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WO2019086195A1 - Procédé de préparation de formulations topiques au moyen d'ultrasons et formulations obtenues par ce procédé - Google Patents

Procédé de préparation de formulations topiques au moyen d'ultrasons et formulations obtenues par ce procédé Download PDF

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Publication number
WO2019086195A1
WO2019086195A1 PCT/EP2018/077029 EP2018077029W WO2019086195A1 WO 2019086195 A1 WO2019086195 A1 WO 2019086195A1 EP 2018077029 W EP2018077029 W EP 2018077029W WO 2019086195 A1 WO2019086195 A1 WO 2019086195A1
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Prior art keywords
weight
oil
base composition
topical formulation
formulations
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.)
Ceased
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PCT/EP2018/077029
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German (de)
English (en)
Inventor
Joachim BIESOLD
Patrick KAMER
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Cosmetolab AG
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Cosmetolab AG
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Publication date
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Priority to DE112018005353.9T priority Critical patent/DE112018005353A5/de
Publication of WO2019086195A1 publication Critical patent/WO2019086195A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K8/34—Alcohols
    • A61K8/345—Alcohols 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
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
    • 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
    • A61K8/55—Phosphorus compounds
    • A61K8/553—Phospholipids, e.g. lecithin
    • 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
    • A61K8/60—Sugars; Derivatives thereof
    • 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
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • 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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/08—Processes employing the direct application of electric or wave energy, or particle radiation; Apparatus therefor
    • B01J19/10—Processes employing the direct application of electric or wave energy, or particle radiation; Apparatus therefor employing sonic or ultrasonic vibrations
    • 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
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/82—Preparation or application process involves sonication or ultrasonication
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/14—Blood; Artificial blood
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01F—MIXING, e.g. DISSOLVING, EMULSIFYING OR DISPERSING
    • B01F31/00—Mixers with shaking, oscillating, or vibrating mechanisms
    • B01F31/80—Mixing by means of high-frequency vibrations above one kHz, e.g. ultrasonic vibrations

