WO2012074285A2 - Agent for stabilizing peptides or proteins - Google Patents

Agent for stabilizing peptides or proteins Download PDF

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Publication number
WO2012074285A2
WO2012074285A2 PCT/KR2011/009190 KR2011009190W WO2012074285A2 WO 2012074285 A2 WO2012074285 A2 WO 2012074285A2 KR 2011009190 W KR2011009190 W KR 2011009190W WO 2012074285 A2 WO2012074285 A2 WO 2012074285A2
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WIPO (PCT)
Prior art keywords
composition
casein
group
protein
proteins
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PCT/KR2011/009190
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French (fr)
Korean (ko)
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WO2012074285A3 (en
Inventor
이창근
김혁
김정환
신홍주
박원석
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(주)아모레퍼시픽
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Publication of WO2012074285A2 publication Critical patent/WO2012074285A2/en
Publication of WO2012074285A3 publication Critical patent/WO2012074285A3/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans

Definitions

  • the present invention relates to agents that stabilize peptides or proteins.
  • Proteins are high-molecular organic compounds that make up the body of every organism. It is important as a constituent of the body of an organism and as a catalyst for various chemical reactions in cells. Based on these characteristics, proteins are widely used in various fields such as food, medicine, or cosmetics.
  • the present invention seeks to provide a peptide or protein stabilizer and a composition in which the peptide or protein remains stable.
  • the present invention also provides a method of stabilizing a peptide or protein.
  • One aspect of the present invention provides a peptide or protein stabilizer comprising at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein, and derivatives thereof.
  • Another aspect of the invention provides at least one of peptides and proteins; And it provides a composition comprising at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
  • Another aspect of the invention provides at least one of peptides and proteins; And it provides a peptide or protein stabilization method comprising the step of preparing a composition by mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
  • At least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof of the present invention is excellent in stabilizing peptides or proteins.
  • the composition comprising at least one of the peptides and proteins according to one aspect of the invention comprises at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof, so that the peptide or protein is not degraded for a long time. Can be kept stable.
  • compositions containing a peptide or protein in a dissolved state by including one or more selected from the group consisting of panthenol, polyalcohol ester compound, casein, and derivatives thereof, since the peptide or protein is hardly decomposed, immediately before use There is no need to dissolve the peptide or protein and it is easy to store and distribute with the peptide or protein included.
  • Peptides or proteins are used in various fields, such as food, medicine or cosmetics, but they are unstable under external physical and chemical conditions, especially at high temperature, and are not easy to formulate. In addition, since the peptide or protein is easily dissolved when dissolved, it is inconvenient to dissolve immediately before use if the peptide or protein is to be used. In order to solve this problem, attempts have been made to include peptides such as sucrose, trehalose, fructose and mannitol in a composition containing at least one of peptides and proteins to stabilize peptides or proteins, but the degree of effect is satisfactory. no.
  • One aspect of the present invention provides a peptide or protein stabilizer comprising one or more selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof.
  • the at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof can physically and chemically protect the peptide or protein to prevent the peptide or protein from being degraded, thereby keeping the peptide or protein stable for a long time. .
  • One aspect of the invention is at least one of a peptide and a protein; And it provides a composition comprising at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
  • the composition comprises at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof, so that the peptide or protein contained therein can be stably maintained without prolonged degradation.
  • One aspect of the invention is at least one of a peptide and a protein; And it provides a peptide or protein stabilization method comprising the step of preparing a composition by mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
  • the peptide or protein is mixed with one or more selected from the group consisting of panthenol, polyalcohol ester compound, casein, and derivatives thereof, so that the peptide or protein can be stably maintained without degradation for a long time.
  • panthenol is an alcohol derivative of pantothenic acid, which is one of the vitamin B groups, and may be represented by the following Chemical Formula 1.
  • the derivative of panthenol includes all compounds that can be obtained by chemically changing a part of panthenol, and includes hydrogen or a specific atomic group all substituted with another atom or atomic group. More specifically, derivatives of panthenol include allantoin calcium pantothenate, calcium pantothenate, ethyl dicarboethoxy pantothenate (C 17 H 29 NO 9 , formula 2), Hydroxyethyl Pantothenamide MEA (C 13 H 26 N 2 O 6 , Formula 3), Pantothenamide MEA, C 11 H 22 N 2 O 5 , Formula 4), Pantothenic Acid , C 9 H 17 NO 5 , Formula 5), Pantothenoyl Dipeptide-13, Sodium Pantothenate, PanthenylEthylether, PanthenylEthylether acetate, C 13 H 25 NO 5 , formula 6) and panthenyl triacetate (C 15 H 25 NO 7 , formula 7
  • a polyalcohol ester compound refers to a compound including a polyalcohol ester group.
  • the polyalcohol ester compound and derivatives thereof include a compound in which the ester of polyalcohol and stearic acid is esterified, and specifically, polyglyceryl stearate, polyglyceryl distearate, PEG stearate, PEG distearate, polyglyceryl methylglucose distearate or PEG methyl glucose distearate, and more particularly polyglyceryl-3 methylglucose distearate or PEG-20 methyl glucose distearate do.
  • the polyalcohol ester compound includes a compound that acts as a surfactant.
  • a casein derivative is a concept including all compounds that can be obtained by chemically changing a part of casein.
  • the casein or derivative thereof includes a casein salt such as casein hydrolysate or casein sodium hydrolyzed casein with an acid or enzyme.
  • the casein or derivative thereof may stabilize other proteins included in the composition in addition to itself.
  • a peptide refers to a polymerized molecule of amino acids, from 2 to 10 amino acids are linked, it is a concept including a polypeptide of 10 to 20 or more than 20 linked. In another aspect of the present invention, the peptide comprises about 10 amino acids linked.
  • proteins generally include all substances that can be classified as proteins.
  • the peptide or protein may refer to a potent ingredient generally included in a pharmaceutical, cosmetic or food composition.
  • peptides or proteins include those extracted from animals or plants.
  • the peptide or protein comprises one or more of growth factors, hormones, interferons, vaccines, recombinant proteins, recombinant peptides and enzymes. More specifically, the peptide or protein may include epidermal growth factor, basic fibroblast growth factor, platelet derived growth factor, and vascular endothelial growth factor.
  • CC Motif Chemokine Ligand 5 CC Motif Chemokine Ligand 5
  • Human Growth Hormone Insulin, Acyl Coenzyme A Desaturase, Albumin (Albumin), Alkaline Phosphatase, Aminopeptidase, Amylase (Amylase), Amyloglucosidase, Apo-Lactoferrin, Arthrospira Extract, Bromelain, Casein, Catalase, Cellulase, Cellulase, Collagen, Crystallins, Cytochrome C, Deoxyribonuclease, Elastin Elastin, Fibronectin, Ficin, Fish Plasma Protein, Galactose Dehydrogenase, Gelatin, Gelidium Pulchrum Protein, Glia Gliadin, Glucose Oxidase, Glycoproteins
  • casein or derivative thereof when the casein or derivative thereof is selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof, at least one selected from peptides and proteins does not comprise casein or milk protein .
  • the composition comprising the peptide or protein is panthenol depending on the storage conditions such as the content of the peptide or protein, the viscosity of the composition comprising the peptide or protein or the storage temperature and duration of the composition comprising the peptide or protein, etc.
  • Polyalcohol ester compounds, casein and derivatives thereof may include one or more selected from the group consisting of various contents. More specifically, at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof is 0.1 to 50% by weight, specifically 0.5 to 30% by weight, and more specifically 1 to 20% by weight, based on the total weight of the composition. It may include. When included in the weight percent, not only is it appropriate to exhibit the intended effect of the present invention, but also satisfies both the stability and safety of the composition, it may be appropriate to include in the above range in terms of cost-effectiveness.
  • the weight ratio of at least one of the peptides and proteins and at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof is 50,000,000: 1 to 1: 1 or 1: 1: 1 to 50,000,000
  • it may be 10,000,000: 1 to 1: 1 or 1: 1 to 1: 10,000,000, more specifically 500,000: 1 to 1: 1 or 1: 1 to 500,000.
  • When included in the weight ratio not only is it appropriate to exhibit the intended effect of the present invention, but also satisfies both the stability and safety of the composition, and may be appropriate in terms of cost-effectiveness.
  • a composition comprising at least one of a peptide and a protein may have a viscosity of 5,000 cP to 30,000 cP. In another aspect of the invention, a composition comprising one or more of peptides and proteins may have a viscosity of 8,000 cP to 25,000 cP. In another aspect of the invention, a composition comprising one or more of peptides and proteins may have a viscosity of 10,000 cP to 20,000 cP.
  • composition comprising at least one of a peptide and a protein has a viscosity in the above range
  • the peptide or protein stabilizing effect of panthenol, a polyalcohol ester compound, casein or a derivative thereof can be exerted better.
  • Peptide or protein stabilization method is one or more of peptides and proteins; And mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein, and derivatives thereof to prepare the composition, wherein the prepared composition is -30 ° C to 30 ° C, specifically -24 ° C to 4 ° C.
  • the freezing conditions and the refrigeration conditions of -10 °C to 10 °C may further comprise the step of storing at room temperature conditions of 4 °C to 30 °C.
  • One aspect of the invention provides a cosmetic, pharmaceutical or food composition comprising a peptide or protein stabilizer comprising at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof.
  • Another aspect of the invention provides at least one of peptides and proteins; And it provides a cosmetic, pharmaceutical or food composition comprising at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
  • Another aspect of the invention provides at least one of peptides and proteins; And it provides a peptide or protein stabilization method comprising the step of preparing a cosmetic, pharmaceutical or food composition by mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
  • Cosmetic compositions according to the invention may be provided in all formulations suitable for topical application.
  • These compositions can be prepared according to conventional methods in the art.
  • the cosmetic composition according to the present invention may include other ingredients in addition to the above-mentioned substances within the range not impairing the main effect, preferably giving a synergistic effect to the main effect.
  • the cosmetic composition according to the present invention may further include a moisturizer, an emulsifier, an ultraviolet absorber, a preservative, a fungicide, an antioxidant, a pH adjuster, organic and inorganic pigments, flavors, coolants, or limiting agents.
  • the blending amount of the above components can be easily selected by those skilled in the art within the range that does not impair the object and effect of the present invention, the blending amount may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight based on the total weight of the composition. have.
  • the pharmaceutical composition according to an aspect of the present invention is not limited to the treatment of a particular disease, and includes a composition that can be used for medicinal purposes including peptides or proteins, and examples thereof include pharmaceutical compositions for promoting skin regeneration and wound healing. It is not limited.
  • composition according to one aspect of the present invention may be administered orally, rectally, topically, transdermally, intravenously, intramuscularly, intraperitoneally, subcutaneously, and the like.
  • Formulations for oral administration may be tablets, pills, soft and hard capsules, granules, powders, granules, solutions, emulsions or pellets, but are not limited thereto. It is not. These formulations may contain, in addition to the active ingredient, diluents (e.g. lactose, dextrose, sucrose, mannitol, sorbitol, cellulose or glycine), glidants (e.g. silica, talc, stearic acid or polyethylene glycol), or binders (e.g. magnesium aluminum Silicates, starch pastes, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose or polyvinylpyrrolidine). It may optionally contain pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, or sweeteners.
