GB2076285A - Dermatological compositions - Google Patents
Dermatological compositions Download PDFInfo
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- GB2076285A GB2076285A GB8017078A GB8017078A GB2076285A GB 2076285 A GB2076285 A GB 2076285A GB 8017078 A GB8017078 A GB 8017078A GB 8017078 A GB8017078 A GB 8017078A GB 2076285 A GB2076285 A GB 2076285A
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- Prior art keywords
- composition according
- composition
- starch
- acid
- water
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 63
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 32
- 229920002472 Starch Polymers 0.000 claims abstract description 25
- 239000008107 starch Substances 0.000 claims abstract description 24
- 235000019698 starch Nutrition 0.000 claims abstract description 24
- 239000004342 Benzoyl peroxide Substances 0.000 claims abstract description 11
- OMPJBNCRMGITSC-UHFFFAOYSA-N Benzoylperoxide Chemical compound C=1C=CC=CC=1C(=O)OOC(=O)C1=CC=CC=C1 OMPJBNCRMGITSC-UHFFFAOYSA-N 0.000 claims abstract description 11
- 235000019400 benzoyl peroxide Nutrition 0.000 claims abstract description 11
- 238000011065 in-situ storage Methods 0.000 claims abstract description 7
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 claims abstract description 6
- 239000003349 gelling agent Substances 0.000 claims abstract description 5
- 230000009974 thixotropic effect Effects 0.000 claims abstract description 4
- 239000004480 active ingredient Substances 0.000 claims abstract description 3
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 8
- 229960001484 edetic acid Drugs 0.000 claims description 8
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 8
- 239000002253 acid Substances 0.000 claims description 7
- 239000000839 emulsion Substances 0.000 claims description 7
- 150000003248 quinolines Chemical class 0.000 claims description 7
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
- 239000008387 emulsifying waxe Substances 0.000 claims description 6
- 229940057995 liquid paraffin Drugs 0.000 claims description 6
- 229910052708 sodium Inorganic materials 0.000 claims description 6
- 239000011734 sodium Substances 0.000 claims description 6
- 239000002738 chelating agent Substances 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000002002 slurry Substances 0.000 claims description 5
- 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
- 239000004310 lactic acid Substances 0.000 claims description 4
- 235000014655 lactic acid Nutrition 0.000 claims description 4
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 4
- 229930195734 saturated hydrocarbon Natural products 0.000 claims description 4
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 3
- 230000015572 biosynthetic process Effects 0.000 claims description 3
- 229910052700 potassium Inorganic materials 0.000 claims description 3
- 239000011591 potassium Substances 0.000 claims description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- QCDFBFJGMNKBDO-UHFFFAOYSA-N Clioquinol Chemical compound C1=CN=C2C(O)=C(I)C=C(Cl)C2=C1 QCDFBFJGMNKBDO-UHFFFAOYSA-N 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims description 2
- YYVFXSYQSOZCOQ-UHFFFAOYSA-N Oxyquinoline sulfate Chemical compound [O-]S([O-])(=O)=O.C1=C[NH+]=C2C(O)=CC=CC2=C1.C1=C[NH+]=C2C(O)=CC=CC2=C1 YYVFXSYQSOZCOQ-UHFFFAOYSA-N 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 2
- 239000004202 carbamide Substances 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 229960003333 chlorhexidine gluconate Drugs 0.000 claims description 2
- 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 claims description 2
- 235000015165 citric acid Nutrition 0.000 claims description 2
- KCIDZIIHRGYJAE-YGFYJFDDSA-L dipotassium;[(2r,3r,4s,5r,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] phosphate Chemical class [K+].[K+].OC[C@H]1O[C@H](OP([O-])([O-])=O)[C@H](O)[C@@H](O)[C@H]1O KCIDZIIHRGYJAE-YGFYJFDDSA-L 0.000 claims description 2
- 229960000890 hydrocortisone Drugs 0.000 claims description 2
- UXZFQZANDVDGMM-UHFFFAOYSA-N iodoquinol Chemical compound C1=CN=C2C(O)=C(I)C=C(I)C2=C1 UXZFQZANDVDGMM-UHFFFAOYSA-N 0.000 claims description 2
- ZBJWWKFMHOAPNS-UHFFFAOYSA-N loretin Chemical compound C1=CN=C2C(O)=C(I)C=C(S(O)(=O)=O)C2=C1 ZBJWWKFMHOAPNS-UHFFFAOYSA-N 0.000 claims description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 2
- 239000011976 maleic acid Substances 0.000 claims description 2
- 235000016337 monopotassium tartrate Nutrition 0.000 claims description 2
- 229920001206 natural gum Polymers 0.000 claims description 2
