CN101291651A - External composition for hair growth - Google Patents
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- CN101291651A CN101291651A CNA200680038602XA CN200680038602A CN101291651A CN 101291651 A CN101291651 A CN 101291651A CN A200680038602X A CNA200680038602X A CN A200680038602XA CN 200680038602 A CN200680038602 A CN 200680038602A CN 101291651 A CN101291651 A CN 101291651A
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Abstract
The present invention relates to a hair growth-promoting composition for external application. More particularly, it relates to a hair growth-promoting composition for external application, which contains 4-pyrrolidine 2,6- diaminopyrimidine 1 -oxide and one or more selected from the group consisting of Thujae semen, vitamin B5 derivatives (panthenol derivatives), Swertia extract (Swertiall), Coicis semen, Glycyrrhiza extracts (glycyrrhizin and glycyrrhetic acid), nicotinamide (niacinamide), vitamin E derivatives (tocopherol acetate, etc.), adenosine, glyceryl pentadecanoate (PDG), 6-benzyl aminopurine, eugenol, saw palmetto, dialkylmonoamine derivatives, isoflavone, hinokitiol and benzylnicotinate. Thus, the composition smoothly supplies nutrients necessary for hair growth through the vasodilation of blood vessels around hair follicles to promote the transition from the telogen phase to the anagen phase of the hair cycle and to maintain the anagen phase for a long period of time.
Description
Technical field
The present invention relates to a kind of trichogenous topical composition, relate in particular to a kind of 4-of containing pyrrolidine-2,6-di-amino-pyrimidine-1-oxide and one or more are selected from by thujae semen, vitamin B5 derivant (panthenol derivant), Herba Swertiae bimaculatae extract, Semen Coicis, Radix Glycyrrhizae extract (glycyrrhizin and glycyrrhetinic acid), niacin amide (nicotiamide), vitamin e derivative (vitamin e acetate etc.), adenosine, tripentadecanoin (PDG), the 6-benzylaminopurine, acetaminol, GAIWUZONGLV, the dialkyl monoamine derivant, isoflavone, the trichogenous topical composition of the material in the group that hinokitiol and benzyl nicotinate are formed.Described compositions is supplied with the necessary nutrient substance of hair growth reposefully by near the vasorelaxation action the hair follicle, with promote in the hair life cycle telogen to the anagen change and keep for a long time make the anagen.
Background technology
In current society, owing to the h and E factor causes making some masculinity and femininities experience psychic pain to giving the significant hair minimizing of aesthetic feeling, therefore, worldwide very active about the minimizing and the trichogenous various research of the hair for the treatment of these masculinity and femininities.
People's hair is about 100,000-150, and 000, everyone hair growth also comes off behind the many wheels of experience growth cycle of hair.Three different periods of the growth of hair experience: the anagen, catagen and telogen.The anagen of described be hair the anagen, be exactly the catagen that hair structure is kept and metabolic process is slack-off subsequently.Diminish and period that hair follicle is degenerated and to be caused hair shaft to be easy to come off thereby be hair papilla the telogen after catagen.The life cycle of hair changes because of the variation of multiple factor, and described factor comprises nutriture, pharmacohistory, heredity, physique, hormone secretion and aging.
In the treatment reagent that existing prevention hair reduces, it is reported by the medicine for external use minoxidil (minoxidil) of U.S. food and drug administration (USA FDA) approval that except having the vasodilation function it also has the anagen that hair being induced to from telogen of hair life cycle and activity (the British Journal of Dermatology.2004 continue to keep inductive the anagen as typical potassium channel openers (opener); 150:186-194).
In addition, a kind ofly be called finasteride (Finasteride) (Propecia by U.S. food and drugs administration approved; MSD) oral medicine can suppress the 5-5 alpha-reductases and go on the market as the generation of the dihydrotestosterone of potential androgen and as the hair growth stimulus object with inhibition.Yet because this medicine is expensive and have some side effect, thereby its use is restricted.Therefore, still need a kind of two kinds of main medicines to compare the medicine that has the hair growth facilitation effect but be free from side effects with the prior art exploitation.