  • the tablets can be prepared by conventional mixing, granulating or coating methods.
  • Formulations for parenteral administration may be, but are not limited to, injections, drops, lotions, ointments, gels, creams, suspensions, emulsions, suppositories, patches or sprays.
  • the active ingredient of the pharmaceutical composition according to one aspect of the present invention will vary depending on the age, sex, weight, pathology and severity of the subject to be administered, the route of administration or the judgment of the prescriber. Dosage determination based on these factors is within the level of one skilled in the art and its daily dosage may be, for example, from 0.1 mg / kg / day to 100 mg / kg / day, more specifically from 5 mg / kg / day to 50 mg / kg. May be, but is not limited to.
  • the formulation of the food composition according to one aspect of the present invention is not particularly limited, but may be, for example, formulated into tablets, granules, drinks, caramels, diet bars and the like.
  • the food composition of each formulation may be suitably selected by a person skilled in the art according to the formulation or purpose of use in addition to the active ingredient, and may be synergistic when applied simultaneously with other raw materials.
  • the determination of the dosage of the active ingredient is within the level of those skilled in the art, and its daily dosage may vary depending on various factors such as the age, health condition, complications, etc. of the subject to be administered.
  • Example 1 includes panthenol, and Comparative Examples 1-4 comprise sugars.
  • the mixture was sufficiently mixed at 7000 rpm for 3 minutes while first adding an oil phase component to the aqueous phase component. Then, the epidermal growth factor solution was added and mixed well by homomixing for 1-2 minutes.
  • each composition was stored at 4 ° C, 25 ° C, and 50 ° C, and the content thereof was determined by ELISA (Enzyme-Linked ImmunoSorbent Assay). ) was confirmed by a measurement method. Measure the content value when stored at 4 °C and 25 °C for 2 weeks, then divide the content value after 2 weeks of storage at 4 °C from 2 weeks after storage at 25 °C to obtain relative thermal stability (%). After obtaining, it is shown in the table below.
  • the stability of epidermal cell growth factor in the example composition is significantly better than that of the comparative examples. That is, it can be seen that panthenol inhibits the reduction of the protein content, thereby increasing the stability of the protein composition.
  • Example 2 The cosmetic composition (emulsion) of Example 2 and Comparative Examples 6 to 8 was prepared in the same manner as in Example 1 and Comparative Examples 1 to 5 with the configuration of Table 3 below (unit: wt%).
  • Example 1 includes polyglyceryl-3 methylglucose distearate, which is a polyalcohol ester compound, while Comparative Examples 6 to 8 do not include it.
  • the epidermal growth factor content of each composition was measured (initial value), and at 4 ° C. and 25 ° C. for 1 year. After storage, the content of epidermal growth factor was confirmed by ELISA. The results are shown in the table below.
  • the hydrogenated series materials hydrogenated lecithin / C 12-16 alcohol / palmitic acid
  • sugar-based fatty acid esters that have been used as ingredients for formulating proteins.
  • the epithelial cell growth factor content is higher after one year of the example composition than the composition of the comparative examples comprising the expected surfactant (C 14-22 alcohol / C 12-20 alkyl glucoside or sucrose fatty acid ester).
  • the polyalcohol ester compound can increase the stability of the protein, and particularly, the effect is better when refrigerated than when stored at room temperature. Through this, it can be seen that the polyalcohol ester compound has an effect of stabilizing the protein because it inhibits the reduction of the protein content for a long storage period.
  • Example 3 contains casein hydrolysates, while Example 4 contains casein sodium, whereas Comparative Examples 9-14 do not.
  • the initial content of epithelial cell growth factor of each composition was confirmed by ELISA. After storage for 1 year at 4 °C, 25 °C and 45 °C and then measured the epidermal growth factor content in the same way, and after calculating the relative thermal stability (%) compared with the initial content for each storage temperature It is shown in the table below.
  • the epithelial cell growth factor content of the composition of the Example composition is higher than that of the comparative examples comprising lactoferrin, gelatin, glycoprotein (glycoprotein), whey or L-theanine, which are known as conventional protein stabilizing substances. high.
  • casein and its derivatives can increase the stability of epidermal growth factor, and particularly, the effect is better when stored at a temperature below room temperature.
  • casein and its derivatives have an effect of increasing the stability of the epidermal growth factor composition because it inhibits the decrease of the epidermal growth factor content for a long storage period.
  • Panthenol 2.0 100 ppm solution of epidermal growth factor 5.0 glycerin 3.0 Butylene glycol 2.0 Propylene glycol 2.0 Carboxy Vinyl Polymer 0.1 Fiji-12 nonylphenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 Preservative, coloring, flavoring Quantity Purified water Remaining amount
  • Table 8 ingredient Content (% by weight) Polyglyceryl-3 Methylglucose Distearate 5.0 100 ppm solution of epidermal growth factor 5.0 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxy Vinyl Polymer 0.1 Beeswax 4.0 Polysorbate 60 1.5 Caprylic / Capric Triglycerides 5.0 Squalane 5.0 Sorbitassquioleate 1.5 Liquid paraffin 0.5 Cetearyl Alcohol 1.0 Triethanolamine 0.2 Preservative, coloring, flavoring Quantity Purified water Remaining amount
  • Nutritional creams are prepared by conventional methods according to the compositions set forth in the table below.
  • Massage cream is prepared in a conventional manner according to the composition described in the table below.
  • Panthenol 8.0 100 ppm solution of epidermal growth factor 5.0 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 45.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / Capric Triglycerides 3.0 Beeswax 4.0 Cetearyl Glucoside 1.5 Sesqui oleic acid sorbitan 0.9 Vaseline 3.0 paraffin 1.5 Preservative, coloring, flavoring Quantity Purified water Remaining amount
  • Packs are prepared by conventional methods according to the compositions described in the table below.
  • Injections are prepared by conventional methods according to the compositions listed in the table below.
  • Ointments are prepared by conventional methods according to the compositions described in the table below.
  • Table 14 ingredient Content (% by weight) Polyglyceryl-3 Methylglucose Distearate 0.1 glycerin 8.0 Butylene glycol 4.0 Floating paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / Capric Triglycerides 3.0 Squalane 1.0 Cetearyl Glucoside 1.5 Sorbitan stearate 0.4 Cetearyl Alcohol 1.0 Beeswax 4.0 Preservative, coloring, flavoring Quantity Purified water Remaining amount

Abstract

The present invention relates to a composition for stabilizing peptides or proteins which comprises at least one selected from the group consisting of panthenol, polyalcohol ester-based compound, casein, and derivatives thereof. In addition, the invention relates to a composition comprising at least one selected from the group consisting of: at least one of peptides or proteins; and at least one of panthenol, polyalcohol ester-based compound, casein, and derivatives thereof. Furthermore, the invention relates to a method for stabilizing peptides or proteins, which comprises a step for preparing a composition by mixing at least one of peptides or proteins with at least one selected from the group consisting of panthenol, polyalcohol ester-based compound, casein, and derivatives thereof.

Description

펩타이드 또는 단백질 안정화제Peptide or Protein Stabilizer
본 발명은 펩타이드 또는 단백질을 안정하게 하는 제제에 관한 것이다.The present invention relates to agents that stabilize peptides or proteins.
단백질은 모든 생물의 몸을 구성하는 고분자 유기물로 수많은 아미노산(amino acid)의 연결체이다. 이는 생물체의 몸의 구성 성분으로서, 또 세포 내의 각종 화학 반응의 촉매 물질로서 중요하다.  이러한 특성을 기초로 단백질은 식품, 의약품 또는 화장료 분야 등을 예로 들 수 있는 다양한 분야에서 널리 활용되고 있다.Proteins are high-molecular organic compounds that make up the body of every organism. It is important as a constituent of the body of an organism and as a catalyst for various chemical reactions in cells. Based on these characteristics, proteins are widely used in various fields such as food, medicine, or cosmetics.
본 발명은 펩타이드 또는 단백질 안정화제 및 펩타이드 또는 단백질이 안정하게 유지되는 조성물을 제공하고자 한다. 또한 본 발명은 펩타이드 또는 단백질을 안정화시키는 방법을 제공하고자 한다.The present invention seeks to provide a peptide or protein stabilizer and a composition in which the peptide or protein remains stable. The present invention also provides a method of stabilizing a peptide or protein.
본 발명의 일측면은 판테놀(panthenol), 폴리알코올 에스터계 화합물, 카제인(casein) 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 펩타이드 또는 단백질 안정화제를 제공한다.One aspect of the present invention provides a peptide or protein stabilizer comprising at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein, and derivatives thereof.
본 발명의 다른 일측면은 펩타이드 및 단백질 중 하나 이상; 및 판테놀(panthenol), 폴리알코올 에스터계 화합물, 카제인(casein) 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 조성물을 제공한다.Another aspect of the invention provides at least one of peptides and proteins; And it provides a composition comprising at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
본 발명의 또 다른 일측면은 펩타이드 및 단백질 중 하나 이상; 및 판테놀(panthenol), 폴리알코올 에스터계 화합물, 카제인(casein) 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 혼합하여 조성물을 제조하는 단계를 포함하는 펩타이드 또는 단백질 안정화 방법을 제공한다.Another aspect of the invention provides at least one of peptides and proteins; And it provides a peptide or protein stabilization method comprising the step of preparing a composition by mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
본 발명의 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상은 펩타이드 또는 단백질을 안정화시키는 효과가 뛰어나다. 본 발명의 일측면에 따른 펩타이드 및 단백질 중 하나 이상을 포함하는 조성물은 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함함으로써, 펩타이드 또는 단백질이 오랜 기간 분해되지 않고 안정하게 유지될 수 있다. 특히, 펩타이드 또는 단백질을 용해된 상태로 포함하는 조성물의 경우 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함함으로써, 펩타이드 또는 단백질의 분해가 거의 이루어지지 않으므로 사용 직전 펩타이드 또는 단백질을 용해시킬 필요가 없으며 펩타이드 또는 단백질을 포함한 상태로 보관 및 유통이 용이하다.At least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof of the present invention is excellent in stabilizing peptides or proteins. The composition comprising at least one of the peptides and proteins according to one aspect of the invention comprises at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof, so that the peptide or protein is not degraded for a long time. Can be kept stable. In particular, in the case of a composition containing a peptide or protein in a dissolved state, by including one or more selected from the group consisting of panthenol, polyalcohol ester compound, casein, and derivatives thereof, since the peptide or protein is hardly decomposed, immediately before use There is no need to dissolve the peptide or protein and it is easy to store and distribute with the peptide or protein included.