- KYKNRZGSIGMXFH-ZVGUSBNCSA-M potassium bitartrate Chemical compound [K+].OC(=O)[C@H](O)[C@@H](O)C([O-])=O KYKNRZGSIGMXFH-ZVGUSBNCSA-M 0.000 claims description 2
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 claims description 2
- 235000011004 sodium tartrates Nutrition 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 239000011975 tartaric acid Substances 0.000 claims description 2
- 235000002906 tartaric acid Nutrition 0.000 claims description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 2
- 229940045136 urea Drugs 0.000 claims description 2
- 238000000034 method Methods 0.000 claims 7
- 239000000499 gel Substances 0.000 claims 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229910021653 sulphate ion Inorganic materials 0.000 claims 1
- 239000012071 phase Substances 0.000 description 14
- 239000000126 substance Substances 0.000 description 12
- 238000003756 stirring Methods 0.000 description 11
- 239000002537 cosmetic Substances 0.000 description 6
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 6
- 229940082500 cetostearyl alcohol Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 description 4
- YNCMTKURLYZSQT-UHFFFAOYSA-L dipotassium;quinolin-8-ol;sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O.C1=CN=C2C(O)=CC=CC2=C1 YNCMTKURLYZSQT-UHFFFAOYSA-L 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 2
- 235000019759 Maize starch Nutrition 0.000 description 2
- 239000000470 constituent Substances 0.000 description 2
- 230000001804 emulsifying effect Effects 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- 239000006210 lotion Substances 0.000 description 2
- 235000019271 petrolatum Nutrition 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 235000019980 sodium acid phosphate Nutrition 0.000 description 2
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 2
- DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical compound C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 description 1
- GLKBRIDXWLXQCG-ZPHPHTNESA-N (z)-1-hexadecoxyoctadec-9-ene Chemical group CCCCCCCCCCCCCCCCOCCCCCCCC\C=C/CCCCCCCC GLKBRIDXWLXQCG-ZPHPHTNESA-N 0.000 description 1
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical group C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 239000004141 Sodium laurylsulphate Substances 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 125000000129 anionic group Chemical group 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 239000003899 bactericide agent Substances 0.000 description 1
- 210000000746 body region Anatomy 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 229960000691 diiodohydroxyquinoline Drugs 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 239000003410 keratolytic agent Substances 0.000 description 1
- 229910021645 metal ion Inorganic materials 0.000 description 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- 239000012875 nonionic emulsifier Substances 0.000 description 1
- 239000007764 o/w emulsion Substances 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 150000002978 peroxides Chemical class 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 229940100486 rice starch Drugs 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- SOBHUZYZLFQYFK-UHFFFAOYSA-K trisodium;hydroxy-[[phosphonatomethyl(phosphonomethyl)amino]methyl]phosphinate Chemical compound [Na+].[Na+].[Na+].OP(O)(=O)CN(CP(O)([O-])=O)CP([O-])([O-])=O SOBHUZYZLFQYFK-UHFFFAOYSA-K 0.000 description 1
- 229940100445 wheat starch Drugs 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K8/042—Gels
-
- 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
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/22—Peroxides; Oxygen; Ozone
-
- 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
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/732—Starch; Amylose; Amylopectin; Derivatives thereof
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Birds (AREA)
- Inorganic Chemistry (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Dispersion Chemistry (AREA)
- Cosmetics (AREA)
- Medicinal Preparation (AREA)
Abstract
A dermatological composition containing an oil phase dispersed in a water phase is in the form of a thixotropic gel. Starch which is gelled in situ may be used as the gelling agent. The composition may contain hydrogen peroxide or benzoyl peroxide as a dermatologically active ingredient.
Description
SPECIFICATION
Dermatological compositions
This invention relates to dermatological compositions particularly although not exclusively for human therapeutic use.
