CN104666144A - 5alpha-reductase inhibitor and application thereof - Google Patents
5alpha-reductase inhibitor and application thereof Download PDFInfo
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- CN104666144A CN104666144A CN201310625349.XA CN201310625349A CN104666144A CN 104666144 A CN104666144 A CN 104666144A CN 201310625349 A CN201310625349 A CN 201310625349A CN 104666144 A CN104666144 A CN 104666144A
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- 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
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
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Abstract
The invention discloses a 5alpha-reductase inhibitor and application thereof and particularly discloses application of a litchi shell extract as the 5alpha-reductase inhibitor, application of the litchi shell extract as an additive with the functions of the 5alpha-reductase inhibitor in preparation of personal care products having efficacies of controlling oil and resisting acne and application of the litchi shell extract as an additive with the functions of the 5alpha-reductase inhibitor in preparation of personal care products having efficacy of preventing hair loss.
Description
Technical field
The present invention relates to and a kind of there is the inhibiting Chinese medicine of 5α-reductase and the application in personal care product thereof, be specifically related to Litchi Pericarp Extract and the application in personal care product thereof.
Background technology
Acne, alopecia are all clinical common pertinacious diseases, crowd occur extensive, although acne, hair loss disorders can't critical life, usually cause serious mental burden to patient.Along with society competition, living environment worsens, and acne, alopecia incidence rate have the trend of rising in recent years, but still deficienter for effective product of acne, alopecia at present.
Cause acne, alopecia factor a lot, but modern medicine thinks that local androgen Developmental and Metabolic Disorder may be the topmost cause of disease.Because sebaceous gland volume can be caused to increase for Hyperandrogenism and sebum secretion increases, and abnormal cornification of pilosebaceous duct, causes sebum drainage difficulty, forms fat bolt, causes acne; In hair, androgen excessively can impel hair follicle atrophy, shortens the growth cycle of hair, cause hair soft, sparse, come off.Testosterone (T), dihydrotestosterone (DHT) are two kinds of important endogenous androgens, can combine produce corresponding physiological action to androgen receptor.It should be noted that testosterone changes into dihydrotestosterone by 5α-reductase, and the affinity of dihydrotestosterone is more than 5 times of testosterone.So 5α-reductase increased activity or increasing number all may cause acne, the generation of alopecia and deterioration.
In human body, found 5α-reductase 3 hypotypes, studying more is 1 type and 2 types.I type 5α-reductase is mainly present in non-genital skin, hair follicle (ball top, fiber, superior lateral cutaneous root sheath), sebaceous gland, liver, brain, mainly relevant to hirsutism, acne, male pattern baldness; II type 5α-reductase is mainly expressed in prostate, and inside seminal vesicle, genital skin, hair follicle, epithelial root sheath also has certain existence, main as relevant in benign prostatic hyperplasia, polycystic ovary syndrome with some androgenic disorder associated diseases; III type 5α-reductase is expressed in liver, prostate, kidney, skin, relevant with the nascent protein glycosylation that N-connects.Current research is thought, acne, alopecia are the most relevant to 1 type 5α-reductase, so 1 type 5α-reductase can as molecule target when controlling fat secretion, anti-acne, the screening of Anti-hair loss functional component.
Along with the proposition that natural, safety and environment protection require, green personal care product is more and more by people are favored.Natural resources of Chinese medicinal materials enriches, and has the applicating history of several thousand, has natural safe feature, so the additive of effective personal care product in exploitation Chinese medicine source, will obtain the welcome of consumer.
