CN101530407A - Hair growing preparation for treating androgenetic alopecia and preparation method thereof - Google Patents
Hair growing preparation for treating androgenetic alopecia and preparation method thereof Download PDFInfo
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- CN101530407A CN101530407A CN200910049146A CN200910049146A CN101530407A CN 101530407 A CN101530407 A CN 101530407A CN 200910049146 A CN200910049146 A CN 200910049146A CN 200910049146 A CN200910049146 A CN 200910049146A CN 101530407 A CN101530407 A CN 101530407A
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Abstract
The invention discloses a hair growing preparation for treating androgenetic alopecia and a preparation method thereof. The hair growing preparation comprises more than one of chlorogenic acid or chlorogenic acid isomers with treatment effective dose, a pharmaceutically accepted carrier and other active substances. Human tests prove that the hair growing preparation with the effect of treating androgenetic alopecia has significant action on treating the androgenetic alopecia without toxicity or other side effects, and can be applied to a patient to be treated by a smearing mode, wherein the amount of administration is 0.2 to 0.5ml per time and 2 to 3 times per day. The hair growing preparation and the preparation method thereof have the advantages of active ingredients from natural plant ingredient, convenient preparation, easy use, good treatment effect and small side effect.
Description
Technical field
The present invention relates to a kind of preparation for the treatment of alopecia, relate in particular to a kind of external preparation with the effect of treatment androgenetic alopecia.
Background technology
Androgenetic alopecia is owing to the local androgen of scalp causes that too much 5a-reductase has important related with this disease unusually.Testosterone changes into dihydrotestosterone in the scalp hair follicle under the effect of 5a reductase, and dihydrotestosterone diminishes hair follicle gradually, and pigment generates and reduces, and the anagen phase shortens, and resting stage prolongs, and causes alopecia.Therefore, suppress the activity of 5a reductase and can block the dihydro of testosterone, thereby improve the alopecia symptom of android type.Patient's alopecia district 5a reductase distributes many, and is active high, local androgen receptor sensitivity height.II type 5a-reductase is distributed in external root sheath internal layer, hair follicle proximal end region, inner root sheath and infundibulum of hair follicle portion.Finasteride is the oral drugs that are used for alopeciaing therapeutic of the first approval of FDA, be selectivity II type 5a-reductase inhibitor, 1998 in U.S.'s Initial Public Offering, external existing a large amount of clinical datas confirm its curative effect, the domestic randomized, double-blind experiment of 228 male patients being carried out by Peking University First Hospital's Dermatology ﹠ STD Dept. 6 months shows the 1mg finasteride tablet--guarantor's method is ended
RCan effectively control hair continue come off, promote the growth of hair.But oral finasteride exists such as side effect such as sexual hypofunctions.Therefore, seek natural 5a-reductase inhibitor from natural plants, by the mode of local topical, through lesion root of hair with the toxic and side effects of avoiding oral administration to bring, is an important topic of this area.
Summary of the invention
One of purpose of the present invention is open chlorogenic acid or the application of its isomer in preparation treatment androgenetic alopecia disease medicament, to overcome the above-mentioned defective that prior art exists.
Two of purpose of the present invention provides a kind of germinal preparation with the effect of treatment androgenetic alopecia.
The inventor finds, chlorogenic acid or chlorogenic acid isomer, have and concentration dependent 5a reductase inhibitory action, be made into the external hair preparation, can suppress alopecia district 5a reductase activity, stop the interior testosterone of scalp hair follicle under the effect of 5a reductase, to change into DHT, thereby prolong the anagen phase, reduce alopecia;
Therefore, described chlorogenic acid or chlorogenic acid isomer can be used to prepare the medicine for the treatment of the androgenetic alopecia disease;
Preferably, described chlorogenic acid or chlorogenic acid isomer derive from natural plants, as the Cortex Eucommiae, Flos Lonicerae, Helianthi, continue flower, coffee or cocoa tree etc., can adopt document: precious traditional Chinese medical science traditional Chinese medicines 2007,18 (2): 446-448 when the extraction purification of chlorogenic acid is studied [J] in the Folium Eucommiae; The chlorogenic acid extraction process is relatively inquired into [J] Liaoning Journal of Traditional Chinese Medicine 2008,35 (2): 262-264 with optimization in the Flos Lonicerae; Chlorogenic acid and extraction separation method thereof are commented [J] Chinese patent medicine, and reported method such as 2001,23 (2): 135-138 are prepared and extract;
Described chlorogenic acid isomer is made up of single caffeoyl guinic acid and dicaffeoyl quinic acid, comprises neochlorogenic acid, 4-dicaffeoylquinic acid, isochlorogenic acid A, isochlorogenic acid B, isochlorogenic acid C or Lay silibin;
Described chlorogenic acid molecular structure is as follows:
English Chlorogenic acid by name, molecular formula C
16H
18O
9, molecular weight is 354.31, CAS accession number: 327-97-9;
Described isochlorogenic acid A molecular structure is as follows:
English name is Isochlorogenic acid A, and molecular formula is C25H24O12, and molecular weight is 516.45, CAS accession number: 2450-53-5
The chemical constitution of neochlorogenic acid, 4-dicaffeoylquinic acid, isochlorogenic acid B, isochlorogenic acid C or Lay silibin is commented [J] Chinese patent medicine, 2001,23 (2): on 135-138, clear and definite report is arranged also at document chlorogenic acid and extraction separation method thereof.
