KR102524312B1 - Water-soluble emulsion composition comprising ecdysteroid - Google Patents
Water-soluble emulsion composition comprising ecdysteroid Download PDFInfo
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Abstract
본 발명은 수용성 항산화제 유화물을 함유하는 엑디스테로이드 함유 수용성 유화 조성물에 관한 것이다.
본 발명의 일 구현예에 따른 엑디스테로이드 함유 수용성 유화 조성물은 기능성 수난용 물질을 수용화 시킴으로써 물질의 흡수율과 효능을 증대시킬 수 있어, 물질이 갖는 기능성을 다양한 분야에 활용될 수 있도록 한다.
또한, 수용성 항산화제 유화물을 함유하여, 수용액 상에서 산소에 의한 산화를 예방할 수 있는 산화 안정성이 우수하다. The present invention relates to an ecdysteroid-containing water-soluble emulsion composition containing a water-soluble antioxidant emulsion.
The water-soluble emulsified composition containing ecdysteroids according to one embodiment of the present invention can increase the absorption rate and efficacy of the material by soluble in the water, so that the functionality of the material can be used in various fields.
In addition, it contains a water-soluble antioxidant emulsion and has excellent oxidation stability capable of preventing oxidation by oxygen in an aqueous solution.
Description
본 발명은 수용성 항산화제 유화물을 함유하는 엑디스테로이드 함유 수용성 유화 조성물에 관한 것이다. The present invention relates to an ecdysteroid-containing water-soluble emulsion composition containing a water-soluble antioxidant emulsion.
엑디스테로이드(Ecdysteroid)는 곤충의 탈피를 조절하는 스테이로이드성 호르몬이며 기원에 따라 절지동물과 갑각류에서 생산되는 zooecdysteroid와 식물에서 생산되는 파이토엑디스테로이드(phytoecdysteroid)로 구분되는데, 파이토엑디스테로이드(phytoecdysteroid)는 트리테르페노이드(triterpenoid), 트리테르페노이드 사포닌(triterpene saponin)을 포함하는 화합물의 일종으로 파이토스테롤(phytosterol)과 파이토엑디스테로이드(phytoecdysteroid)로 구분되며, acetyl-CoA를 선구물질로 하여 식물 세포 내 메발론산 경로에서 메발론산(mevalonic acid)에 의하여 합성된다. 이들 중 처음으로 알려진 것은 α-엑디손(ecdysone)으로 누에의 유충으로부터 단리하였다. 그 후 누에번데기에서 α-엑디손 보다 활성이 큰 β-엑디손이 단리되었고 이후 엑디손과 유사한 구조와 활성을 가진 많은 스테로이드 화합물이 알려져 엑디스테로이드(ecdysteroid)로 불리고 있다. 이러한 엑디스테로이드는 스테로이드핵에 cholest-7-en-6-one이라는 구조적 특징을 가지며, 3, 14, 22번 탄소에 공통적으로 수산기를 가지고있다.Ecdysteroid is a steroid hormone that regulates the molt of insects and is divided into zooecdysteroids produced by arthropods and crustaceans and phytoecdysteroids produced by plants according to their origin. Phytoecdysteroids are It is a kind of compound that includes triterpenoid and triterpene saponin, and is divided into phytosterol and phytoecdysteroid. Acetyl-CoA is used as a precursor for plant cell It is synthesized by mevalonic acid in the endogenous mevalonic acid pathway. The first known of these was α-ecdysone, which was isolated from silkworm larvae. After that, β-ecdysone, which is more active than α-ecdysone, was isolated from silkworm pupae, and many steroid compounds having similar structures and activities to ecdysone are known and are called ecdysteroids. These ecdysteroids have the structural characteristic of cholest-7-en-6-one in the steroid nucleus, and have a common hydroxyl group at carbons 3, 14, and 22.
엑디스테로이드는 곤충뿐만 아니라 식물에서도 발견되는데, 그 함량은 곤충보다 많은 것으로 알려져 있다. 봉작고사리, 뱀고사리 등 양치식물과 주목, 죽백나무, 비자나무, 으름, 비름, 쇠무릎, 나한송, 금창초, 국화 등에 함유되어 있다. 식물에서 이들의 작용은 완전하게 알려지지는 않았으나, 식물의 엑디스테로이드는 일부 비순응 식식성 곤충(nonadapted phytophagous insect)에 대해서 섭식 저해, 기피 및 살충 등의 효과를 보여 식물 방어 기전에 영향을 미치는 것으로 알려져 있다.Ecdysteroids are found in plants as well as insects, and their content is known to be higher than that of insects. It is contained in ferns such as bongjak bracken and snake fern, yew, jukbaek tree, bija tree, eureum, amaranth, ox knee, Arhan pine, geumchangcho, and chrysanthemum. Although their action in plants is not completely known, ecdysteroids in plants are known to affect plant defense mechanisms by showing effects such as inhibition of feeding, avoidance, and insecticide against some nonadapted phytophagous insects. there is.
미국 특허 제5,609,873호에는 엑디스테로이드 유도체가 케라티노사이트 분화를 조절한다는 사실과 이를 화장품 재료 및 피부 체세포 배양 배지의 성분으로 사용할 수 있음이 보고되어 있다.U.S. Patent No. 5,609,873 reports that ecdysteroid derivatives regulate keratinocyte differentiation and that they can be used as cosmetic materials and components of skin somatic cell culture media.