Both greasy (water in oil) and non-greasy (oil in water) dermatological compositions are known. High water content non-greasy compositions which are of 'thin' consistency may be preferred in certain contexts, for example for treating distressing conditions such as acne, due to the ease with which they can be spread over a region of skin to be treated and also having regard to their 'vanishing' properties and general cosmetic acceptability. In these respects a composition having the consistency of a lotion may be particularly advantageous but problems may arise with this due to the likelihood of the composition running away from a skin region to which it is applied whereby the efficacy thereof may be reduced and there is the danger that discomfort may be caused in the case where the lotion is applied close to a sensitive body region such as the eyes.
An object of the present invention is to provide a dermatological compositions which is readily spreadable and has good vanishing properties and general cosmetic acceptability yet which has little or no tendency to run away when applied to a skin region to be treated.
According to the invention therefore there is provided a dermatological composition which comprising an oil phase and a water phase, characterised in that the composition is formed by mixing starch with oil and water components, and then converting the starch to a gel in situ thereby to give a stable oil-inwater emulsion having the consistency of a gel.
In this way, it has been found possible to obtain a higher water content non-greasy composition which is readily spreadable and has good vanishing properties and general cosmetic acceptability and yet which has sufficient 'thickness' when first applied to the skin to prevent or at least apprecjably reduce the possiblility of undesired running away thereof.
This is due to the fact that the starch gel, as formed in situ, becomes integrally incorporated in the oil-in-water emulsion and imparts thixotropic properties thereto. That is, the composition is in form of a gel which when brought into contact with the skin region to be treated will be retained in position thereon yet which when rubbed into the skin will adopt a 'thin' consistency suited to speedy vanishing and good spreadability.
The starch used in forming the composition of the invention may be of any suitable origin, for example, it may be maize starch, rice starch, potato starch, wheat starch.
The starch may be incorporated by adding same in the form of an aqueous slurry to a preformed emulsion of the water and oil components, the resulting mixture then being heated and stirred to form the gel. The emulsion may be preformed by adding the water component at a temperature of about 70"C (or higher) to the oil component also at a temperature of about 70"C (or higher) with stirring. The starch slurry may be added to such emulsion, the mixture then being further heated to 95-100 C with stirring and the resulting gel being allowed to cool with stirring.
The said oil component with which the starch is mixed prior to gel formation may comprise some or all of the total oil phase of the composition. Where the oil component forms only part of the oil phase the remainder thereof will be added and incorporated in any suitable manner subsequent to gelling of the starch. The said oil phase may be of any suitable form appropriately selected such that it is dermatologically innocuous and such that it is compatible with the remaining constituents of the preparation. Thus the oil phase may comprise a saturated hydrocarbon and an emulsifying wax.The saturated hydrocarbon will be one or more substances selected from the group consisting of hydrocarbons of general formula CnH2n+2 and fatty acids of general formula CnH2n+, COOH and may comprise for example liquid paraffin, hard paraffin wax, liquid paraffin Adeps Solidus, white or yellow soft paraffin wax. Preferably, and in order to facilitate attainment of a 'thin' consistency, liquid paraffin is used. The emulsifying wax may be a non-ionic substance of general formula R-Ck12-O(CH2.CCH2.0)nH and may be for example the substance known as Emulgade F or the substance known as Lanbritol
Wax N 21 (Trade Mark) which is a mixture of 86% cetostearyl alcohol with 14% of a nonionic emulsifier.The cetostearyl alcohol contains 30% cetyl alcohol and 70% stearyl alcohol and the emulsifier is a cetyl-oleyl ether of polyethylene glycol having a mean chain length of 14 ethylene oxide units. Alternatively, or additionally, the substance known as
Cetomacrogol Emulsifying Wax BPC may be used. This substance comprises a compound having the formula CH3(CH2)m-O-OCH2 (CH2.0.CH2)nCH20H where m is 1 5 to 1 7 and n is j 9 to 23, and four times its weight of cetostearyl alcohol.Alternatively or additionally, an anionic emulsifying wax may be used, such as the substance known as Eumulgin B2 or Emulsifying Wax BPC, comprising nine parts by weight cetostearyl alcohol and one part sodium lauryl sulphate or other sodium salt of a sulphated higher primary aliphatic alcohol or any mixture of salts.