The trichogenous mechanism of minoxidil (2,4-diaminourea-6-piperidyl-pyridine-3-oxide) as pyrimidine derivatives is not clear.The trichogenous effect of only knowing described chemical compound is because the vasodilation that the effect of potassium channels opening causes causes, and the effect of described potassium channels opening is found when this medicine of exploitation.
From then on, reported hair growth effect (the J Invest Dermatol 2,005 124 (4): 686-94) that various pyrimidine derivatives and new chemical compound have general potassium channels opening effect and cause thus, and submitted to the hair growth effect of the derivant that relates to various pyrimidine oxides technology (as, US5,034,387 and US 4,945,093).The patent about the hair growth effect of pyrimidine oxide derivatives in the past comprises the derivant structure of wide range, and comprising the structure of known minoxidil medicine, it is general that the hair growth effect of these derivants is considered to.And former patent does not disclose the data of the hair growth effect (as vasodilator effect) of minoxidil.
Summary of the invention
Therefore, the present inventor finds in pyrimidine oxide derivatives, the chemical compound of the pyrrolidine on the position of describing in international cosmetic composition dictionary (International Cosmetic Ingredient Dictionary) with the basic chemical structure that is connected to pyrimidine oxide 6 also has the propagation of the important skin papilla cell of potassium channels opening effect and promotion control hair life cycle except the function with curling and stretching hair.Therefore, the present inventor is applied to mice with this chemical compound, to check of the influence of this chemical compound to hair growth, found that 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide shows the potassium channels opening effect by the antagonism that potassium channels opening is suppressed medicine, and have the effect that promotes skin papilla cell propagation and promote the anagen that the hair life cycle of the mice with telogen forwarded to from telogen, thereby realize the present invention.
The invention provides a kind of topical composition, said composition contains with 4-pyrrolidine-2, thereby 6-di-amino-pyrimidine-1-oxide suppresses common male's formula as active component or women's formula hair reduces and the growth of promotion hair.
4-pyrrolidine-2 of the present invention, 6-di-amino-pyrimidine-1-oxide are used as the active component of external preparation and promote the growth of hair.Therefore, topical composition of the present invention contains 4-pyrrolidine-2, and therefore 6-di-amino-pyrimidine-1-oxide has the potassium channel development effectiveness as active component, reduces and trichogenous effect thereby produce the prevention hair.
Description of drawings
Fig. 1 is an expression 4-pyrrolidine-2, the sketch map of the potassium channels opening effect of 6-di-amino-pyrimidine-1-oxide;
Fig. 2 is an expression 4-pyrrolidine-2, and 6-di-amino-pyrimidine-1-oxide has the sketch map of the effect that promotes skin papilla cell propagation;
Fig. 3 shows 4-pyrrolidine-2, and 6-di-amino-pyrimidine-1-oxide has the mice of promotion hair growth effect.
The specific embodiment
The present invention relates to trichogenous topical composition, said composition contains 4-pyrrolidine-2, and therefore 6-di-amino-pyrimidine-1-oxide has the potassium channels opening effect and promote the effect that hair follicle cell is bred as active component.
To describe the present invention in detail hereinafter.
The 4-pyrrolidine-2 that uses among the present invention, 6-di-amino-pyrimidine-1-oxide belongs to pyrimidine oxide derivatives by following formula 1 expression, and as cosmetic composition, its effect in vivo is unclear.
[formula 1]
When 4-pyrrolidine-2 of the present invention, the 6-di-amino-pyrimidine-when the 1-oxide is used to promote hair growth, 4-pyrrolidine-2, the consumption of 6-di-amino-pyrimidine-1-oxide depends on application target and its preparation, gross weight with described compositions is a benchmark, 4-pyrrolidine-2, the consumption of 6-di-amino-pyrimidine-1-oxide are 0.001-10 weight %.Consider 4-pyrrolidine-2, the dissolubility of 6-di-amino-pyrimidine-1-oxide and its stability of formulation, its consumption is preferably 0.001-5 weight %.Usually, if 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide does not dissolve in particular formulations or when having stability problem, it may be gathered into crystal or may be modified, and therefore causes variable color or spoiled.