한편 미국 특허 제5,922,702호에는 엑디손 화합물이 반추 동물의 반추위에 존재하는 원생동물에 작용하여 그 수, 생식, 활성을 효과적으로 줄여 생산성을 향상시킬 수 있다고 기재하고 있다.Meanwhile, US Patent No. 5,922,702 discloses that the ecdysone compound can effectively reduce the number, reproduction, and activity of protozoa present in the rumen of ruminants to improve productivity.
이와 같은 엑디스테로이드를 비롯한 기능성 천연물들은 대부분 수난용성이며 체내흡수성이 매우 낮아 생체 이용률이 떨어지는 문제점이 있다. 따라서 이들이 갖는 생리활성물질을 활용한 식품, 의약품, 사료 등의 적용에 제한점이 있다. 또한 기존의 수용화된 기능성 유화물들은 O/W형의 유화물로 수상인 물과 물에 함유되어 산소에 의해서 산화되어 항산화 효능을 소실하거나 산패되는 문제점을 가지고 있다. Functional natural products, including ecdysteroids, are mostly poorly water-soluble and have very low body absorption, resulting in poor bioavailability. Therefore, there is a limit to the application of food, medicine, feed, etc. using these physiologically active substances. In addition, existing water-soluble functional emulsions are O / W type emulsions, which are contained in aqueous phase water and water, and are oxidized by oxygen, resulting in loss of antioxidant effect or rancidity.
한편, α-Tocopherol은 대표적인 천연 항산화제로써 종자유(Seed oil)나 곡류 그리고 녹색 잎을 갖는 야채에 많이 분포되어 있으며, 비타민 E로써 세포막에 존재하는 주요한 지용성의 항산화제이며, 지방의 산화를 막아준다. 비타민 E는 퍼옥시 라디칼(ROO·), CCl3, HO· 포함하는 다양한 산소 라디칼뿐만 아니라 수퍼옥사이드 라디칼(O2·)과 직접 반응할 수 있다. 항산화력은 δ > γ > β> α 순으로 높다. 작용기작으로 세포막을 구성하는 다가불포화지방산은 세포에서 만들어진 자유라디칼에 의해 쉽게 산화되는데, 토코페롤은 이러한 산화과정을 중단시키고 자유라디칼을 제거해 세포막을 산화적 손상으로부터 보호해준다. On the other hand, α-Tocopherol is a representative natural antioxidant and is widely distributed in seed oil, grains, and green leafy vegetables. As vitamin E, it is a major fat-soluble antioxidant present in cell membranes and prevents fat oxidation. . Vitamin E can directly react with a variety of oxygen radicals, including peroxy radicals (ROO·), CCl 3 , HO·, as well as superoxide radicals (O 2 ·). The antioxidant power is high in the order of δ > γ > β > α. As a mechanism of action, polyunsaturated fatty acids constituting cell membranes are easily oxidized by free radicals produced in cells. Tocopherol stops this oxidation process and removes free radicals to protect cell membranes from oxidative damage.
본 발명의 과제는 기능성 난용성 물질을 수용화 시켜 물질의 흡수율과 효능을 증대시킬 수 있을 뿐만 아니라 수용액 상에서 산화 안정성이 우수한 엑디스테로이드 함유 수용성 유화 조성물을 제공하는 것이다. An object of the present invention is to provide an ecdysteroid-containing water-soluble emulsion composition capable of increasing the absorption rate and efficacy of a functional poorly soluble substance by water-solubilization and having excellent oxidative stability in an aqueous solution.
상기한 과제를 달성하기 위해 본 발명은 In order to achieve the above object, the present invention
(1) 전체 100 중량%를 만족하도록 하기 성분을 포함하는 수용성 항산화제 유화물: (1) A water-soluble antioxidant emulsion containing the following components to satisfy 100% by weight of the total:
토코페롤 1 내지 40 중량%,1 to 40% by weight of tocopherol;
카테킨 1 내지 40 중량%,1 to 40% by weight of catechin;
HLB 3 내지 HLB 7의 제1 계면활성제 1 내지 30 중량%,1 to 30% by weight of a first surfactant of HLB 3 to HLB 7;
HLB 10 내지 HLB 14의 제2 계면활성제 10 내지 80 중량%;10 to 80% by weight of a second surfactant of HLB 10 to HLB 14;
공계면활성제 10 내지 45 중량%, 및10 to 45% by weight of a cosurfactant, and
식용 유지 1 내지 35 중량%,1 to 35% by weight of edible fat and oil;
(2) 전체 100 중량%를 만족하도록 하기 성분을 포함하는 엑디스테로이드 유화물:(2) Ecdysteroid emulsion containing the following components to satisfy 100% by weight of the total:
엑디스테로이드 1 내지 30 중량%,1 to 30% by weight of an ecdysteroid;
HLB 3 내지 HLB 7의 제1 계면활성제 1 내지 10 중량%,1 to 10% by weight of a first surfactant of HLB 3 to HLB 7;
HLB 10 내지 HLB 14의 제2 계면활성제 1 내지 20 중량%, 및1 to 20% by weight of a second surfactant of HLB 10 to HLB 14, and
공계면활성제 40 내지 97 중량%, 40 to 97% by weight of a cosurfactant;
를 포함하는, 수용성 항산화제 유화물을 함유하는 엑디스테로이드 함유 수용성 유화 조성물을 제공한다. It provides an ecdysteroid-containing water-soluble emulsion composition containing a water-soluble antioxidant emulsion.