The oil phase may make up 5% to 40% by weight of the composition of the invention.
The total proportion of water in the composi tion of the invention must be in excess of the proportion of the oil phase and may be in the range 43% to 76% by weight. The said water component with which the starch is mixed prior to gelling may comprise sorne or all of the total water phase. Where the water component forms only part of the water phase the remainder thereof will be added and incorporated in any suitable manner subsequent to gelling of the starch. As explained hereinafter, whilst the water phase may consist wholly of water most preferably such phase will comprise water with one or more substances dissolved and/or dispersed therein. Additionally to the oil and water phases and the starch, the composition of the invention may also comprise suitably dispersed solid material, also as explained hereinafter.
Preferably, the composition of the invention contains one or more dermatologically active ingredients. One possible ingredient is hydrogen peroxide and reference is made to British
Patent No. 1,539,771 in this respect. Alternatively, benzoyl peroxide in solid finely divided form may be used and this may be ground and incorporated with other ingredients of the composition in an emulsifying valve as described in British Patent No.
1,185,685. The benzoyl peroxide may be present in an amount of 1 to 25% by weight of the composition. In one embodiment, approximately 10% by weight benzoyl peroxide is used, and in an alternative embodiment approximately 5% by weight.
If desired, the composition may incorporate one or more of: a buffer, a chelating agent, a pharmaceutically active quinoline derivative, chlorhexidine gluconate, urea, hydrocortisone, a corticosteriod, and other substances which provide an auxiliary therapeutic or cosmetic effect or act to improve possible synergistically) the therapeutic or cosmetic effect of one or more of the other constituents.
With regard to the quinoline derivative, the composition may incorporate such a derivative which is a bactericidal and keratolytic agent for example a substance selected from potassium 8-hydroxyquinoline sulphate, 8-hydroxyquinoline sulphate, iodochlorhydroxyquinoline, diiodohydroxyquinoline and di(8-hydroxy-7-iodoquinoline-5-sulphonate). Such quinoline derivative will be dissolved in the water phase and may be present in an amount of say 0.01% to 6% by weight of the comp,osition, preferably about 0.5%.
With regard to the chelating agent, this may be provided for the purpose of minimising any loss of activity and discolouration of the quinoline derivative, where such derivative is provided, and in order to minimise any loss of available oxygen from the peroxide (where this is provided) particularly due to the presence of metal ions in the preparation. Such chelating agent may be any suitable substance for example ethylene-diamine tetra-acetic acid (EDTA) or any of the disodium, trisodium, dipotassium and tripotassium salts of
EDTA.
With regard to the buffer, this may be provided to improve stability, and may be such as to maintain the pH at 2.5 to 6.5 (preferably 3 5 to 4) and any suitable buffer may be used for this purpose. Thus, for example, there may be used an acid such as lactic acid, citric acid, tartaric acid, maleic acid, hydroxysuccinic acid with an acid salt. Said acid salt may be any of sodium and potassium acid phosphate, sodium and potassium acid citrate, sodium and potassium acid tartrate.
The invention will now be described further in the following Example. All percentages are by weight:
Example:
The following ingredients are used: 1. Liquid paraffin BP 10% 2. Emulgade F 3. Ethylene diamine tetra acetic acid
(98%) 0.09% 4. Sodium Acid Phosphate BP 0.5% 5. Maize starch BP 3% 6. Benzoyl peroxide 13.33% 7. Lactic Acid BP 0.5% 8. Potassium 8-hydroxyquinoline
sulphate BPC 0.5% 9. Eumulgin B2 0.5% 10. Water to 100%
The liquid paraffin, Emulgade F, EDTA and some of the water are introduced into the bowl of a Hobart mixer. The bowl is placed in a water bath and the contents are heated to 95"C and stirred for a period of time (say about 60 minutes).
The sodium acid phosphate is dissolved in water (at say 50-60"C) and the starch is blended in with stirring to give a smooth slurry. This slurry is added to the mixture in the Hobart bowl and the temperature is brought back up to 95"C with stirring until a gel is formed. The gel is allowed to cool to below 40"C with further stirring.
