CN1375290A - Method for releasing L-asorbic substance to dermis layer of skin and composition thereof - Google Patents
Method for releasing L-asorbic substance to dermis layer of skin and composition thereof Download PDFInfo
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- CN1375290A CN1375290A CN 01117867 CN01117867A CN1375290A CN 1375290 A CN1375290 A CN 1375290A CN 01117867 CN01117867 CN 01117867 CN 01117867 A CN01117867 A CN 01117867A CN 1375290 A CN1375290 A CN 1375290A
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- ascorbic acid
- skin
- hydrophilic
- carrier
- hygroscopicity
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Abstract
The present invention has provided a method and its medicine combination to coat on the skin portion for curing and preventing skin aging or relative skin disturbance. The method to release L-ascorbic acid (vitaminc), L-ascorbic acid derivative and/or extractive containing ascorbic acid on the skin epidermic is characterized as that only the medicine combinations of phamary allowable carrier containing 1%-about 20% L-ascorbic acid, L-ascorbic acid derivative and/or extractive containing L-ascorbic aid with hydroscopicity, water affinity and solubility can be coated on the skin portion.
Description
The present invention relates to method and composition that the anti-hematic acid of L-(vitamin C), L-ascorbic acid derivates and/or the extract that contains the L-ascorbic acid are discharged to dermal layer of the skin.And by to local skin coating said composition, for example can be used for treating and/or preventing day burn, wrinkle, skin color are bad, dyschromasia etc.
Always, the L-ascorbic acid all is known for the beneficial effect of the blood flow of dermal layer of the skin with for the effect that produces collagen or elastin laminin simultaneously.Below enumerate the nearest document relevant with the present invention.
S.R.Pinnell, " the biosynthetic adjustment of collagen that causes by the L-ascorbic acid " YaleJ.Biol.Med.58:554-559 (1985).
Dumas etc., " the I type that is caused by the human skin fibroblast of aged donor and the external biological of III Collagen Type VI are synthetic " Mechanism of Aging and Development, vol.73 (1994) pp.179-187.
Phillips etc., " propagation and the synthetic effect of collagen that the L-ascorbic acid is relevant with donor age to human skin fibroblast " Journal of Investigative Dermatology, vol.103, No.2, Aug.1994, pp.228-232.
Sephel etc., " generation of the elastin laminin in the human skin fibroblast cultivation and the minimizing that increases with the age " Journal of Investigative Dermatology, vol.86, No.3, Mar.1986, pp, 279-285.
Takema etc., " character of the elastin laminin of human face's skin and thickness are with the variation at age " British Journal of Dermatology, vol.131,1994, pp.641-648.
For the big obstacle that the L-ascorbic acid is used for the treatment of, be the actual skin corium that is discharged into of the L-ascorbic acid that fills part high concentration that will enable to bring into play above-mentioned beneficial effect.We thrust microelectrode to skin corium, measure oxidation-reduction potential, and when having proved oral administration L-ascorbic acid, the L-ascorbic acid concentrations in the skin corium increases hardly.If support L-ascorbic acid is to the dermal layer of the skin transfer and add the L-ascorbic acid in medium, the probability of carrying out local coating to skin has been arranged then.In patent documentation, many systems relevant or prescription (composition) have been narrated with the local coating ascorbic acid.
These patent documentations comprise following several: U.S. Patent No. 4938969 (Schinitsky), U.S. Patent No. 5140043 (Darr), U.S. Patent No. 5281196 (Sultenfuss), U.S. Patent No. 5801192 (Dumas), U.S. Patent No. 5843411 (Hernandez), U.S. Patent No. 5853741, and the document of being put down in writing in the middle of them.
These prescriptions of said past are to the actual L-ascorbic acid that discharged of skin corium, and this is by these prescriptions the conclusion that to be inferred in the experiment of fine wrinkle effect.In these experiments, the concentration of L-ascorbic acid in the skin corium is not directly measured, and the result who observes to have also may be to be caused owing to testing other a lot of composition of various quantity sometimes contained in the component.Therefore, the objective of the invention is, (with evincible method) provides a kind of L-of support ascorbic acid, the anti-hematic acid derivant of L-and/or contains the method for releasing and the compositions of the extract of L-ascorbic acid to the infiltration (but avoiding stimulating) of application on human skin.