펩타이드 또는 단백질은 식품, 의약품 또는 화장료 분야 등 다양한 분야에서 이용되고 있으나, 외부의 물리적 및 화학적 조건, 특히 고온 조건에서 불안정하여 제제화하기가 용이하지 않다. 또한 펩타이드 또는 단백질을 용해시키면 쉽게 분해되므로 용해된 펩타이드 또는 단백질을 사용하고자 하는 경우 사용 직전 용해시켜야 하는 불편함이 있다. 이러한 문제점을 해결하기 위해 슈크로스, 트레할로스, 프럭토스, 만니톨 등과 같은 당류를 펩타이드 및 단백질 중 하나 이상을 포함하는 조성물에 포함시켜 펩타이드 또는 단백질 안정화를 꾀하려는 시도가 있었으나, 그 효과가 만족스러운 정도는 아니다.Peptides or proteins are used in various fields, such as food, medicine or cosmetics, but they are unstable under external physical and chemical conditions, especially at high temperature, and are not easy to formulate. In addition, since the peptide or protein is easily dissolved when dissolved, it is inconvenient to dissolve immediately before use if the peptide or protein is to be used. In order to solve this problem, attempts have been made to include peptides such as sucrose, trehalose, fructose and mannitol in a composition containing at least one of peptides and proteins to stabilize peptides or proteins, but the degree of effect is satisfactory. no.
이하, 본 발명을 상세하게 설명한다.EMBODIMENT OF THE INVENTION Hereinafter, this invention is demonstrated in detail.
본 발명의 일측면은 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 펩타이드 또는 단백질 안정화제를 제공한다. 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상은 펩타이드 또는 단백질을 물리적 및 화학적으로 보호하여 펩타이드 또는 단백질이 분해되는 것을 방지하므로 펩타이드 또는 단백질을 장기간 안정하게 유지시킬 수 있다.One aspect of the present invention provides a peptide or protein stabilizer comprising one or more selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof. The at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof can physically and chemically protect the peptide or protein to prevent the peptide or protein from being degraded, thereby keeping the peptide or protein stable for a long time. .
본 발명의 일측면은 펩타이드 및 단백질 중 하나 이상; 및 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 조성물을 제공한다. 상기 조성물은 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함함으로써, 그에 포함된 펩타이드 또는 단백질이 장기간 분해되지 않고 안정하게 유지될 수 있다.One aspect of the invention is at least one of a peptide and a protein; And it provides a composition comprising at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof. The composition comprises at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof, so that the peptide or protein contained therein can be stably maintained without prolonged degradation.
본 발명의 일측면은 펩타이드 및 단백질 중 하나 이상; 및 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 혼합하여 조성물을 제조하는 단계를 포함하는 펩타이드 또는 단백질 안정화 방법을 제공한다. 이와 같은 방법으로 펩타이드 또는 단백질과 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 혼합함으로써, 펩타이드 또는 단백질을 오랜 기간 분해 없이 안정하게 유지시킬 수 있다.One aspect of the invention is at least one of a peptide and a protein; And it provides a peptide or protein stabilization method comprising the step of preparing a composition by mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof. In this way, the peptide or protein is mixed with one or more selected from the group consisting of panthenol, polyalcohol ester compound, casein, and derivatives thereof, so that the peptide or protein can be stably maintained without degradation for a long time.
본 명세서에서 판테놀(panthenol)은 비타민 B군 중 하나인 판토텐산(pantothenic acid)의 알코올 유도체이며, 아래와 같은 화학식 1로 표현될 수 있다.In this specification, panthenol is an alcohol derivative of pantothenic acid, which is one of the vitamin B groups, and may be represented by the following Chemical Formula 1.
화학식 1
Figure PCTKR2011009190-appb-C000001
Formula 1
Figure PCTKR2011009190-appb-C000001
본 명세서에서 판테놀의 유도체는 판테놀의 일부를 화학적으로 변화시켜서 얻을 수 있는 모든 화합물을 포함하는 개념으로, 수소 또는 특정 원자단이 다른 원자 또는 원자단으로 치환된 것을 모두 포함한다. 보다 구체적으로 판테놀의 유도체는 알란토인 칼슘 판토테이트(Allantoin Calcium Pantothenate), 칼슘 판토테네이트(Calcium Pantothenate), 에틸 디카르보에톡시 판토테네이트(Ethyl Dicarboethoxy Pantothenate, C17H29NO9, 화학식 2), 하이드록시에틸 판토텐아마이드 MEA(Hydroxyethyl Pantothenamide MEA, C13H26N2O6, 화학식 3), 판토텐아마이드 MEA(Pantothenamide MEA, C11H22N2O5, 화학식 4), 판토텐산(Pantothenic Acid, C9H17NO5, 화학식 5), 판토테노일 디펩타이드-13(Pantothenoyl Dipeptide-13), 소듐 판토테네이트(Sodium Pantothenate), 판테닐에틸에테르(PanthenylEthylether), 판테닐에틸에테르 아세테이트(PanthenylEthylether acetate, C13H25NO5, 화학식 6) 및 판테닐 트리아세테이트(panthenyl triacetate, C15H25NO7, 화학식 7)로 이루어진 군에서 선택된 하나 이상을 포함한다.As used herein, the derivative of panthenol includes all compounds that can be obtained by chemically changing a part of panthenol, and includes hydrogen or a specific atomic group all substituted with another atom or atomic group. More specifically, derivatives of panthenol include allantoin calcium pantothenate, calcium pantothenate, ethyl dicarboethoxy pantothenate (C 17 H 29 NO 9 , formula 2), Hydroxyethyl Pantothenamide MEA (C 13 H 26 N 2 O 6 , Formula 3), Pantothenamide MEA, C 11 H 22 N 2 O 5 , Formula 4), Pantothenic Acid , C 9 H 17 NO 5 , Formula 5), Pantothenoyl Dipeptide-13, Sodium Pantothenate, PanthenylEthylether, PanthenylEthylether acetate, C 13 H 25 NO 5 , formula 6) and panthenyl triacetate (C 15 H 25 NO 7 , formula 7).
화학식 2
Figure PCTKR2011009190-appb-C000002
Formula 2
Figure PCTKR2011009190-appb-C000002
화학식 3
Figure PCTKR2011009190-appb-C000003
Formula 3
Figure PCTKR2011009190-appb-C000003
화학식 4
Figure PCTKR2011009190-appb-C000004
Formula 4
Figure PCTKR2011009190-appb-C000004
화학식 5
Figure PCTKR2011009190-appb-C000005
Formula 5
Figure PCTKR2011009190-appb-C000005
화학식 6
Figure PCTKR2011009190-appb-C000006
Formula 6
Figure PCTKR2011009190-appb-C000006
화학식 7
Figure PCTKR2011009190-appb-C000007
Formula 7
Figure PCTKR2011009190-appb-C000007
본 명세서에서, 폴리알코올 에스터(polyalcohol estesr)계 화합물은 폴리알코올 에스터기를 포함하는 화합물을 의미한다. 본 발명의 일측면에서, 폴리알코올 에스터계 화합물 및 그 유도체는 폴리알코올과 스테아르산(stearic acid)이 에스터 결합하고 있는 화합물을 포함하며, 구체적으로 폴리글리세릴 스테아레이트, 폴리글리세릴 디스테아레이트, PEG 스테아레이트, PEG 디스테아레이트, 폴리글리세릴 메틸글루코스 디스테아레이트 또는 PEG 메틸 글루코스 디스테아레이트, 보다 더 구체적으로 폴리글리세릴-3 메틸글루코스 디스테아레이트 또는 PEG-20 메틸 글루코스 디스테아레이트를 포함한다. 본 발명의 다른 일측면에서, 폴리알코올 에스터계 화합물은 계면 활성제로 작용하는 화합물을 포함한다.In the present specification, a polyalcohol ester compound refers to a compound including a polyalcohol ester group. In one aspect of the present invention, the polyalcohol ester compound and derivatives thereof include a compound in which the ester of polyalcohol and stearic acid is esterified, and specifically, polyglyceryl stearate, polyglyceryl distearate, PEG stearate, PEG distearate, polyglyceryl methylglucose distearate or PEG methyl glucose distearate, and more particularly polyglyceryl-3 methylglucose distearate or PEG-20 methyl glucose distearate do. In another aspect of the present invention, the polyalcohol ester compound includes a compound that acts as a surfactant.
본 명세서에서, 카제인(casein) 유도체는 카제인의 일부를 화학적으로 변화시켜서 얻을 수 있는 모든 화합물을 포함하는 개념이다. 본 발명의 일측면에서, 카제인 또는 그 유도체는 카제인을 산 또는 효소로 가수 분해한 카제인 가수 분해물 또는 카제인 나트륨과 같은 카제인 염을 포함한다. 본 발명의 일측면에서, 카제인 또는 그 유도체는 자신 외에 조성물에 함께 포함된 다른 단백질을 안정화시킬 수 있다.In this specification, a casein derivative is a concept including all compounds that can be obtained by chemically changing a part of casein. In one aspect of the invention, the casein or derivative thereof includes a casein salt such as casein hydrolysate or casein sodium hydrolyzed casein with an acid or enzyme. In one aspect of the invention, the casein or derivative thereof may stabilize other proteins included in the composition in addition to itself.
본 발명의 일측면에서, 펩타이드는 아미노산의 중합 분자를 의미하며, 아미노산이 2개 내지 10개 연결된 것에서부터, 10 내지 20개 또는 20개 이상 연결된 폴리펩타이드를 포함하는 개념이다. 본 발명의 다른 일측면에서, 펩타이드는 10개 내외의 아미노산이 연결된 것을 포함한다.In one aspect of the invention, a peptide refers to a polymerized molecule of amino acids, from 2 to 10 amino acids are linked, it is a concept including a polypeptide of 10 to 20 or more than 20 linked. In another aspect of the present invention, the peptide comprises about 10 amino acids linked.
본 발명의 일측면에서, 단백질은 일반적으로 단백질로 분류될 수 있는 모든 물질을 포함한다.In one aspect of the invention, proteins generally include all substances that can be classified as proteins.