Topical composition of the present invention removes and contains described 4-pyrrolidine-2, outside 6-di-amino-pyrimidine-1-oxide, can also contain one or more and be selected from by thujae semen (Thujae semen), vitamin B5 derivant (panthenol derivant), Herba Swertiae bimaculatae extract (Swertia extract), Semen Coicis (Coicissemen), Radix Glycyrrhizae extract (glycyrrhizin and glycyrrhetinic acid), niacin amide (nicotiamide), vitamin e derivative (vitamin e acetate etc.), adenosine, tripentadecanoin (PDG), the 6-benzylaminopurine, acetaminol, GAIWUZONGLV (saw palmetto), the dialkyl monoamine derivant, isoflavone, material in the group that hinokitiol and benzyl nicotinate are formed.Gross weight with said composition is a benchmark, this optionally the content of composition in compositions be preferably 0.005-5 weight %.
Can be used on normally pantothenic acid derivative of panthenol derivant of the present invention, pantothenic acid is found to be zymic essential growth factor, is stable in neutral solution, and its disadvantage is that pantothenic acid can be destroyed, especially thermo-labile in acidity or alkaline solution.Owing to these reasons, use in the present invention as D-panthenol previtamin and that be converted into vitamin B5, D-ethyl panthenol or D-calcium pantothenate, because they have more stable structure.The effect of vitamin B5 is summed up as the panthenol based on D-usually, and it is reported that it comes from effect aspect following three in skin and multiple effect in the hair: 1) porous is to the relative darker position with hair of skin; 2) can combine with skin; With 3) in skin and hair, be transformed into pantothenic acid to produce the effect of vitamin B5.In cosmetic field, when the D-panthenol uses with the amount of 0.1-5%, because its high penetrating power will be sent to skin corium dearly, owing to its wettability power, it will have moistening effect by situation and the distribution that influences water in the skin corium again.In nineteen forty-three, H.Pfaltz finds that indirectly panthenol is absorbed and is converted into pantothenic acid, he also reports with 10% D-panthenol and respectively handles rat and 6 weeks of mice with the form of ointment, found that with oral situation and compare, the phenomenon that hemoglobin and hair reduce obtains more effective improvement the (Pfaltz H., Vitaminforschung, 1943,13,236-249).In addition, also reported panthenol to the influence of epiderm skin cell in the healing that is in wound and burn (Gartner F., Dtsch.Zahnarztl.Z, 1955,10,813-5, Cortesse J., G.M.deFrance, 1968,75,4171-4).When panthenol is applied to hair; it will be penetrated into hair shaft and root of hair, thereby be present in the hair and be enclosed in around the hair to keep the moisture in the hair and to protect hair not to be subjected to the influence of extraneous dry environment with the form of thin layer with the form of elastica.
Can be used on thujae semen of the present invention is the seed of east (west) Japanese arborvitae (Thuja orientalis (occidentalis)) (Cupressaceae (Cupressaceae)), the long avette or long cylinder bodily form, and long is that 3-5mm and diameter are 2-3mm.Thujae semen has tranquil emotion and makes the effect that is heightened in spirits, its motion of intestinal gently (east research introduction (Introduction to Oriental Studies)).Known it contain a large amount of fatty oils.According to the description of Dong-Eui-Bo-Gam (Korean traditional medicine textbook) hair part, known can the making of mixture of Aconitum carmichjaelii Debx. (Aconitum carmichaeli), Fructus Viticis (Viticis Fructus) and thujae semen grows new beard and hair.Especially, Dong-Eui-Bo-Gam discloses the part that described mixture is used baldness makes the part of baldness grow new hair, described mixture is by Aconitum carmichjaelii Debx., Fructus Viticis and the thujae semen of each 20g are pulverized, and these powder are mixed with Korea S Gallus Domesticus oil (Korean black (Ogol) chicken oil), dry and sealing is kept in the ware 100 days with mixture, from ware, take out the mixture (Dong-Eui-Bo-Gam that preserves, HairSection, Namsandang Publishing Co.).In addition, thujae semen shows 5 and suppresses active in two kinds of animal models, and demonstrate high hair growth activity, therefore, can be used for the treatment of effectively by the transformation of control androgen hair reduce (Journal of DermatologicalScience (2003) 31,91-98).
