriasis, anti-pruritics, anti-acne agents and bleaching agents.
11. A composition according to any preceding claim in the form of a suntan lotion.
12. A composition according to any of claims 1 to lOin the form of a moisturising cream.
13. A composition according to any of claims 1 to 10 in the form of rub-down emulsions.
14. A composition according to any of claims 1 to 10 in the form of cleansing baby oil emulsions.
15. A composition according to any of claims 1 to 10 in the form of wax creams.
16. A composition according to any of claims 1 to 10 in the form petrolatum creams.
17. Acomposition according to any of claims 1 to lOin the form of hair care creams.
18. A composition according to any of claims 1 to 10 in the form of tooth polish.
19. A composition according to any of claims 1 to 10 in the form of acne cream.
20. A composition according to any of claims 1 to 10 in the form oftresaderm cream.
21. A composition according to any of claims 1 to 10 in the form of hydrocortisone cream.
22. A composition according to any of claims 1 to 10 in the form of antiperspirant.
23. A composition according to any of claims 1 to 10 in the form of protective lotions.
24. A composition according to claim 1, substantially as herein described with reference to any of the
Examples.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB08313456A GB2139919A (en) | 1983-05-16 | 1983-05-16 | Stable high internal phase ratio topical emulsions |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB08313456A GB2139919A (en) | 1983-05-16 | 1983-05-16 | Stable high internal phase ratio topical emulsions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB8313456D0 GB8313456D0 (en) | 1983-06-22 |
| GB2139919A true GB2139919A (en) | 1984-11-21 |
Family
ID=10542817
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB08313456A Withdrawn GB2139919A (en) | 1983-05-16 | 1983-05-16 | Stable high internal phase ratio topical emulsions |
Country Status (1)
| Country | Link |
|---|---|
| GB (1) | GB2139919A (en) |
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0244405A1 (en) * | 1985-10-31 | 1987-11-11 | Kv Pharm Co | Vaginal delivery systems. |
| EP0281394A2 (en) * | 1987-03-06 | 1988-09-07 | Richardson-Vicks, Inc. | Oil-in-water-in-silicone emulsion compositions |
| EP0451461A2 (en) * | 1990-02-23 | 1991-10-16 | BASF Aktiengesellschaft | Use of mixtures of polyglycerol fatty acid esters as emulsifiers in cosmetic and pharmaceutical compositions |
| US5266329A (en) * | 1985-10-31 | 1993-11-30 | Kv Pharmaceutical Company | Vaginal delivery system |
| EP0760842A1 (en) * | 1994-06-20 | 1997-03-12 | Kv Pharmaceutical Corporation | Improved long acting gi and esophageal protectant |
| US8299127B2 (en) | 2009-03-11 | 2012-10-30 | Conopco, Inc. | Method and composition for evenly applying water soluble actives |
| US8398959B2 (en) | 2010-12-06 | 2013-03-19 | Conopco, Inc. | Compositions and methods for imparting a sunless tan with functionalized adjuvants |
| US8425882B2 (en) | 2008-04-01 | 2013-04-23 | Conopco, Inc. | In-shower and bath compositions |
| US8821839B2 (en) | 2010-10-22 | 2014-09-02 | Conopco, Inc. | Compositions and methods for imparting a sunless tan with a vicinal diamine |
| US8961942B2 (en) | 2011-12-13 | 2015-02-24 | Conopco, Inc. | Sunless tanning compositions with adjuvants comprising sulfur comprising moieties |
| EP1863438A4 (en) * | 2005-03-18 | 2015-06-17 | Lg Household & Health Care Ltd | Tooth whitener |
| US11324681B2 (en) | 2017-12-20 | 2022-05-10 | 3M Innovative Properties Company | Oral compositions and methods of use |
| US11779446B2 (en) | 2017-11-21 | 2023-10-10 | 3M Innovative Properties Company | Oral compositions and methods of use |
| US11801231B2 (en) | 2017-12-20 | 2023-10-31 | 3M Innovative Properties Company | Oral compositions and methods of use |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1341094A (en) * | 1970-05-15 | 1973-12-19 | Beiersdorf Ag | Manufacture of water-in-oil emulsions using partial esters of wool wax acids and glycerine |
-
1983
- 1983-05-16 GB GB08313456A patent/GB2139919A/en not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1341094A (en) * | 1970-05-15 | 1973-12-19 | Beiersdorf Ag | Manufacture of water-in-oil emulsions using partial esters of wool wax acids and glycerine |
Cited By (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0244405A1 (en) * | 1985-10-31 | 1987-11-11 | Kv Pharm Co | Vaginal delivery systems. |
| EP0244405A4 (en) * | 1985-10-31 | 1988-08-23 | Kv Pharm Co | Vaginal delivery systems. |
| US5266329A (en) * | 1985-10-31 | 1993-11-30 | Kv Pharmaceutical Company | Vaginal delivery system |
| EP0281394A2 (en) * | 1987-03-06 | 1988-09-07 | Richardson-Vicks, Inc. | Oil-in-water-in-silicone emulsion compositions |
| EP0281394A3 (en) * | 1987-03-06 | 1990-05-16 | Richardson-Vicks, Inc. | Oil-in-water-in-silicone emulsion compositions |
| EP0451461A2 (en) * | 1990-02-23 | 1991-10-16 | BASF Aktiengesellschaft | Use of mixtures of polyglycerol fatty acid esters as emulsifiers in cosmetic and pharmaceutical compositions |
| EP0451461A3 (en) * | 1990-02-23 | 1992-12-23 | Basf Aktiengesellschaft | Use of mixtures of polyglycerol fatty acid esters as emulsifiers in cosmetic and pharmaceutical compositions |
| EP0760842A4 (en) * | 1994-06-20 | 1998-07-15 | Kv Pharmaceutical Corp | Improved long acting gi and esophageal protectant |
| EP0760842A1 (en) * | 1994-06-20 | 1997-03-12 | Kv Pharmaceutical Corporation | Improved long acting gi and esophageal protectant |
| EP1863438A4 (en) * | 2005-03-18 | 2015-06-17 | Lg Household & Health Care Ltd | Tooth whitener |
| US8425882B2 (en) | 2008-04-01 | 2013-04-23 | Conopco, Inc. | In-shower and bath compositions |
| US8299127B2 (en) | 2009-03-11 | 2012-10-30 | Conopco, Inc. | Method and composition for evenly applying water soluble actives |
| US8821839B2 (en) | 2010-10-22 | 2014-09-02 | Conopco, Inc. | Compositions and methods for imparting a sunless tan with a vicinal diamine |
| US8398959B2 (en) | 2010-12-06 | 2013-03-19 | Conopco, Inc. | Compositions and methods for imparting a sunless tan with functionalized adjuvants |
| US8961942B2 (en) | 2011-12-13 | 2015-02-24 | Conopco, Inc. | Sunless tanning compositions with adjuvants comprising sulfur comprising moieties |
| US11779446B2 (en) | 2017-11-21 | 2023-10-10 | 3M Innovative Properties Company | Oral compositions and methods of use |
| US11324681B2 (en) | 2017-12-20 | 2022-05-10 | 3M Innovative Properties Company | Oral compositions and methods of use |
| US11801231B2 (en) | 2017-12-20 | 2023-10-31 | 3M Innovative Properties Company | Oral compositions and methods of use |
Also Published As
| Publication number | Publication date |
|---|---|
| GB8313456D0 (en) | 1983-06-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |