CN1331587A - Spray-type consmetic compsn. and matrix used in said compsn. for dermal administration - Google Patents
Spray-type consmetic compsn. and matrix used in said compsn. for dermal administration Download PDFInfo
- Publication number
- CN1331587A CN1331587A CN99814967A CN99814967A CN1331587A CN 1331587 A CN1331587 A CN 1331587A CN 99814967 A CN99814967 A CN 99814967A CN 99814967 A CN99814967 A CN 99814967A CN 1331587 A CN1331587 A CN 1331587A
- Authority
- CN
- China
- Prior art keywords
- compositions
- active substance
- octyl nitrite
- acid
- absorption enhancer
- 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.)
- Pending
Links
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 58
- 239000013543 active substance Substances 0.000 claims description 50
- 239000002904 solvent Substances 0.000 claims description 42
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 39
- -1 aliphatic fatty acid ester Chemical class 0.000 claims description 36
- 238000010521 absorption reaction Methods 0.000 claims description 34
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- 239000001856 Ethyl cellulose Substances 0.000 claims description 31
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 31
- 239000000758 substrate Substances 0.000 claims description 29
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- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical group ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 9
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 9
- OBETXYAYXDNJHR-UHFFFAOYSA-N alpha-ethylcaproic acid Natural products CCCCC(CC)C(O)=O OBETXYAYXDNJHR-UHFFFAOYSA-N 0.000 claims description 9
- 238000001704 evaporation Methods 0.000 claims description 9
- 239000000284 extract Substances 0.000 claims description 9
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 claims description 8
- 238000009835 boiling Methods 0.000 claims description 8
- MWKFXSUHUHTGQN-UHFFFAOYSA-N decan-1-ol Chemical compound CCCCCCCCCCO MWKFXSUHUHTGQN-UHFFFAOYSA-N 0.000 claims description 8
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- 239000001273 butane Substances 0.000 claims description 5
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- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 claims description 5
- FRPZMMHWLSIFAZ-UHFFFAOYSA-N 10-undecenoic acid Chemical compound OC(=O)CCCCCCCCC=C FRPZMMHWLSIFAZ-UHFFFAOYSA-N 0.000 claims description 4
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 4
- CMBYOWLFQAFZCP-UHFFFAOYSA-N Hexyl dodecanoate Chemical compound CCCCCCCCCCCC(=O)OCCCCCC CMBYOWLFQAFZCP-UHFFFAOYSA-N 0.000 claims description 4
- 125000004423 acyloxy group Chemical group 0.000 claims description 4
- KHAVLLBUVKBTBG-UHFFFAOYSA-N caproleic acid Natural products OC(=O)CCCCCCCC=C KHAVLLBUVKBTBG-UHFFFAOYSA-N 0.000 claims description 4
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- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
-
- 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
- A61K35/66—Microorganisms or materials therefrom
- A61K35/74—Bacteria
-
- 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
- A61K35/66—Microorganisms or materials therefrom
- A61K35/74—Bacteria
- A61K35/741—Probiotics
- A61K35/742—Spore-forming bacteria, e.g. Bacillus coagulans, Bacillus subtilis, clostridium or Lactobacillus sporogenes
-
- 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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/99—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from microorganisms other than algae or fungi, e.g. protozoa or bacteria
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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Abstract
The invention concerns a novel composition for dermal administration of a substance or of an active principle. More precisely, the invention concerns a slimming composition for dermal administration, capable of forming a soft film after drying on the skin and a matrix capable of being used in said composition.
Description
The present invention relates to the dermal administration compositions of new active substance or active component.Said composition can be a cosmetic composition, such as Weight reducing compound.
Term " active component " and " active substance " are meant one or more medical or non-medicinal active compositions.Therefore, it can be, such as peptide or non-peptide compound, the cell or tissue extract of animal or plant raw material, or see through the product that microorganism such as antibacterial or fungi fermentation obtain.So in present specification, according to above-mentioned given definition, term " active component " and " active substance " do not have difference in use.
More specifically, the present invention relates to the dermal administration compositions, it can form a flexible membrane after drying on the skin, also relates to spendable substrate in this compositions.
The dermal administration of active substance is a kind of excellent technique, has some advantage as having no side effect.
Yet, for effectively, this technology must be in long-time and penetrate to the skin in the mode of enough arrival designated cells and the required effect of acquisition in.
Up to now, multiple system that this type of is used or device are provided.They can produce the active substance of controlled doses.
For example, known transdermal delivery device is acknowledged as " patch ", and this device is made up of the bank that the synthetic plastic that contains active component constitutes.Can cover with perforated membrane on this bank, its surface and contact skin, this perforated membrane is regulated its diffusion to the permeability of active substance, regulates and control its dosage thus.
Though this device can provide definite probability, particularly for a kind of application, preferred other device.Because known patch may separate with skin, and often has indecency outward appearance.
The gel that contains active substance also is proposed.Yet this application mode has some shortcoming in practice, and common sticky sense can make its user discomfort, and the restive dosage of using.
Other help the system of active substance transdermal administration that report had been arranged already.
In this respect, especially can mention and contain and to spray compositions being touched on the skin the using of polymer that forms thin film and discharge active component through skin.This based composition for example is disclosed among the patent EP319555, contains: active component; Dry back forms the polymeric matrix of flexible film; The solvent that the control active substance discharges, just sorbitan polyethylene glycol laurate (Sorbitane macrogollaurate), paraffin, medium-chain fatty acid diglyceride or triglyceride or Allyl carbonate; With other substrate solvent, this solvent can evaporate on skin; And be to be contained in the propellant of the composition spray in the appropriate device at last.
In addition, because the existence of polymethacrylic acid derivant, the compositions of patent EP319555 produces distinctive abnormal smells from the patient, makes the user and stays quite unhappy abnormal smells from the patient on every side.
Other pharmaceutical compositions of topical that contain active component, solvent and multiple other components are also known.
For example, can mention disclosing the antifungal compositions among the patent EP55396 that it is made up of following:
Cellulose ether
The 2%-10% spreading agent is as isopropyl myristate or isopropyl palmitate
The 1%-8% solubilizing agent,
The 0.05%-1% active component and
Solvent is as isopropyl alcohol
Yet, though these compositionss can be used for the local skin coating, find that they are not suitable for spray application fully, even also like this later on according to being recommended in adding 10% to 40% propellant gas, because as if they are thickness and be easy to produce multiple shortcoming too, as blocking sprayer unit.
Also can mention disclose can film forming antifungal composition patent EP319964, contain:
0.1%-1.5% toluene phthalic acid ester (tolnaphtalate)
10%-20% dimethyl amino ethyl methacrylate/methacrylic acid copolymer
The 0.5%-10% fatty acid ester
The solvent of alcohols and the cellulose derivative of 0.1%-5% randomly.
As if this compositions be not suitable for spraying.In addition, mention above, the existence of methacrylic acid analog derivative produces a kind of unacceptable abnormal smells from the patient.
Be worth in addition mentioning the patent EP289900 that discloses antibacterial composition for topical, wherein contain:
0.5%-10% antibacterial activity composition,
1%-30% non-soluble polymer, particularly ethyl cellulose or polyvinylpyrrolidone copolymer,
The 0.5%-40% plasticizer generally is a quintessence oil, and it also plays the promoter effect that absorbs through skin,
The 50%-95% solvent is as ethanol.
At last, can mention patent application WO96/30000, its main purpose is the pharmaceutical composition of transdermal administration, contains:
1) can form the polymerization release matrix of flexible film after the drying,
2) active component,
3) promoter of active component percutaneous absorption,
4) physiology that can dissolve substrate, active component and the Percutaneous absorption enhancer of release can be accepted nonaqueous solvent, this solvent after the administration also can by with specify contact skin after evaporate and is removed rapidly, produce prevention or treatment responds.
The curable product that is specially adapted to this patent application is an estradiol.
Therefore, research still is that people pay close attention to through skin by a small amount of obducent zone and not have the compositions of above-mentioned defective with speed diffusion for the treatment of compatibility and while for making active substance.
At present, be surprisingly found out that, the present invention can provide the compositions of dermal administration by film forming on skin, cosmetic composition particularly, there is not above-mentioned defective in these compositionss, and the covering that can utilize little and controlled range to transmit evenly, continuously active substance, and speed can fully reach the probability that obtains Expected Results.
Therefore, an object of the present invention is the skin cosmetic compositions, contain:
1) can form the polymerization release matrix of flexible film after the drying,
2) one or more active substances,
3) promoter of active component Transdermal absorption,
4) can molten described release matrix, active component and Percutaneous absorption enhancer and nonaqueous solvent by being removed fast with the contact skin evaporation,
5) at least a propellant gas.
In this application, promptly in description and claims, term " predetermined substance " (Substance destin é e) is meant uses the material that the back produces prevention or treatment response, or the cooperative programs of two or more these type of materials.
Polymeric matrices generally is selected from the polymerization or the copolymer substance that can form flexible film and release of active agent after solvent evaporation.
This substrate is formed in horny layer (Stratum corn é um) after can the solvent evaporation of release of active agent.
This substrate generally exists with 0% to 7% ratio of present composition weight, and 4%-7% for example is as 3%.Preferred 1% to 5% weight that adopts substrate weight, particularly preferred 3% weight.
This choice of base relates generally to and dissolves in polymerization or the copolymer substance that the physiology acceptable solvent forms homogeneous solution thus.
In polymer that can satisfy above-mentioned standard or copolymer, those of special more selection are cellulosic polymer or copolymer, especially because they have suitable scouring intensity and mechanical stability after drying.Reason for this reason, this type of cellulose matrix can be placed with water and contact, and does not worry going bad.
As the cellulosic polymer or the copolymer example that can use at the present composition, can mention grafting or not grafted ethyl cellulose, cellulose acetate-butyrate, cellulose-acetate propionate or hydroxypropyl emthylcellulose, as HPMC-AS.
Yet ethyl cellulose is represented preferred cellulosic polymer, so the polymerization release matrix of selection forms softish thin film on contact skin.
In addition, polymeric matrices can be made up of vinylpyrrolidone/vinyl acetate co-polymer such as polyvinylpyrrolidone/vinyl acetate (hereinafter being called PVP/VA).
So, according to a further aspect, an object of the present invention is the cosmetic composition of dermal administration, contain:
1) the polymerization release matrix of flexible film be can form after the drying, cellulosic polymer or copolymer or vinyl pyrrolidone/vinyl acetate copolymer are selected from,
2) active substance,
3) promoter of active component Transdermal absorption,
4) can dissolve release matrix, active component and Percutaneous absorption enhancer and by contacting the nonaqueous solvent that evaporation is removed rapidly on the skin,
5) at least a propellant gas.
For active substance, it should be selected from these materials: be dissolved in the solvent and can see through continuously epidermis and/or corium simultaneously flow be enough to little and skin area generation valid density enough scopes.
These active substances should be blended in the compositions of the present invention with certain proportion, particularly 0.1% of these composition weights to 20%, should understand each active substance and should introduce with the concentration that affiliated field become known for the independent concentration of dermal administration or be fit to this route of administration.
For the valid density that obtains active component but do not cover excessive skin area, Percutaneous absorption enhancer combines with polymeric matrices and active component.This promoter suitable with said composition weight 15% to 30%, preferred 15% to 25%, mixed as 20% is in compositions of the present invention.
This absorption enhancer is chosen as and can produces big skin flow, and purpose is to obtain Expected Results by the mode that can accept the skin covering, promptly covers less than 150cm
2And preferably at 10-40cm
2Between, as 30cm
2
For effectively, the skin absorption promoter that is considered must be destroyed skin barrier moment and improve the permeability of skin and chafe not thus, and promote diffusion according to the selected active component of kinetics simultaneously, and concentration enough acts on and can keep the regular hour.
Described skin absorption promoter should be selected from and can contact the compatible material of nonaqueous solvent that evaporates rapidly on the skin.Preferred being listed in down has required dissolubility and in conjunction with above-mentioned chemical compound best in quality, that is to say in the physiology solvent that is considered:
The aliphatic series fatty acid ester, especially contain the total carbon atom of 10-30 randomly by one or two hydroxyl, carboxyl or C
1-C
4The ester that acyloxy such as acetoxyl group replace, or randomly by one or two ethylene linkage or the isolated ester of one or two ether oxygen;
The aliphatic series aliphatic alcohol is especially randomly by one or two hydroxyl, carboxyl or C
1-C
4Acyloxy such as acetoxyl group replace, or randomly by one or two ethylene linkage or by the isolated C of one or two ether oxygen
10-C
30Alcohol.
The particularly preferred absorption enhancer that can be selected from above-mentioned aliphatic fatty acid ester and aliphatic aliphatic alcohol is as described below:
A) the aliphatic fatty acid ester of following general formula:
Wherein R represents randomly by hydroxyl, carboxyl or C
1-C
4The straight or branched C that acyloxy replaces
2-C
7Alkyl or alkenyl, and R
1The straight or branched C that expression is randomly replaced by one or two hydroxyl
3-C
8Alkyl, as isopropyl, 2-ethyl dihydroxy ethyl or R
1Expression-CH
2-CH
2-O-(CH
2)
2-O-CH
2-CH
3, this aliphatic series fatty acid ester contains at least 10 carbon atoms and 2 hydroxyls at the most;
B) the aliphatic fatty acid alcohol of following general formula:
R
2-OH????II
R wherein
2Expression C
10-C
20Alkyl.
As the specific compound of the most effective promotion active substance Transdermal absorption, can mention:
2 ethyl hexanoic acid 2-Octyl Nitrite
Isopropyl myristate
The carbiphene myristinate
Isopropyl palmitate
2-octyl group decanol
9-undecylenic acid 2-Octyl Nitrite
Succinic acid 2-Octyl Nitrite
12-hydroxy stearic acid 2-Octyl Nitrite
12-acetoxyl group stearic acid 2-Octyl Nitrite
Iso stearic acid of glycerine ester
Lauric acid hexyl ester
Isononyl isononanoate
Palmic acid 2-Octyl Nitrite
Stearic acid 2-Octyl Nitrite
Carbiphene
2 ethyl hexanoic acid 2-Octyl Nitrite is preferred absorption enhancer, particularly for cosmetic composition of the present invention.This chemical compound is with Dragoxat
Trade name sell and be also referred to as octyl octanoate.
Because nonaqueous solvent can dissolve release matrix, active component and Percutaneous absorption enhancer, it is selected from the lower chemical compound of boiling point, that is to say that boiling point is lower than 100 ℃ under the normal pressure, can be removed rapidly by on contact skin, evaporating thus, and help equally to form thin film, and do not cause any local excitation by drying.
This kind solvent generally is to use with the ratio of the 44%-84.9% of final composition weight, and can be selected from volatile compound, as dichloromethane, ethanol, isopropyl alcohol or ethyl acetate.
Ethanol and isopropyl alcohol are selective solvents.Yet ethanol is the preferred solvent of the present invention, because it effectively forms thin film on skin, can evaporate rapidly when contacting skin simultaneously.
The spendable propellant gas of the present invention is selected from:
Butane
Propane
Iso-butane
Carbon dioxide
Dimethyl ether
The chlorine fluorohydrocarbon
Fluorohydrocarbon
Nitrogen
Isopentane
Nitrogen oxide
Pentane
Preferred butane or propane.
So, according to a particular aspects, the present invention relates to a kind of cosmetic composition, wherein contain:
1) the polymerization release matrix of flexible film be can form after the 0%-7% drying, cellulosic polymer or copolymer are selected from especially, as ethyl cellulose,
2) 0.1%-20% active substance,
3) fatty acid ester of the promoter of 15%-30% active component Transdermal absorption, particularly 15%-25% or aliphatic alcohol are selected from:
2 ethyl hexanoic acid 2-Octyl Nitrite
Isopropyl myristate
The carbiphene myristinate
Isopropyl palmitate
2-octyl group decanol
9-undecylenic acid 2-Octyl Nitrite
Succinic acid 2-Octyl Nitrite
12-hydroxy stearic acid 2-Octyl Nitrite
12-acetoxyl group stearic acid 2-Octyl Nitrite
Iso stearic acid of glycerine ester
Lauric acid hexyl ester
4) 44%-84.9% can dissolve the nonaqueous solvent of described release matrix, active component and Percutaneous absorption enhancer, and this solvent also can be removed rapidly by evaporating on contact skin, particularly ethanol or isopropyl alcohol;
5) at least a propellant gas.
In scope of the present invention, studied by the sprayed compositions that is coated in the metering spray device bottle on the skin its satisfactory and its area of application and dose characteristics is controlled and can reappear on cosmetics especially.
So on skin, form " thin film ".Therefore, active substance can be coated on the skin with the form of thin film according to the present invention.
The bio-compatible preparation for preparing some promotion transdermal penetrations.
Used active substance can be used for preparing the thin film of expection, as being the thin film of purpose with the fat-reducing.
Particularly, thin film of the present invention relates to the cosmetic composition that contains the material of losing weight.This fat-reducing material can be a neuropeptide Y receptor antagonist.Neuropeptide tyrosine (after this be called for short do " NPY ") is to participate in the neurotransmitter that some plants physiological process, and verified its relates to be regulated lipolysis (P.Valet. " Journal of Clinical Investigation " (J.C1in.Invest.) 1990,85,291-295).
Disclose the NPY-antagonist among the EP838217 and can be used for preparing cosmetic composition.
These cosmetic compositions that contain NPY-antagonist composition can be used as the steatolysis/lipogenesis regulator on the skin, but do not disturb the natural function of skin.
The fat-reducing cosmetic composition of the disclosed in addition NPY-of containing antagonist composition and α 2-antagonist composition is suitable especially.
Therefore, according to an aspect, the present invention relates to a kind of thin film that contains the cosmetic composition of losing weight, said composition contains at least a NPY-antagonist composition and another kind of active substance such as α 2-antagonist.The NPY-antagonist that is contained in this cosmetic composition can be the cell or tissue extract in non-peptide compound, peptide, animal or plant source, or the product of fermentative microorganism such as antibacterial or fungus acquisition.
These compositions itself are non-peptide synthetic compound, peptide or the product that obtains by fermentative microorganism such as antibacterial or fungus, or the product that obtains by the cell or tissue that extracts the animal or plant raw material.
Obviously, sedimentary thin film need tolerate well, but also must have pleasant beauty treatment outward appearance, not residual any residue on skin surface in the evaporation rapidly at carrier.
Be coated in the preparation that becomes thin film on the skin conduct and learning evaluation of making up to a series of.
Particularly, purpose is the qualitative whole cosmetic conduct and learning characteristics that go out can spray solution of mode by organoleptic analysis's research.
Whether pleasant this be one and identify sense organ research (scheme of enforcement and the type of calculating meet the corresponding AFNOR standard of agricultural food product department establishment) according to 6 standards.
These standards are as follows:
Be easy to infiltration: absorb and evaporation,
Residue: greasy/dry (on deposit film slide assess sensation by forefinger)
Gloss (existence of visible residue)
Viscosity (by the sensation that obtains with the light button of forefinger)
Overall assessment to product: only consider above-mentioned standard.
Coating method is as described below:
Start atomizing pump by pushing some this, preparation is sprayed at measures distance on the skin of 10cm.Apply and began in back 10 minutes to observe, carry out standardization by organoleptic analysis's scheme during this period.
Once spraying is equivalent to the preparation of 130 μ l is sprayed at about 35-40cm
2The zone on.
Used excipient is as described below:
Film former: ethyl cellulose 99 N7NF (7mpa.s:Aqualon)
Solvent: isopropyl alcohol (SDS), ethanol (Labover),
Promoter and structural agent (agent de texture): Dragoxat
E.H. (the permeability cosmetics oil: Dragoco), Dow Corning 556 polysiloxanes, liquid paraffin,light (Sanofi Winthrop Gentilly).
Used spraying system is as described below:
VP7/130 pump: Valois
Push button allotter IN3 GP4/5:Valois
20ml ONC paints aluminium pot.
Preparation contains:
66%-67% solvent: the cooperative programs of ethanol, isopropyl alcohol or two kinds.
20%-30% promoter: Dragoxat
E.H.
The 3%-5% ethyl cellulose
The disclosed preparation of WO98/30000 can be used as reference and is called (R) hereinafter, and said preparation is the theme of research, uses estradiol as medicament.
The details of compositions is as described in the Table A.
All bioassay standards and be under+3 to-4 grade, to evaluate with (statistical) rectangular histogram to the net assessment of each preparation.
The meansigma methods that is obtained by 10 tests is attended by high value and low value.
Can influence or improve that cosmetic is apparent comes the detailed assessment preparation with respect to reference preparation (R) to it by the change that confirms compositions.
Table B has summarized the main explanation of relevant multiple excipient to reference preparation.
Be limited to the sensation (greasy is low, and cohesiveness is low and residual few) that 3% (A) improves reference preparation (R) by amount with ethyl cellulose.The sprayability of the pump of use device by the better dispersive mode of said preparation obtained to improve.When the ethyl cellulose amount is 3%, even can be with the Dragoxat that adds
Bring up to 30%, keep the very good sensation of spray agent simultaneously.
The preparation that grade follows closely after (E) has slightly a large amount of residues.It still contains 3% ethyl cellulose, but solvent contains the isopropyl alcohol of some difficult spraying.The area of application must be less than the solution of equal volume, and residue must stiff on skin thus.The preparation of finding least pleasant (B, R, F and G) all contains 4 to 5% ethyl cellulose, because their too greasy or adhesions.The result is identical with employing ethanol or isopropyl alcohol.Do not observe improve to some extent (F and G) by adding 1% the chemical compound that is described to optimize spraying (polysiloxanes or liquid paraffin).Preparation (D) produces very dispersive result.It contains 4% ethyl cellulose and 30%Dragoxat
Solution is not easy to spraying.
Use ethanol on the whole or isopropyl alcohol is equal to.
The greasy slightly and adhesion of reference preparation.Only need the amount of ethyl cellulose is limited to 0.5-3%, just can improve the result greatly and the result is satisfactory.
Residue from less to considerably less, quite glossy thus but non-greasy, and be difficult to adhesion fully.
Infiltration is by enough reaching very fast soon.
More especially, according to the present invention, developed the thin film formulations that contains the activating agent of losing weight.
These fat-reducing activating agents are neuropeptide tyrosine (NPY) receptor antagonist or α 2-receptor antagonist preferably.These type of a large amount of activating agents are described among the patent application EP838217.
In cosmetology and also aspect fat-reducing, the Transdermal absorption of active component is similar to passive diffusion, and conditioning step is to pass the cuticular time, and its impermeability is higher 1000 times than epidermis or corium.
One of desired main advantages of thin film of the present invention is to remove this transdermal resistance to diffusion.The enhancing of Transdermal absorption will cause moistening and the raising horny layer temperature, provide semi-closed with rear film for the coating site.
The Expected Results of fat-reducing thin film relates generally to and is characterized as the body area that has intractable loose connective tissue inflammation (cellulite).
For the site that these loose connective tissue inflammation (cellulite) have firmly been set up, must before fall by fat cell natural metabolism, they upgrade and keep the effect of active substance.
Utilize active substance, thin film technique can produce the bank effect on horny layer, by this bank effect realize activating agent evenly and continuous diffusion to the lower floor of skin.Because this seriality diffusion guarantees to exist for a long time activating agent in the zone of fat cell.
This makes the storage receptor saturated all the time, can effectively reduce the alligator effect that exists in the scorching zone of intractable loose connective tissue thus.
The advantage aspect of thin film at first is to be produced by the matrix structure that contains active substance, and second is produced by its coating system.
Because it can be sprayed on the skin by preparation, thin film forms thin and soft and invisible thin film, and film diffusion goes out active substance thus.
Film forming low thickness can not hinder the gas that exists between skin and the external environment and the exchange of moisture, and the toleration of product further is provided thus.The flexibility of thin film also provides comfort preferably.
For active substance, thin film contains NPY antagonist and α 2 antagonist activities agent, and disclosed conventional liq keeps concentration high 10 times among concentration ratio such as the EP838217.
Therefore, because its bioavailability is subjected to dual control in time by the continuous diffusion mode of active substance, with localize by the mode that makes active strictness be limited in spraying position, thin film can provide effective and long saturation to fat cell storage receptor by npy receptor antagonist and alpha-2 receptor antagonist, and the zone that habitual opposing fat-reducing is handled reduces.
Percutaneous drug delivery compositions of the present invention can be in the usual way, by the known mode of one of ordinary skill in the art, by various ingredients is prepared according to selected mixed together.
For example, can under agitation Percutaneous absorption enhancer be dissolved in the solvent, add active component subsequently and add release matrix at last.
The all substances that constitute present composition part are that known product maybe can prepare by known method, and some these products are commercially available.
Thus obtained skin composition of the present invention can be coated in the skin area by any way, utilizes 10-40cm
2Scope in, as 30cm
2, particularly and preferably utilize a kind of known and dosing pump that sell directly to spray, spraying by means of propellant as compression or liquid gas.
Though prior art is made opposite asserting, wonderful discovery: adopt said composition, the release matrix that is formed by ethyl cellulose can not cause any because of blocking that obstruction fog-spray nozzle jet expansion causes, therefore compositions of the present invention can be sprayed in the presence of propellant gas, and need not to worry degenerating of any automiser spray.
Therefore compositions of the present invention can utilize the container that is equipped with metering valve to use by spraying, and this container contains the low oxide of excessive propellant gas such as nitrogen or nitrogen, or liquid gas such as butane or propane.
According to another purpose, the present invention relates to be suitable for the substrate of the cosmetic composition of dermal administration, this substrate contains:
A) be used for the polymeric matrices of release of active ingredients, can form flexible film after its drying,
B) promoter of active component Transdermal absorption,
C) can dissolve release matrix and Percutaneous absorption enhancer and also by contacting the nonaqueous solvent that evaporation is removed rapidly on the skin,
D) propellant gas.
Polymeric matrices should be selected from polymerization and copolymer substance, particularly is selected from cellulosic polymer or copolymer as defined above, and Percutaneous absorption enhancer should be selected from the alcohols of aforesaid aliphatic fatty acid ester or aliphatic aliphatic alcohol, the particularly esters of formula I or formula II simultaneously.
For nonaqueous solvent, it is that boiling point is lower than 100 ℃ chemical compound under a kind of normal pressure, as mentioned above.
The heterogeneity of the substrate of these suitable skin cosmetic compositionss should be dispensed in the relevant cosmetic composition that contains active component, this release matrix accounts for 0%-7%, Percutaneous absorption enhancer accounts for 15%-30% and nonaqueous solvent accounts for 44%-84.9%, and these percentage ratios are the weight in final cosmetic composition.
The substrate of these suitable skin compositions of the present invention can prepare various ingredients according to selected mixed by conventional method together.
Propellant gas is preferably selected from propanol and butanols.
The substrate of film-forming composition of the present invention and skin composition of the present invention has impeccable superiority, because they can cause the transdermal diffusion of active substance, thereby by about 10-40cm
2Skin coverage constant and controlled effect level of generation at least 12 hours long-time.
In addition, there is not any undesirable abnormal smells from the patient in the substrate of compositions of the present invention and skin composition, can be coated on and form homogeneous film in the whole zone of selecting skin.
These thin film are enough soft and wear-resisting, avoid the deterioration of any user skin thus and have better toleration with device than known skin, this is owing to its thin thickness, and owing to do not have any covering, so not have gas and exchange of moisture between obstruction and the external environment.
At last, the compositions of flexible film form of taking of the present invention provides bigger comfort for user, and transparent invisible fully because of it.
Carry out multiple external and in vivo test and confirm the feature and the characteristic of the present composition.
Cosmetic composition of the present invention preferably contains the fat-reducing active substance.
The fat-reducing active substance is preferably selected from NPY or alpha-2 receptor antagonist.
Under these circumstances, used active substance for example is: the extract of streptomyces bacterial strain SEBR2794 (C.N.C.M. that must learn (Institut Pasteur) at Bath is with numbering I-1332 preservation), and bacillus licheniformis (Bacillus licheniformis) bacterial strain SEBR 2464 (C.N.C.M. that must learn at Bath is with numbering I-1778 preservation).They will be known as the fat-reducing active substance hereinafter.
Clinical effectiveness research adopts the Weight reducing compound that contains NYP and alpha-2 receptor antagonist to carry out.The purpose of this research is to estimate and Lipofactor
The effect of the thin film that fluid is used in combination (registered trade mark of Lipofactor:Sanofi).
A) scheme
In 28 days time 31 women are carried out this test.The experimenter presents back admittance the in the scorching zone of loose connective tissue in clinical examination and alleged occurrence.These experimenters apply described fluid and thin film on same thigh, by the random fashion definition, one leg is as untreated control in addition.
Be coated in from knee whole thigh to gluteal fold place on scheduled volume this fluid.Coating is to carry out in night, must product the massage of infiltration outside required.
In the morning with the height locate mode with thin film cladding in following 4 positions:
The external upper face of thigh,
The inside upper surface of thigh
Buttocks surface (buttocks layer)
The inner surface of knee
The consumption of thin film was equivalent to twice and connected spraying every day, covered domain of dependence thus.
The evaluation of effect is at T
0(before the processing) and T
28It carries out and adopts three kinds of diverse ways:
Echography is measured three positions of thigh and position fat tissue thicknesses of knee;
The big burr (alligator effect) of clinical evaluation thigh outer surface;
The graphical analysis that alligator effect is alleviated.
B) result
Echography
Table 1 demonstrates experimenter's principal character.
Experimenter's body weight is to measure when experiment finished on the 28th day.Observing does not have significant change, therefore can confirm observed result and the active relation of test products.
Table 1: individual characteristic
| Standard | On average | Maximum | Minimum |
| Age | 37 years old | 53 years old | 19 years old |
| ????BMI(a) | ????21.8 | ????26.9 | ????18.5 |
(a) Body Mass Index
Table 2 and Fig. 1 show that the thickness of test obesity tissue after 1 month all reduces.
According to the difference in zone, and at T
0The value contrast of measuring, the thickness of observing obesity tissue obviously reduces, and reaches-10% rank.
Table 2: according to the decreased average rate of the obesity tissue of processed position
(with respect to T
0The variation percentage ratio of expression)
*S(p＜＜0.05)
| The position | Handle | Contrast | Processing-contrast | Standard deviation |
| Outer thigh | ??-10.1％ | ????0.5％ | ???-10.5％* | ????±2.8％ |
| The thigh back of the body | ??-11.6％ | ????0.8％ | ???-12.4％* | ????±2.4％ |
| Interior thigh | ??-11.0％ | ???-0.7％ | ???-10.3％* | ????±2％ |
| Inside the knee | ??-10.6％ | ???-1.5％ | ????-9.1％ | ????±1.9％ |
Fig. 1: T
0And T
28The variation percentage ratio of each position between it
These results seem very obviously and are only relevant with processed side.Simultaneously, observing the control sides control site has very stable effect, and its excursion is not obvious to be-0.3 to ± 0.1mm.
The clinical evaluation of big burr (relief) is to utilize photographic negative to be finished by 5 evaluators.Behind the random distribution, by the evaluator by with calibration range (reference photograph) to recently with all egative film classifications, constitute about 7 other intensity of level.
For 5 experimenters, carry out profile in advance and measure (profilometric) and analyze the average burr that calculates appointed area on each image thus and corresponding to the skin area that is equal to of 3 * 130mm.
Utilize 31 volunteers' the processing and the egative film of contrast lateral surface of thigh, after analyzing by 5 evaluators, confirm that from clinical angle the skin burr makes moderate progress.
At T
0And T
28The improvement of handling thigh between it is (p＜＜0.05) clearly, at one time in, untreated side does not obtain tangible result.
Table 3: contrast the result between 5 experimenter's clinical change and the graphical analysis
| The experimenter | Clinical change | Graphical analysis (weakening of skin fluctuating) |
| ????1 | ????30％ | ????-35％ |
| ????2 | ????43％ | ????-24％ |
| ????3 | ????18％ | ????-14％ |
| ????4 | ????18％ | ????-22％ |
| ????5 | ????52％ | ????-11％ |
In this research process, 113 recruitment women with loose connective tissue inflammation are carried out the evaluation of thin film notion.
With twice spray application 4 all thin film in succession, cover domain of dependence thus.The effect of evaluation thin film when research finishes.
By this research obviously as can be seen, with regard to effect, thin film generally can significantly improve the alligator effect that is positioned on the lower limb.
The skin composition that embodiment 1 comprises
Preparation 100g has the skin composition of following prescription:
% weight
Ethyl cellulose 6mpa.s 5%
Fat-reducing active substance 2%
2 ethyl hexanoic acid 2-Octyl Nitrite 20%
Ethanol 73%
Propylene glycol 0.5%
Propellant gas
73g ethanol and 20g2-thylhexoic acid Octyl Nitrite are mixed 30 seconds with magnetic stirrer, fat-reducing active substance gradation with 2g subsequently adds in the gained mixture, after the dissolving, under vigorous stirring, add 5g ethyl cellulose 6mPa.s fully, avoid the formation of luming thus.The whole solution of gained evenly and slightly is creamy white.For purpose by spray application, be filled in the aluminium pot the above-mentioned gained solution of 5ml and fit on crimping air pump, this pump comprises the press-button type allotter.This pump need drive twice and starts before using first.
The substrate of embodiment 2 skin compositions
By 73g ethanol and 20g2-thylhexoic acid 2-Octyl Nitrite are mixed the skin substrate that prepared 98g in 30 seconds together.Under vigorous stirring, add the ethyl cellulose 6mPa.s of 5g subsequently, avoid the formation of luming thus.The substrate that makes thus is suitable for admitting activating agent by mixing, forms the cosmetic composition that contains 2% this activating agent of weight thus, and it can pass through spray application.
The substrate of embodiment 3 skin compositions
According to embodiment 2 described processing, following component is mixed:
Component % weight
Ethanol 75
And n-nonanoic acid ester in the different ninth of the ten Heavenly Stems 20
Ethyl cellulose 5
The substrate of embodiment 4 skin compositions
According to embodiment 2 described processing, following component is mixed:
Component % weight
Ethanol 80
Isononyl isononanoate 15
Ethyl cellulose 5
The substrate of embodiment 5 skin compositions
According to embodiment 2 described processing, following component is mixed:
Component % weight
Ethanol 75
Isononyl isononanoate 15
Ethyl cellulose 5
Carbiphene 5
The substrate of embodiment 6 skin compositions
According to embodiment 2 described processing, following component is mixed:
Component % weight
Ethanol 70
Isononyl isononanoate 15
Ethyl cellulose 5
Carbiphene 10
The following compositions of embodiment 7 preparations:
Component % weight
Alcohol 44.016
Butane 23.20
Octyl octanoate 12.00
Propane 11.20
Iso-butane 5.60
Ethyl cellulose 3.00
Pantothenylol 0.30
Propylene glycol 0.30
Diethyl phthalate 0.258
Fat-reducing active substance 0.126
Table A: the composition of preparation
| Reference preparation | A | B | R | C | D | E | F | G |
| Percentage | ||||||||
| Alcohol 95 | 77 | 76 | 75 | 67 | 66 | 18 | ||
| Isopropyl alcohol | 54 | 74 | 74 | |||||
| Dragoxat EH | 20 | 20 | 20 | 30 | 30 | 25 | 20 | 20 |
| Ethyl cellulose 7mPa.s. | 3 | 4 | 5 | 3 | 4 | 3 | 5 | 5 |
| Polysiloxanes DC556 | 1 | |||||||
| Liquid paraffin,light | 1 |
All the other materials of reference preparation: 95 ° of ethanol: 75%; Dragoxat: 20%; Ethyl cellulose: 5%.
Table B: excipient is with respect to the assessment classification of reference preparation
| Standard | Total evaluation | Skin adherent | Osmosis | Gloss | Greasy | Residual | Smell |
| Effect for reference | |||||||
| (+better ,-more abominable ,=equivalence) | |||||||
| Excipient isopropyl alcohol 3% ethyl cellulose | ＝ + | ＝ + | ＝ + | ＝ + | ＝ + | - + | - + |
| 4% ethyl cellulose | ＝ | ＝ | ＝ | ＝ | ＝ | ＝ | ＝ |
| 25％Dragoxat | - | - | - | - | ＝ | - | ＝ |
| 30％Dragoxat | - | - | - | - | ＝ | - | ＝ |
Claims (40)
1. skin cosmetic compositions is characterized in that containing:
A) randomly a kind of polymerization release matrix that can form flexible film after drying is selected from cellulosic polymer or copolymer;
B) active component;
C) in the active component Percutaneous absorption enhancer of said composition weight 5% to 30%;
D) can dissolve described release matrix, active component and Percutaneous absorption enhancer and by contacting the nonaqueous solvent that evaporation is removed rapidly on the skin, described Percutaneous absorption enhancer is selected from:
Dissolve in the aliphatic fatty acid ester that physiology can be accepted in the nonaqueous solvent and general formula is following:
Wherein R represents randomly by hydroxyl, carboxyl or C
1-C
4The straight or branched C that acyloxy replaces
2-C
17Alkyl or alkenyl, and R
1The straight or branched C that expression is randomly replaced by one or two hydroxyl
3-C
8Alkyl, or R
1Expression group-CH
2-CH
2-O-(CH
2)
2-O-CH
2-CH
3, this aliphatic series fatty acid ester has at least 10 carbon atoms and maximum 2 hydroxyls,
But solution physiology can be accepted nonaqueous solvent and the following aliphatic aliphatic alcohol of general formula,
R
2-OH II is R wherein
2Expression C
10-C
20Alkyl,
E) at least a propellant gas.
2. according to the compositions of claim 1, it is characterized in that described polymerization release matrix is that ratio in said composition weight 0% to 7% exists.
3. according to the compositions of claim 2, it is characterized in that described polymerization release matrix is that ratio in said composition weight 1% to 5% exists.
4. according to the described compositions of one of claim 1-3, it is characterized in that described active component is that ratio in said composition weight 0.1% to 20% exists.
5. according to the described compositions of one of claim 1-4, it is characterized in that described Percutaneous absorption enhancer is that ratio in said composition weight 15% to 25% exists.
6. according to the described compositions of one of claim 1-5, it is characterized in that described nonaqueous solvent is that ratio in said composition weight 44% to 84.9% exists.
7. according to the compositions of one of claim 1-6, it is characterized in that the polymerization release matrix is cellulosic polymer or the copolymer that dissolves in nonaqueous solvent.
8. according to the compositions of claim 7, it is characterized in that described cellulosic polymer or copolymer are can grafting or not grafted ethyl cellulose, cellulose acetate-butyrate, cellulose-acetate propionate or hydroxypropyl emthylcellulose.
9. according to the compositions of claim 7, it is characterized in that described cellulosic polymer or copolymer are ethyl celluloses.
10. according to the compositions of claim 1-9, it is characterized in that described active component is the fat-reducing active substance, this material is npy receptor antagonist and/or alpha-2 receptor antagonist.
11. according to the described compositions of one of claim 1-10, it is extract obtained to it is characterized in that active component is selected from by fermentative microorganism.
12., it is characterized in that active substance is that 0.5% to 6% ratio with said composition weight exists according to the compositions of claim 11.
13., it is characterized in that described active substance is that 1% to 2% ratio with said composition weight exists according to the compositions of claim 12.
14. according to the described compositions of one of claim 1-10, the cooperative programs that contain the active substance of forming by NPY antagonist and α 2 antagonisies, it is characterized in that used active substance is with the extract of the streptomyces bacterial strain SEBR 2794 of numbering I-1332 preservation with belong to the extract of bacterial strain SEBR2464 with the bacillus licheniformis of numbering I-1778 preservation at the C.N.C.M. of Pasteur association at the C.N.C.M. of Pasteur association.
15. the compositions according to one of claim 1-14 is characterized in that R
1Expression isopropyl, 2-ethylhexyl or 1, the 2-dihydroxy ethyl.
16., it is characterized in that Percutaneous absorption enhancer is selected from according to the compositions of claim 1:
2 ethyl hexanoic acid 2-Octyl Nitrite
Isopropyl myristate
The diethylene glycol monoethyl ether myristinate
Isopropyl palmitate
2-octyl group decanol
9-undecylenic acid 2-Octyl Nitrite
Succinic acid 2-Octyl Nitrite
12-hydroxy stearic acid 2-Octyl Nitrite
12-acetoxyl group stearic acid 2-Octyl Nitrite
Iso stearic acid of glycerine ester
Lauric acid hexyl ester
17., it is characterized in that described Percutaneous absorption enhancer is a 2 ethyl hexanoic acid 2-Octyl Nitrite according to the compositions of claim 1 or 15.
18., it is characterized in that described nonaqueous solvent is that boiling point is lower than 100 ℃ chemical compound under the normal pressure according to the compositions of one of claim 1-17.
19., it is characterized in that it is dichloromethane, ethanol, isopropyl alcohol or ethyl acetate that described boiling point is lower than 100 ℃ chemical compound according to the compositions of claim 18.
20., it is characterized in that described nonaqueous solvent is an ethanol according to the pharmaceutical composition of claim 18.
21. the compositions according to claim 1 is characterized in that
Described cellulosic polymer or copolymer are ethyl celluloses
Described active substance is the fat-reducing active substance
Described Percutaneous absorption enhancer is a 2 ethyl hexanoic acid 2-Octyl Nitrite
Described solvent is an ethanol
Propellant gas is butane.
22., it is characterized in that it contains according to the compositions of claim 21:
3% ethyl cellulose;
2% fat-reducing active substance;
20%2-thylhexoic acid 2-Octyl Nitrite; With
75% ethanol
Propellant gas.
23., it is characterized in that it contains according to the compositions of claim 1 or 21:
5% ethyl cellulose;
2% fat-reducing active substance;
20%2-thylhexoic acid 2-Octyl Nitrite; With
73% ethanol
Propellant gas.
24., it is characterized in that it contains according to the compositions of claim 1:
5% ethyl cellulose;
2% fat-reducing active substance;
20%2-thylhexoic acid 2-Octyl Nitrite; With
74% ethanol
Propellant gas.
25., it is characterized in that it contains according to the compositions of claim 1:
2% ethyl cellulose;
1% fat-reducing active substance;
20%2-thylhexoic acid 2-Octyl Nitrite; With
77% ethanol
Propellant gas.
26., it is characterized in that utilizing compression or liquefaction propellant gas to apply by spraying according to the described compositions of one of claim 1-25.
27., it is characterized in that being coated in skin 10-40cm according to the described compositions of one of claim 1-26
2The zone on.
28. supply the substrate of the cosmetic composition of dermal administration, it is characterized in that wherein containing:
A) release of active ingredients can film forming polymeric matrices after drying, it is selected from cellulosic polymer or copolymer;
B) in the active component Percutaneous absorption enhancer of said composition weight 15% to 30%;
C) can dissolve described release matrix with Percutaneous absorption enhancer and by contacting the nonaqueous solvent that evaporation is removed rapidly on the skin, described Percutaneous absorption enhancer is selected from:
Dissolve in the aliphatic fatty acid ester that physiology can be accepted in the nonaqueous solvent and general formula is following:
Wherein R represents randomly by hydroxyl, carboxyl or C
1-C
4The straight or branched C that acyloxy replaces
2-C
17Alkyl or alkenyl, and R
1The straight or branched C that expression is randomly replaced by one or two hydroxyl
3-C
8Alkyl, or R
1Expression group-CH
2-CH
2-O-(CH
2)
2-O-CH
2-CH
3, this aliphatic series fatty acid ester has at least 10 carbon atoms and maximum 2 hydroxyls,
Dissolve in the following aliphatic aliphatic alcohol of nonaqueous solvent and general formula,
R
2-OH II is R wherein
2Expression C
10-C
20Alkyl,
D) at least a propellant gas.
29., it is characterized in that described cellulosic polymer or copolymer are can grafting or not grafted ethyl cellulose, cellulose acetate-butyrate, cellulose-acetate propionate or hydroxypropyl emthylcellulose according to the compositions substrate of claim 28.
30., it is characterized in that cellulosic polymer or copolymer are ethyl celluloses according to the compositions substrate of claim 29.
31., it is characterized in that described Percutaneous absorption enhancer is selected from according to the compositions substrate of one of claim 28-30:
2 ethyl hexanoic acid 2-Octyl Nitrite
Isopropyl myristate
The diethylene glycol monoethyl ether myristinate
Isopropyl palmitate
2-octyl group decanol
9-undecylenic acid 2-Octyl Nitrite
Succinic acid 2-Octyl Nitrite
12-hydroxy stearic acid 2-Octyl Nitrite
12-acetoxyl group stearic acid 2-Octyl Nitrite
Iso stearic acid of glycerine ester
Lauric acid hexyl ester
32., it is characterized in that described Percutaneous absorption enhancer is a 2 ethyl hexanoic acid 2-Octyl Nitrite according to the compositions substrate of claim 31.
33., it is characterized in that described nonaqueous solvent is that boiling point is lower than 100 ℃ chemical compound under the normal pressure according to the described compositions substrate of one of claim 28-32.
34., it is characterized in that it is dichloromethane, ethanol, isopropyl alcohol or ethyl acetate that described boiling point is lower than 100 ℃ chemical compound according to the compositions substrate of claim 33.
35., it is characterized in that it is ethanol that described boiling point is lower than 100 ℃ chemical compound according to the compositions substrate of claim 33.
36. according to the described compositions substrate of one of claim 28 to 35, it is characterized in that described compositions contains: active substance accounts for the 0-7% of this release matrix; Account for the Percutaneous absorption enhancer of 15%-30% and account for the 44%-84.9% nonaqueous solvent, these percentage ratios are the weight in final composition.
37. contain the pump spray formula device of each described compositions of claim 1-27.
38., it is characterized in that it contains at least a fat-reducing active substance according to the cosmetic composition of claim 1.
39., it is characterized in that it contains npy receptor antagonist and alpha-2 receptor antagonist according to the described cosmetics Weight reducing compound of claim 38.