Definitions

  • the present invention relates to a process for the preparation of topical cosmetic or medical formulations, as well as formulations produced by this process.
  • a topical formulation means a product which is applied to the skin.
  • Topical cosmetic and topical medical Formulierun ⁇ gen are usually provided as emulsions. Depending on its nature, it may be an oil-in-water emulsion (o / w) 15 or a water-in-oil emulsion (w / o).
  • Emulsions are prepared by known emulsification processes.
  • an aqueous phase and an oil phase are processed together to form an emulsion with the aid of an emulsifier and a mixer.
  • Topically applied cosmetic products and Medizinalproduk ⁇ te must meet several requirements. For example, they may be neutral in odor as possible after the application of non-fat to the skin target 25 th, have sufficient Wasserre ⁇ consistency and do not contain ingredients harmful to health.
  • DE 198 57 492 A1 describes a formulation which contains a phosphatidylcholine as emulsifier.
  • Phosphatidylcholine is an ingredient of lecithin and is able to form a lamellar structure (DMS structure (dermatological matrix structure).)
  • DMS structure skin surface structure
  • Especially hydrogenated phosphatidylcholine described in DE 198 57 492 A1 is suitable for topical formulations.
  • formulations based on phosphatidylcholine and in particular hydrogenated phosphatidylcholine have disadvantages. These formulations can only be prepared in a complicated manner by using high-pressure homogenization (Hans Lauteneller, ⁇ tschische maschinerzeitung, 56 (14), 679 (2002)). In addition, it is necessary to add medium-chain triglycerides in significant amounts to the formulation in order to achieve the above-described property profile. This gives the formulation after application to the skin but an undesirable odor. It has been proposed in CH 711598 A2 to prepare such formulations by means of a fermentation process with bacterial or yeast cultures. However, this manufacturing process takes several days and is associated with the usually occurring in Fermentati ⁇ onsluien disadvantages.
  • Phosphatidylcholine is also expensive and can only absorb a comparatively small amount of oily substances or lipid substances.
  • DE 691 12 849 T2 it has therefore been proposed, instead of using pure phosphatidylcholine, to use a phospholipid basic substance which, in addition to phosphatidylcholine, also contains other phosphatide components. Nevertheless, according to this document, it is still necessary to use a not inconsiderable amount of phosphatidylcholine.
  • DE 10 2011 110 749 AI and the associated WO 2013/023641 A2 it has therefore been proposed, instead of using phosphatidylcholine, to use a sugar fatty acid ester, preferably sucrose tristearate, as emulsifier.
  • sugar fatty acid ester (more than 6% by weight). This is disadvantageous because these compounds are expensive.
  • sugar fatty acid esters do not have some of the benefits of phosphatidylcholine-based formulations (such as water resistance) to the same extent.
  • the present invention relates to a process for the preparation of a topical formulation, wherein the cosmetic formulation comprises a basic composition and at least one dermatologically or cosmetically or pharmacologically active substance, characterized in that a treatment with ultrasound is carried out for the preparation of the basic composition.
  • the process interruption problem occurring in particular in connection with high-pressure homogenization is markedly reduced.
  • the method according to the invention is very easy to carry out due to ideally adjustable process parameters, resulting in considerably reduced personnel costs.
  • the process according to the invention can in principle be used for the preparation of any topical formulation, but is particularly suitable for the preparation of the above-described DMS formulations (formulations with a dermatological matrix structure) which are otherwise difficult to prepare.
  • the required amount of emulsifier can be considerably reduced without thereby impairing the required properties or the structure / consistency of the formulation.
  • it is sufficient not more than 2.5 wt .-%, preferably 0.1 to 2 wt .-%, more preferably 0.1 to 1.6 wt .-%, particularly preferably 0.2 to 1.4 wt .-% of at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester in the base composition.
  • the Formu ⁇ -regulation in particular the base composition of the formulation medium chain triglycerides to add.
  • the formulations according to the invention fulfill the requirement profile for topical formulations despite the small amounts of emulsifier and despite the absence of medium-chain triglycerides.
  • a medium-chain triglyceride is understood as meaning a compound in which fatty acids with chain lengths of C8 to C16 (the number indicates the number of carbon atoms in the fatty acid) are esterified with glycerol.
  • fatty acids with chain lengths of C8 to C16 the number indicates the number of carbon atoms in the fatty acid
  • glycerol the number indicates the number of carbon atoms in the fatty acid
  • the formulations according to the invention produced as compared to conventionally prepared formulations, in particular DMS formulations, an increased capacity for lip- ide or other additives have, especially water-soluble set materials to ⁇ without the need for thickening additive additives ⁇ must be zugege ben which the skin Sensitivity that affects moisture-wicking properties, as well as the structure and consistency of the formulation.
  • substantially finer structured lipid / water distributions can be generated by means of the method according to the invention which, despite a lipid fraction which may be incorporated at a higher level, but in particular despite a higher water content, can considerably better preserve the desired structure (or consistency).
  • the formulations according to the invention have a high temperature resistance and can therefore be used even if they persist warm ambient conditions (temperatures up to 40 ° C) can be used reliably.
  • formulations according to the invention are more compact than conventionally prepared formulations, in particular DMS formulations.
  • formulations according to the invention have a smaller proportion of air inclusions
  • the core of the present invention is the implementation of the homogenization by means of an ultrasonic treatment.
  • the novel formulations are designed as conventional topical formulations, for example DMS formulations based on water-oil.
  • the inventive formulations have to be homogenized, that is, the formulation must have a uniform consistency without local differences (eg phases ⁇ limits).
  • the aqueous phase and the oil phase must be combined to form an emulsion.
  • An emulsion is a homogeneous system on liquid phases in which droplets of one phase are homogeneously distributed in the other liquid phase.
  • droplets of a ⁇ lpha ⁇ se dispersed in an aqueous phase it is called an oil-in-water emulsion (o / w).
  • the inventive formulation comprises a so-called Ba ⁇ sis composition and which of the Ba sis composition is added at least one dermatologically or cosmetically or pharmacologically active substance.
  • the process improvement of the present invention relates to the step of preparing the base composition, namely the homogenization of the base composition.
  • Ultrasonic treatment according to a preferred embodiment of the present invention at a temperature of the base composition in the range of 35 ° C to 85 ° C, preferably in the range of 50 ° C to 85 ° C, more preferably in the range of 60 ° C to 80 ° C performed.
  • any conventional ultrasound apparatus can be used for ultrasound treatment for homogenizing the base composition, which provides adequate performance.
  • a preferred embodiment of the present invention should be achieved in the basic composition by treatment with ultrasound an energy input which is in the range of 200 Ws / g to 600 Ws / g, preferably ⁇ , in the range of 250 Ws / g to 500 Ws / g, more preferably in the range of 300 Ws / g to 450 Ws / g, based on the Men ⁇ ge to be homogenized composition.
  • wel ⁇ cher In the case of sequential homogenization of the base composition due to sequential addition of different phases, the above standing energy entry on the entire energy entry, wel ⁇ cher is to be fed to the system over all sequential Homogenmaschines syndromen.
  • the method of the present invention can be carried out, for example, with ultrasonic devices from Hielscher. Such devices are commercially available.
  • the duration of the ultrasound treatment according to the invention depends on the base composition to be homogenized.
  • the at least one aqueous phase in this case comprises water as solvent and optionally water-soluble constituents of the basic composition.
  • water-soluble constituents of the Ba ⁇ sis composition preferably moisturizing substances come into question. It is also conceivable, for example, the addition Physiologist ⁇ cally acceptable salts.
  • Moisturizing substances which can be used according to the invention can be polyols, urea or mixtures thereof. The polyols must be physiologically acceptable. Examples include glycol, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, glycerol, carbohydrates such as inositol (inositol), sorbitol (sorbitol),
  • Mannitol palatinit, maltodextrin, dextrin, cyclodextrin, glucose, fructose, lactose, mannose, galactose and other saccharides.
  • Particularly preferred are glycerol, propylene glycol, pen ⁇ tylene glycol and urea.
  • An exemplary aqueous phase of an inventive Ba ⁇ sis composition consists of a mixture of water and at least one polyol as a moisturizer substance. Preference is given to a mixture of 60-90% by weight of water and 40-10% by weight of a mixture of glycerol and pentylene glycol.
  • the at least one aqueous phase is usually by ⁇
  • mixing and heating sammentrade prepared are placed in a container such as a reaction flask and in a conventional manner
  • the at least one oil phase here comprises the emulsifier, which is preferably selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester, and further non-water-soluble constituents of the novel base composition.
  • a preferred emulsifier according to the invention is phosphatidylcholine.
  • Phosphatidylcholine is a constituent of lecithin and is chemically composed of a glycerol unit, of which three roxyl groups two groups are esterified with (usually unsaturated) fatty acids, while the last hydroxyl group is connected to ei ⁇ nem Phosphocholinrest.
  • Lecithin is a naturally occurring mixture of various phospholipids in various plants, for example soybeans, or egg yellow.
  • Phosphatidylcholine can be extracted from lecithin and is commercially available.
  • the emulsifier is a hydrogenated phosphate diylcholine.
  • Hydrogenated phosphatidylcholines are known and commercially available ⁇ Lich.
  • the product Lipoid P-100-3 of the company called Lip ⁇ oid cosmetics.
  • Hydrogenated phosphatidylcholines can be prepared from naturally occurring phosphatidylcholines by hydrogenating the double bonds in the unsaturated fatty acid chains.
  • sucrose fatty acid ester is a sucrose fatty acid ester.
  • mono-, di- or triflic acid esters or polyesters of sucrose can be used.
  • sucrose stearates sucrose mono-, di- or tristearate
  • sucrose tristearate is the most preferred.
  • the inventive base composition comprises in a preferred embodiment as non-water soluble Bestandtei ⁇ le at least one oil and / or at least one lipid.
  • the oil used is preferably jojoba oil, almond oil or sunflower oil.
  • oils conventionally used in topical formulations and in particular DMS formulations such as, for example, neutral oil, can likewise be used.
  • lipid lipids conventionally used in topical formulations and in particular DMS formulations can be used in the base composition according to the invention. Examples include: phytosterols phytosterols (eg in Shea Butter), ceramide III and squalane.
  • the basic composition according to the invention may comprise further auxiliaries which are conventionally used in topical formulations and in particular DMS formulations. ⁇ to these excipients in the aqueous phase or the oil phase depending on the water solubility formulated.
  • fatty acids and fatty acid esters may be mentioned.
  • the at least one oil phase can be prepared in a conventionally known manner.
  • the at least one oil phase is prepared by combining the corresponding ingredients, mixing and heating. The ingredients are added to a container such as a reaction flask and mixed in a conventional manner (eg manually with a rod or preferably with a stirrer). Subsequently, the mixture is preferably heated to 60 ° C. to 120 ° C., preferably 90 ° C. to 110 ° C.
  • the at least one oil phase should be mixed and heated until a clear or milky liquid is present.
  • all components of the oil phase are mixed together to form a single oil phase.
  • a part of the components of the oil phase for example emulsifier, oil and lipids, are mixed together to ei ⁇ ner oil phase and another part of the components of Oil phase, for example, additives such as fatty acids and Fett Text ⁇ ester, mixed together to form another oil phase.
  • the two oil phases are then added sequentially to the aqueous phase, wherein preferably the oil phase with emulsifier of the aqueous phase is added first.
  • separately prepared phases are mixed together sequentially or in one step and subjected to the inventive ultrasound treatment after each mixing.
  • the respective phases are combined in the desired order and subjected to the inventive ultrasound treatment after each mixing.
  • the ultrasonic treatment is to be carried out at a temperature in the range of 35 ° C to 85 ° C, preferably in the range of 50 ° C to 85 ° C, more preferably in the range of 35 ° C to 75 ° C is it optionally erforder ⁇ Lich, the cool down phase at least one oil to this temperature range, before it is combined with the aqueous phase.
  • a preferred base composition of the present invention contains from 0.1 to 2.5% by weight, preferably from 0.1 to 2% by weight, more preferably from 0.1 to 1.6% by weight, most preferably from 0.2 to 1 4% by weight of at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester; 10 to 30% by weight of an oil; 5 to 15 wt .-% of at least one humectant, 1 to 10 wt .-% of at least one lipid, 0 to 15 wt .-% of at least one additive, and 83.9 to 27.5 wt .-% water, wherein all percentages are based on the weight of the base composition and the sum of all components is 100%.
  • a particularly preferred base composition of the present invention contains from 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, most preferably 0.2 to 1.4 % By weight, phosphate diylcholine; 10 to 30% by weight of an oil; From 5 to 15% by weight of at least one humectant, from 1 to 10% by weight of at least one lipid, from 0 to 15% by weight of at least one additive, and from 83.9 to 27.5% by weight of water, all of them Percentages based on the weight of the base composition and the sum of all components is 100%.
  • Another particularly preferred base composition of the ahead ⁇ invention contains 0.1 to 2.5 wt .-%, preferably 0.1 to 2 wt .-%, more preferably 0 0.1 to 1.6 wt .-%, particularly preferably 0.2 to 1.4% by weight, sucrose fatty acid ester; 10 to 30% by weight of an oil; 5 to 15 wt .-% of at least one Feuchthal ⁇ testoffs, 1 to 10 wt .-% of at least one lipid, 0 to 15 wt .-% of at least one additive, and 83.9 to 27.5 wt .-% water, wherein all percentages are based on the weight of the base composition and the sum of all components is 100%.
  • the topical formulation is subsequently prepared by combining the base composition prepared by ultrasound treatment with at least one dermatologically or cosmetically or pharmacologically active substance and mixing the components.
  • the dermato- logically or cosmetically active substance selected from the group consisting of water-soluble active substance extracts, oil-based active substance extracts, medicinal herbs, powdered active ingredients, and active ingredient solutions.
  • Examples which may be mentioned are: 12-hydroxystearin and 11-hydroxypalmitic acid, castor oil, hydrogenated castor oil, octyl dodecyl ricinoleic acid, octyl 12-hydroxy-stearate,
  • vitamins and provitamins in particular A, B complex, C, E, D and their usual derivatives such as vitamin A acid, vitamin A acetate, vitamin A palmitate, vitamin C palmitate, vitamin E acetate, palmitate and linoleate, alfacalcidol, calcitriol, colecalciferol, ergocalciferol, transcalcifediol, calciprotriol, calcifediol, vitamin D3, beta-carotene, or panthenol, pantothenic acid, biotin).
  • vitamins and provitamins in particular A, B complex, C, E, D and their usual derivatives such as vitamin A acid, vitamin A acetate, vitamin A palmitate, vitamin C palmitate, vitamin E acetate, palmitate and linoleate, alfacalcidol, calcitriol, colecalciferol, ergocalciferol, transcalcifediol, calciprotriol, calcifediol
  • the pharmacologically active substance a pain medication or blood, preferably autologous blood, his.
  • the pharmacologically active substance a pain medication or blood, preferably autologous blood, his.
  • ⁇ materials include: local anesthetics (eg, lidocaine, benzocaine, buttocks lidocanol, isoprenaline, crotamiton, quinisocaine) HI antihistamines (eg meclizine, cetirizine, promethazine, Terfena- din), antifungals (eg.
  • aloe vera extract green tea extract, Algenex- extract, Echinacea extract, arnica extract, cucumber extract, Hopfenex gas tract, carrot extract, Kleieex Audit, Hamamelisex tract, He ⁇ fairy extract, gingko biloba extract
  • vegetable oils with specific effects eg. As rosemary oil, camomile oil, sage oil, calendula oil, lavender oil, St. John's wort oil, melissa oil, Sanddomöl, tea tree oil, cedar oil, cypress oil
  • accessible stabilizing acids eg. B. linoleic acid, 12-hydroxystearic acid, stearic acid, Isoste ⁇ arinkladonic acid, 11-hydroxypalmitic
  • the active ingredients include mutatis mutandis, covering substances and pigments such.
  • All active ingredients can be used alone or in a correspondingly meaningful combination in the formulations according to the invention. be hold. If it should be necessary to adjust the pH of the formulation due to the presence of specific active ingredients, this can be done by means of suitable bases such as sodium hydroxide, potassium hydroxide, trometamol, arginine or lysine.
  • suitable bases such as sodium hydroxide, potassium hydroxide, trometamol, arginine or lysine.
  • the present invention therefore also relates to a topical formulation obtainable by the process according to the invention described above, comprising
  • the amount of the at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester, preferably hydrogenated phosphate diylcholine oriser, in the topical formulation is preferably 0.3 to 2.5% by weight, preferably 0.1 to 2 wt .-% before ⁇ ferred 0.1 to 1.6 wt .-%, more preferably 0.2 to 1.4 wt .-%, particularly preferably 0.4 to 0.7 wt .-%, based on the Weight of the topical formulation.
  • the amount of oil, preferably selected from the group best ⁇ starting from jojoba oil, almond oil, and sunflower oil, in the topi ⁇ rule formulation is preferably 10 to 25 wt .-%, particularly preferably 15 to 25 wt .-%, based on the weight to ⁇ European formulation.
  • the amount of lipid, preferably selected from the group ⁇ be detached from shea butter, Ceramide III B or squalane, in the topical formulation is preferably 1 to 5 wt .-%, particularly preferably 1.5 to 4 wt .-%, based on the weight of to ⁇ European formulation.
  • the amount of moisturizing substance, preferably selected from the group consisting of glycerol and glycols such as Pentylengly- glycol, in the topical formulation is preferably 7 to 12 wt .-%, particularly preferably 8 to 10 wt .-%, based on the weight Ge ⁇ the topical formulation.
  • the amount of the at least one optional additive, before ⁇ preferably selected from the group consisting of fatty acids and Fettchureestern is preferably 1 to 9 wt .-%, particularly preferably 2 to 8 wt .-%, based on the weight of the topical formulation.