Another object of the present invention is, a kind of warp over-exposure or increase rheological processes naturally and also can make L-ascorbic acid, L-ascorbic acid derivates that creasy surface reduces and/or method for releasing and the compositions that contains the extract of L-ascorbic acid in sunray is provided.
To achieve the object of the present invention, the 1st method is with L-ascorbic acid, L-ascorbic acid derivates and/or contains the method for the extract of L-ascorbic acid to dermal layer of the skin release, it is characterized in that, will in the carrier that the pharmaceutics that contains hygroscopicity, hydrophilic and water-soluble liquid is allowed, contain the compositions of having an appointment 1%～about 20% L-ascorbic acid, L-ascorbic acid derivates and/or containing the extract of L-ascorbic acid and apply.
In addition, the 2nd invention is, to it is characterized in that as above-mentioned hygroscopicity, hydrophilic and water miscible liquid, use has the polyhydric alcohol of 3～4 hydroxyls and 3～10 carbon atoms according to the 1st described invention.
The 3rd invention is, according to the 1st described invention, it is characterized in that, as above-mentioned hygroscopicity, hydrophilic and water miscible liquid, uses the mixture of two or more carriers.
The 4th compositions is characterised in that, in the carrier that the pharmaceutics that contains hygroscopicity, hydrophilic and water miscible liquid is allowed, contains and has an appointment 1%～about 20% L-ascorbic acid, L-ascorbic acid derivates and/or contain the extract of L-ascorbic acid.
The 5th invention is, to it is characterized in that above-mentioned hygroscopicity, hydrophilic and water miscible liquid are with the ethylene of following general formula and the linear polymer of propylene oxide according to the 4th described invention.
RO-[CH
2CH(CH
3)O]
n-[CH
2CH
2O]
m-H
In the formula, R is hydrogen or the alkyl with 1～18 carbon atom, 1≤n+m≤40.
The 6th invention is, to it is characterized in that above-mentioned hygroscopicity, hydrophilic and water miscible liquid are the mixture of carrier more than 2 kinds according to the 4th described invention.
Embodiments of the present invention
The present invention is based on following opinion: the highest and organic solvent of hygroscopic molecular weight below 2000 of polarity, can dissolve the L-ascorbic acid of appropriate amount, and suitable to the carrier of L-ascorbic acid through epithelium.Example to appropriate carrier does not limit, and below this carrier is enumerated.
1. by general formula R O-[CH
2CH (CH
3) O]
n-[CH
2CH
2O]
mThe linear polymer formula (1) of ethylene that-H represents and ethylene oxide.
In this general formula, R is hydrogen or the alkyl with 1～18 carbon atom, and condition is 1≤n+m≤40.As the concrete example of this compounds, can select propylene glycol, dipropylene glycol, four propylene glycol, polyethers (1 and 2 of hydroxyl).
2. have the linear polymer of ethylene of above-mentioned general formula and the mixture of propylene oxide.Concrete example as this kind chemical compound has, and (R=H in above-mentioned general formula, the mixture of polypropylene glycol m=0) are the Acclaim of Lyondell company to have mean molecule quantity 1000
TM(below
TMBe expressed as trade (brand) name) and (R=butyl in above-mentioned general formula, the mixture of poly-(oxyalkylene) copolymer n=m) is the UCON of Union Carbide Corporation to have mean molecule quantity 270
TM50-HB-55.
3. the polyalcohols that has 3～individual hydroxyl and 3～10 carbon atoms.
Concrete example as this compounds has glycerol.
Embodiment
Use the following voltammeter technology of recording and narrating, the effect of instrumentation carrier matrix.
The ultramicroelectrode (anode) that will be formed by 5 microns the platinum fine rule that thrusts glass and 2 ultramicroelectrodes of another electrode (reference electrode is a negative electrode) laterally thrust under the skin of shoulder or upper breast, notice that the electrode front end will enter skin corium.Distance keeps about 1mm between the front end of two electrodes.Above-mentioned ultramicroelectrode is put down in writing in following document: [R.Mark Wightman and Davicl O.Wipf, Electroanalytical Chemistry " voltammetry that ultramicroelectrode is used " " Voltammetry at UltrmicrodesElectrodes " in Electoanalytical Chemistry, Vol 15, pp267～253, the editor, Allan J.Bard, Marcel Dekker, 1989].
