KR101851388B1 - Composition for enhancing percutaneous absorption of ginsenosides, manufacturing method thereof and cosmetic preparations for hair growth - Google Patents
Composition for enhancing percutaneous absorption of ginsenosides, manufacturing method thereof and cosmetic preparations for hair growth Download PDFInfo
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- KR101851388B1 KR101851388B1 KR1020170108195A KR20170108195A KR101851388B1 KR 101851388 B1 KR101851388 B1 KR 101851388B1 KR 1020170108195 A KR1020170108195 A KR 1020170108195A KR 20170108195 A KR20170108195 A KR 20170108195A KR 101851388 B1 KR101851388 B1 KR 101851388B1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0295—Liquid crystals
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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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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- 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
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
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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
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
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Abstract
The present invention relates to a composition for promoting hair loss prevention and hair wool efficacy by promoting absorption of ginsenoside having excellent effect on hair loss and excellent effect on wool through transdermal preparation, a method for producing the same, and a cosmetic for preventing hair loss comprising the composition , And cosmetics developed through this method have an advantage that they contain nanosized ginsenoside emulsified particles and are excellent in transdermal absorption and stable.
Description
The present invention relates to a composition for preparing a red ginseng concentrate containing a large amount of ginsenoside having excellent effect on hair loss prevention wool and promoting absorption of ginsenoside in a large amount through the scalp to prevent hair loss and promote wool efficacy, The present invention relates to the development of a cosmetic composition for preventing hair loss, which comprises the above composition, and the cosmetic composition developed therefrom has nanoscale ginsenoside emulsified particles and has an advantage of excellent transdermal absorption and stability.
Hair loss refers to a state in which there is no hair in the area where hair should normally exist, and it is known that hair loss occurs in genetic or aging. However, recently, it has been known that various acquired causes are related, and in particular, excessive stress, poor circulation of the scalp, excessive secretion of androgen, seborrheic dermatitis, genetic shortage, malnutrition, iron deficiency, . Many drugs and therapies for treating hair loss caused by these causes have been actively studied.
Currently, domestic hair loss population is estimated to reach 10 million people according to the Korean Hair Association. According to the results of the Health Insurance Review and Evaluation Center in 2011, nearly half (45.8%) of such patients reported that they were young people in their 20s and 30s.
Drugs approved by the US Food and Drug Administration (FDA) include Minoxidil and Finasteride (Propecia), which promote hair growth. Minoxidil from Pharmacia & Upjohn Co. was initially developed as a vasodilator for the treatment of hypertension, but as a side effect, it was reported to be a hair restorer (Br J Dermatol. 1979 Nov; 101 (5) 593-5 ). Although the mechanism of action of the minoxidil on the hair growth effect has not been clarified to date, it is known to induce hair growth by promoting nutritional supply through vasodilation and potassium channel opening (Meisheri et al. 1988 Buhletal., 1990a, 1990b). Minoxidil is mainly applied to male hormonal alopecia, which is effective for both alopecia areata, but it has little effect on temporo-alopecia alopecia and also has the potential to cause side effects such as hypotonia, hypotension, tachycardia, and cardiovascular complications due to antihypertensive action It is not suitable for long term use. Pinasteride, which inhibits the production, binding and metabolism of the androgen, the male hormone, can lead to feminization of males and the problem of birth defects in fertile women. As such, the drug therapy using a chemical causes an imbalance in the homeostasis of the body, and various unexpected side effects occur. Therefore, research on a hair growth agent using a natural material having no side effect has actively been conducted.
Meanwhile, Korean Patent No. 10-1063147, which is related to ginsenoside, has been tested in ten patients with hair loss, and it has been reported that ginsenoside Ro has hair growth effect similar to minoxidil, 10-134857 has reported that ginsenoside F2 derived from fermented red ginseng promotes hair growth. Korean Patent No. 10-1132246 discloses a cosmetic composition for accelerating hair growth comprising ginsenoside Rg3 and Rh2 as main components, wherein the composition ratio of Rg3 and Rh2 ranges from 2: 1 to 8: 1, I have reported excellent.