본 발명의 일측면에서, 펩타이드 또는 단백질은 일반적으로 의약품, 화장료 또는 식품 조성물에 포함되는 효능 성분을 의미할 수 있다. 본 발명의 다른 일측면에서, 펩타이드 또는 단백질은 동물 또는 식물에서 추출한 것을 포함한다. 본 발명의 또 다른 일측면에서, 펩타이드 또는 단백질은 성장 인자, 호르몬, 인터페론, 백신, 재조합 단백질, 재조합 펩타이드 및 효소 중 하나 이상을 포함한다. 보다 구체적으로, 펩타이드 또는 단백질은 상피 세포 성장 인자(Epidermal Growth Factor), 염기성 섬유모세포 증식 인자(basic Fibroblast Growth Factor), 혈소판 유래 성장 인자(Platelet Derived Growth Factor), 혈관 내피 성장 인자 (Vascular Endothelial Growth Factor), 티로신 키나아제 리간드(Tyrosine Kinase Ligand), 인터루킨 1 알파(IL1α, Interleukin 1 Alpha), 인터루킨 1 베타(IL1β, Interleukin 1 Beta), 인터루킨 17 알파(Interleukin 17 Alpha), C-C 모티프 케모카인 리간드 5(C-C Motif Chemokine Ligand 5), 인간 성장 호르몬(Human Growth Hormone), 인슐린, 아실 코엔자임 A 디새튜라아제(Acyl Coenzyme A Desaturase), 알부민(Albumin), 알칼라인 포스파타아제(Alkaline Phosphatase), 아미노펩티다아제(Aminopeptidase), 아밀라아제(Amylase), 아밀로글루코시다아제(Amyloglucosidase), 아포-락토페린(Apo-Lactoferrin), 아르트로스피라 추출물(Arthrospira Extract), 브로멜라인(Bromelain), 카제인(Casein), 카탈라아제(Catalase), 셀룰라아제(Cellulase), 콜라겐(Collagen), 크리스탈린(Crystallins), 시토크롬 C(Cytochrome C), 디옥시리보뉴클레아제(Deoxyribonuclease), 엘라스틴(Elastin), 피브로넥틴(Fibronectin), 피신(Ficin), 피쉬 플라즈마 단백질(Fish Plasma Protein), 갈락토오스 디하이드로게나아제(Galactose Dehydrogenase), 젤라틴(Gelatin), 젤리듐 펄크룸 단백질(Gelidium Pulchrum Protein), 글리아딘(Gliadin), 글루코즈 옥시다아제(Glucose Oxidase), 글리코프로테인(Glycoproteins), 헤모글로빈(Hemoglobin), 헤스페리디나아제(Hesperidinase), 호올스디쉬 퍼옥시다아제(Horseradish Peroxidase), 인간 플라센타 효소(Human Placental Enzymes), 플라센타 단백질(Placental Protein), 인간 플라센타 단백질(Human Placental Protein), 히알루로니다아제(Hyaluronidase), 하이드록시스테로이드 산화환원효소(Hydroxysteroid Oxidoreductase), 칼리크레인(Kallikrein), 케라틴(Keratin), 라카아제(Laccase), 락테이트 디하이드로게나아제(Lactate Dehydrogenase), 락티스 프로테늄(Lactis Proteinum), 락토페린(Lactoferrin), 락토글로불린(Lactoglobulin), 락토퍼옥시다아제(Lactoperoxidase), 리그니나아제(Ligninase), 리파아제(Lipase), 루피너스 알부스 단백질(Lupinus Albus Protein), 리소자임(Lysozyme), 리소자임 베타-글루칸(Lysozyme Beta-Glucan), 마크로시스티스 피리페라(켈프) 단백질(Macrocystis Pyrifera (Kelp) Protein), 우유 단백질(Milk Protein), 진주 단백질(Nacre Protein), 오리자 사티바(라이스) 브란 단백질(Oryza Sativa (Rice) Bran Protein), 오리자 사티바(라이스) 씨드 단백질(Oryza Sativa (Rice) Seed Protein), 산화환원효소(Oxido Reductases), 판크레아틴(Pancreatin), 파파인(Papain), 파파인 베타-글루칸(Papain Beta-Glucan), 펩신(Pepsin), 프로테아제(Protease), 프루누스 아미그달루스 둘시스(스위트 아몬드) 단백질(Prunus Amygdalus Dulcis (Sweet Almond) Protein), r-크로스트리듐 히스토일티쿰 콜라게나아제(r-Clostridium Histolyticum Collagenase), 세라리신(Serralysin), 세럼 알부민(Serum Albumin), 세럼 프로테인(Serum Protein), 실크(Silk), 용해성 엘라스틴(Soluble Elastin), 용해성 케라틴(Soluble Keratin), 용해성 프로테오글리칸(Soluble Proteoglycan), 소이빈 퍼옥시다아제(Soybean Peroxidase), 서브틸리신(Subtilisin), 서틸레인(Sutilains), 트립신(Trypsin), 티로시나아제(Tyrosinase), 유레아제(Urease), 훼이 단백질(Whey Protein), 제인(Zein), aFGF(Fibroblast Growth Factor), FGF-1, FGF-2, FGF-7, FGF-10, 인슐린 유사 성장 인자-1(IGF-1, Insulin-like growth factor), IGF-2, 케라티노사이트 성장 인자(KGF, Keratinocyte Growth Factor), KGF-2, β-NGF(Nerve Growth factor), 단백질 태반 성장 인자-1CG(Protein PIGF-1CG), 전환 성장 인자(TGF)-α, TGF-beta-1, TGF-3, 티오레독신(Thioredoxin), 줄기 세포 인자(Stem Cell Factor), Il-2, IL-10, IL-4, 메탈로프로테이나아제-2의 조직 저해제(Tissue Inhibitor of Metalloproteinases-2), 플라센타 성장 인자(Placenta Growth Factor), 태아 간 키나아제-2(fetal liver kinase-2), SOD(Superoxide dismutase), 트리파타이트 모티프-포함 단백질(Tripartite motif-containing protein), 티모신(Thymosin), 인간 베타 디펜신(Human Beta Defensin), 일반적으로 보톡스®라고 불리는 보툴리늄 톡신(botulinum toxin) 및 소아마비, 디프테리아, 백일해, 홍역, 풍진, 장티푸스, 파라장티푸스, 콜레라, 페스트, 결핵, 파상열, 야토병(野兎病), 포도상구균 또는 연쇄상구균에 의한 만성 감염증, 파상풍, 독감, 황열, 뇌염, 로키산홍반열, 발진티푸스 또는 B형 간염 등에 대한 백신에 사용되는 항원으로 이루어진 그룹에서 선택된 하나 이상을 포함하나, 이에 제한되는 것은 아니다. 본 발명의 또 다른 일측면에서, 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 것이 카제인 또는 그 유도체인 경우, 펩타이드 및 단백질 중 선택된 하나 이상은 카제인 또는 우유 단백질을 포함하지 않는다.In one aspect of the invention, the peptide or protein may refer to a potent ingredient generally included in a pharmaceutical, cosmetic or food composition. In another aspect of the invention, peptides or proteins include those extracted from animals or plants. In another aspect of the invention, the peptide or protein comprises one or more of growth factors, hormones, interferons, vaccines, recombinant proteins, recombinant peptides and enzymes. More specifically, the peptide or protein may include epidermal growth factor, basic fibroblast growth factor, platelet derived growth factor, and vascular endothelial growth factor. ), Tyrosine Kinase Ligand, Interleukin 1 Alpha, Interleukin 1 Beta, Interleukin 17 Alpha, CC Motif Chemokine Ligand 5 (CC Motif) Chemokine Ligand 5), Human Growth Hormone, Insulin, Acyl Coenzyme A Desaturase, Albumin (Albumin), Alkaline Phosphatase, Aminopeptidase, Amylase (Amylase), Amyloglucosidase, Apo-Lactoferrin, Arthrospira Extract, Bromelain, Casein, Catalase, Cellulase, Cellulase, Collagen, Crystallins, Cytochrome C, Deoxyribonuclease, Elastin Elastin, Fibronectin, Ficin, Fish Plasma Protein, Galactose Dehydrogenase, Gelatin, Gelidium Pulchrum Protein, Glia Gliadin, Glucose Oxidase, Glycoproteins, Hemoglobin, Hesperidinase, Horsadish Peroxidase, Human Placenta Enzyme, Human Enzyme, Enzyme Placental Enzyme Placenta Protein, Human Placental Protein, Hyaluronidase, Hydroxysteroid Oxygen idoreductase, Kallikrein, Keratin, Lacase, Lactate Dehydrogenase, Lactis Proteinum, Lactoferrin, Lactoglobulin , Lactoperoxidase, Ligninase, Ligninase, Lipase, Lupineus Albus Protein, Lysozyme, Lysozyme Beta-Glucan, Macrosistis Macrocystis Pyrifera (Kelp) Protein, Milk Protein, Nacre Protein, Oryza Sativa (Rice) Bran Protein, Orissa Oryza Sativa (Rice) Seed Protein, Oxido Reductases, Pancreatin, Papain, Papain Beta-Glucan, Pepsin ), Protease, Prunus Prunus Amygdalus Dulcis (Sweet Almond) Protein, r-Clostridium Histolyticum Collagenase, Serralysin, Serum Albumin Albumin, Serum Protein, Silk, Soluble Elastin, Soluble Keratin, Soluble Proteoglycan, Soybean Peroxidase, Subtilisin ), Sutilains, Trypsin, Tyrosinase, Urease, Whey Protein, Zein, Fibroblast Growth Factor, FGF-1, FGF -2, FGF-7, FGF-10, Insulin-like growth factor-1 (IGF-1), IGF-2, Keratinocyte Growth Factor (KGF), KGF-2, β-NGF (Nerve Growth factor), Protein Placental Growth Factor-1CG (Protein PIGF-1CG), Converting Growth Factor (TGF) -α, TGF-beta-1, TGF-3, Thioredoxin, Stem Cell Factor, Tissue Inhibitors of Il-2, IL-10, IL-4, Metalloproteinase-2 Inhibitor of Metalloproteinases-2), Placenta Growth Factor, Fetal Liver Kinase-2, Superoxide Dismutase, Tripartite Motif-Containing Protein, Thymosin, Human Beta Defensin, botulinum toxin, commonly referred to as Botox ® , and polio, diphtheria, pertussis, measles, rubella, typhoid fever, paratyphoid fever, cholera, plague, tuberculosis, One selected from the group consisting of antigens used for vaccines against tetanus, yato disease, staphylococcus or streptococci, chronic infections, tetanus, flu, yellow fever, encephalitis, roche erythematosus, rash typhus or hepatitis B Including the above, It is not limited to this. In another aspect of the invention, when the casein or derivative thereof is selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof, at least one selected from peptides and proteins does not comprise casein or milk protein .
본 발명의 일측면에서, 펩타이드 또는 단백질을 포함하는 조성물은 펩타이드 또는 단백질의 함량, 펩타이드 또는 단백질을 포함하는 조성물의 점도 또는 펩타이드 또는 단백질을 포함하는 조성물의 보관 온도 및 기간 등과 같은 보관 조건 등에 따라 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 다양한 함량으로 포함할 수 있다. 보다 구체적으로 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 조성물 전체 중량 대비 0.1 내지 50 중량%, 구체적으로 0.5 내지 30 중량%, 더 구체적으로 1 내지 20 중량%로 포함할 수 있다. 상기 중량%로 포함되는 경우 본 발명의 의도한 효과를 나타내기에 적절할 뿐만 아니라, 조성물의 안정성 및 안전성을 모두 만족할 수 있으며, 비용 대비 효과의 측면에서도 상기 범위로 포함하는 것이 적절할 수 있다.In one aspect of the invention, the composition comprising the peptide or protein is panthenol depending on the storage conditions such as the content of the peptide or protein, the viscosity of the composition comprising the peptide or protein or the storage temperature and duration of the composition comprising the peptide or protein, etc. , Polyalcohol ester compounds, casein and derivatives thereof may include one or more selected from the group consisting of various contents. More specifically, at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof is 0.1 to 50% by weight, specifically 0.5 to 30% by weight, and more specifically 1 to 20% by weight, based on the total weight of the composition. It may include. When included in the weight percent, not only is it appropriate to exhibit the intended effect of the present invention, but also satisfies both the stability and safety of the composition, it may be appropriate to include in the above range in terms of cost-effectiveness.