Contrast test
(to standard calomel electrode) with the sweep speed of 550 volts of per seconds, 25 scanning curves between making-0.2～+ 0.2 volt, and the integrated value of the anode cycle part of recording voltage current curve, and by Computer Storage.With the meansigma methods of these 25 times scannings, as the background value of finding oxidation place linear module in the anode cycle.
Permeability:
To under test contain the solution of L-ascorbic acid 3% with 0.05ml/cm in the carrier matrix
2Partly (total surface covered is about 5cm to be coated in skin on the electrode
2), cause above-mentioned periodic wave after 20 seconds, the linear module of the total oxidation of instrumentation discovery place.This value is poor with the oxidation background value that obtains with reference to test, as the oxidation linear module of L-ascorbic acid.This promptly is the linear module of the L-ascorbic acid concentrations (permeability) in the skin corium.
These values of gained can not be construed to the real concentration of L-ascorbic acid simply, the precision of mensuration also not high (± 10%).
In order to make certain dependency that has of measured value and L-ascorbic acid corium concentration in the body, same electrode is immersed among the human blood 0.5ml that remains on 37 ℃, carry out amperometric determination like that by above-mentioned, in this blood sample, add L-ascorbic acid (1ml blood 7.5mg), carry out amperometric determination again.The difference of these two oxidation numbers is amplified 100 times arbitrarily and is represented.Table 1 shows several measurement results of implementing with this yardstick.Test portion in the table is that the L-ascorbic acid directly is dissolved in the carrier solvent, quickens for making course of dissolution, heats in case of necessity and operates.
Table 1
Oxidation number when being coated on the skin in the treatment prescription composition body with the L-ascorbic acid
| The carrier base | The % of L-ascorbic acid | Oxidation number |
| Propylene glycol | ????0 | ????0 |
| Propylene glycol | ????3 | ????50 |
| Glycerol | ????0 | ????0 |
| Glycerol | ????3 | ????20 |
| Four propylene glycol | ????0 | ????0 |
| Four propylene glycol | ????3 | ????40 |
| Propylene glycol 400 1 | ????0 | ????0 |
| Propylene glycol 400 1 | ????3 | ????15 |
| ????Acclaim TM?1000 2 | ????0 | ????0 |
| ????Acclaim TM?1000 2 | ????3 | ????10 |
| ????UCON TM50-HB-55 3 | ????0 | ????0 |
| ????UCON TM50-HB-55 3 | ????3 | ????60 |
| ????UCON TM50-HB-100 4 | ????0 | ????0 |
| ????UCON TM50-HB-100 4 | ????3 | ????25 |
| ????UCON TM50-HB-2000 5 | ????0 | ????0 |
| ????UCON TM50-HB-2000 5 | ????3 | ????20 |
| ????UCON TM50-LB-65 6 | ????0 | ????0 |
| ????UCON TM50-LB-65 6 | ????3 | ????20 |
In the table 1, polypropylene glycol 400
1It is mixture by the polypropylene glycol of the deutero-mean molecule quantity 400 of propylene oxide polymerization.
Acclaim
TM1000
2Be mixture (supplier: Lyondell company) by the polypropylene glycol of the deutero-mean molecule quantity 1000 of propylene oxide polymerization.
UCON
TM50-HB-55
3Be in the aforementioned formula (1), R=butyl, n=m and mean molecule quantity are the mixture (supplier: Union Carbide Corporation) of 270 polyethers.
UCOM
TM50-HB-100
4Be in the above-mentioned formula (1), R=butyl, n=m and mean molecule quantity are the mixture (supplier: Union Carbide Corporation) of 520 polyethers.
UCOM
TM50-HB-2000
5Be in the above-mentioned formula (1), R=butyl, n=m and mean molecule quantity are the mixture (supplier: Union Carbide Corporation) of 2660 polyethers.