In addition, ginsenosides have limited absorption in the body and high absorption in the skin, so there are various studies and patents to promote ginsenoside transdermal absorption. Korean Patent Laid-Open Publication No. 2003-0060017 discloses microemulsified particles containing ginsenoside F1 by nano-emulsification technology and a composition for external application of skin using the same, thereby improving a transdermal absorption rate. The present invention provides a cosmetic which improves the effect of accelerating collagen biosynthesis and enhances the anti-aging effect. Korean Patent Laid-Open No. 10-2005-0087567 has invented self-assembled polymer nanoparticles containing a ginsenoside component and a cosmetic composition containing the same, and has succeeded in exploiting the hydrophobic polymer, polycaprolactone, and a hydrophilic polymer, Suggesting the stabilization of the nanosized nanosized form of senoside and the improvement of transdermal delivery. Korean Patent No. 10-1496239 also discloses a method for enhancing the pharmacological effect of pharmacological ingredients and pharmacological effects by converting the pharmacological components of ginsenosides and poorly soluble drugs into nano-micelles.
Under these circumstances, in the present invention, in order to stabilize a cosmetic composition containing a red ginseng concentrate having a high content of various ginsenosides and excellent anti-hair loss and wool effect, and to enhance the transdermal absorption effect of ginsenoside, The present invention is to provide a stable emulsified cosmetic composition having a small percutaneous absorption rate.
[Patent Document 1] Korean Patent Registration No. 2003-0060017
[Patent Document 2] Korean Patent No. 10-2005-0087567
[Patent Document 3] Korean Patent No. 10-1496239
Accordingly, one object of the present invention is to provide a composition for promoting transdermal absorption, which stabilizes a formulation and accelerates transdermal absorption of ginsenosides in a topical composition containing a large amount of ginsenoside, and a method for producing the same.
It is still another object of the present invention to provide a cosmetic for preventing or improving hair loss or promoting hair growth comprising the composition for promoting transdermal absorption of ginsenoside.
In order to solve the above-mentioned object, the present invention provides a method for preparing a red ginseng nanobase, comprising the step of first preparing a first red ginseng nanobase having nanoparticles of particles containing a large amount of red ginseng concentrate, And a method for producing a composition for promoting gynecoid percutaneous absorption.
Specifically, the method for preparing a composition for promoting gynecoid transdermal absorption according to the present invention comprises the steps of:
a) preparing a first red ginseng nanobase by treating the red ginseng concentrate with a high-pressure emulsifier at a rate of 500 to 1500 psi for 1-3 times to nano-size the red ginseng concentrate particle; and
b) heating the oil component and the water component, adding the first red ginseng nanobase prepared in step a), and emulsifying the composition at 1,000-5,000 rpm for 5 to 20 minutes with an emulsifying mixer to prepare a composition having a lamellar formulation .
The step (a) is a step of preparing red ginseng nano-base by nanosizing particles of ginsenoside-containing liquid having lamellar form, and the red ginseng concentrate used in this step is a concentrate of red ginseng Means a substance in the form of a liquid. The red ginseng concentrate used in the present invention may be commercially available ones, and those prepared using known methods for extracting red ginseng and extracts may be used without limitation. In particular, the red ginseng concentrate used in the present invention preferably contains a large amount of ginsenoside, preferably ginsenoside Rd having the following structure. The ginsenoside Rd is a (3β, 12β) -20- (β-D-glucopyranosyloxy) -12-hydroxydamar-24-en-3-yl-2-O- β-D-glucopyranosyl β-D-glucopyranoside (ββ-D-glucopyranosyloxy) -12-hydroxydammar-24-en-3-yl- D-glucopyranoside) and is a substance having a structure of the following formula (1), which is present in ginseng or red ginseng.
[Chemical Formula 1]
Specifically, the step (a) may be performed by mixing and heating an oil component to prepare an oil component, preparing a water component including a red ginseng concentrate, mixing the components, adding ethanol thereto, stirring the mixture and then adding a microfludizier ). ≪ / RTI > Preferably, at least one component selected from the group consisting of phospholipids, ester oils, moisturizers, non-ionic emulsifiers and ethanol is further contained in addition to the above-mentioned red ginseng concentrate as a component included in the step (a) for preparing the primary red ginseng nanobase .