본 발명의 일 구현예에 따른 엑디스테로이드 함유 수용성 유화 조성물은 기능성 수난용 물질을 수용화 시킴으로써 물질의 흡수율과 효능을 증대시킬 수 있어, 물질이 갖는 기능성을 다양한 분야에 활용될 수 있도록 한다.The water-soluble emulsified composition containing ecdysteroids according to one embodiment of the present invention can increase the absorption rate and efficacy of the material by soluble in the water, so that the functionality of the material can be used in various fields.
또한, 수용성 항산화제 유화물을 함유하여, 수용액 상에서 산소에 의한 산화를 예방할 수 있는 산화 안정성이 우수하다. In addition, it contains a water-soluble antioxidant emulsion and has excellent oxidation stability capable of preventing oxidation by oxygen in an aqueous solution.
도 1은 비교예 33의 엑디스테로이드 함유 수용성 유화 조성물의 유화 입자를 광학현미경으로 관찰한 사진이다.
도 2는 실시예 1의 엑디스테로이드 함유 수용성 유화 조성물의 유화 입자를 광학현미경으로 관찰한 사진이다. 1 is a photograph of emulsified particles of an ecdysteroid-containing water-soluble emulsion composition of Comparative Example 33 observed under an optical microscope.
2 is a photograph of emulsified particles of the water-soluble emulsion composition containing ecdysteroids of Example 1 observed under an optical microscope.
이하 본 발명의 일 구현예에 따른 수용성 항산화 유화물과 엑디스테로이드 유화물을 상세히 설명한다. Hereinafter, the water-soluble antioxidant emulsion and the ecdysteroid emulsion according to an embodiment of the present invention will be described in detail.
본 발명의 일 구현예에 따른 엑디스테로이드 함유 수용성 유화 조성물은 수용성 항산화 유화물과 엑디스테로이드 유화물을 포함한다. An ecdysteroid-containing water-soluble emulsion composition according to one embodiment of the present invention includes a water-soluble antioxidant emulsion and an ecdysteroid emulsion.
상기 수용성 항산화제 유화물은 전체 100 중량%를 만족하도록, 토코페롤 1 내지 40 중량%, 카테킨 1 내지 40 중량%, HLB 3 내지 HLB 7의 제1 계면활성제 1 내지 30 중량%, HLB 10 내지 HLB 14의 제2 계면활성제 10 내지 80 중량%, 공계면활성제 10 내지 45 중량%, 및 식용 유지 1 내지 35 중량%를 포함한다. The water-soluble antioxidant emulsion contains 1 to 40% by weight of tocopherol, 1 to 40% by weight of catechin, 1 to 30% by weight of the first surfactant of HLB 3 to HLB 7, and 1 to 30% by weight of HLB 10 to HLB 14, so as to satisfy 100% by weight of the water-soluble antioxidant emulsion. 10 to 80% by weight of a second surfactant, 10 to 45% by weight of a cosurfactant, and 1 to 35% by weight of edible oil and fat.
상기 토코페롤과 카테킨은 각각 지용성, 수용성 항산화제로서 유화물 내에 포함된다. 이때 토코페롤과 카테킨의 함량이 상기 범위 미만이면 첨가에 따른 항산화 효과가 미미하고, 이와 반대로 상기 범위를 초과하면 유화물의 유화 안정성이 현저히 저하되는 문제점이 있다. The tocopherol and catechin are included in the emulsion as fat-soluble and water-soluble antioxidants, respectively. At this time, if the content of tocopherol and catechin is less than the above range, the antioxidant effect according to addition is insignificant, and on the contrary, if it exceeds the above range, there is a problem that the emulsion stability of the emulsion is significantly reduced.
상기 HLB(Hydrophile-Lipophile Balance)는 계면활성제가 물과 기름에 대한 친화성 정도를 나타내는 값이며, HLB는 그 값이 작을수록 분자 전체로서 친유성이 강하고, 그 값이 커질수록 친수성이 강한 것을 나타낸다. The Hydrophile-Lipophile Balance (HLB) is a value representing the degree of affinity of a surfactant for water and oil. The smaller the HLB value, the stronger the lipophilicity of the molecule as a whole, and the higher the HLB value, the stronger the hydrophilicity. .