본 발명의 일측면에서, 펩타이드 및 단백질 중 하나 이상과 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상의 중량비는 50,000,000 : 1 내지 1 : 1 또는 1 : 1 내지 1 : 50,000,000, 구체적으로 10,000,000 : 1 내지 1 : 1 또는 1 : 1 내지 1 : 10,000,000, 더 구체적으로 500,000 : 1 내지 1 : 1 또는 1 : 1 내지 500,000일 수 있다. 상기 중량비로 포함되는 경우 본 발명의 의도한 효과를 나타내기에 적절할 뿐만 아니라, 조성물의 안정성 및 안전성을 모두 만족할 수 있으며, 비용 대비 효과의 측면에서도 적절할 수 있다.In one aspect of the invention, the weight ratio of at least one of the peptides and proteins and at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof is 50,000,000: 1 to 1: 1 or 1: 1: 1 to 50,000,000 For example, it may be 10,000,000: 1 to 1: 1 or 1: 1 to 1: 10,000,000, more specifically 500,000: 1 to 1: 1 or 1: 1 to 500,000. When included in the weight ratio, not only is it appropriate to exhibit the intended effect of the present invention, but also satisfies both the stability and safety of the composition, and may be appropriate in terms of cost-effectiveness.
본 발명의 일측면에서, 펩타이드 및 단백질 중 하나 이상을 포함하는 조성물은 5,000 cP 내지 30,000 cP의 점도를 가질 수 있다. 본 발명의 다른 일측면에서, 펩타이드 및 단백질 중 하나 이상을 포함하는 조성물은 8,000 cP 내지 25,000 cP의 점도를 가질 수 있다. 본 발명의 또 다른 일측면에서, 펩타이드 및 단백질 중 하나 이상을 포함하는 조성물은 10,000 cP 내지 20,000 cP의 점도를 가질 수 있다. 펩타이드 및 단백질 중 하나 이상을 포함하는 조성물이 상기와 같은 범위의 점도를 가질 때, 판테놀, 폴리알코올 에스터계 화합물, 카제인 또는 그들의 유도체의 펩타이드 또는 단백질 안정화 효과가 보다 잘 발휘될 수 있다. In one aspect of the invention, a composition comprising at least one of a peptide and a protein may have a viscosity of 5,000 cP to 30,000 cP. In another aspect of the invention, a composition comprising one or more of peptides and proteins may have a viscosity of 8,000 cP to 25,000 cP. In another aspect of the invention, a composition comprising one or more of peptides and proteins may have a viscosity of 10,000 cP to 20,000 cP. When a composition comprising at least one of a peptide and a protein has a viscosity in the above range, the peptide or protein stabilizing effect of panthenol, a polyalcohol ester compound, casein or a derivative thereof can be exerted better.
본 발명의 일측면에 따른 펩타이드 또는 단백질 안정화 방법은 펩타이드 및 단백질 중 하나 이상; 및 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 혼합하여 조성물을 제조하는 단계 이후에, 제조한 조성물을 -30℃ 내지 30℃, 구체적으로 -24℃ 내지 4℃의 냉동 조건과 -10℃ 내지 10℃의 냉장 조건, 4℃ 내지 30℃의 실온 조건에서 보관하는 단계를 더 포함할 수 있다.Peptide or protein stabilization method according to an aspect of the present invention is one or more of peptides and proteins; And mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein, and derivatives thereof to prepare the composition, wherein the prepared composition is -30 ° C to 30 ° C, specifically -24 ° C to 4 ° C. The freezing conditions and the refrigeration conditions of -10 ℃ to 10 ℃, may further comprise the step of storing at room temperature conditions of 4 ℃ to 30 ℃.
본 발명의 일측면은 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 펩타이드 또는 단백질 안정화제를 포함하는 화장료, 약학 또는 식품 조성물을 제공한다. 본 발명의 다른 일측면은 펩타이드 및 단백질 중 하나 이상; 및 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 화장료, 약학 또는 식품 조성물을 제공한다. 본 발명의 또 다른 일측면은 펩타이드 및 단백질 중 하나 이상; 및 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 혼합하여 화장료, 약학 또는 식품 조성물을 제조하는 단계를 포함하는 펩타이드 또는 단백질 안정화 방법을 제공한다.One aspect of the invention provides a cosmetic, pharmaceutical or food composition comprising a peptide or protein stabilizer comprising at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein and derivatives thereof. Another aspect of the invention provides at least one of peptides and proteins; And it provides a cosmetic, pharmaceutical or food composition comprising at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof. Another aspect of the invention provides at least one of peptides and proteins; And it provides a peptide or protein stabilization method comprising the step of preparing a cosmetic, pharmaceutical or food composition by mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
본 발명에 따른 화장료 조성물은 국소 적용에 적합한 모든 제형으로 제공될 수 있다. 예를 들면, 용액, 겔, 고체, 페이스트, 반죽 무수 생성물, 수상에 유상을 분산시켜 얻은 에멀젼, 유상에 수상을 분산시켜 얻은 에멀젼, 현탁액, 분말, 페이스트, 마이크로 니들, 포말(foam) 또는 에어로졸 조성물의 형태로 제공될 수 있다. 이들 조성물은 당해 분야의 통상적인 방법에 따라 제조될 수 있다.Cosmetic compositions according to the invention may be provided in all formulations suitable for topical application. For example, emulsions obtained by dispersing the oil phase in solutions, gels, solids, pastes, anhydrous products, water phases, emulsions obtained by dispersing the oil phases in water, suspensions, powders, pastes, microneedles, foams or aerosol compositions. It may be provided in the form of. These compositions can be prepared according to conventional methods in the art.
본 발명에 따른 화장료 조성물은 상기한 물질 이외에 주 효과를 손상시키지 않는 범위 내에서, 바람직하게는 주 효과에 상승 효과를 줄 수 있는 다른 성분들을 포함할 수 있다. 또한 본 발명에 따른 화장료 조성물은 보습제, 에몰리언트제, 자외선 흡수제, 방부제, 살균제, 산화 방지제, pH 조정제, 유기 및 무기 안료, 향료, 냉감제 또는 제한(制汗)제를 더 포함할 수 있다. 상기 성분의 배합량은 본 발명의 목적 및 효과를 손상시키지 않는 범위 내에서 당업자가 용이하게 선정 가능하며, 그 배합량은 조성물 전체 중량을 기준으로 0.01 내지 5 중량%, 구체적으로 0.01 내지 3 중량%일 수 있다.The cosmetic composition according to the present invention may include other ingredients in addition to the above-mentioned substances within the range not impairing the main effect, preferably giving a synergistic effect to the main effect. In addition, the cosmetic composition according to the present invention may further include a moisturizer, an emulsifier, an ultraviolet absorber, a preservative, a fungicide, an antioxidant, a pH adjuster, organic and inorganic pigments, flavors, coolants, or limiting agents. The blending amount of the above components can be easily selected by those skilled in the art within the range that does not impair the object and effect of the present invention, the blending amount may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight based on the total weight of the composition. have.
본 발명의 일측면에 따른 약학 조성물은 특정 질병 치료에 한정되지 않고 펩타이드 또는 단백질을 포함하여 의약적 용도로 사용될 수 있는 조성물을 포함하며, 피부 재생 및 상처 치유 촉진용 약학 조성물을 예로 들 수 있으나 이에 제한되는 것은 아니다.The pharmaceutical composition according to an aspect of the present invention is not limited to the treatment of a particular disease, and includes a composition that can be used for medicinal purposes including peptides or proteins, and examples thereof include pharmaceutical compositions for promoting skin regeneration and wound healing. It is not limited.
본 발명의 일측면에 따른 약학 조성물은 경구, 직장, 국소, 경피, 정맥 내, 근육 내, 복강 내, 피하 등으로 투여될 수 있다.The pharmaceutical composition according to one aspect of the present invention may be administered orally, rectally, topically, transdermally, intravenously, intramuscularly, intraperitoneally, subcutaneously, and the like.
경구 투여를 위한 제형은 정제(錠劑), 환제(丸劑), 연질 및 경질 캅셀제, 과립제(顆粒劑), 산제, 세립제, 액제, 유탁제(乳濁濟) 또는 펠렛제일 수 있으나, 이에 제한되는 것은 아니다. 이들 제형은 유효 성분 이외에 희석제(예: 락토오스, 덱스트로오스, 수크로오스, 만니톨, 솔비톨, 셀룰로오스 또는 글리신), 활택제(예: 실리카, 탈크, 스테아르산 또는 폴리에틸렌 글리콜), 또는 결합제(예: 마그네슘 알루미늄 실리케이트, 전분 페이스트, 젤라틴, 트라가칸스, 메틸셀룰로오스, 나트륨 카르복시메틸셀룰로오스 또는 폴리비닐피롤리딘)를 함유할 수 있다. 경우에 따라 붕해제, 흡수제, 착색제, 향미제, 또는 감미제 등의 약제학적 첨가제를 함유할 수 있다. 상기 정제는 통상적인 혼합, 과립화 또는 코팅 방법에 의해 제조될 수 있다.Formulations for oral administration may be tablets, pills, soft and hard capsules, granules, powders, granules, solutions, emulsions or pellets, but are not limited thereto. It is not. These formulations may contain, in addition to the active ingredient, diluents (e.g. lactose, dextrose, sucrose, mannitol, sorbitol, cellulose or glycine), glidants (e.g. silica, talc, stearic acid or polyethylene glycol), or binders (e.g. magnesium aluminum Silicates, starch pastes, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose or polyvinylpyrrolidine). It may optionally contain pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, or sweeteners. The tablets can be prepared by conventional mixing, granulating or coating methods.
비경구 투여를 위한 제제는 주사제, 점적제, 로션, 연고, 겔, 크림, 현탁제, 유제, 좌제(坐劑), 패취 또는 분무제일 수 있으나, 이에 제한되는 것은 아니다.Formulations for parenteral administration may be, but are not limited to, injections, drops, lotions, ointments, gels, creams, suspensions, emulsions, suppositories, patches or sprays.
본 발명의 일측면에 따른 약학 조성물의 유효 성분은 투여 받을 대상의 연령, 성별, 체중, 병리 상태 및 그 심각도, 투여 경로 또는 처방자의 판단에 따라 달라질 것이다. 이러한 인자에 기초한 적용량 결정은 당업자의 수준 내에 있으며, 이의 1일 투여 용량은 예를 들어 0.1mg/kg/일 내지 100mg/kg/일, 보다 구체적으로는 5 mg/kg/일 내지 50 mg/kg/일이 될 수 있으나, 이에 제한되는 것은 아니다.The active ingredient of the pharmaceutical composition according to one aspect of the present invention will vary depending on the age, sex, weight, pathology and severity of the subject to be administered, the route of administration or the judgment of the prescriber. Dosage determination based on these factors is within the level of one skilled in the art and its daily dosage may be, for example, from 0.1 mg / kg / day to 100 mg / kg / day, more specifically from 5 mg / kg / day to 50 mg / kg. May be, but is not limited to.
본 발명의 일측면에 따른 식품 조성물의 제형은 특별히 한정되지 않으나, 예를 들어, 정제, 과립제, 드링크제, 캐러멜, 다이어트바 등으로 제형화될 수 있다. 각 제형의 식품 조성물은 유효 성분 이외에 해당 분야에서 통상적으로 사용되는 성분들을 제형 또는 사용 목적에 따라 당업자가 어려움 없이 적의 선정하여 배합할 수 있으며, 다른 원료와 동시에 적용할 경우 상승 효과가 일어날 수 있다.The formulation of the food composition according to one aspect of the present invention is not particularly limited, but may be, for example, formulated into tablets, granules, drinks, caramels, diet bars and the like. In addition to the active ingredient, the food composition of each formulation may be suitably selected by a person skilled in the art according to the formulation or purpose of use in addition to the active ingredient, and may be synergistic when applied simultaneously with other raw materials.