  • the amount of at least one dermatologically or cosmetically or pharmacologically active substance in the topical formulation is preferably 3 to 8% by weight, more preferably 4 to 7% by weight, based on the weight of the topical formulation.
  • the inventive formulation may further contain one or more additives such as are commonly used in topical Formulie ⁇ approximations used.
  • additives such as are commonly used in topical Formulie ⁇ approximations used.
  • fillers, pigments or pH-modifying agents may be mentioned.
  • these additives are used in a total amount of 0.1 to 5% by weight, preferably 1 to 3% by weight, based on the weight of the topical formulation.
  • the remaining amount of the topical formulation up to 100% by weight consists of water.
  • the creams are suitable for dermatological, cosmetic or me ⁇ dizinische applications. They are particularly suitable for the medi ⁇ ical cosmetics, as they form must contain no allergy potential, no preservatives, no synthetic ingredients or no Farbstof ⁇ fe according to a preferred execution. Disorders of the skin barrier can be repaired immediately by applying the formulation according to the invention to the skin. Inflammation decreases, and as a result, environmental allergens are no longer able to penetrate the skin. In addition, the moisture content of the skin can no longer escape ⁇ uncontrollably. This improved skin moisture content is generated, which is manifested in a marmeidi ⁇ Geren complexion and good skin feel.
  • inventive formulation can be provided in the usual topical Pro ⁇ -products dosage forms. Examples include ointments, creams, lotions and gels. Derar- term formulations are known in the art and need not be further described here.
  • the topical formulation according to the invention can be applied by simple application to the skin.
  • the quantities to be applied and the application intervals depend on the type and amount of active ingredient.
  • Example 1 Preparation of a base composition based on phosphatidylcholine with ultrasound treatment
  • An aqueous phase according to Table 1 was prepared by mixing the components and heating to 75-80 ° C.
  • Aqueous phase (% by weight based on the total aqueous phase)
  • a first oil phase according to Table 2 was prepared by mixing the components and heating to 100-110 ° C.
  • Oil phase I (wt .-% based on total oil phase I)
  • a second oil phase according to Table 3 was prepared by mixing the components and heating to 70-75 ° C Table 3
  • Oil phase II (wt .-% based on total oil phase II)
  • Joj oba oil 0-10% by weight
  • a base composition of a 1: 1: 1 mixture of the three above phases was prepared as follows. First, the heated above aqueous phase and the like vorste ⁇ starting heated oil phase I were added together and at a temperature of 60-85 ° C with an ultrasonic instrument from Hielscher
  • the above heated oil phase II ⁇ be supplied, and it was (UP200ST) homogenised at a temperature of 60-85 ° C with an ultrasonic instrument from Hielscher with an energy input from 350 to 390 Ws / g.
  • a base composition was prepared analogously as described above in Example 1 with the difference that the homogenization was carried out as follows.
  • Comparative Example 2 Preparation of a phosphatidylcholine-based base composition with high-pressure homogenization
  • a base composition was prepared analogously as described above in Example 1 with the difference that the homogenization was carried out as follows.
  • composition was homogenized in a known manner at 960 bar and 90 ° C. After cooling, no homogeneously crystallizable Cre ⁇ me. Even after two times high-pressure homogenization under the above conditions, nothing changed in this result.
  • a base composition according to Example 1 was mixed with water and a mixture of various cosmetic active ingredients at 30 to 40 ° C. It could be obtained without problems a night cream with the composition given in Table 4.
  • a base composition according to Example 1 was mixed with water and a mixture of various cosmetic active ingredients at 30 to 40 ° C. It could be easily obtained a very flowable lotion with the composition shown in Table 5.
  • An aqueous phase according to Table 1 was prepared by mixing the components and heating to 75-80 ° C.
  • a base composition of a 1: 1: 1 mixture of the three above phases was prepared as follows. First, the heated above aqueous phase and the like vorste ⁇ starting heated oil phase I were added together and at a temperature from 60-85 ° C with an ultrasonic device from Hielscher
  • a base composition was prepared analogously as described above in Example 4 with the difference that the homogenization was carried out as follows.
  • a base composition was prepared analogously as described above in Example 4 with the difference that the homogenization was carried out as follows. First, the above-heated aqueous phase and the above-heated oil phases I and II were combined and stirred for 3 minutes. homogenized at 20000 rpm with a conventional rotor-stator homogenizer (instrument type: WiseT HG-15A; dispersing tool type: DH.WHG02015).
  • composition was homogenized in a known manner at 960 bar and 80 ° C.