상기 수용성 항산화 유화물과 엑디스테로이드 유화물은 각 유화물의 유화 안정성을 확보하고, 친수성 공계면활성제 내에 잘 녹으면서 계면활성 효과를 나타내기 위한 측면에서 HLB(Hydrophile-Lipophile Balance)가 상이한 2종의 계면활성제를 포함한다. The water-soluble antioxidant emulsion and the ecdysteroid emulsion are two types of surfactants with different HLB (Hydrophile-Lipophile Balance) in terms of securing the emulsion stability of each emulsion and showing the surfactant effect while being well dissolved in the hydrophilic cosurfactant include
상기 제1 계면활성제는 HLB가 3 내지 7인 것을 사용하고, 제2 계면활성제는 HLB가 10 내지 14인 것을 사용하는 것이 유화 입자 간 응집을 방지하고, 친수성 공계면활성제와 식용 유지 내에서 항산화제인 토코페롤과 카테킨이 각각의 항산화력을 유지하기 위한 측면에서 더욱 효과적이다. 상기 제1 계면활성제의 HLB가 3 미만인 경우 에멀젼이 잘 형성되지 않으며, HLB가 7을 초과하는 경우 입자 간 응집이 발생하여 유화 안정성이 저하된다. 상기 제2 계면활성제의 HLB가 10 미만인 경우 유화가 어렵고, 반대로 HLB 14를 초과하는 경우 유화 안정성이 떨어진다. The first surfactant is used with an HLB of 3 to 7, and the second surfactant is used with an HLB of 10 to 14 to prevent aggregation between emulsified particles, and is an antioxidant in hydrophilic cosurfactants and edible oils. Tocopherol and catechin are more effective in terms of maintaining their respective antioxidant power. When the HLB of the first surfactant is less than 3, an emulsion is not easily formed, and when the HLB is greater than 7, aggregation between particles occurs and emulsion stability is deteriorated. When the HLB of the second surfactant is less than 10, emulsification is difficult, and when the HLB exceeds 14, emulsion stability is deteriorated.
상기 HLB 3 내지 HLB 7의 제1 계면활성제는 공지된 것이라면 제한 없이 사용할 수 있으며, 예컨대 글리세린 지방산 에스테르, 폴리글리세린 지방산 에스테르, 솔비탄 지방 에스테르, 레시틴, 프로필렌글리콜 지방산 에스테르 및 이들의 혼합물로 이루어진 군에서 선택된 1종이 가능하다. 이때 제1 계면활성제의 함량은 수용성 항산화제 유화물 전체 중량에 대해 1 내지 30 중량%이다. 제1 계면활성제의 함량이 상기 범위 미만이면 식용 유지의 유화 입자에 대한 유화 작용이 약화되어 에멀젼 형성이 어렵고, 상기 범위를 초과하면 유화 안정성이 떨어지는 문제점이 있다. The first surfactants of HLB 3 to HLB 7 may be used without limitation as long as they are known, for example, in the group consisting of glycerin fatty acid esters, polyglycerin fatty acid esters, sorbitan fatty esters, lecithin, propylene glycol fatty acid esters, and mixtures thereof One selected paper is possible. At this time, the content of the first surfactant is 1 to 30% by weight based on the total weight of the water-soluble antioxidant emulsion. If the content of the first surfactant is less than the above range, the emulsification action of the emulsified particles of edible oil and fat is weakened, making it difficult to form an emulsion, and if it exceeds the above range, there is a problem in that emulsion stability is poor.
상기 HLB 10 내지 HLB 14의 제2 계면활성제는 폴리글리세린 지방산 에스테르, 폴리옥시에틸렌 솔비탄 지방산 에스테르, 자당 지방산 에스테르, 효소분해 레시틴 및 이들의 혼합물로 이루어진 군에서 선택된 1종이 가능하나, 이에 한정되는 것은 아니다. 상기 제2 계면활성제의 함량이 상기 수치 범위를 만족하는 경우, 토코페롤과 카테킨의 항산화능을 해하지 않으면서, 수용성 항산화제 유화물 내에 토코페롤과 카테킨이 안정적으로 분산될 수 있도록 한다. The second surfactant of HLB 10 to HLB 14 may be one selected from the group consisting of polyglycerin fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sucrose fatty acid ester, enzymatically degraded lecithin, and mixtures thereof, but is not limited thereto. no. When the content of the second surfactant satisfies the above numerical range, tocopherol and catechin can be stably dispersed in the water-soluble antioxidant emulsion without damaging the antioxidant ability of tocopherol and catechin.
상기 공계면활성제는 유화에 보조적인 역할을 할 뿐만 아니라 용해제로 사용된다. 상기 공계면활성제는 글리세린, 솔비톨, 폴리에틸렌글리콜, 프로필렌글리콜, 트리아세틴 및 이들의 혼합물로 이루어진 군에서 선택된 1종이 가능하나, 이에 한정되는 것은 아니다. 이러한 공계면활성제의 함량은 수용성 항산화제 유화물 총 중량 대비 10 내지 45 중량%인 것이 바람직하다. 공계면활성제 함량이 10 중량% 미만이면 카테킨을 용해시키는 것이 용이하지 않으며, 45 중량%를 초과하여 사용하면 유화 입자가 잘 형성되지 않고 유화 안정성이 저하되는 문제가 있다. The cosurfactant plays an auxiliary role in emulsification and is used as a solubilizing agent. The cosurfactant may be one selected from the group consisting of glycerin, sorbitol, polyethylene glycol, propylene glycol, triacetin, and mixtures thereof, but is not limited thereto. The content of these cosurfactants is preferably 10 to 45% by weight based on the total weight of the water-soluble antioxidant emulsion. If the cosurfactant content is less than 10% by weight, it is not easy to dissolve catechin, and if it is used in excess of 45% by weight, emulsion particles are not formed well and emulsion stability is deteriorated.