상기 유효 성분의 투여량 결정은 당업자의 수준 내에 있으며, 이의 1일 투여 용량은 투여하고자 하는 대상의 연령, 건강 상태, 합병증 등의 다양한 요인에 따라 달라질 수 있다.The determination of the dosage of the active ingredient is within the level of those skilled in the art, and its daily dosage may vary depending on various factors such as the age, health condition, complications, etc. of the subject to be administered.
이하, 실시예, 비교예 및 실험예를 들어 본 발명의 구성 및 효과를 보다 구체적으로 설명한다. 그러나 이들 실시예, 비교예 및 실험예는 본 발명에 대한 이해를 돕기 위해 예시의 목적으로만 제공된 것일 뿐 본 발명의 범주 및 범위가 그에 의해 제한되는 것은 아니다.Hereinafter, the configuration and effects of the present invention will be described in more detail with reference to Examples, Comparative Examples and Experimental Examples. However, these Examples, Comparative Examples and Experimental Examples are provided only for the purpose of illustration in order to help the understanding of the present invention, but the scope and scope of the present invention is not limited thereto.
[실시예 1 및 비교예 1 내지 5] 화장료 조성물의 제조Example 1 and Comparative Examples 1 to 5 Preparation of Cosmetic Composition
아래 표 1의 구성으로 실시예 1 및 비교예 1 내지 5의 화장료 조성물(에멀젼)을 통상적인 방법으로 제조하였다(단위: 중량%). 실시예 1은 판테놀(panthenol)을 포함하며, 비교예 1 내지 4는 당류를 포함한다.The cosmetic composition (emulsion) of Example 1 and Comparative Examples 1 to 5 was prepared according to the configuration of Table 1 below (unit: wt%). Example 1 includes panthenol, and Comparative Examples 1-4 comprise sugars.
제조 방법을 보다 구체적으로 설명하자면, 먼저 수상 성분에 유상 성분을 투입하면서 7000rpm으로 3분간 충분히 섞어주었다. 그 후 상피 세포 성장 인자 용액을 투입하여 1-2분간 호모믹싱으로 충분히 섞어주었다.To explain the production method in more detail, the mixture was sufficiently mixed at 7000 rpm for 3 minutes while first adding an oil phase component to the aqueous phase component. Then, the epidermal growth factor solution was added and mixed well by homomixing for 1-2 minutes.
표 1
성분 실시예 1 비교예 1 비교예 2 비교예 3 비교예 4 비교예 5
스쿠알란 5 5 5 5 5 5
상피세포성장인자 100ppm 용액 1 1 1 1 1 1
DL-판테놀 10 - - - - -
트레할로오스 - 10 - - - -
슈크로스 - - 10 - - -
자일리톨 - - - 10 - -
만니톨 - - - - 10 -
카보머 2 2 2 2 2 2
수산화나트륨 0.2 0.2 0.2 0.2 0.2 0.2
증류수 81.8 81.8 81.8 81.8 81.8 81.8
Table 1
ingredient Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5
Squalane 5 5 5 5 5 5
100 ppm solution of epidermal growth factor One One One One One One
DL-panthenol 10 - - - - -
Trehalos - 10 - - - -
Sucrose - - 10 - - -
Xylitol - - - 10 - -
Mannitol - - - - 10 -
Carbomer 2 2 2 2 2 2
Sodium hydroxide 0.2 0.2 0.2 0.2 0.2 0.2
Distilled water 81.8 81.8 81.8 81.8 81.8 81.8
[실험예 1] 판테놀의 단백질 안정화도 평가Experimental Example 1 Evaluation of Protein Stabilization of Panthenol
상기의 실시예 1 및 비교예 1 내지 5 조성물에 포함된 상피 세포 성장 인자의 안정도를 알아보기 위하여 각 조성물을 4℃, 25℃ 및 50℃에서 보관한 후 그 함량을 ELISA(Enzyme-Linked ImmunoSorbent Assay) 측정법으로 확인하였다. 4℃ 및 25℃에서 2주간 보관하였을 때의 함량 값을 측정한 다음, 25℃ 보관 2주 후 함량값에서 4℃ 보관 2주 후 함량 값을 나누어서 상대적 열 안정도(Relative thermal stability)(%)를 구한 후 아래 표에 나타내었다.In order to determine the stability of the epidermal growth factor contained in the composition of Example 1 and Comparative Examples 1 to 5, each composition was stored at 4 ° C, 25 ° C, and 50 ° C, and the content thereof was determined by ELISA (Enzyme-Linked ImmunoSorbent Assay). ) Was confirmed by a measurement method. Measure the content value when stored at 4 ℃ and 25 ℃ for 2 weeks, then divide the content value after 2 weeks of storage at 4 ℃ from 2 weeks after storage at 25 ℃ to obtain relative thermal stability (%). After obtaining, it is shown in the table below.
표 2
시료 상대적 열 안정도(%)
실시예 1 94.0
비교예 1 45.4
비교예 2 30.7
비교예 3 16.5
비교예 4 32.8
비교예 5 10.4
TABLE 2
sample Relative Thermal Stability (%)
Example 1 94.0
Comparative Example 1 45.4
Comparative Example 2 30.7
Comparative Example 3 16.5
Comparative Example 4 32.8
Comparative Example 5 10.4
상기 결과에서 보듯이, 비교예들의 조성물보다 실시예 조성물에서 상피 세포 성장 인자의 안정도가 현저히 우수하다. 즉, 판테놀은 단백질 함량의 감소를 저지시키므로 단백질 조성물의 안정성을 높이는 효과가 있음을 확인할 수 있다.As can be seen from the above results, the stability of epidermal cell growth factor in the example composition is significantly better than that of the comparative examples. That is, it can be seen that panthenol inhibits the reduction of the protein content, thereby increasing the stability of the protein composition.
[실시예 2 및 비교예 6 내지 8] 화장료 조성물의 제조Example 2 and Comparative Examples 6 to 8 Preparation of Cosmetic Composition
아래 표 3의 구성으로 실시예 2 및 비교예 6 내지 8의 화장료 조성물(에멀젼)을 실시예 1 및 비교예 1 내지 5과 실질적으로 동일한 방법으로 제조하였다(단위: 중량%). 실시예 1은 폴리알코올 에스터계 화합물인 폴리글리세릴-3 메틸글루코스 디스테아레이트를 포함함에 반해, 비교예 6 내지 8은 이를 포함하지 않는다.The cosmetic composition (emulsion) of Example 2 and Comparative Examples 6 to 8 was prepared in the same manner as in Example 1 and Comparative Examples 1 to 5 with the configuration of Table 3 below (unit: wt%). Example 1 includes polyglyceryl-3 methylglucose distearate, which is a polyalcohol ester compound, while Comparative Examples 6 to 8 do not include it.
표 3
성분 실시예 2 비교예 6 비교예 7 비교예 8
스쿠알란 5 5 5 5
상피세포성장인자 100ppm 용액 1 1 1 1
폴리글리세릴-3 메틸글루코스 디스테아레이트 2 - - -
하이드로제네이티드 레시틴/C12-16 알코올/팔미트산(0.65:0.175:0.175) - 2 - -
C14-22 알코올/C12-20 알킬 글루코사이드(0.2:0.8) - - 2 -
수크로오스 지방산 에스터 - - - 2
카보머 2 2 2 2
수산화나트륨 0.2 0.2 0.2 0.2
증류수 89.8 89.8 89.8 89.8
TABLE 3
ingredient Example 2 Comparative Example 6 Comparative Example 7 Comparative Example 8
Squalane 5 5 5 5
100 ppm solution of epidermal growth factor One One One One
Polyglyceryl-3 Methylglucose Distearate 2 - - -
Hydrogenated Lecithin / C 12-16 Alcohol / Palmite Acid (0.65: 0.175: 0.175) - 2 - -
C 14-22 Alcohol / C 12-20 Alkyl Glucoside (0.2: 0.8) - - 2 -
Sucrose fatty acid ester - - - 2
Carbomer 2 2 2 2
Sodium hydroxide 0.2 0.2 0.2 0.2
Distilled water 89.8 89.8 89.8 89.8
[실험예 2] 폴리알코올 에스터계 화합물의 단백질 안정화도 평가Experimental Example 2 Evaluation of Protein Stabilization of Polyalcohol Ester Compound
상기의 실시예 2 및 비교예 6 내지 8 조성물에 포함된 상피 세포 성장 인자의 안정도를 알아보기 위하여 각 조성물의 상피 세포 성장 인자 함량을 측정하고(초기값), 4℃와 25℃에서 1년 동안 보관한 후 상피 세포 성장 인자의 함량을 ELISA 측정법으로 확인하였다. 그 결과를 아래 표에 나타내었다.In order to determine the stability of the epidermal growth factor contained in the composition of Examples 2 and Comparative Examples 8 to 8 above, the epidermal growth factor content of each composition was measured (initial value), and at 4 ° C. and 25 ° C. for 1 year. After storage, the content of epidermal growth factor was confirmed by ELISA. The results are shown in the table below.
표 4
  성장 인자 함량(ppm)
  초기값 냉장 보관 1년 후 25℃ 보관 1년 후
실시예 2 0.1175 0.0184 0.0059
비교예 6 0.1138 -0.0019 -0.0191
비교예 7 0.0971 0.0091 0.0012
비교예 8 0.1192 0.0091 -0.0019
Table 4
Growth factor content (ppm)
Initial value 1 year after cold storage 1 year after storage at 25 ℃
Example 2 0.1175 0.0184 0.0059
Comparative Example 6 0.1138 -0.0019 -0.0191
Comparative Example 7 0.0971 0.0091 0.0012
Comparative Example 8 0.1192 0.0091 -0.0019
상기 결과에서 보듯이, 기존에 단백질을 제형화하는 성분으로 사용되던 하이드로제네이티드 계열 물질(하이드로제네이티드 레시틴/C12-16 알코올/팔미트산) 또는 당류계 지방산 에스터로서 안정화에 도움이 될 것으로 예상되는 계면 활성제(C14-22 알코올/C12-20 알킬 글루코사이드 또는 수크로오스 지방산 에스터)를 포함하는 비교예들의 조성물보다 실시예 조성물의 1년 후 상피 세포 성장 인자 함량이 높다. 이는 폴리알코올 에스터계 화합물이 단백질의 안정도를 높일 수 있음을 의미하며, 특히 실온에서 보관하는 경우보다 냉장 보관하는 경우 그 효과가 더욱 우수함을 의미한다. 이를 통해, 폴리알코올 에스터계 화합물은 오랜 보관 기간 동안 단백질 함량의 감소를 저지시키므로 단백질을 안정화시키는 효과가 있음을 확인할 수 있다. As can be seen from the above results, it may be helpful to stabilize the hydrogenated series materials (hydrogenated lecithin / C 12-16 alcohol / palmitic acid) or sugar-based fatty acid esters that have been used as ingredients for formulating proteins. The epithelial cell growth factor content is higher after one year of the example composition than the composition of the comparative examples comprising the expected surfactant (C 14-22 alcohol / C 12-20 alkyl glucoside or sucrose fatty acid ester). This means that the polyalcohol ester compound can increase the stability of the protein, and particularly, the effect is better when refrigerated than when stored at room temperature. Through this, it can be seen that the polyalcohol ester compound has an effect of stabilizing the protein because it inhibits the reduction of the protein content for a long storage period.