The invention still further relates to a kind of germinal preparation with treatment androgenetic alopecia effect, described germinal preparation comprise the described chlorogenic acid for the treatment of effective dose or in the chlorogenic acid isomer more than one, pharmaceutically acceptable carrier and other active substances;
Preferably, the content of chlorogenic acid or chlorogenic acid isomer is 0.1g～10g/1000ml;
Described other active substances comprise tea polyphenols or caffeine etc., and consumption is 0.1～10g/1000ml;
Described carrier comprises more than one in diluent, transdermal enhancer, antiseptic, antioxidant or the emulsifying agent etc., and consumption is 980～1000g/1000ml hair growth promoter;
Described diluent such as water, ethanol, Polyethylene Glycol, glycerol, lanoline, vaseline, octadecanol or carbopol etc.;
Described transdermal enhancer such as oleic acid, lauric acid, azone, propylene glycol or menthol etc.;
Described antiseptic such as sorbic acid, benzalkonium chloride, chlorobutanol, methyl hydroxybenzoate, ethyl hydroxybenzoate or propyl ester etc.;
Described antioxidant such as sodium sulfite, cysteine, L-ascorbic acid or disodiumedetate etc.;
Described emulsifying agent such as span, tween, arabic gum or sodium carboxymethyl cellulose etc.;
The inventor finds, the selection of carrier also will produce material impact to therapeutic effect, and preferred, the weight portion of each component is:
0.1～10 part of chlorogenic acid and/or its isomer
0～10 part of other active substance
0～50 part of transdermal enhancer
0.25～0.5 part of antiseptic
0～1000 part of diluent
0～1 part in antioxidant
0～50 part of emulsifying agent.
Further preferred, the weight portion of each component is:
0.1～10 part of chlorogenic acid and/or its isomer
0.1～10 part of other active substance
10～50 parts of transdermal enhancers
0.25～0.5 part of antiseptic
250～1000 parts of diluent
0.5～1 part in antioxidant
10～50 parts of emulsifying agents.
Can adopt method well known in the art, described germinal preparation be made multiple exterior-applied formulations such as unguentum, Emulsion, spray, liniment or lotion.
Human trial proves, germinal preparation with the effect of treatment androgenetic alopecia of the present invention, has significant effect for the treatment androgenetic alopecia, and avirulence and other side effect, can adopt the patient that the mode of smearing puts on needs treatment, dosage is for once smearing 0.2～0.5ml, one day 2～3 times.
Advantage of the present invention is fairly obvious, and the external hair formulation preparation that contains chlorogenic acid and/or its isomer is convenient, use easily, and good effect, side effect is little.
The specific embodiment
In following examples, the evaluation methodology of alopecia degree is as follows:
In general, androgenetic alopecia can be divided into seven grades, alopecia originally, and a lot of people may not mind; But in second～Pyatyi of following, the hair line of forehead can be the M font and constantly move backward, and the alopecia scope on the crown also can enlarge gradually; Promptly claim " Mediterranean " to the six～seven grade.First and second level is slight alopecia, and the 3rd～Pyatyi is the moderate alopecia, and the 6th, seven grade is the severe alopecia.
Document Male pattern baldness:classification and incidence[J] South MedJ, 1975,68:1359-1365 has reported a kind of (classification of Norwood-Hamilton Hamilton) chart is specialist is used for assessing the male pattern alopecia different phase under no instrument helps a standard grading.