상기 식용 유지는 식물 또는 동물로부터 얻은 원유나 이를 원료로 하여 제조, 가공한 것이라면 제한 없이 사용 가능하다. 예컨대, 대두유, 옥수수유, 채종유, 고올레산 채종유, 홍화유, 미강유, 팜유, 올리브유, 해바라기유, 야자유, 소맥 배아유, 중쇄중성지방(MCT Oil)에서 선택된 1종 이상의 유지가 가능하다. 이러한 식용 유지의 함량은 조성물 총 중량에 대해 1 내지 35 중량%일 수 있다. 1 중량% 미만에서는 오일의 양이 너무 적어 토코페롤의 용해가 어렵고, 35 중량%를 초과하면 에멀젼의 경시 안정성이 불량하다. The edible oil can be used without limitation as long as it is crude oil obtained from plants or animals or manufactured and processed using it as a raw material. For example, one or more oils selected from soybean oil, corn oil, rapeseed oil, high oleic acid rapeseed oil, safflower oil, rice bran oil, palm oil, olive oil, sunflower oil, palm oil, wheat germ oil, and medium chain triglycerides (MCT Oil) may be used. The content of these edible fats and oils may be 1 to 35% by weight based on the total weight of the composition. If the amount is less than 1% by weight, the amount of oil is too small to dissolve the tocopherol, and if it exceeds 35% by weight, the stability over time of the emulsion is poor.
상기 엑디스테로이드 유화물은 전체 100 중량%를 만족하도록, 엑디스테로이드 1 내지 30 중량%, HLB 3 내지 HLB 7의 유중 수적형 계면활성제 1 내지 10 중량%, HLB 10 내지 HLB 14의 수중 유적형 계면활성제 1 내지 20 중량%, 및 공계면활성제 40 내지 97 중량%를 포함한다. The ecdysteroid emulsion contains ecdysteroid 1 to 30 wt%, HLB 3 to HLB 7 water-in-oil surfactant 1 to 10 wt%, HLB 10 to HLB 14 oil-in-water surfactant 1 to satisfy 100 wt% of the total. to 20% by weight, and 40 to 97% by weight of cosurfactant.
상기 엑디스테로이드는 경구 투여시 포유동물에서 생물학적인 영향을 미치는 것은 제한 없이 사용할 수 있다. 일 예로, 시아스테론(Cyasterone), 24(28)-디하이드로마키스테론 A(24(28)-Dehydromakisterone A), 2-디옥시엑디손(2-Deoxyecdysone), 2-디옥시-20-하이드록시엑디손(2-Deoxy-20-hydroxyecdysone), 2-디옥시-20-하이드록시엑디손--22-O-β-D-글루코피라노사이드(2-Deoxy-20-hydroxyecdysone-22-O-β-D-glucopyranoside), 5α-2-디옥시인테그리스테론 A(5α-2-Deoxyintegristerone A), 2-디옥시-폴리포딘 B(2-Deoxy-polypodine B), 22-디옥시-20-하이드록시엑디손(22-Deoxy-20-hydroxyecdysone), 22-디옥시-인테그리스테론 A(22-Deoxy-integristerone A), 9α,20-디하이드로엑디손(9α,20-Dihydroxyecdysone), 20,26-디하이드록시엑디손(20,26-Dihydroxyecdysone), 디하이드로포스트스테론(Dihydropoststerone), 디하이드로루브로스레론(Dihydrorubroslerone), 엑디손, 5-하이드록시아부타스테론(5-Hydroxyabutasterone), 20-하이드록시엑디손(20-Hydroxyecdysone), 5α-20-하이드록시엑디손(5α-20-hydroxyecdysone), 20-하이드록시엑디손 22-아세테이트(20-Hydroxyecdysone 22-acetate), 20-하이드록시엑디손 2,3,22-트리아세테이트(20-Hydroxyecdysone 2,3,22-triacetate), 이노코스테론(Inokosterone), 인테그리스테론 A(Integristerone A), 인테그리스테론 B(Integristerone B), 마키스테론 A(Makisterone A), 마키스테론 C(Makisterone C), 무리스테론 A(Muristerone A), 누실스테론(Nusilsterone), 폴리포딘 B(Polypodine B), 포나스테론 A(Ponasterone A), 포나스테론 C(Ponasterone C), 포스트스테론(Poststerone), 프테로스테론(Pterosterone), 루브로스테론(Rubrosterone), 시디스테론(Sidisterone), 실레네오사이드 A(Sileneoside A), 튜케스테론(Turkesterone), 비티코스테론 E(Viticosterone E)이 가능하나, 이에 제한되는 것은 아니다. 일 구체예에서, 상기 엑디스테로이드는 시아스테론(Cyasterone), 엑디손, 20-하이드록시엑디손(20-Hydroxyecdysone), 5α-20-하이드록시엑디손(5α-20-hydroxyecdysone), 20-하이드록시엑디손 22-아세테이트(20-Hydroxyecdysone 22-acetate), 20-하이드록시엑디손 2,3,22-트리아세테이트(20-Hydroxyecdysone 2,3,22-triacetate), 폴리포딘 B(Polypodine B), 포나스테론 A(Ponasterone A), 포나스테론 C(Ponasterone C), 포스트스테론(Poststerone), 루브로스테론(Rubrosterone), 또는 튜케스테론(Turkesterone)이다. The ecdysteroid can be used without limitation as long as it has a biological effect on mammals when administered orally. For example, cyasterone, 24(28)-dihydromakisterone A, 2-deoxyecdysone, 2-deoxy-20-hydroxy 2-Deoxy-20-hydroxyecdysone, 2-Deoxy-20-hydroxyecdysone--22-O-β-D-glucopyranoside (2-Deoxy-20-hydroxyecdysone-22-O -β-D-glucopyranoside), 5α-2-deoxyintegristerone A, 2-deoxy-polypodine B, 22-deoxy- 20-hydroxyecdysone, 22-deoxy-integristerone A, 9α,20-dihydroecdysone, 20,26-Dihydroxyecdysone, Dihydropoststerone, Dihydrorubroslerone, Ecdysone, 5-Hydroxyabutasterone ), 20-hydroxyecdysone, 5α-20-hydroxyecdysone, 20-hydroxyecdysone 22-acetate, 20- Hydroxyecdysone 2,3,22-triacetate (20-Hydroxyecdysone 2,3,22-triacetate), Inokosterone, Integristerone A, Integristerone B, Makisterone A, Makisterone C, Muristerone A, Nusilsterone, Polypodine B, Ponasterone A, Phosphate Ponasterone C, Poststerone, Pterosterone, Rubrosterone, Sidisterone, Sileneoside A, Turkesterone ), viticosterone E (Viticosterone E) is possible, but is not limited thereto. In one embodiment, the ecdysteroid is cyasterone, ecdysone, 20-hydroxyecdysone, 5α-20-hydroxyecdysone, 20-hydroxyecdysone 20-Hydroxyecdysone 22-acetate, 20-Hydroxyecdysone 2,3,22-triacetate, Polypodine B, Ponasterone A, Ponasterone C, Poststerone, Rubrosterone, or Turkesterone.