[실시예 3과 4 및 비교예 9 내지 14] 화장료 조성물의 제조[Examples 3 and 4 and Comparative Examples 9 to 14] Preparation of Cosmetic Composition
아래 표 5의 구성으로 실시예 3과 4 및 비교예 9 내지 14의 화장료 조성물(에멀젼)을 실시예 1 및 비교예 1 내지 5과 실질적으로 동일한 방법으로 제조하였다(단위: 중량%). 실시예 3은 카제인 가수분해물을, 실시예 4는 카제인 나트륨을 각각 포함함에 반해, 비교예 9 내지 14는 이를 포함하지 않는다.The cosmetic composition (emulsion) of Examples 3 and 4 and Comparative Examples 9 to 14 with the configuration of Table 5 below was prepared in substantially the same manner as Example 1 and Comparative Examples 1 to 5 (unit: wt%). Example 3 contains casein hydrolysates, while Example 4 contains casein sodium, whereas Comparative Examples 9-14 do not.
표 5
성분 실시예 3 실시예 4 비교예 9 비교예 10 비교예 11 비교예 12 비교예 13 비교예 14
스쿠알란 5 5 5 5 5 5 5 5
상피세포성장인자 100ppm 용액 1 1 1 1 1 1 1 1
카제인 가수분해물 1% 1 - - - - - - -
카제인 나트륨 1% - 1 - - - - - -
락토페린 용액 1% - - - 1 - - - -
젤라틴 1% - - - - 1 - - -
당단백질 1% - - - - - 1 - -
유청 1% - - - - - - 1 -
L-테아닌 1% - - - - - - - 1
카보머 2 2 2 2 2 2 2 2
수산화나트륨 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2
증류수 90.8 90.8 91.8 90.8 90.8 90.8 90.8 90.8
Table 5
ingredient Example 3 Example 4 Comparative Example 9 Comparative Example 10 Comparative Example 11 Comparative Example 12 Comparative Example 13 Comparative Example 14
Squalane 5 5 5 5 5 5 5 5
100 ppm solution of epidermal growth factor One One One One One One One One
Casein Hydrolyzate 1% One - - - - - - -
Casein sodium 1% - One - - - - - -
Lactoferrin solution 1% - - - One - - - -
Gelatin 1% - - - - One - - -
Glycoprotein 1% - - - - - One - -
Whey 1% - - - - - - One -
L-Theanine 1% - - - - - - - One
Carbomer 2 2 2 2 2 2 2 2
Sodium hydroxide 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2
Distilled water 90.8 90.8 91.8 90.8 90.8 90.8 90.8 90.8
[실험예 3] 카제인 및 그 유도체의 단백질 안정도 평가Experimental Example 3 Evaluation of Protein Stability of Casein and Its Derivatives
상기의 실시예 3과 4 및 비교예 9 내지 14 조성물에 포함된 상피 세포 성장 인자의 안정도를 알아보기 위하여 각 조성물의 상피 세포 성장 인자 초기 함량을 ELISA 측정법으로 확인하였다. 이후 4℃, 25℃ 및 45℃에서 1년 보관한 다음 상피 세포 성장 인자 함량을 동일한 방법으로 측정하고, 각 보관 온도 별로 초기 함량과 비교한 상대적인 열 안정도(Relative thermal stability)(%)를 구한 후 아래 표에 나타내었다.In order to determine the stability of the epidermal growth factor contained in the composition of Examples 3 and 4 and Comparative Examples 9 to 14, the initial content of epithelial cell growth factor of each composition was confirmed by ELISA. After storage for 1 year at 4 ℃, 25 ℃ and 45 ℃ and then measured the epidermal growth factor content in the same way, and after calculating the relative thermal stability (%) compared with the initial content for each storage temperature It is shown in the table below.
표 6
시료 4℃ 상대적 열 안정도(%) 25℃ 상대적 열 안정도(%) 45℃ 상대적 열 안정도(%)
실시예 3 81.9 57.0 18.2
실시예 4 90.3 65.2 11.8
비교예 9 45.4 38.8 11.5
비교예 10 46.6 38.2 8.6
비교예 11 45.2 35.1 18.5
비교예 12 44.0 9.5 -0.3
비교예 13 54.3 29.1 10.3
비교예 14 44.1 36.0 10.9
Table 6
sample 4 ℃ Relative Thermal Stability (%) 25 ℃ relative thermal stability (%) 45 ℃ Relative Thermal Stability (%)
Example 3 81.9 57.0 18.2
Example 4 90.3 65.2 11.8
Comparative Example 9 45.4 38.8 11.5
Comparative Example 10 46.6 38.2 8.6
Comparative Example 11 45.2 35.1 18.5
Comparative Example 12 44.0 9.5 -0.3
Comparative Example 13 54.3 29.1 10.3
Comparative Example 14 44.1 36.0 10.9
상기 결과에서 보듯이, 기존의 단백질 안정화 물질로 알려진 락토페린, 젤라틴, 당단백질(글리코 프로테인), 유청 또는 L-테아닌을 포함하는 비교예들의 조성물보다 실시예 조성물의 1년 후 상피 세포 성장 인자 함량이 높다. 이는 카제인 및 그 유도체가 상피 세포 성장 인자의 안정도를 높일 수 있음을 의미하며, 특히 실온 이하의 온도에서 보관하는 경우 그 효과가 더욱 우수함을 의미한다. 이를 통해, 카제인 및 그 유도체는 오랜 보관 기간 동안 상피 세포 성장 인자 함량의 감소를 저지시키므로 상피 세포 성장 인자 조성물의 안정성을 높이는 효과가 있음을 확인할 수 있다.As can be seen from the above results, the epithelial cell growth factor content of the composition of the Example composition is higher than that of the comparative examples comprising lactoferrin, gelatin, glycoprotein (glycoprotein), whey or L-theanine, which are known as conventional protein stabilizing substances. high. This means that casein and its derivatives can increase the stability of epidermal growth factor, and particularly, the effect is better when stored at a temperature below room temperature. Through this, it can be confirmed that casein and its derivatives have an effect of increasing the stability of the epidermal growth factor composition because it inhibits the decrease of the epidermal growth factor content for a long storage period.
이하 본 발명의 일측면에 따른 조성물의 제형예를 보다 상세하게 설명하나, 상기 조성물은 여러 가지 제형으로 응용 가능하고, 이는 본 발명을 한정하고자 함이 아닌 단지 구체적으로 설명하고자 함이다.Hereinafter, the formulation of the composition according to an aspect of the present invention will be described in more detail, but the composition is applicable to various formulations, which is intended to explain in detail only, not intended to limit the present invention.
[제형예 1] 유연 화장수Formulation Example 1 Flexible Lotion
아래 표에 기재된 조성에 따라 통상적인 방법으로 유연 화장수를 제조한다.According to the composition described in the table below to prepare a flexible lotion in a conventional manner.
표 7
성분 함량 (중량 %)
판테놀 2.0
상피 세포 성장 인자 100 ppm 용액 5.0
글리세린 3.0
부틸렌글리콜 2.0
프로필렌글리콜 2.0
카르복시비닐폴리머 0.1
피이지-12 노닐페닐에테르 0.2
폴리솔베이트 80 0.4
에탄올 10.0
트리에탄올아민 0.1
방부제, 색소, 향료 적량
정제수 잔량
TABLE 7
ingredient Content (% by weight)
Panthenol 2.0
100 ppm solution of epidermal growth factor 5.0
glycerin 3.0
Butylene glycol 2.0
Propylene glycol 2.0
Carboxy Vinyl Polymer 0.1
Fiji-12 nonylphenyl ether 0.2
Polysorbate 80 0.4
ethanol 10.0
Triethanolamine 0.1
Preservative, coloring, flavoring Quantity
Purified water Remaining amount
[제형예 2] 영양 화장수(밀크 로션)Formulation Example 2 Nutritional Lotion (Milk Lotion)
아래 표에 기재된 조성에 따라 통상적인 방법으로 영양 화장수를 제조한다.To prepare a nourishing lotion according to the composition described in the table below.
표 8
성분 함량 (중량 %)
폴리글리세릴-3 메틸글루코스 디스테아레이트 5.0
상피 세포 성장 인자 100 ppm 용액 5.0
글리세린 3.0
부틸렌글리콜 3.0
프로필렌글리콜 3.0
카르복시비닐폴리머 0.1
밀납 4.0
폴리솔베이트 60 1.5
카프릴릭/카프릭 트리글리세라이드 5.0
스쿠알란 5.0
솔비타세스퀴올레이트 1.5
유동파라핀 0.5
세테아릴 알코올 1.0
트리에탄올아민 0.2
방부제, 색소, 향료 적량
정제수 잔량
Table 8
ingredient Content (% by weight)
Polyglyceryl-3 Methylglucose Distearate 5.0
100 ppm solution of epidermal growth factor 5.0
glycerin 3.0
Butylene glycol 3.0
Propylene glycol 3.0
Carboxy Vinyl Polymer 0.1
Beeswax 4.0
Polysorbate 60 1.5
Caprylic / Capric Triglycerides 5.0
Squalane 5.0
Sorbitassquioleate 1.5
Liquid paraffin 0.5
Cetearyl Alcohol 1.0
Triethanolamine 0.2
Preservative, coloring, flavoring Quantity
Purified water Remaining amount
[제형예 3] 영양 크림Formulation Example 3 Nutrition Cream
아래 표에 기재된 조성에 따라 통상적인 방법으로 영양 크림을 제조한다.Nutritional creams are prepared by conventional methods according to the compositions set forth in the table below.
표 9
성분 함량(중량%)
카제인 가수 분해물 7.0
상피 세포 성장 인자 용액 7.0
글리세린 3.0
부틸렌글리콜 3.0
유동파라핀 7.0
베타글루칸 7.0
카보머 0.1
카프릴릭/카프릭 트리글리세라이드 3.0
스쿠알란 5.0
세테아릴 글루코사이드 1.5
소르비탄 스테아레이트 0.4
폴리솔베이트 60 1.2
트리에탄올아민 0.1
방부제, 색소, 향료 적량
정제수 잔량
Table 9
ingredient Content (% by weight)
Casein hydrolyzate 7.0
Epithelial Growth Factor Solution 7.0
glycerin 3.0
Butylene glycol 3.0
Liquid paraffin 7.0
Beta Glucan 7.0
Carbomer 0.1
Caprylic / Capric Triglycerides 3.0
Squalane 5.0
Cetearyl Glucoside 1.5
Sorbitan stearate 0.4
Polysorbate 60 1.2
Triethanolamine 0.1
Preservative, coloring, flavoring Quantity
Purified water Remaining amount
[제형예 4] 마사지 크림Formulation Example 4 Massage Cream
아래 표에 기재된 조성에 따라 통상적인 방법으로 마사지 크림을 제조한다.Massage cream is prepared in a conventional manner according to the composition described in the table below.