In following examples, the evaluation methodology of curative effect is as follows:
Alopecia place hair grows fully, basic identically before its thickness and color and luster and the alopecia is recovery from illness, and alopecia district or alopecia sheet growth hair be produce effects 70% or more, has hair or hair to grow 30-70% but density is little, lighter color is improvement; Alopecia place does not have any variation person for invalid.
Embodiment 1
Chlorogenic acid 0.6g, caffeine 1g are dissolved in 1000ml70% ethanol, add 3g transdermal enhancer azone and 0.25g antiseptic benzalkonium chloride, mix, and promptly obtain germinal preparation 1000ml;
15 male are light, hair growth promoter twice is smeared in moderate hair loss patient alopecia every day district, and dosage is for once smearing 0.5ml, use 7 people improvement after March, 5 people's produce effects, and 3 people are invalid, effective percentage 80%.Do not see any side effect.
Embodiment 2
Neochlorogenic acid 3g, tea polyphenols 0.5g are dissolved in 300ml water, add 50g transdermal enhancer propylene glycol, the 20mg cysteine, and 200g lanoline, 550g vaseline are made unguentum 1000ml.
Hair growth promoter twice is smeared in 12 30～50 years old male pattern baldness patient alopecia every day districts, and dosage is for once smearing 0.2ml, and 5 people take a turn for the better after treatment March, 4 people's produce effects, and 3 people are invalid, and effective percentage 75% is not seen any side effect.
Embodiment 3
Isochlorogenic acid A, B, C mixture 6g are dissolved in the 500ml30% ethanol, add 20g transdermal enhancer menthol, 250g octadecanol, 50g polyoxyethylene (40) monostearate, 250g vaseline and 0.3g methyl hydroxybenzoate, make Emulsion 1000ml.
21 30～50 years old male are light, hair growth promoter twice is smeared in moderate hair loss patient alopecia every day district, and dosage is for once smearing 0.3ml, 3 people recovery from illness after treatment March, and 6 people improvement, 10 people's produce effects, 3 people are invalid, and effective percentage 76% is not seen any side effect.
Embodiment 4,5a reductase inhibition test
Test method: adopt document: high performance liquid chromatography in-vitro screening model [J] the University of Fuzhou journal of steroidal 5a-reductase inhibitor, 2005,33 (5): the 661-664. reported method.
Chlorogenic acid/hair growth promoter or finasteride, substrate testosterone, tris buffer, zyme extract (rat liver extraction), coenzyme NADP 11 are sequentially added into centrifuge tube, mix homogeneously, 37 ℃ of water-bath 30min, 0,30min sampling, add the ethyl acetate stopped reaction, measure the substrate testosterone concentration.Chromatographic condition: Diamonsil C18 chromatographic column (250 * 4.6mm, 5um); Column temperature: room temperature; Mobile phase: 70% methanol; Flow velocity: 1ml/min; Detect wavelength: 242nm.Result such as table 1:
The enzyme inhibition of table 1. chlorogenic acid and/or its isomer
Above experimental result explanation chlorogenic acid and/or its isomer have 5a reductase inhibitory action, can suppress alopecia district 5a reductase activity, have hair regrowth.
Claims (10)
1. chlorogenic acid or the chlorogenic acid isomer application in preparation treatment androgenetic alopecia disease medicament.
2. application according to claim 1 is characterized in that, described chlorogenic acid isomer comprises neochlorogenic acid, 4-dicaffeoylquinic acid, isochlorogenic acid A, isochlorogenic acid B, isochlorogenic acid C or Lay silibin.
3. application according to claim 1 is characterized in that, described chlorogenic acid or chlorogenic acid isomer derive from natural plants or synthetic.
4. one kind has the germinal preparation for the treatment of the androgenetic alopecia effect, it is characterized in that, described germinal preparation comprise each chlorogenic acid of claim 1～3 for the treatment of effective dose or in the chlorogenic acid isomer more than one, pharmaceutically acceptable carrier and other active substances.
5. germinal preparation according to claim 4 is characterized in that, the content of chlorogenic acid or chlorogenic acid isomer is 0.1g～10g/1000ml.
6. germinal preparation according to claim 4 is characterized in that, described other active substances are more than one in tea polyphenols or the caffeine, and consumption is 0.1～10g/1000mL.