UCOM
TM50-LB-65
6Be in the above-mentioned formula (1), the R=butyl, n=0, and mean molecule quantity is the mixture (supplier: Union Carbide Corporation) of 340 polyethers.
Local coating uses the transepithelial permeability of solution of hygroscopicity carrier, and also ascorbyl palmitate being used the same method proves.
Distinguish in addition, in method and composition of the present invention, the L-ascorbic acid that contains in the carrier that the pharmaceutics that contains hygroscopicity, hydrophilic and water miscible liquid is allowed, L-ascorbic acid derivates and/or the amount that contains the extract of L-ascorbic acid are in 1%～20% the scope, the action effect that can obtain expecting, optimum scope is 3%～10%.
The effect of invention
The present invention makes L-AA (vitamin C), L-AA derivative and/or contains the extract of the anti-hematic acid of L-to the method for dermal layer of the skin release, be in the molten carrier of being permitted of the pharmacy that contains hygroscopicity, hydrophily and water-soluble liquid, contain L-AA, the L-AA derivative of effective deal and/or contain the composition of the extract of L-AA. This hygroscopicity base makes L-AA continue aptly diffusion by the skin epithelium to skin corium becomes possibility. By such composition is applied to local skin, can be used for treating and/or preventing light skin aging or relevant skin barrier, such as burn day, wrinkle, skin color are bad, dermatodyschroia etc.
Claims (6)
1. the method that L-ascorbic acid, L-ascorbic acid derivates and/or the extract that contains the L-ascorbic acid are discharged to dermal layer of the skin, it is characterized in that, will in the carrier that the pharmaceutics that contains hygroscopicity, hydrophilic and water miscible liquid is allowed, contain the compositions of having an appointment 1%～about 20% L-ascorbic acid, L-ascorbic acid derivates and/or containing the extract of L-ascorbic acid and apply.
2. the described method that L-ascorbic acid, L-ascorbic acid derivates and/or the extract that contains the L-ascorbic acid are discharged to dermal layer of the skin of claim 1, it is characterized in that, as above-mentioned hygroscopicity, hydrophilic and water miscible liquid, use polyhydric alcohol with 3～4 hydroxyls and 3～10 carbon atoms.
3. the described method that L-ascorbic acid, L-ascorbic acid derivates and/or the extract that contains the L-ascorbic acid are discharged to dermal layer of the skin of claim 1, it is characterized in that, as above-mentioned hygroscopicity, hydrophilic and water miscible carrier, use the carrier mixture more than 2 kinds.
4. compositions is characterized in that, contains 1%～about 20% make L-ascorbic acid, L-ascorbic acid derivates and/or contain the extract of L-ascorbic acid of having an appointment in the carrier that the pharmaceutics that contains hygroscopicity, hydrophilic and water miscible liquid is allowed.
5. the described compositions of claim 4 is characterized in that, above-mentioned hygroscopicity, hydrophilic and water miscible liquid are by the ethylene of following general formula and the linear polymer of propylene oxide,
RO-[CH
2CH (CH
3) O]
n-[CH
2CH
2O]
mIn this general formula of-H, R is hydrogen or the alkyl with 1～18 carbon atom, 1≤n+m≤40.
6. the described compositions of claim 4 is characterized in that, above-mentioned hygroscopicity, hydrophilic and water miscible liquid are the mixture of the carrier more than 2 kinds.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01117867 CN1375290A (en) | 2001-03-20 | 2001-03-20 | Method for releasing L-asorbic substance to dermis layer of skin and composition thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01117867 CN1375290A (en) | 2001-03-20 | 2001-03-20 | Method for releasing L-asorbic substance to dermis layer of skin and composition thereof |
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| CN1375290A true CN1375290A (en) | 2002-10-23 |
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|---|---|---|---|
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103764115A (en) * | 2011-08-11 | 2014-04-30 | 施泰福研究澳大利亚有限公司 | Antioxidant topical compositions |
-
2001
- 2001-03-20 CN CN 01117867 patent/CN1375290A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103764115A (en) * | 2011-08-11 | 2014-04-30 | 施泰福研究澳大利亚有限公司 | Antioxidant topical compositions |
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