이러한 엑디스테로이드는 엑디스테로이드 유화물 전체 중량에 대해 1 내지 30 중량%로 포함된다. 만약 엑디스테로이드의 함량이 상기 범위 미만이면 첨가에 따른 효과가 미미하고, 30 중량%를 초과하면 유화 입자 형성이 어려운 문제점이 있다. These ecdysteroids are included in an amount of 1 to 30% by weight based on the total weight of the ecdysteroid emulsion. If the content of ecdysteroid is less than the above range, the effect of addition is insignificant, and if it exceeds 30% by weight, it is difficult to form emulsified particles.
엑디스테로이드 유화물은 친수성 공계면활성제 내에 잘 녹으면서 계면활성 효과를 나타내어 유화 조성물의 유화 안정성을 유지하기 위해 상기한 HLB 값을 갖는 제1 계면활성제와 제2 계면활성제를 포함한다.The ecdysteroid emulsion contains a first surfactant and a second surfactant having the HLB value described above in order to maintain the emulsion stability of the emulsion composition by exhibiting a surfactant effect while being well dissolved in the hydrophilic cosurfactant.
HLB가 3 내지 7인 제1 계면활성제는 엑디스테로이드 유화물 전체 중량에 대해 1 내지 10 중량%로 포함된다. 제1 계면활성제의 함량이 1 중량% 미만이면 엑디스테로이드 유화 입자에 대한 유화 작용이 약화되어 에멀젼 형성이 어려운 문제점이 있고, 10 중량%를 초과하면 유화 안정성이 저하되는 문제점이 있다. The first surfactant having an HLB of 3 to 7 is included in an amount of 1 to 10% by weight based on the total weight of the ecdysteroid emulsion. If the content of the first surfactant is less than 1% by weight, the emulsification action of the ecdysteroid emulsified particles is weakened, making it difficult to form an emulsion, and if it exceeds 10% by weight, there is a problem in that emulsion stability is reduced.
HLB가 10 내지 14인 제2 계면활성제는 엑디스테로이드 유화물 전체 중량에 대해 1 내지 20 중량%로 함유된다. 이때 제2 계면활성제의 함량이 1 중량% 미만이면 친수성 공계면활성제에 대한 유화 작용이 약화되어 유화가 어렵고, 20 중량%를 초과하면 유화 안정성을 유지가 어려운 문제점이 있다. The second surfactant having an HLB of 10 to 14 is contained in an amount of 1 to 20% by weight based on the total weight of the ecdysteroid emulsion. At this time, if the content of the second surfactant is less than 1% by weight, the emulsification action of the hydrophilic co-surfactant is weakened, making it difficult to emulsify, and if it exceeds 20% by weight, it is difficult to maintain emulsion stability.
제1 계면활성제와 제2 계면활성제의 구체적인 종류는 상기에서 언급한 바를 따른다. The specific types of the first surfactant and the second surfactant are as described above.
상기 공계면활성제는 엑디스테로이드를 분산, 용해시키고, 유화에 보조적인 역할을 하기 위해 첨가되는 것으로, 엑디스테로이드 유화물 중 그 함량은 40 내지 97 중량%이다. 40 중량% 미만에서는 유화 안정성 유지가 어렵고, 97 중량%를 초과하면 엑디스테로이드의 안정적인 분산이 어렵다. The cosurfactant is added to disperse and dissolve the ecdysteroid and play an auxiliary role in emulsification, and the content thereof in the ecdysteroid emulsion is 40 to 97% by weight. If it is less than 40% by weight, it is difficult to maintain emulsion stability, and if it exceeds 97% by weight, it is difficult to stably disperse the ecdysteroid.
상기 엑디스테로이드 함유 수용성 유화 조성물은 상기 수용성 항산화제 유화물 0.1 내지 20 중량%; 및 상기 엑디스테로이드 유화물 80 내지 99.9 중량%를 포함한다. The ecdysteroid-containing water-soluble emulsion composition includes 0.1 to 20% by weight of the water-soluble antioxidant emulsion; and 80 to 99.9% by weight of the ecdysteroid emulsion.