In addition, can be used on Herba Swertiae bimaculatae extract of the present invention is Japanese Herba Swertiae bimaculatae (Swertia japonicaMakino) extract, is referred to as " extract in gloomy (Senburi extract) " in Japan.In Korea S, can be used on the medicine " Dan-Ya Ke (Dang-yak) " by name of Herba Swertiae bimaculatae extract of the present invention, " gloomy Pu'er (sseun-pul) " of science Japanese Herba Swertiae bimaculatae extract by name.This extract is a kind of traditional drugs, is widely used in treatment abdominal pain, skin infection, insecticide (insects) and flu in Japan.Herba Swertiae bimaculatae extract contains swertiamarin (swertiamarin), Swertianolin (swertianolin), erthrocentaurin (erythrocentaurin), swertianol (swertianol), caryophyllin and the erythricine (gentianine) of 2-4% usually.Known Herba Swertiae bimaculatae extract contain comprise swertiamarin join sugar as main component, it is reported that Herba Swertiae bimaculatae extract and the Mylabris that derives from animal and plant (cantharide) are the same with capsicum tincture (capsicum tincture) can improve skin temperature and promote hair growth.Physiologic effect or vasodilator effect that cholinomimetic energy medicine improves skin temperature can stimulate the blood flow of keeping skin function.The article of Shuji Iwao (" about the prospect (about prospect of hairgrowth stimulants) of hair growth stimulant ", Fragrance Journal (1996)) having described Herba Swertiae bimaculatae extract is blood circulation accelerant, and blood circulation accelerant is the main component of commercial hair growth stimulant.
Other composition that can be contained in the present composition comprises Semen Coicis, Radix Glycyrrhizae extract (glycyrrhizin and glycyrrhetinic acid), niacin amide (nicotiamide), vitamin e derivative (vitamin e acetate etc.), adenosine, tripentadecanoin (PDG), 6-benzylaminopurine, acetaminol, GAIWUZONGLV, dialkyl monoamine derivant, isoflavone, hinokitiol and benzyl nicotinate.As long as these components do not have safety problem, it uses without any specific restriction.In addition, their mechanism of action is without any problem.Yet with performance vasodilation function and when activating hair follicle cell, they can adopt commercially available raw material to prepare in accordance with known methods to these compositions as commercial hair growth stimulant.
Contain 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide can be made hair moisturizer (hair tonic), anti-dandruff hair conditioner (scalp treatment), shampoo, hair care breast (hair cream), general ointment (general ointment), skin cream (skin lotion), milk skin cream, eye cream, nourishing cream, massage cream (massage cream), cleansing cream (cleansing cream), cleaning foam or cleaning powder as the topical composition of active component, but scope of the present invention is not limited to these.
For the hair growth facilitation effect that obtains to produce owing to above-mentioned vasorelaxation action, those skilled in the art does not have special difficulty just can suitably select and use described 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide.
Hereinafter the present invention is described in more detail for reference example and test case.Yet should be understood that these embodiment only are used for illustrative purposes and do not limit the scope of the invention.