The lactic acid and the potassium 8-hydroxyquinoline sulphate are separately dissolved in water and added to the cooled gel.
The benzoyl peroxide is then blended into the contents of the Hobart bowl with stirring, such stirring being continued for at least 30 minutes to give a uniform mixture.
In a further Hobart bowl, further Emulgade
F and Eumulgin B2 are mixed with water and heated to 95"C with stirring. This mixture is then added to the uniform mixture in the first mentioned Hobart bowl with stirring. The contents of the latter bowl are then cooled to 30"C with stirring.
The resulting mixture is subjected to physical treatment to reduce the particle size of the benzoyl peroxide. This is effected with a
Raney Homogeniser (or similar emulsifying valve) at a pressure of about 2000 Ibs/square inch.
The resulting dermatological composition is in the form of a smooth non-greasy gel having thixotropoic properties. The composition does not tend to run when first applied to a skin region to be treated yet can be easily rubbed in and spread over such region and has good vanishing properties and is generally of excellent cosmetic acceptability.
It is of course to be understood that the invention is not intended to be restricted to the details of the above example.
Thus, whereas reference is made herein to the use of starch gelled in situ it is possible that a similar effect, that is, the formation of an oil-in-water dermatological composition in which a gel forms the aqueous phase and which has thixotropic properties, may be achieved utilising, additionally or alternatively to the starch, a different gelling agent which may be added already in gel form to the mixed oil and water components or alternatively which may be aded to such mixed components and then gelled in situ. Such different gelling agent may be, for example, one or more substances selected from: chemically modified cellulose such as hydroxypropylmethylcellulose, carboxy vinyl polymer, natural gums and the like.
Claims (27)
1. A dermatological composition comprising an oil phase and a water phase characterised in that said composition is in the form of a thixotropic gel.
2. A composition according to claim 1, wherein said oil phase comprises a saturated hydrocarbon and an emulsifying wax.
3. A composition according to claim 2, wherein said saturated hydrocarbon comprises liquid paraffin.
4. A composition according to any one of claims 1 to 3, wherein the oil phase makes up 5% to 40% by weight of the composition.
5. A composition according to any one of claims 1 to 4, containing 43% to 76% by weight of water.
6. A composition according to any one of claims 1 to 5, containing at least one dermatologically active ingredient.
7. A composition according to claim 6, containing hydrogen peroxide.
8. A composition according to claim 6, containing benzoyl peroxide in solid finely divided form.
9. A composition according to claim 6, containing 1 to 25% by weight benzoyl peroxide.
10. A composition according to claim 9, containing 1 0% by weight benzoyl peroxide.
11. A composition according to claim 9, containing 5% by weight benzoyl peroxide.
1 2. A composition according to any one of claims 1 to 11, containing one or more of a buffer, a chelating agent, a pharmaceutically active quinoline derivative, chlorhexidine gluconate, urea, hydrocortisone, a corticosteroid.
1 3. A composition according to claim 12, containing a quinoline derivative selected from potassium 8-hydroxquinoline sulphate, 8-hydroxyquinoline sulphate, iodochlorhydroxyquinoline, di-iodohydroxyquinoline and di(8-hydroxy-7-iodoquinoline-5-sulphonate).
14. A composition according to claim 13, whrein the quinoline derivative is dissolved in the water phase and comprises 0.01% to 6% by weight of the composition.
1 5. A composition according to any one of claims 1 2 to 14, containing a chelating agent selected from ethylenediamine tetra-acetic acid (EDTA) and disodium, triosodium dipotassium salts of EDTA.
1 6. A composition according to any one 9f claims 1 2 to 15, containing a buffer adapted to maintain the pH at 2.5 to 6.5.
1 7. A composition according to claim 16, wherein the buffer is an acid selected from lactic acid, citric acid, tartaric acid, maleic acid, hydroxysuccinic acid with an acid salt selected from sodium and potassium acid phosphate, sodium and potassium acid citrate, sodium and potassium acid tartrate.
1 8. A composition according to any one of claims 1 to 17, containing as a gelling agent one or more of: starch, chemically modified cellulose, carboxvinyl polymer, natural gums.