Exocarpium Litchi, the outer peel of Sapindaceae Fructus Litchi platymiscium Fructus Litchi (Litchi Chinensis Sonn.) is one of by-product of Fructus Litchi, and greatly, development and application values is high for easily acquisition, output.Exocarpium Litchi nature and flavor are bitter, cold, enter heart channel.The traditional Chinese medical science is thought that Exocarpium Litchi has and is regulated the flow of vital energy, pain relieving, promotes the production of body fluid, beneficial blood, controls excessive thirst, astringent therapy effect, cures mainly dysentery, metrorrhagia, eczema; Stomachache, toothache, traumatic hemorrhage; Gastric abscess, colicky, women's pricking caused by the stagnation of QI and blood etc.According to bibliographical information, Exocarpium Litchi contains the compositions such as flavonoid, phenolic acid, polysaccharide, has antioxidation, regulates the functions such as HypercholesterolemicRats, anticancer, immunomodulating, whitening; In the existing patent that Exocarpium Litchi is relevant, report the acquisition methods of some composition in Exocarpium Litchi, as extract from litchi rind phlorhizin technique (CN201110219029.5), a kind of from Fructus Litchi, extract lichee polyphenol method (CN200510093663.3), the method for purification (CN201010172018.1) of phloretin powder, a kind of extraction process (CN102898411A) of procyanidin, a kind of phlorizin in litchi peels Isolation and purification method (CN102086220A) etc.Also scholar's another medicinal part to plant Fructus Litchi is had to do some researchs, the i.e. dry mature seed Semen Litchi of Fructus Litchi, think that it has the effects such as blood sugar lowering, blood fat reducing, antitumor, anti-bacteria and anti-virus, in skin, there is the effect such as antioxidation, defying age, anti-saccharifying open, as the natural product inhibitor (CN200980121805.2) of patent 3-deoxyglucosone, patent anti-gfycation agent (CN201010546567.0).
Litchi pulp is conventional food, and Fructus Litchi pit is the Chinese crude drug of regulating QI to relieve pain simply, also very insufficient to the utilization of Exocarpium Litchi at present.In Fructus Litchi processing and process of consumption, Exocarpium Litchi directly cleans out usually used as garbage.Inventor is in research process, and unexpected discovery Exocarpium Litchi has good 5α-reductase inhibitory action, and the Chinese herbal medicine additive that can be developed to as control oil, anti-acne, Anti-hair loss is applied in cosmetics.Because with low cost, wide material sources, have good application prospect, also can improve the present situation of the Exocarpium Litchi wasting of resources.Exocarpium Litchi there is no any report to 5α-reductase inhibitory action.Late Cambrian Litchi Pericarp Extract of the present invention can add in personal care product as oil-control secretion, anti-acne or Anti-hair loss active component and uses.
Summary of the invention
The object of the invention is to provide one to have the inhibiting Chinese medicine extract of 5α-reductase, and it can be used as additive and adds in the personal care product with oil-control secretion, anti-acne or Anti-hair loss function.
Litchi Pericarp Extract can extract in the following manner:
Pure Chinese crude drug, fully mixes with the solvent of certain proportioning consumption, is positioned in extractor, extract with corresponding extracting method.After end to be extracted, recycling design obtains extract powder, directly applies to personal care product; Also addible solvent in extract water or glycerol or butanediol or the personal care product formulations such as propylene glycol or oils and fats can be carried out redissolving to finite concentration, also can add appropriate antiseptic as required, be applied to personal care product.
Producing of Litchi Pericarp Extract also can take supercritical extraction, subcritical abstraction, organic solvent extraction.The solvent of organic solvent extraction comprises the ethanol of low polar solvent and variable concentrations in normal hexane, ethyl acetate, ether, petroleum ether, acetone etc., methanol and polyhydric alcohol etc.Extracting method can be the methods such as reflux, extract, dipping, percolation.And, method that is ultrasonic or microwave can also be used in leaching process to assist.
First aspect, the present invention relates to the purposes of Litchi Pericarp Extract in 5α-reductase suppresses.
Second aspect, the present invention relates to Litchi Pericarp Extract and is preparing as having the inhibiting additive of 5α-reductase the purposes had in the personal care product controlling oily anti-acne effect.
The third aspect, the present invention relates to Litchi Pericarp Extract and is preparing as having the inhibiting additive of 5α-reductase the purposes had in the personal care product of Anti-hair loss effect.
According to of the present invention one preferred embodiment, by weight percentage, the consumption of Litchi Pericarp Extract is 0.0001%-100%, preferred 0.01%-50%, more preferably 0.1%-10%.
Personal care product of the present invention can be the acceptable any dosage form of skin or hair, comprising: facial milk cleanser, astringent, emulsion, cream frost, gel, facial film, shampoo, hair conditioner, hair-care essence, fancy soap, but is not limited thereto.In one embodiment, personal care product of the present invention comprises Litchi Pericarp Extract and acceptable adjuvant.
In one embodiment, personal care product comprises the Litchi Pericarp Extract of 0.0001-100 % by weight.In another embodiment, personal care product comprises the Litchi Pericarp Extract of 0.01%-50 % by weight.In another embodiment, personal care product comprises the Litchi Pericarp Extract of 0.1%-10 % by weight.
Accompanying drawing explanation
The 5α-reductase that Fig. 1 shows the Litchi Pericarp Extract of normal group, matched group and variable concentrations urgees reaction rate.