Preferably, 0.1 to 5.0% by weight of hydrogenated lecithin as a phospholipid, 0.1 to 25.0% by weight of caprylic / capric triglyceride, diisopropyl adipate and the like as ester oil is added to the total weight of red ginseng primary nano- 0.1 to 3.0% by weight of
In one specific example, in order to prepare the first red ginseng nanobase according to the present invention, the components contained in the oil phase portion include hydrogenated lecithin, caprylic / capric triglyceride, potassium cetylsulfate, diisopropyl adipate, cholesterol , Cetearyl alcohol and ceramide were mixed and heated at 75 to 80 ° C to be completely dissolved. Then, a water phase portion (glycerin, purified water, EDTA and red ginseng concentrate) was prepared separately, and the oil phase and water phase were mixed with each other and stirred for 5 minutes. After stirring, the mixture was cooled, ethanol was added thereto, and the mixture was stirred for 3 minutes. The contents were treated three times at 1000 bar using a high-pressure emulsifier (Microfluidizer) to prepare the first red ginseng nanobase according to the present invention.
Step b) is a step of preparing a composition having a lamellar formulation by using the primary red ginseng nanobase prepared in step a), specifically, mixing and heating the oil and water components, The first red ginseng nanobase may be added and emulsified with an emulsifying mixer at 2,000 to 5,000 rpm for 5 to 20 minutes to form a lamellar formulation.
Preferably, the oil and water components may be at least one selected from the group consisting of emulsifiers, fatty alcohols, moisturizers, and thickeners. In the present invention, in particular, a combination of a phosphoric acid type emulsifier and a nonionic emulsifier is used as an emulsifier, specifically, a combination of hydrogenated lecithin / polyglyceryl-10 distearate / hydroxypropyl bislauramide maei and cetearyl alcohol / A stable lamellar formulation can be made that comprises tess-20 phosphate / dicetyl phosphate. Preferably, the hydrogeneated lecithin / polyglyceryl-10 distearate / hydroxypropyl bislauraimide maei and cetearyl alcohol / ceteth-20 phosphate / dicetyl phosphate are mixed with the final composition of the lamellar formulation 0.1 to 5.0% by weight of hydrogensilized lecithin / polyglyceryl 10 distearate / hydroxypropyl bislauraimide emulsion with respect to the total weight, 0.1 to 5.0% by weight of cetearyl alcohol / ceteth-20 phosphate / dicetyl phosphate %. ≪ / RTI >
Examples of the fatty alcohol may include cetearyl alcohol, behenyl alcohol, cetostearyl alcohol and myristyl alcohol. Examples of the moisturizing agent include panthenol, macadamia oil, glycerin, propylene glycol, cholesterol, Call, betaine and the like, and the incremental zero may be carbomer or xanthan gum.
In a preferred embodiment, the oily and aqueous feedstocks are heated at 75-80 < 0 > C until the ingredients are completely dissolved. The mixture is cooled to 50 ° C. or lower, preferably 25 to 50 ° C., 0.1 to 20% by weight of the primary red ginseng nanobase prepared in the step a) is added, and a composition having a lamellar formulation can be prepared using an emulsifying mixer have.
Accordingly, the present invention provides a composition for enhancing transdermal absorption of ginsenoside having a lamellar formulation and a cosmetic comprising the same, which is produced by the above production method.
In the case of the composition prepared by the method according to the present invention, although the red ginseng concentrate containing a large amount of ginsenoside is contained, the formulation is stable and excellent in particle size, Absorbing effect. In a specific example, the transdermal absorption of red ginseng ginsenosides Rd in the first red ginseng nanobase prepared according to the present invention was increased by more than 104% after 12 hours and the absorption of ginsenoside Rd was increased by 30% or more in the final formulation Respectively.
The cosmetic composition containing the composition for promoting transdermal absorption may be manufactured into various forms of cosmetic formulations. Hair shampoo, hair conditioner, hair moisturizing cream, hair massage cream, hair tonic, hair essence, hair oil, hair pack, hair cream, hair mousse, hair spray, hair wax, Hair soap, hair cleansing foam, hair treatment, hair nail polish, hair mascara or hair dye, and in addition to the above components, a flavor-acceptable carrier and / or additive may be included.
In addition, the cosmetic material according to the present invention has a high content of ginsenoside, especially ginsenoside Rd, and excellent transdermal absorption rate, and thus can be used for preventing or improving hair loss, or for promoting hair growth.
The cosmetic preparation method and composition according to the present invention have high ginsenoside content and excellent transdermal absorption, and thus can be effectively used as a manufacturing method for producing a stable cosmetic preparation having an excellent hair loss preventing effect.
FIG. 1 is a graph showing the particle sizes before and after the treatment of the high-pressure emulsion of the nano-base prepared as a result of Example 4 of the present invention.
2 is a schematic view showing the structure of a lamellar formulation.