19. A composition according to claim 18, containing as gelling agent starch gelled in situ.
20. A composition substantially as hereinbefore described in the Example.
21. A method of forming a composition according to claim 1, wherein starch is added to a preformed emulsion of water and oil components, and the resulting mixture is heated so that the starch gels in situ.
22. A method according to claim 21, wherein the starch is added in the form of an aqueous slurry.
23. A method according to claim 21 or 22, wherein the said emulsion is preformed by adding the water component to the oil component at a temperature of 70"C or higher.
24. A method according to claim 23, wherein the emulsion is heated to 95-100"C after addition of the starch.
25. A method according to any one of claims 21 to 24, wherein the said oil component with which the- starch is mixed prior to gel formation comprises only part of the total oil phase of the composition, the remainder of such phase being added subsequent to gelling of the starch.
26. A method according to claim 21, substantially as hereinbefore described in the Example.
27. A composition formed by the method of any one of claims 21 to 25.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8017078A GB2076285B (en) | 1980-05-23 | 1980-05-23 | Dermatological compositions |
| GB8103106A GB2076286B (en) | 1980-05-23 | 1981-02-02 | Dermatological hydrogen peroxide compositions |
| DK226981A DK162374C (en) | 1980-05-23 | 1981-05-22 | PROCEDURE FOR THE PREPARATION OF A DERMATOLOGICAL CREAM PREPARATION CONTAINING HYDROGEN PEROXIDE |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8017078A GB2076285B (en) | 1980-05-23 | 1980-05-23 | Dermatological compositions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB2076285A true GB2076285A (en) | 1981-12-02 |
| GB2076285B GB2076285B (en) | 1984-04-04 |
Family
ID=10513627
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB8017078A Expired GB2076285B (en) | 1980-05-23 | 1980-05-23 | Dermatological compositions |
Country Status (1)
| Country | Link |
|---|---|
| GB (1) | GB2076285B (en) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4781923A (en) * | 1987-07-20 | 1988-11-01 | Pellico Michael A | Antiseptic gels |
| US4826681A (en) * | 1985-02-26 | 1989-05-02 | L'oreal | Anhydrous solution of hydrogen peroxide in an organic solvent and the use of the same in therapeutic and cosmetic formulations |
| US5084268A (en) * | 1991-06-17 | 1992-01-28 | Dental Concepts, Inc. | Tooth whitening dentifrice |
| WO1992019219A1 (en) * | 1991-04-26 | 1992-11-12 | Wella Aktiengesellschaft | Hair treatment agent |
| US5817675A (en) * | 1993-07-05 | 1998-10-06 | Diomed Developments Limited | Compositions for the treatment of psoriasis and their use |
| EP1374856A1 (en) * | 2002-06-18 | 2004-01-02 | Impetus AG | Oily thixotropic nasal spray |
| USD889973S1 (en) | 2016-11-18 | 2020-07-14 | Can't Live Without It, LLC | Bottle |
-
1980
- 1980-05-23 GB GB8017078A patent/GB2076285B/en not_active Expired
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4826681A (en) * | 1985-02-26 | 1989-05-02 | L'oreal | Anhydrous solution of hydrogen peroxide in an organic solvent and the use of the same in therapeutic and cosmetic formulations |
| US4781923A (en) * | 1987-07-20 | 1988-11-01 | Pellico Michael A | Antiseptic gels |
| WO1992019219A1 (en) * | 1991-04-26 | 1992-11-12 | Wella Aktiengesellschaft | Hair treatment agent |
| US5084268A (en) * | 1991-06-17 | 1992-01-28 | Dental Concepts, Inc. | Tooth whitening dentifrice |
| US5817675A (en) * | 1993-07-05 | 1998-10-06 | Diomed Developments Limited | Compositions for the treatment of psoriasis and their use |
| EP1374856A1 (en) * | 2002-06-18 | 2004-01-02 | Impetus AG | Oily thixotropic nasal spray |
| USD889973S1 (en) | 2016-11-18 | 2020-07-14 | Can't Live Without It, LLC | Bottle |
| USD926580S1 (en) | 2016-11-18 | 2021-08-03 | Can't Live Without It, LLC | Bottle |
Also Published As
| Publication number | Publication date |
|---|---|
| GB2076285B (en) | 1984-04-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PCNP | Patent ceased through non-payment of renewal fee |
Effective date: 19970523 |