본 발명의 엑디스테로이드 함유 수용성 유화 조성물은 기능성 수난용 물질인 엑디스테로이드를 수용화 시킴으로써 물질의 흡수율과 효능을 증대시킬 수 있어, 물질이 갖는 기능성을 다양한 분야에 활용될 수 있도록 한다. 또한, 수용성 항산화제 유화물을 함유하여, 수용액 상에서 산소에 의한 산화를 예방할 수 있는 산화 안정성이 우수하다. The water-soluble emulsified composition containing ecdysteroid of the present invention can increase the absorption rate and efficacy of the substance by solubilizing ecdysteroid, a functional water substance, so that the functionality of the substance can be used in various fields. In addition, it contains a water-soluble antioxidant emulsion and has excellent oxidation stability capable of preventing oxidation by oxygen in an aqueous solution.
이하 본 발명을 실시예를 통해 상세히 설명한다. 그러나 이러한 실시예들로 본 발명의 범위를 한정하는 것은 아니다.Hereinafter, the present invention will be described in detail through examples. However, these examples are not intended to limit the scope of the present invention.
실시예Example
하기 표 1 내지 표 9의 조성으로 각각 수용성 항산화제 유화물과 엑디스테로이드 유화물을 제조한 후 최종 엑디스테로이드 함유 수용성 유화 조성물을 제조하였다. After preparing water-soluble antioxidant emulsions and ecdysteroid emulsions, respectively, with the compositions shown in Tables 1 to 9 below, final ecdysteroid-containing water-soluble emulsion compositions were prepared.
(HLB: 4)Glycerin Fatty Acid Esters
(HLB: 4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB:12)Polyglycerin fatty acid ester
(HLB:12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
제1계면활성제, 제2계면활성제를 호모 믹서에 투입한 후, 온도를 50 ℃ 이상으로 유지하면서 500 rpm 이하로 교반하였다. 이후 카테킨, 대두유, 토코페롤을 순차적으로 투입하여 원료 1을 제조하였다. After the first surfactant and the second surfactant were added to the homomixer, the mixture was stirred at 500 rpm or less while maintaining the temperature at 50 °C or higher. Then, raw material 1 was prepared by sequentially adding catechin, soybean oil, and tocopherol.
이와는 별도로 글리세린에 제2계면활성제를 투입하여 원료 2를 제조하였다.Separately, raw material 2 was prepared by adding a second surfactant to glycerin.
이때 제2계면활성제는 원료 1과 원료 2에 총 사용량 중 30 중량%와 70 중량%를 각각 사용하였다. At this time, 30% by weight and 70% by weight of the total amount of the second surfactant were used for raw material 1 and raw material 2, respectively.
원료 2에 원료 1을 혼합하면서 호모믹서로 5,000 rpm 이상으로 유화 분산을 진행하여 수용성 항산화제 유화물을 제조하였다. A water-soluble antioxidant emulsion was prepared by emulsifying and dispersing at 5,000 rpm or more with a homomixer while mixing raw material 1 with raw material 2.
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
(HLB:4)Glycerin Fatty Acid Esters
(HLB:4)
(HLB: 2)Sucrose Fatty Acid Esters
(HLB: 2)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 12)Polyglycerin fatty acid ester
(HLB: 12)
(HLB: 8)Polyglyceryl-6 diisostearate
(HLB: 8)
(HLB: 18)PEG-18 Stearate
(HLB: 18)
제1계면활성제, 제2계면활성제를 호모 믹서에 투입한 후, 온도를 50도 이상으로 유지하면서 500 rpm 이하로 교반하였다. 이후 엑다이손 원료를 투입하고 엑타이손이 유화물에 습윤되기 시작하면, 호모믹서의 교반을 시작하여 서서히 rpm을 올리면서 5,000 rpm 이상에서 유화 분산을 진행하였다. 유화가 완료되면 글리세린을 투입한 후 500 rpm 이하에서 교반하여 엑다이손 유화물을 제조하였다.After putting the first surfactant and the second surfactant into the homomixer, the mixture was stirred at 500 rpm or less while maintaining the temperature at 50 degrees or more. Then, when the ecdysone raw material was introduced and the ectysone began to wet the emulsion, stirring of the homomixer was started, and the emulsification and dispersion were performed at 5,000 rpm or more while gradually increasing the rpm. When the emulsification was completed, glycerin was added and stirred at 500 rpm or less to prepare an ecdysone emulsion.
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유화물20-hydroxyecdysone
oil
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유화물Polypodin B
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상기 표 10 내지 표 17에 기재된 조성에 따라 이렇게 얻은 엑디스테로이드 유화물에 상기에서 제조된 수용성 항산화제 유화물을 투입한 후 유화액의 성상을 확인하면서 500 rpm 이하에서 혼합 분산 작업을 진행하여 수용성 항산화제 유화물을 함유하는 엑디스테로이드 함유 수용성 유화 조성물을 제조하였다. After adding the water-soluble antioxidant emulsion prepared above to the ecdysteroid emulsion thus obtained according to the composition shown in Tables 10 to 17, a mixing and dispersing operation was performed at 500 rpm or less while checking the properties of the emulsion to obtain a water-soluble antioxidant emulsion. A water-soluble emulsion composition containing ecdysteroids was prepared.