7. germinal preparation according to claim 4 is characterized in that described carrier comprises more than one in diluent, transdermal enhancer, antiseptic, antioxidant or the emulsifying agent, and consumption is 980～1000g/1000mL hair growth promoter;
Described diluent is selected from water, ethanol, Polyethylene Glycol, glycerol, lanoline, vaseline, octadecanol or carbopol etc.;
Described transdermal enhancer is selected from oleic acid, lauric acid, azone, propylene glycol or menthol etc.;
Described antiseptic is selected from sorbic acid, benzalkonium chloride, chlorobutanol, methyl hydroxybenzoate, ethyl hydroxybenzoate or propyl ester etc.;
Described antioxidant is selected from sodium sulfite, cysteine, L-ascorbic acid or disodiumedetate etc.;
Described emulsifying agent is selected from polyoxyethylene (40) stearate, span, tween, arabic gum or sodium carboxymethyl cellulose etc.
8. germinal preparation according to claim 4 is characterized in that, the weight portion of each component is:
0.1～10 part of chlorogenic acid and/or its isomer
0～10 part of other active substance
0～50 part of transdermal enhancer
0.25～0.5 part of antiseptic
0～1000 part of diluent
0～1 part in antioxidant
0～50 part of emulsifying agent.
9. germinal preparation according to claim 4 is characterized in that, the weight portion of each component is:
0.1～10 part of chlorogenic acid and/or its isomer
0.1～10 part of other active substance
10～50 parts of transdermal enhancers
0.25～0.5 part of antiseptic
250～1000 parts of diluent
0.5～1 part in antioxidant
10～50 parts of emulsifying agents.
10. according to each described germinal preparation of claim 4～9, it is characterized in that described germinal preparation is unguentum, Emulsion, spray, liniment or the lotion that is applicable to the external transdermal administration.
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| CN200910049146A CN101530407A (en) | 2009-04-10 | 2009-04-10 | Hair growing preparation for treating androgenetic alopecia and preparation method thereof |
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| CN200910049146A CN101530407A (en) | 2009-04-10 | 2009-04-10 | Hair growing preparation for treating androgenetic alopecia and preparation method thereof |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011129399A1 (en) * | 2010-04-15 | 2011-10-20 | 花王株式会社 | Srebp inhibitor |
| EP2873440A1 (en) * | 2013-11-19 | 2015-05-20 | DSM IP Assets B.V. | Use of an edelweiss extract in hair care for stimulating hair growth |
| CN104287996B (en) * | 2013-07-15 | 2018-02-16 | 江西普正制药有限公司 | A kind of bark of eucommia shampoo and preparation method thereof |
| CN109010182A (en) * | 2018-09-26 | 2018-12-18 | 名臣健康用品股份有限公司 | A kind of Anti-hair loss composition and its application in hair products is washed in preparation |
| EP3328406A4 (en) * | 2015-07-27 | 2019-05-01 | MOREIRA, Nivaldo José | Mulateiro-derived compositions and use thereof for preventing hair loss and promoting hair growth |
| CN110403882A (en) * | 2019-09-02 | 2019-11-05 | 佛山科学技术学院 | A kind of shampoo with hair-growing and hair care effect |
-
2009
- 2009-04-10 CN CN200910049146A patent/CN101530407A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011129399A1 (en) * | 2010-04-15 | 2011-10-20 | 花王株式会社 | Srebp inhibitor |
| JP2011225455A (en) * | 2010-04-15 | 2011-11-10 | Kao Corp | Srebp inhibitor |
| CN104287996B (en) * | 2013-07-15 | 2018-02-16 | 江西普正制药有限公司 | A kind of bark of eucommia shampoo and preparation method thereof |
| EP2873440A1 (en) * | 2013-11-19 | 2015-05-20 | DSM IP Assets B.V. | Use of an edelweiss extract in hair care for stimulating hair growth |
| EP3328406A4 (en) * | 2015-07-27 | 2019-05-01 | MOREIRA, Nivaldo José | Mulateiro-derived compositions and use thereof for preventing hair loss and promoting hair growth |
| CN109010182A (en) * | 2018-09-26 | 2018-12-18 | 名臣健康用品股份有限公司 | A kind of Anti-hair loss composition and its application in hair products is washed in preparation |
| CN110403882A (en) * | 2019-09-02 | 2019-11-05 | 佛山科学技术学院 | A kind of shampoo with hair-growing and hair care effect |
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Open date: 20090916 |