The Litchi Pericarp Extract that Fig. 2 shows positive control and variable concentrations urgees the suppression ratio reacted to 5α-reductase.
Detailed description of the invention
The inhibitory action of Exocarpium Litchi to 5α-reductase has no any report, belongs to Late Cambrian.And inventor surprisingly finds by experiment, the inhibitory action of Exocarpium Litchi to 5α-reductase is remarkable.Exocarpium Litchi wide material sources, safety non-toxic, therefore considering can as the functional additive of desirable personal care product.In addition, because inventor has surprisingly found the inhibitory action of Litchi Pericarp Extract to 5α-reductase, Litchi Pericarp Extract can as additive for the preparation of the various personal care products with oil-control secretion, anti-acne, Anti-hair loss function.
The present inventor finds after have passed through extensive and deep research: Litchi Pericarp Extract has 5α-reductase inhibitory action.
Therefore, Litchi Pericarp Extract can be used as functional additive and joins in personal care product.
All do not relate to Litchi Pericarp Extract in document and have 5α-reductase inhibitory action, also the not mentioned functional additive that it can be used as adds in personal care product.Therefore, the present invention proposes Litchi Pericarp Extract first and has 5α-reductase inhibitory action, can add in personal care product as functional additive, add in personal care product the effect playing control oil, anti-acne as personal care product's additive to, or Anti-hair loss effect can be played when adding in hair products.
In personal care product's application, Litchi Pericarp Extract application form can be any dosage forms that can be applied to human body skin or hair such as facial milk cleanser, astringent, emulsion, cream frost, gel, facial film, shampoo, hair conditioner, hair-care essence, fancy soap.
Other compositions beyond Litchi Pericarp Extract can be any compositions that personal care product formulations needs, as: water, ethanol, butanediol, propylene glycol, oils and fats, emulsifying agent, thickening agent, antiseptic etc.; Also can add other functional components and reach complex function, as: add moisturizing ingredient and become the oily moisturizing personal care product of control, add whitening composition to make to become pox-eliminating whitening personal care product, add aging ingredient and become the oily defying age personal care product of control, add scalp tonic and become to be divided into nourishing anticreep shampoo/hair conditioner/hair-care essence, add anti-dandruff agent and become oily dandruff control shampoo containing/hair conditioner/hair-care essence of control etc.
Generally speaking, by weight percentage, the working concentration of Litchi Pericarp Extract can in 0.0001%-100% scope.Preferably, the working concentration of Litchi Pericarp Extract can in 0.01-50% scope.More preferably, the working concentration of Litchi Pericarp Extract can in 0.1%-10% scope.
In one embodiment, the working concentration of Litchi Pericarp Extract is 0.001-10 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.001-5 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.001-1 % by weight.In one embodiment, the working concentration of Litchi Pericarp Extract is 0.01-10 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.01-5 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.01-1 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.1-10 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.1-5 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.1-1 % by weight.In another embodiment, the working concentration of Litchi Pericarp Extract is 0.1-0.5 % by weight.
Litchi Pericarp Extract can be added in various personal care product according to the ratio of 0.01-50 % by weight.Such as, the consumption of Litchi Pericarp Extract can be 0.01-20 % by weight, such as 0.01-10 % by weight, such as 0.01-5 % by weight.In another embodiment, Litchi Pericarp Extract can be added in various personal care product according to the ratio of 0.1-10 % by weight.In one preferred embodiment, in personal care product, the consumption of Litchi Pericarp Extract is 0.1-2 % by weight.Another preferred embodiment in, in personal care product, the consumption of Litchi Pericarp Extract is 0.5-2 % by weight.
The present invention is set forth further below in conjunction with specific embodiment.But, should be understood that these embodiments only do not form limitation of the scope of the invention for illustration of the present invention.The test method of unreceipted actual conditions in the following example, usually conveniently condition, or according to the condition that manufacturer advises.Except as otherwise noted, all percentage ratio and number are by weight.
Embodiment 1: the extraction of Exocarpium Litchi
Exocarpium Litchi 50g, adds 30% ethanol of 8 times amount, heating and refluxing extraction 1h, filters.Get filtrate, decompression recycling ethanol dry Litchi Pericarp Extract.