표 10
성분 함량(중량%)
판테놀 8.0
상피 세포 성장 인자 100 ppm 용액 5.0
글리세린 8.0
부틸렌글리콜 4.0
유동파라핀 45.0
베타글루칸 7.0
카보머 0.1
카프릴릭/카프릭 트리글리세라이드 3.0
밀납 4.0
세테아릴 글루코사이드 1.5
세스퀴 올레인산 소르비탄 0.9
바세린 3.0
파라핀 1.5
방부제, 색소, 향료 적량
정제수 잔량
Table 10
ingredient Content (% by weight)
Panthenol 8.0
100 ppm solution of epidermal growth factor 5.0
glycerin 8.0
Butylene glycol 4.0
Liquid paraffin 45.0
Beta Glucan 7.0
Carbomer 0.1
Caprylic / Capric Triglycerides 3.0
Beeswax 4.0
Cetearyl Glucoside 1.5
Sesqui oleic acid sorbitan 0.9
Vaseline 3.0
paraffin 1.5
Preservative, coloring, flavoring Quantity
Purified water Remaining amount
[제형예 5] 팩[Formulation Example 5] Pack
아래 표에 기재된 조성에 따라 통상적인 방법으로 팩을 제조한다.Packs are prepared by conventional methods according to the compositions described in the table below.
표 11
성분 함량(중량%)
폴리글리세릴-3 메틸글루코스 디스테아레이트 8.0
상피 세포 성장 인자 100 ppm 용액 8.0
글리세린 4.0
폴리비닐알콜 15.0
히알루론산 추출물 5.0
베타글루칸 7.0
알란토인 0.1
노닐 페닐에테르 0.4
폴리솔베이트 60 1.2
에탄올 6.0
방부제, 색소, 향료 적량
정제수 잔량
Table 11
ingredient Content (% by weight)
Polyglyceryl-3 Methylglucose Distearate 8.0
100 ppm solution of epidermal growth factor 8.0
glycerin 4.0
Polyvinyl alcohol 15.0
Hyaluronic acid extract 5.0
Beta Glucan 7.0
Allantoin 0.1
Nonyl Phenyl Ether 0.4
Polysorbate 60 1.2
ethanol 6.0
Preservative, coloring, flavoring Quantity
Purified water Remaining amount
[제형예 6] 주사제Formulation Example 6 Injection
아래 표에 기재된 조성에 따라 통상적인 방법으로 주사제를 제조한다.Injections are prepared by conventional methods according to the compositions listed in the table below.
표 12
성분 함량(중량%)
카제인 나트륨 0.5
상피 세포 성장 인자 100 ppm 용액 0.5
NaCl 0.4
정제수 잔량
Table 12
ingredient Content (% by weight)
Casein sodium 0.5
100 ppm solution of epidermal growth factor 0.5
NaCl 0.4
Purified water Remaining amount
표 13
성분 함량(중량%)
판테놀 5
NaCl 0.4
알부민 1.0
보툴리늄 톡신 100 유닛
정제수 잔량
Table 13
ingredient Content (% by weight)
Panthenol 5
NaCl 0.4
albumin 1.0
Botulinum Toxin 100 units
Purified water Remaining amount
[제형예 7] 연고Formulation Example 7 Ointment
아래 표 에 기재된 조성에 따라 통상적인 방법으로 연고를 제조한다.Ointments are prepared by conventional methods according to the compositions described in the table below.
표 14
성분 함량(중량%)
폴리글리세릴-3 메틸글루코스 디스테아레이트 0.1
글리세린 8.0
부틸렌글리콜 4.0
유동 파라핀 15.0
베타글루칸 7.0
카보머 0.1
카프릴릭/카프릭 트리글리세라이드 3.0
스쿠알란 1.0
세테아릴 글루코사이드 1.5
소르비탄 스테아레이트 0.4
세테아릴 알코올 1.0
밀납 4.0
방부제, 색소, 향료 적량
정제수 잔량
Table 14
ingredient Content (% by weight)
Polyglyceryl-3 Methylglucose Distearate 0.1
glycerin 8.0
Butylene glycol 4.0
Floating paraffin 15.0
Beta Glucan 7.0
Carbomer 0.1
Caprylic / Capric Triglycerides 3.0
Squalane 1.0
Cetearyl Glucoside 1.5
Sorbitan stearate 0.4
Cetearyl Alcohol 1.0
Beeswax 4.0
Preservative, coloring, flavoring Quantity
Purified water Remaining amount

Claims (15)

  1. 판테놀(panthenol), 폴리알코올 에스터계 화합물, 카제인(casein) 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 펩타이드 또는 단백질 안정화제.Peptide or protein stabilizer comprising at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof.
  2. 제 1 항에 있어서,The method of claim 1,
    펩타이드 또는 단백질은 성장 인자, 호르몬, 인터페론, 백신, 재조합 단백질, 재조합 펩타이드 및 효소로 이루어진 그룹에서 선택된 하나 이상을 포함하는 안정화제.The peptide or protein is a stabilizer comprising one or more selected from the group consisting of growth factors, hormones, interferons, vaccines, recombinant proteins, recombinant peptides and enzymes.
  3. 제 1 항에 있어서,The method of claim 1,
    폴리알코올 에스터계 화합물 또는 그 유도체는 폴리글리세릴 디스테아레이트, PEG 디스테아레이트, 폴리글리세릴 메틸글루코스 디스테아레이트 및 PEG 메틸글루코스 디스테아레이트로 이루어진 그룹에서 선택된 하나 이상을 포함하는 안정화제.The polyalcohol ester compound or derivative thereof comprises at least one selected from the group consisting of polyglyceryl distearate, PEG distearate, polyglyceryl methylglucose distearate and PEG methylglucose distearate.
  4. 제 1 항에 있어서,The method of claim 1,
    카제인 또는 그 유도체는 카제인 가수 분해물 및 카제인 염으로 이루어진 그룹에서 선택된 하나 이상을 포함하는 안정화제.Casein or a derivative thereof is a stabilizer comprising at least one selected from the group consisting of casein hydrolyzate and casein salt.
  5. 제 1 항 내지 제 4 항 중 어느 한 항에 따른 안정화제를 포함하는 화장료 조성물.Cosmetic composition comprising a stabilizer according to any one of claims 1 to 4.
  6. 제 1 항 내지 제 4 항 중 어느 한 항에 따른 안정화제를 포함하는 약학 조성물.A pharmaceutical composition comprising a stabilizer according to any one of claims 1 to 4.
  7. 펩타이드 및 단백질 중 하나 이상; 및 One or more of peptides and proteins; And
    판테놀(panthenol), 폴리알코올 에스터계 화합물, 카제인(casein) 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 포함하는 조성물.A composition comprising at least one selected from the group consisting of panthenol, polyalcohol ester compounds, casein, and derivatives thereof.
  8. 제 7 항에 있어서,The method of claim 7, wherein
    펩타이드 및 단백질 중 하나 이상은 성장 인자, 호르몬, 인터페론, 백신, 재조합 단백질, 재조합 펩타이드 및 효소로 이루어진 그룹에서 선택된 하나 이상을 포함하고, At least one of the peptides and proteins comprises at least one selected from the group consisting of growth factors, hormones, interferons, vaccines, recombinant proteins, recombinant peptides and enzymes,
    폴리알코올 에스터계 화합물 또는 그 유도체는 폴리글리세릴 디스테아레이트, PEG 디스테아레이트, 폴리글리세릴 메틸글루코스 디스테아레이트 및 PEG 메틸글루코스 디스테아레이트로 이루어진 그룹에서 선택된 하나 이상을 포함하며,The polyalcohol ester compound or derivative thereof includes at least one selected from the group consisting of polyglyceryl distearate, PEG distearate, polyglyceryl methylglucose distearate and PEG methylglucose distearate,
    카제인 또는 그 유도체는 카제인 가수 분해물 및 카제인 염으로 이루어진 그룹에서 선택된 하나 이상을 포함하는 조성물.Casein or a derivative thereof comprises at least one selected from the group consisting of casein hydrolyzate and casein salt.
  9. 제 7 항에 있어서,The method of claim 7, wherein
    조성물은 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 조성물 전체 중량 대비 0.1 내지 50 중량%로 포함하는 조성물.The composition comprises 0.1 to 50% by weight of at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof, based on the total weight of the composition.
  10. 제 7 항에 있어서,The method of claim 7, wherein
    조성물은 5,000 cP 내지 30,000 cP의 점도를 가지는 조성물.The composition has a viscosity of 5,000 cP to 30,000 cP.
  11. 제 7 항 내지 제 10 항 중 어느 한 항에 있어서,The method according to any one of claims 7 to 10,
    화장료 조성물인 조성물.A composition which is a cosmetic composition.
  12. 제 7 항 내지 제 10 항 중 어느 한 항에 있어서,The method according to any one of claims 7 to 10,
    약학 조성물인 조성물.A composition that is a pharmaceutical composition.
  13. 펩타이드 및 단백질 중 하나 이상; 및 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 혼합하여 조성물을 제조하는 단계를 포함하는 펩타이드 또는 단백질 안정화 방법.One or more of peptides and proteins; And mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein, and derivatives thereof to prepare a composition.
  14. 제 13 항에 있어서,The method of claim 13,
    펩타이드 및 단백질 중 하나 이상은 성장 인자, 호르몬, 인터페론, 백신, 재조합 단백질, 재조합 펩타이드 및 효소로 이루어진 그룹에서 선택된 하나 이상을 포함하고,At least one of the peptides and proteins comprises at least one selected from the group consisting of growth factors, hormones, interferons, vaccines, recombinant proteins, recombinant peptides and enzymes,
    폴리알코올 에스터계 화합물 또는 그 유도체는 폴리글리세릴 디스테아레이트, PEG 디스테아레이트, 폴리글리세릴 메틸글루코스 디스테아레이트 및 PEG 메틸글루코스 디스테아레이트로 이루어진 그룹에서 선택된 하나 이상을 포함하며,The polyalcohol ester compound or derivative thereof comprises at least one selected from the group consisting of polyglyceryl distearate, PEG distearate, polyglyceryl methylglucose distearate and PEG methylglucose distearate,
    카제인 또는 그 유도체는 카제인 가수 분해물 및 카제인 염으로 이루어진 그룹에서 선택된 하나 이상을 포함하는 방법.Casein or a derivative thereof comprises at least one selected from the group consisting of casein hydrolysate and casein salt.
  15. 제 13 항에 있어서,The method of claim 13,
    조성물을 제조하는 단계는 판테놀, 폴리알코올 에스터계 화합물, 카제인 및 그들의 유도체로 이루어진 그룹에서 선택된 하나 이상을 조성물 전체 중량 대비 0.1 내지 50 중량%로 혼합하여 조성물을 제조하는 방법.The step of preparing the composition is a method for preparing the composition by mixing at least one selected from the group consisting of panthenol, polyalcohol ester compound, casein and derivatives thereof in 0.1 to 50% by weight relative to the total weight of the composition.
PCT/KR2011/009190 2010-11-30 2011-11-30 Agent for stabilizing peptides or proteins WO2012074285A2 (en)

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