Embodiment 1:4-pyrrolidine-2, the potassium channels opening effect of 6-di-amino-pyrimidine-1-oxide
Hyclone with 5% and 100IU penicillin join and contain in the phenol red DMEM culture medium, and culture medium is joined in the 24 hole porous culture plates.Is that 10000 cells/well are suspended in the 24 hole porous culture plates with mice source fibroblast NIH3T3 cell line with concentration.Potassium channel antagonist tolbutamide is joined in the culture medium; making its final concentration is 2.5mM; with 4-pyrrolidine-2; 6-di-amino-pyrimidine-1-oxide (Proderma; Italy) dilution joins in the culture medium after 100 times; making its concentration is 1 μ M, 50 μ M and 100 μ M, and culture medium was hatched under 37 ℃ 3 days.After hatching, and 0.2% of adding 200 μ l MTT in every hole of titer plate ((3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyl tetrazolium bromide)) solution, culture medium is continued down to cultivate 3 days at 37 ℃.Be dissolved among the DMSO (dimethyl sulfoxine) generating De Jia Za (formazane) then.Measure the absorbance of dissolved Jia Za at 570nm with the microwell plate reader.4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide has all suppressed the potassium channel antagonism of tolbutamide in each concentration, to promote the propagation of NIH3T3.The promotion result who compares with matched group (100%) of chemical compound is illustrated among Fig. 1.In Fig. 1, matched group is the group that potassium channel antagonist tolbutamide of no use is handled, and negative matched group is the group of only handling with tolbutamide.As can be seen from Figure 1; 4-pyrrolidine-2; 6-di-amino-pyrimidine-1-oxide does not have to show because having the potassium channel development effectiveness hair growth facilitation effect with the matched group par, but shows the growth-promoting effect that only is higher than the negative matched group of handling with tolbutamide.
Embodiment 2: to the test of the facilitation effect of skin papilla cell
With the rat source skin papilla cell of cultivating containing the DMEM of 2% hyclone (Dulbecco ' s Modified Eagle ' sMedia) is that 1000 cells/well are suspended in the 96 hole porous culture plates with concentration, with minoxidil and the 4-pyrrolidine-2 as positive matched group of each 10 μ g/ml, 6-di-amino-pyrimidine-1-oxide joins in the culture medium.In addition, with thujae semen, vitamin B5 derivant (panthenol derivant), Herba Swertiae bimaculatae extract, Semen Coicis, Radix Glycyrrhizae extract (glycyrrhizin and glycyrrhetinic acid), niacin amide (nicotiamide), vitamin e derivative (vitamin e acetate etc.), adenosine, tripentadecanoin (PDG), 6-benzylaminopurine, acetaminol, GAIWUZONGLV, dialkyl monoamine derivant, isoflavone, hinokitiol and benzyl nicotinate and the described 4-pyrrolidine-2 of each 10 μ g/ml, 6-di-amino-pyrimidine-1-oxide joins in the culture medium together.Then culture medium was hatched under 37 ℃ 48 hours.After hatching, in every hole of titer plate, add 0.2% MTT ((3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyl tetrazolium bromide)) solution, culture medium is continued down to cultivate 4 hours at 37 ℃ with the density of 50 μ l.Be dissolved among the DMSO (dimethyl sulfoxine) generating De Jia Za then.Measure the absorbance of dissolved Jia Za at 570nm with the microwell plate reader.With the testing result of test group with only compare with the matched group of DMSO solution-treated, contain 4-pyrrolidine-2 with mensuration, the absorbance difference between the test group of 6-di-amino-pyrimidine-1-oxide the results are shown in the following table 1.
[table 1]
| Processed group | Papilla cell propagation (%) |
| The DMSO-processed |
100 |
| Minoxidil-processed |
120 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 118 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+thujae semen | 124 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+D-panthenol | 145 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+Herba Swertiae bimaculatae extract | 135 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+Semen Coicis | 130 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+Radix Glycyrrhizae extract | 146 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+niacin amide | 138 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+vitamin e acetate | 142 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+adenosine | 132 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+tripentadecanoin | 142 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+benzylaminopurine | 135 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+acetaminol | 136 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+GAIWUZONGLV | 120 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+dialkyl monoamine derivant | 124 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+isoflavone | 142 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+hinokitiol | 125 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+benzyl nicotinate | 129 |
From last table 1 as can be seen, 4-pyrrolidine-2 of the present invention, such your ability that papilla cell is bred is identical to the ability of papilla cell propagation and rice for 6-di-amino-pyrimidine-1-oxide.Using 4-pyrrolidine-2, in the common groups of cells of handling of each material in 6-di-amino-pyrimidine-1-oxide and 16 kinds, it is independent with 4-pyrrolidine-2, the value-added ability of promotion cell of the group of 6-di-amino-pyrimidine-1-oxide process to promote the value-added ability of cell to be higher than.