Embodiment 2: Litchi Pericarp Extract is to the inhibitory action of 5α-reductase
With 45% (v/v) DMSO(Tris buffer 55%) the Litchi Pericarp Extract dissolved dilution embodiment 1 prepared becomes 5 Concentraton gradient: 3.4 % by weight, 1.7 % by weight, 0.85 % by weight, 0.43 % by weight, 0.21 % by weight.As described belowly carry out 5α-reductase Inhibition test.The reaction system of experiment porch is 1ml, and sample additive capacity is 0.1ml, so initial concentration is from crude drug 0.34 % by weight, system concentration respectively: 0.34 % by weight, 0.17 % by weight, 0.085 % by weight, 0.043 % by weight, 0.021 % by weight; Because the DMSO containing 4.5% (v/v) in system, so arrange 4.5% (v/v) DMSO solvent control simultaneously, the dutasteride of 1mg/L is positive control.
5α-reductase experiment porch
Extract enzyme from SD rat liver, freezen protective is for subsequent use; Containing substrate testosterone (T) in enzyme reaction system, coenzyme NADP 11, enzyme, enzyme reaction temperature 37 DEG C, pH is 7.Not adding the reaction that any sample carries out intervening is normal enzymatic reaction, and the reaction rate obtained is normal reaction speed.Add the later reaction rate of sample compared with normal reaction speed, decrease, think that sample is inhibited.
5α-reductase experimental result
The reaction rate that normal 5α-reductase is urged to react, the dutasteride adding 1mg/L be reaction rate after positive control, add 4.5% (v/v) DMSO after reaction rate and the reaction rate of enzymatic reaction after adding variable concentrations sample as figure below.
From Fig. 1-2, concentration be 0.021 % by weight-0.34 % by weight Litchi Pericarp Extract all there is the effect suppressing 5α-reductase activity, concentration 0.17 % by weight and above effect particularly remarkable, can illustrate and will can play the effect controlling oil, anti-acne or Anti-hair loss accordingly in Litchi Pericarp Extract additive to formula for a product.
Embodiment 3: containing the preparation of the control oil surfactant of Litchi Pericarp Extract
The control oil surfactant of Litchi Pericarp Extract of the present invention is comprised according to the composition of table 1 and consumption preparation.
Table 1
| Composition | % concentration (weight) |
| A phase | |
| Water | 95.58 |
| Glycerol | 1.0 |
| Litchi Pericarp Extract | 0.8 |
| EDTA-2Na | 0.02 |
| B phase | |
| Essence | 0.02 |
| 1,3 butylene glycol | 2.0 |
| HPS | 0.08 |
| C phase | |
| Antiseptic | 0.5 |
Preparation method: take A, B, C three-phase respectively in above ratio, stir evenly separately, is slowly added to A phase by B phase while stirring, adds C phase after stirring evenly, and namely stirring and dissolving evenly obtains the oily surfactant finished product of control.
Embodiment 4: the preparation controlling oily Pimple removing scream
The control oil Pimple removing scream of Litchi Pericarp Extract of the present invention is comprised according to the composition of table 2 and consumption preparation.
Table 2
| Composition | % concentration (weight) |
| A phase | |
| Water | 76.63 |
| HANSHENGJIAO | 0.1 |
| Glycerol | 5.0 |
| Methyl hydroxybenzoate | 0.15 |
| Propylparaben | 0.1 |
| EDTA-2Na | 0.02 |
| B phase | |
| Cetostearyl alcohol | 4.0 |
| Sad/certain herbaceous plants with big flowers acid glycerol three ester | 3.0 |
| Glycerol stearate+ | 1.0 |
| PEG100 | 3.0 |
| Dimethicone | 1.0 |
| C phase | |
| Litchi Pericarp Extract | 1.0 |
| Water | 5.0 |
Preparation method: HANSHENGJIAO to be scattered in water 15 minutes, to add all the components in A phase and be heated to 70-75 DEG C.Separately take all the components in B phase, be heated to 75-80 DEG C.Be added to by B in A phase, homogenizing 5 minutes, is cooled to 45 DEG C, adds C phase, stirs evenly and obtain the oily Pimple removing scream of control.
Embodiment 5: blemish clearing gel
The blemish clearing gel of Litchi Pericarp Extract of the present invention is comprised according to the composition of table 3 and consumption preparation.