FIG. 3 is a polarized microscope photograph showing that the hair growth cosmetic prepared according to Example 5 of the present invention exhibits a lamellar formulation.
FIG. 4 is a HPLC chromatogram of ginsenosides of the red ginseng concentrate contained in the composition according to the present invention.
The present invention will be described in more detail with reference to the following examples. However, the following examples are provided to aid understanding of the present invention, and the scope of the present invention is not limited by these examples in any sense. Hereinafter, the technical and scientific terms used herein will be understood by those skilled in the art without departing from the scope of the present invention. Descriptions of known functions and configurations that may be unnecessarily blurred are omitted.
Example 1: Primary nanobase containing red ginseng concentrate emulsion Manufacturing 1
(Water of purified water, glycerin, EDTA, red ginseng concentrate and polysorbate 20) containing the red ginseng concentrate which is heated by heating at 75 to 80 ° C after completely dissolving the hydrogenated lecithin, lecithin, ceramide and diisopropyl adipate, And the mixture was mixed for 5 minutes, and then the preservative was added. The contents were prepared by treating with a high-pressure emulsifier (1000 bar) three times using a microfluidizer.
Example 2: Primary nanobase containing red ginseng concentrate emulsion Manufacturing 2
Hydrogenated lecithin, lecithin, phenyl trimethicone, ceramide, and diisopropyl adipate are mixed and heated at 75 to 80 ° C to be completely dissolved to prepare an oil phase part. Then, glycerin, EDTA, and red ginseng concentrate are added to the aqueous phase where the purified water and the carbomer are separately released, and the mixture is stirred for 5 minutes. The oil phase thus prepared was then added and stirred for 5 minutes. Then, tromethamine is added as a preservative to neutralize. Thereafter, it was confirmed that a viscosity was formed and then cooled. The prepared contents were prepared by treating with a high-pressure emulsifier (Microfluidizer) at 1000 Bar three times.
Example 3: Primary nanobase containing red ginseng concentrate emulsion Manufacturing 3
Caprylic / capric triglyceride, potassium cetyl phosphate, cholesterol, and ceramide were mixed with hydrogenated lecithin, caprylic / capric triglyceride, and ceramide, respectively, in an experiment using only hydrogenated lecithin with good emulsification stability except for unsaturated lecithin, After completely dissolving by heating at 80 캜, the mixture was mixed with the water phase (glycerin, purified water, EDTA, red ginseng condensate) and stirred for 5 minutes. After stirring, the mixture was cooled, ethanol was added thereto, and the mixture was stirred for 3 minutes. And treated at 1000 Bar for 3 times using a high-pressure emulsifier (Microfluidizer).
Example 4 : Primary containing red ginseng concentrate Nano-base emulsion Manufacturing 4
(Glycerin, purified water, EDTA solution) after completely dissolving by heating at 75 to 80 ° C by mixing glycerin, hydrogenated lecithin, caprylic / capric triglyceride, potassium cetyl phosphate, diisopropyl adipate, cholesterol, cetearyl alcohol, , Red ginseng concentrate) for 5 minutes. After stirring, the mixture was cooled, ethanol was added thereto, and the mixture was stirred for 3 minutes. The contents were prepared by treating with a high pressure emulsifier (Microfluidizer) at 1000 Bar three times.
The formulations according to Examples and Comparative Examples are shown in Table 1, and the content stability in Table 2 are summarized in Table 2. The particle size before and after the high-pressure emulsifier treatment is shown in Fig.
The method and conditions for measuring the particle size are as follows.
*Measuring conditions
(1) Analytical Instruments: Photal OTSUKA ELECTRONICS
Zeta-potential & Particle size Analyzer ELS-Z2
(2) Principle: Dynamic Light Scattering
(3) Light source: Semiconductor laser
(4) Measuring range
1) Concentration range: 0.001% to 40% * 1
2) Zeta potential: -100 to 100 mV
3) Electric mobility: -10 ~ 10 ㎛ · cm / sec · V
4) Particle size: 0.6 nm ~ 7 ㎛
* 1 (Latex 115/262 nm: 0.001-10%, taurocholic acid: ~ 40%)
(5) Pretreatment: After diluting the sample 10 times (A sample) and 100 times (B sample) in the solvent, measure
* Dispersion solvent conditions
(1) Solvent: Water
(2) Temperature: 25.0 DEG C
(3) Refractive Index: 1.332 8
(4) Viscosity: 0.887 8 cp
(*: Cycle is a method to confirm the stability under severe conditions. It is a method to check the stability in a short period of time by inserting the product into a device set at a certain temperature and time. Temperature and time are different for each experiment condition. In this experiment, 20 ° C / 12hr -> 4 ° C / 24hr -> 25 ° C / 24hr -> 40 ° C / 12hr)
As shown in Table 2, the most stable formulations were obtained in Example 4 as a whole, and as shown in [Table 3], Example 4 is superior in nanoparticle size, Red ginseng was applied as a nano-base prescription.