In addition, also detected 4-pyrrolidine-2 of the present invention according to mode same as described above with 0.1,1 concentration different with 10ppm, 6-di-amino-pyrimidine-1-oxide is to the ability of papilla cell propagation, with testing result with only compare with the matched group of DMSO solution-treated, with the relative different of definite absorbance.Testing result is as shown in table 2.As can be seen from Table 2,4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide increases in dosage dependence mode the ability of papilla cell propagation.
Embodiment 3:4-pyrrolidine-2, the test of the 6-di-amino-pyrimidine-hair growth effect of 1-oxide in mice
Remove the hair at 47-53 days mice (C57BL/6) back, and from these mices, select mice with clean back.The mice of selecting is divided into 18 groups, forms by 8 for every group.The mice group continues 21 days respectively for the following substances with 150 μ l every day, and to test the hair growth effect of these materials: negative matched group is made up of water/ethanol/1,3 butylene glycol (5/3/2); By by with 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide is dissolved in the compositions that obtains in the negative control vector with the concentration of 0.5 weight %; With by by each following substances is dissolved in the described 4-of containing pyrrolidine-2 with the concentration of 1 weight %, the compositions that is obtained in the compositions of 6-di-amino-pyrimidine-1-oxide, described following substances are respectively thujae semen, vitamin B5 derivant (panthenol derivant), Herba Swertiae bimaculatae extract, Semen Coicis, Radix Glycyrrhizae extract (glycyrrhizin and glycyrrhetinic acid), niacin amide (nicotiamide), vitamin e derivative (vitamin e acetate etc.), adenosine, tripentadecanoin (PDG), the 6-benzylaminopurine, acetaminol, GAIWUZONGLV, the dialkyl monoamine derivant, isoflavone, hinokitiol and benzyl nicotinate.
After 21 days, take pictures observing the hair growth situation of mice to mice, the weight of the hair that newly grows of weighing test group, and compare with the hair that newly grows of negative matched group.What record the results are shown among table 2 and Fig. 3.
Table 2
| Processed group | Hair weight (mg) |
| Negative matched |
40±18 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 69±12 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+thujae semen | 85±8 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+D-panthenol | 87±12 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+Herba Swertiae bimaculatae abstract | 88±19 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+Semen Coicis | 78±10 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+Radix Glycyrrhizae extract | 82±16 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+niacin amide | 78±8 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+vitamin e acetate | 75±10 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+adenosine | 88±13 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+tripentadecanoin | 79±12 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+benzylaminopurine | 75±10 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+acetaminol | 82±17 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+GAIWUZONGLV | 73±9 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+dialkyl monoamine derivant | 86±12 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+isoflavone | 90±12 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+hinokitiol | 86±11 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide+benzyl nicotinate | 89±14 |
As can be seen from Table 2, compare with the group of using negative matched group (water/ethanol/1,3 butylene glycol), 4-pyrrolidine-2 of the present invention, 6-di-amino-pyrimidine-1-oxide make hair increase about 29mg.In addition, can also observe, with independent use 4-pyrrolidine-2, the processed group of 6-di-amino-pyrimidine-1-oxide is compared, with 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide can optionally be used for the higher hair growth effect of group demonstration that composition of the present invention is used with 16 kinds respectively.
From the result of table 2 as can be seen, the telogen that 4-pyrrolidine-2 of the present invention, 6-di-amino-pyrimidine-1-oxide act on mice with stimulate to the hair life cycle the anagen change, thereby promoted the growth of mice hair.