40. according to the described cosmetics Weight reducing compound of claim 39, it is characterized in that it contains at the C.N.C.M. of Pasteur association with the extract of the streptomyces bacterial strain SEBR 2794 of numbering I-1332 preservation with belong to the extract of bacterial strain SEBR2464 with the bacillus licheniformis of numbering I-1778 preservation at the C.N.C.M. of Pasteur association.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9816422A FR2787712B1 (en) | 1998-12-24 | 1998-12-24 | SPRAYABLE COSMETIC COMPOSITION AND MATRIX FOR USE IN THIS COMPOSITION FOR DERMAL ADMINISTRATION |
| FR98/16422 | 1998-12-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1331587A true CN1331587A (en) | 2002-01-16 |
Family
ID=9534488
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN99814967A Pending CN1331587A (en) | 1998-12-24 | 1999-12-08 | Spray-type consmetic compsn. and matrix used in said compsn. for dermal administration |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1140040A1 (en) |
| JP (1) | JP2002533383A (en) |
| KR (1) | KR20010089699A (en) |
| CN (1) | CN1331587A (en) |
| AU (1) | AU4520500A (en) |
| BR (1) | BR9916814A (en) |
| CA (1) | CA2350685A1 (en) |
| FR (1) | FR2787712B1 (en) |
| HU (1) | HUP0200095A2 (en) |
| IL (1) | IL143144A0 (en) |
| NO (1) | NO20013117L (en) |
| PL (1) | PL365376A1 (en) |
| TR (1) | TR200101569T2 (en) |
| WO (1) | WO2000038658A1 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101312706B (en) * | 2005-11-24 | 2011-07-06 | 株式会社资生堂 | External preparation for skin |
| CN102821756A (en) * | 2010-03-23 | 2012-12-12 | 株式会社爱茉莉太平洋 | Oil-in-water type nano-emulsion composition and method for preparing same |
| CN115335024A (en) * | 2020-03-02 | 2022-11-11 | Elc管理有限责任公司 | Method for repairing skin using nanofibers |
| CN115335025A (en) * | 2020-03-02 | 2022-11-11 | Elc管理有限责任公司 | Delivery of cosmetic agents, compositions and uses thereof |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2754709B1 (en) * | 1996-10-23 | 1999-03-05 | Sanofi Sa | COSMETIC COMPOSITION CONTAINING AN ANTAGONIST OF GAMMA NEUROPEPTIDE RECEPTORS AND ALPHA 2 ANTAGONISTS THAT MAY BE INCORPORATED IN SUCH A COMPOSITION |
| GB0518769D0 (en) | 2005-09-14 | 2005-10-19 | Medpharm Ltd | Topical formulations |
| EP2153836A1 (en) * | 2008-08-04 | 2010-02-17 | Polichem S.A. | Film-forming liquid formulations for drug release to hair and scalp |
| ITCA20120004A1 (en) * | 2012-03-30 | 2012-06-29 | Abdelkrim Harchi | SINGLE DEHYDRATING AND DIAPHANIZING REAGENT FOR HISTOLOGY AND NON-HARMFUL AND NON-TOXIC, BIODEGRADABLE CITOLOGY 88%, LOW VOLATILITY |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0289900A1 (en) * | 1987-04-30 | 1988-11-09 | Abbott Laboratories | Topical antibacterial compositions |
| FR2732223B1 (en) * | 1995-03-30 | 1997-06-13 | Sanofi Sa | PHARMACEUTICAL COMPOSITION FOR TRANSDERMAL ADMINISTRATION |
| FR2754709B1 (en) * | 1996-10-23 | 1999-03-05 | Sanofi Sa | COSMETIC COMPOSITION CONTAINING AN ANTAGONIST OF GAMMA NEUROPEPTIDE RECEPTORS AND ALPHA 2 ANTAGONISTS THAT MAY BE INCORPORATED IN SUCH A COMPOSITION |
-
1998
- 1998-12-24 FR FR9816422A patent/FR2787712B1/en not_active Expired - Fee Related
-
1999
- 1999-12-08 CA CA002350685A patent/CA2350685A1/en not_active Abandoned
- 1999-12-08 AU AU45205/00A patent/AU4520500A/en not_active Abandoned
- 1999-12-08 EP EP99973534A patent/EP1140040A1/en not_active Withdrawn
- 1999-12-08 PL PL99365376A patent/PL365376A1/en not_active Application Discontinuation
- 1999-12-08 TR TR2001/01569T patent/TR200101569T2/en unknown
- 1999-12-08 BR BR9916814-6A patent/BR9916814A/en not_active Application Discontinuation
- 1999-12-08 HU HU0200095A patent/HUP0200095A2/en unknown
- 1999-12-08 CN CN99814967A patent/CN1331587A/en active Pending
- 1999-12-08 KR KR1020017008101A patent/KR20010089699A/en not_active Application Discontinuation
- 1999-12-08 IL IL14314499A patent/IL143144A0/en unknown
- 1999-12-08 JP JP2000590612A patent/JP2002533383A/en not_active Withdrawn
- 1999-12-08 WO PCT/FR1999/003051 patent/WO2000038658A1/en not_active Application Discontinuation
-
2001
- 2001-06-21 NO NO20013117A patent/NO20013117L/en not_active Application Discontinuation
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101312706B (en) * | 2005-11-24 | 2011-07-06 | 株式会社资生堂 | External preparation for skin |
| CN102821756A (en) * | 2010-03-23 | 2012-12-12 | 株式会社爱茉莉太平洋 | Oil-in-water type nano-emulsion composition and method for preparing same |
| CN102821756B (en) * | 2010-03-23 | 2014-11-19 | 株式会社爱茉莉太平洋 | Oil-in-water type nano-emulsion composition and method for preparing same |
| CN115335024A (en) * | 2020-03-02 | 2022-11-11 | Elc管理有限责任公司 | Method for repairing skin using nanofibers |
| CN115335025A (en) * | 2020-03-02 | 2022-11-11 | Elc管理有限责任公司 | Delivery of cosmetic agents, compositions and uses thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| PL365376A1 (en) | 2005-01-10 |
| BR9916814A (en) | 2001-10-16 |
| WO2000038658A1 (en) | 2000-07-06 |
| KR20010089699A (en) | 2001-10-08 |
| FR2787712A1 (en) | 2000-06-30 |
| JP2002533383A (en) | 2002-10-08 |
| CA2350685A1 (en) | 2000-07-06 |
| NO20013117D0 (en) | 2001-06-21 |
| TR200101569T2 (en) | 2001-10-22 |
| FR2787712B1 (en) | 2002-08-30 |
| AU4520500A (en) | 2000-07-31 |
| NO20013117L (en) | 2001-08-24 |
| HUP0200095A2 (en) | 2002-05-29 |
| IL143144A0 (en) | 2002-04-21 |
| EP1140040A1 (en) | 2001-10-10 |
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