Before treatment (nm)
After treatment (nm)
The following Examples 5 to 9 are preparations for preparing various cosmetic compositions containing red ginseng nano-base. The formulations containing red ginseng nanobase were prepared with a lamellar formulation having excellent moisturizing effect and excellent skin-spreading power. As comparative formulations for this, Comparative Examples 5 to 9 were also prepared. All the constituents and their contents are the same as those of Examples 5 to 9 except that the normal red ginseng concentrate was used instead of the red ginseng nanobase according to the present invention.
(% Refers to% by weight unless otherwise noted in the tables below)
hair
treatment
Hair Pack
Hair essence
Scalp
essence
hair
conditioner for hair
As shown in Table 9, it was confirmed that the stability of each cosmetic composition was good.
[Experimental Example 1] Test for measurement of percutaneous absorption
Skin absorption was measured using a Franz permeable cell against Guinea api skin. Immediately prior to the test, the skin of the abdomen of Guinea epigae was taken, cut into an area of 1 cm 2 square, fixed in a transmissive cell with a diameter of 0.9 cm in the transmissive cell and clamped. One surface (donor container) of the skin was diluted with distillation shoe so that 0.05 g of each of the formulation of Example 4 (before / after the high pressure microemulsion treatment) was taken to be 0.5 ml. The opposite side (receptor vessel) was brought into contact with a solvent mixture of purified water and ethanol in a weight ratio of 4: 1. The temperature during the test was maintained at 32 ° C., which is the actual skin temperature. After the start of the test, a portion of the solvent was collected at a predetermined time interval, and the amount of ginsenoside Rd absorbed into the skin was measured using HPLC to show the amount of skin absorption (쨉 g / cm 2 / wt%) per application concentration , And the results are shown in Table 11 below. The specific analytical conditions of HPLC for the analysis of ginsenoside Rd proceeded according to Table 10 below. Further, in order to examine the effect of accelerating the transdermal permeation in the cosmetic, the same test as in the above experiment was carried out, except that on one side (donor vessel) of the skin was added, in place of the primary red ginseng nanobase of Example 4, The contents of 9 were put into each 0.5g, and the experiment was run. The results are shown in Table 12 below.
(250x4.6 mm 5 [mu] m, Phenomex)
High-pressure micro emulsifier
(Before treatment)
(After treatment)
Yes
As shown in Table 11, it was confirmed that the absorption of the red ginseng jinse noa seed was increased by 104% or more after 12 hours in the nano-treated base of the most stable Example 4, and as shown in Table 12, , The absorption of ginsenoside Rd was increased by 30% or more. Thus, it was confirmed that the cosmetic composition was excellent in ginsenoside percutaneous absorption.
Claims (11)
b) 0.1 to 5.0% by weight of hydrogensilized lecithin / polyglyceryl-10 distearate / hydroxypropyl bislauraimide emulsion as an emulsifying agent and 0.1 to 5.0% by weight of cetearyl alcohol / ceteth-20 0.1-3.0 wt.% Of phosphate / dicetyl phosphate; 0.1 to 7.0% by weight fatty alcohol; And 1.0-10.0% by weight of a moisturizing agent, heating the mixture containing the first nanoemulsion prepared in step a), emulsifying the mixture at 1,000 to 5,000 rpm for 5 to 20 minutes with an emulsifying mixer to obtain a composition having a lamellar formulation And a step of preparing a composition for promoting transdermal absorption of ginsenoside.
0.1 to 5.0% by weight of hydrogensilized lecithin / polyglyceryl-10 isostearate / hydroxypropyl bislauraid m Emery and cetearyl alcohol / ceteth-20 phosphate / dicetyl phosphate 0.1 to 5.0% by weight, 3.0% by weight,
A composition for promoting transdermal absorption of ginsenoside, which has a lamellar formulation.
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