Hereinafter, will provide various example of formulations according to described test implementation example.Yet, it will also be apparent to those skilled in the art that the example of formulations that provides is used to illustrate the present invention rather than in order to limit the scope of the invention.
Example of formulations 1: hair moisturizer
Table 3
| Composition | Content (weight %) |
| Ethanol | 55 |
| Oleum Ricini | 5 |
| Glycerol | 3 |
| Piroctone olamine salt (piroctoneolamine) | 0.1 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 1.0 |
| Clock cypress seed | 1.0 |
| Spice and pigment | In right amount |
| Purify waste water | Surplus (to 100) |
Example of formulations 2: hair care dew (Hair lotion)
Table 4
| Composition | Content (weight %) |
| Cetostearyl alcohol (Cetostearylalcohol) | 2.0 |
| The octadecyl triethyl ammonium chloride | 2.0 |
| Hydroxyethyl-cellulose | 0.5 |
| Piroctone olamine salt | 0.1 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 1.0 |
| Semen Coicis | 1.0 |
| Spice and pigment | In right amount |
| Purify waste water | Surplus (to 100) |
Example of formulations 3: trichotrophy reveals (Hair nourishing lotion)
Table 5
| Composition | Content (weight %) |
| Cera Flava | 4.0 |
| Poly-solvate (Polysolvate) 60 | 1.5 |
| Sorbitan sesquioleate | 0.7 |
| Liquid paraffin | 5.0 |
| Squalane | 5.0 |
| Caprylic/capric triglyceride | 5.0 |
| Glycerol | 3.0 |
| Butanediol | 3.0 |
| Propylene glycol | 3.0 |
| Carbopol (Carboxyvinyl polymer) | 0.1 |
| Triethanolamine | 0.2 |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 0.5 |
| Herba Swertiae bimaculatae extract | 0.5 |
| Antiseptic | In right amount |
| Spice and pigment | In right amount |
| Purify waste water | Surplus (to 100) |
Example of formulations 4: skin cream
Table 6
| Composition | Content (weight %) |
| Purify waste water | Surplus (to 100) |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 0.1 |
| Tripentadecanoin | 0.1 |
| Butanediol | 2.0 |
| Propylene glycol | 2.0 |
| CVP Carbopol ETD2050 | 0.1 |
| The PEG-12 nonylplenyl ether | 0.2 |
| Poly- |
0.4 |
| Ethanol | 10.0 |
| Triethanolamine | 0.1 |
| Antiseptic, pigment and spice | In right amount |
Example of formulations 5: milk skin cream
Table 7
| Composition | Content (weight %) |
| Purify waste water | Surplus (to 100) |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 0.1 |
| Niacin amide | 0.1 |
| Cera Flava | 4.0 |
| Poly- |
1.5 |
| Sorbitan sesquioleate | 1.5 |
| Liquid paraffin | 0.5 |
| Caprylic/capric triglyceride | 5.0 |
| Glycerol | 3.0 |
| Butanediol | 3.0 |
| Propylene glycol | 3.0 |
| CVP Carbopol ETD2050 | 0.1 |
| Triethanolamine | 0.2 |
| Antiseptic, pigment and spice | In right amount |
Example of formulations 6: nourishing cream
Table 8
| Composition | Content (weight %) |
| Purify waste water | Surplus (to 100) |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 0.1 |
| Radix Glycyrrhizae extract | 0.1 |
| Cera Flava | 10.0 |
| Poly- |
1.5 |
| The PEF-60 castor oil hydrogenated | 2.0 |
| Sorbitan sesquioleate | 0.5 |
| Liquid paraffin | 10.0 |
| Squalane | 5.0 |
| Caprylic/capric triglyceride | 5.0 |
| Glycerol | 5.0 |
| Butanediol | 3.0 |
| Propylene glycol | 3.0 |
| Triethanolamine | 0.2 |
| Antiseptic, pigment and spice | In right amount |
Example of formulations 7: massage cream
Table 9
| Composition | Content (weight %) |
| Purify waste water | Surplus (to 100) |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 0.1 |
| Isoflavone | 0.1 |
| Cera Flava | 10.0 |
| Poly- |