Table: 3
| Composition | % concentration (weight) |
| A phase | |
| Water | 80.48 |
| Glycerol | 2.0 |
| HANSHENGJIAO | 0.2 |
| Methyl hydroxybenzoate | 0.2 |
| Propylparaben | 0.1 |
| EDTA-2Na | 0.02 |
| Jojoba oil | 3.0 |
| B phase | |
| Sepigel305 | 2.0 |
| C phase | |
| Litchi Pericarp Extract | 2 |
| Water | 10.0 |
Preparation method: take A, B, C three-phase respectively in proportion, by A heat phase to 70-75 DEG C, stirring and dissolving is even, adds B phase, stirs, be cooled to 30-35 DEG C, add C phase, mix and obtain blemish clearing gel.
Embodiment 6: control oil wash floods
Prepare according to the composition of table 4 and consumption the control oil wash comprising Litchi Pericarp Extract of the present invention to flood.
Table: 4
Preparation method: heat water to 70-75 DEG C, adds each composition in proportion respectively, and stirring and dissolving is even, is cooled to 30-35 DEG C, adds Litchi Pericarp Extract, mixes and obtains control oil wash and flood.
Claims (10)
1. Litchi Pericarp Extract is as the purposes of 5α-reductase inhibitor.
2. Litchi Pericarp Extract is preparing as having the inhibiting additive of 5α-reductase the purposes had in the personal care product controlling oily anti-acne effect.
3. Litchi Pericarp Extract is preparing as having the inhibiting additive of 5α-reductase the purposes had in the personal care product of Anti-hair loss effect.
4. the purposes as described in claim 1,2 or 3, is characterized in that, by weight percentage, the consumption of described Litchi Pericarp Extract is 0.0001-100%.
5. purposes as claimed in claim 4, it is characterized in that, by weight percentage, the consumption of described Litchi Pericarp Extract is 0.01%-50%.
6. purposes as claimed in claim 5, it is characterized in that, by weight percentage, the consumption of described Litchi Pericarp Extract is 0.1%-10%.
7. purposes as claimed in claim 2 or claim 3, it is characterized in that, described personal care product is selected from: facial milk cleanser, astringent, emulsion, cream frost, gel, facial film, shampoo, hair conditioner, hair-care essence, fancy soap.
8. purposes as claimed in claim 7, it is characterized in that, described personal care product comprises Litchi Pericarp Extract and acceptable adjuvant.
9. purposes as claimed in claim 7, it is characterized in that, described personal care product comprises the Litchi Pericarp Extract of 0.01-50 % by weight.
10. purposes as claimed in claim 7, it is characterized in that, described personal care product comprises the Litchi Pericarp Extract of 0.1-10 % by weight.
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|---|---|---|---|
| CN201310625349.XA CN104666144A (en) | 2013-11-28 | 2013-11-28 | 5alpha-reductase inhibitor and application thereof |
| PCT/CN2014/092431 WO2015078396A1 (en) | 2013-11-28 | 2014-11-28 | 5α-reductase inhibitor and use thereof |
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| CN201310625349.XA CN104666144A (en) | 2013-11-28 | 2013-11-28 | 5alpha-reductase inhibitor and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN112773735A (en) * | 2021-01-26 | 2021-05-11 | 广东丸美生物技术股份有限公司 | Cosmetic concentrated emulsified matrix and preparation method and application thereof |
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| JP2005075786A (en) * | 2003-09-01 | 2005-03-24 | Maruzen Pharmaceut Co Ltd | TESTOSTERONE 5alpha-REDUCTASE INHIBITOR AND HAIR GROWING COSMETIC |
| JP2007106712A (en) * | 2005-10-14 | 2007-04-26 | Maruzen Pharmaceut Co Ltd | Skin cosmetic and hair cosmetic |
| CN101811949A (en) * | 2010-05-14 | 2010-08-25 | 上海利盛生化有限公司 | Purification method of phloretin powder |
| JP2012092138A (en) * | 2011-12-27 | 2012-05-17 | Maruzen Pharmaceut Co Ltd | Skin cosmetic and hair cosmetic |
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| CN112773735A (en) * | 2021-01-26 | 2021-05-11 | 广东丸美生物技术股份有限公司 | Cosmetic concentrated emulsified matrix and preparation method and application thereof |
| JP2022114423A (en) * | 2021-01-26 | 2022-08-05 | 広東丸美生物技術股▲フン▼有限公司 | Cosmetic concentrated emulsion matrix, preparation method therefor and application thereof |
| JP7153778B2 (en) | 2021-01-26 | 2022-10-14 | 広東丸美生物技術股▲フン▼有限公司 | Concentrated cosmetic emulsifying matrix and its preparation and use |
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