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Abstract

La présente invention concerne un procédé de préparation d'une formulation topique, la formulation cosmétique comprenant une composition de base et au moins une substance dermatologiquement, cosmétiquement ou pharmacologiquement active. L'invention est caractérisée en ce que la composition de base est soumise à un traitement par ultrasons après la réunion de tous les composants. La présente invention concerne en outre des formulations topiques obtenues par ce procédé.
PCT/EP2018/077029 2017-11-06 2018-10-04 Procédé de préparation de formulations topiques au moyen d'ultrasons et formulations obtenues par ce procédé Ceased WO2019086195A1 (fr)

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CH01332/17A CH714305B1 (de) 2017-11-06 2017-11-06 Verfahren zur Herstellung von topischen Formulierungen und hergestellte Formulierungen.

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113967175A (zh) * 2020-07-24 2022-01-25 株式会社爱茉莉太平洋 片型面膜凝胶组合物、包含其的面膜片及面膜片制备方法

Citations (8)

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Publication number Priority date Publication date Assignee Title
DE69112849T2 (de) 1990-02-23 1996-11-07 Nattermann A & Cie Wässrige phospholipidvesikeldispersion, verfahren zu deren herstellung sowie deren verwendung.
DE19857492A1 (de) 1998-12-14 2000-06-15 Hans Lautenschlaeger Wasserhaltige Hautschutzpräparate zur Prävention von Hautschäden
WO2008155389A2 (fr) * 2007-06-19 2008-12-24 Neubourg Skin Care Gmbh & Co. Kg Dms employées dans des crèmes se présentant sous forme de mousses
EP2301523A1 (fr) * 2009-09-22 2011-03-30 Dr. August Wolff GmbH & Co. KG Arzneimittel Formule galénique de forme colloïdale
DE102011110749A1 (de) 2011-08-16 2013-02-21 Gabriele Blume Kosmetische oder pharmazeutische Zusammensetzung mit lamellaren Strukturen unter Verwendung von Sucrose-fettsäure-Triestern - einfache und leichte Herstellung
EP2823803A1 (fr) * 2013-07-12 2015-01-14 L'Oréal Composition changeant de couleur en émulsion O/W sous forme d'oléosomes
CH711598A2 (de) 2015-10-16 2017-04-28 Swiss Cream Cosmetics Scc Gmbh Verfahren zur Herstellung von dermatologischen und kosmetischen Präparaten mit ausgeprägten lamellaren Strukturen unter Verwendung von Phosphatidylcholin und Fermentation durch Mikroorganismen.
WO2018069814A1 (fr) * 2016-10-11 2018-04-19 MAUSER, Johannes, Alois Procédé de fabrication de préparations dermatologiques et cosmétiques

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69112849T2 (de) 1990-02-23 1996-11-07 Nattermann A & Cie Wässrige phospholipidvesikeldispersion, verfahren zu deren herstellung sowie deren verwendung.
DE19857492A1 (de) 1998-12-14 2000-06-15 Hans Lautenschlaeger Wasserhaltige Hautschutzpräparate zur Prävention von Hautschäden
WO2008155389A2 (fr) * 2007-06-19 2008-12-24 Neubourg Skin Care Gmbh & Co. Kg Dms employées dans des crèmes se présentant sous forme de mousses
EP2301523A1 (fr) * 2009-09-22 2011-03-30 Dr. August Wolff GmbH & Co. KG Arzneimittel Formule galénique de forme colloïdale
DE102011110749A1 (de) 2011-08-16 2013-02-21 Gabriele Blume Kosmetische oder pharmazeutische Zusammensetzung mit lamellaren Strukturen unter Verwendung von Sucrose-fettsäure-Triestern - einfache und leichte Herstellung
WO2013023641A2 (fr) 2011-08-16 2013-02-21 Gabriele Blume Procédé pour produire une composition à appliquer sur la peau
EP2823803A1 (fr) * 2013-07-12 2015-01-14 L'Oréal Composition changeant de couleur en émulsion O/W sous forme d'oléosomes
CH711598A2 (de) 2015-10-16 2017-04-28 Swiss Cream Cosmetics Scc Gmbh Verfahren zur Herstellung von dermatologischen und kosmetischen Präparaten mit ausgeprägten lamellaren Strukturen unter Verwendung von Phosphatidylcholin und Fermentation durch Mikroorganismen.
WO2018069814A1 (fr) * 2016-10-11 2018-04-19 MAUSER, Johannes, Alois Procédé de fabrication de préparations dermatologiques et cosmétiques

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113967175A (zh) * 2020-07-24 2022-01-25 株式会社爱茉莉太平洋 片型面膜凝胶组合物、包含其的面膜片及面膜片制备方法

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