1.5 |
| The PEG-60 castor oil hydrogenated | 2.0 |
| Sorbitan sesquioleate | 0.8 |
| Liquid paraffin | 40.0 |
| Squalane | 5.0 |
| Caprylic/capric triglyceride | 4.0 |
| Glycerol | 5.0 |
| Butanediol | 3.0 |
| Propylene glycol | 3.0 |
| Triethanolamine | 0.2 |
| Antiseptic, pigment and spice | In right amount |
Example of formulations 8: hair care scalp pomade (pack)
Table 10
| Composition | Content (weight %) |
| Purify waste water | Surplus (to 100) |
| 4-pyrrolidine-2,6-di-amino-pyrimidine-1-oxide | 0.1 |
| Hinokitiol | 0.1 |
| Polyvinyl alcohol | 13.0 |
| Sodium carboxymethyl cellulose | 0.2 |
| Glycerol | 5.0 |
| Allantoin | 0.1 |
| Ethanol | 6.0 |
| The PEG-12 nonylplenyl ether | 0.3 |
| Poly- |
0.3 |
| Antiseptic, pigment and spice | In right amount |
Claims (6)
1, a kind of trichogenous topical composition, said composition contains the 4-pyrrolidine-2 as active component, and 6-di-amino-pyrimidine-1-oxide and one or more are selected from the material in the group of being made up of thujae semen, vitamin B5 derivant, Herba Swertiae bimaculatae extract, Semen Coicis, Radix Glycyrrhizae extract, niacin amide, vitamin e derivative, adenosine, tripentadecanoin, 6-benzylaminopurine, acetaminol, GAIWUZONGLV, dialkyl monoamine derivant, isoflavone, hinokitiol and benzyl nicotinate.
2, compositions according to claim 1, said composition be a kind of can be in cell the potassium channels opening compositions of horizontal vasodilator and blood circulation promoting.
3, compositions according to claim 1, said composition are a kind of compositionss that can promote hair follicle cell propagation.
4, compositions according to claim 1 wherein, is a benchmark with the gross weight of described compositions, and described 4-pyrrolidine-2, the content of 6-di-amino-pyrimidine-1-oxide are 0.001-10 weight %.
5, compositions according to claim 1, wherein, gross weight with described compositions is a benchmark, and the described content that one or more are selected from the material in the group of being made up of thujae semen, vitamin B5 derivant, Herba Swertiae bimaculatae extract, Semen Coicis, Radix Glycyrrhizae extract, niacin amide, vitamin e derivative, adenosine, tripentadecanoin, 6-benzylaminopurine, acetaminol, GAIWUZONGLV, dialkyl monoamine derivant, isoflavone, hinokitiol and benzyl nicotinate is 0.005-5 weight %.
6, compositions according to claim 1, said composition are formulated into the form that is selected from the group of being made up of hair moisturizer, anti-dandruff hair conditioner, shampoo, hair care breast, general ointment, skin cream, milk skin cream, eye cream, nourishing cream, massage cream, cleansing cream, cleaning foam and cleaning powder.
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| KR10-2005-0097502 | 2005-10-17 | ||
| KR1020050097502A KR100992565B1 (en) | 2005-10-17 | 2005-10-17 | Topical preparations for hair growth |
| PCT/KR2006/002412 WO2007046577A1 (en) | 2005-10-17 | 2006-06-22 | External composition for hair growth |
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| CN101291651B CN101291651B (en) | 2011-05-18 |
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| KR (1) | KR100992565B1 (en) |
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Also Published As
| Publication number | Publication date |
|---|---|
| CN101291651B (en) | 2011-05-18 |
| KR20070041890A (en) | 2007-04-20 |
| WO2007046577A1 (en) | 2007-04-26 |
| KR100992565B1 (en) | 2010-11-08 |
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