실험예 1: 항산화 효과 측정 Experimental Example 1: Antioxidant effect measurement
DPPH 측정법을 이용하여 수용성 항산화제 유화물을 포함하는 엑디스테로이드 함유 수용성 유화 조성물의 항산화 효과를 측정하였다. The antioxidant effect of the ecdysteroid-containing water-soluble emulsion composition containing the water-soluble antioxidant emulsion was measured using the DPPH measurement method.
DPPH 라디칼 소거 활성 측정은 항산화능을 측정하는데 가장 보편적으로 사용되는 방법으로 색상 변화로 항산화능을 평가하는 방법으로, 항산화능이 뛰어난 시료를 처리하면 색의 변화가 뚜렷하고 효과가 떨어지는 시료를 처리하면 보라색에서 많은 변화가 일어나지 않아서 이러한 변화 정도를 spectrophotometer(517nm)로 흡광도를 측정하여 항산화능을 비교하며, 값이 높을수록 항산화 효과도 높다고 평가한다. 실험조건(가혹조건 시험: 40℃에서 1주일간 방치하여 산화 유도)은 아래와 같다. DPPH radical scavenging activity measurement is the most commonly used method for measuring antioxidant activity. It is a method of evaluating antioxidant activity by color change. When a sample with excellent antioxidant activity is treated, the color change is clear, and when a sample with low effect is treated, it changes from purple to purple. Since there is not much change, the degree of change is measured by the absorbance with a spectrophotometer (517 nm) to compare the antioxidant capacity, and the higher the value, the higher the antioxidant effect. The experimental conditions (severe condition test: oxidation induction by leaving at 40 ° C for 1 week) are as follows.
① 용매 - 에탄올① Solvent - Ethanol
② 함량 - 0.1 wt% 분산액, 0.3 wt% 분산액② Content - 0.1 wt% dispersion, 0.3 wt% dispersion
③ 방법 - shaking waterbath 사용. 30℃, 2hr③ Method - Using a shaking waterbath. 30℃, 2hr
④ 필터 - No.5 여과지 사용 자연여과후 0.45μm 카트리지 필터 사용④ Filter - After natural filtration using No.5 filter paper, use 0.45μm cartridge filter
실험 결과는 아래 표 18 내지 표 25에 나타내었다. The experimental results are shown in Tables 18 to 25 below.
상기 표 18 내지 표 25에 나타낸 바와 같이, 수용성 항산화 유화물에 카테킨이나 토코페롤을 포함하지 않은 제조예 3, 제조예 4의 수용성 항산화 유화물을 사용하는 경우 엑디스테로이드 함유 수용성 유화 조성물의 항산화 효과가 낮은 것을 확인할 수 있었다. As shown in Tables 18 to 25, when using the water-soluble antioxidant emulsions of Preparation Examples 3 and 4 that do not contain catechin or tocopherol in the water-soluble antioxidant emulsion, it is confirmed that the antioxidant effect of the water-soluble emulsion composition containing ecdysteroids is low. could
실험예 2: 수용해도 확인 Experimental Example 2: Confirmation of water solubility
상기 표 26 내지 표 41에 기재된 조성에 따라 엑다이손 유화물에 수용성 항산화제 유화물을 투입한 후 유화액의 성상을 확인하면서 500 rpm 이하에서 혼합 분산 작업을 진행하여 수용성 항산화제 유화물을 함유하는 엑디스테로이드 함유 수용성 유화 조성물을 제조하였다. After adding the water-soluble antioxidant emulsion to the ecdysone emulsion according to the composition shown in Tables 26 to 41, mixing and dispersing work was performed at 500 rpm or less while checking the properties of the emulsion to contain ecdysteroids containing water-soluble antioxidant emulsions. A water-soluble emulsion composition was prepared.
제조된 엑디스테로이드 함유 수용성 유화 조성물의 수용해도를 아래와 같이 확인하였다. 증류수 50 ml를 항온수조에서 수온 38 ℃를 유지하고, 100 rpm 속도를 유지하면서 실시예와 비교예의 유화 조성물을 1g을 투입하였다. 1시간 후 원심분리 후 여과한 다음 Karl Fisher method 로 수분함량 측정하여 유기물 함량 정량하였다. The water solubility of the prepared water-soluble emulsion composition containing ecdysteroids was confirmed as follows. 50 ml of distilled water was maintained at a water temperature of 38 ° C in a constant temperature water bath, and 1 g of the emulsified compositions of Examples and Comparative Examples was added while maintaining a speed of 100 rpm. After 1 hour, the mixture was centrifuged, filtered, and the organic matter content was quantified by measuring the water content by the Karl Fisher method.
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상기 표 42 내지 표 50에 나타낸 바와 같이, HLB(Hydrophile-Lipophile Balance)가 상이한 2종의 계면활성제를 포함하는 수용성 항산화 유화물과 엑디스테로이드 유화물을 사용한 실시예 1 내지 15의 조성물은 비교예의 유화물과 비교하여 수용해도가 매우 높은 것으로 나타났다. As shown in Tables 42 to 50, the compositions of Examples 1 to 15 using a water-soluble antioxidant emulsion and an ecdysteroid emulsion containing two types of surfactants having different Hydrophile-Lipophile Balance (HLB) were compared with the emulsions of Comparative Examples It was found that the water solubility was very high.
실험예 3: 수분산 유화 입자 확인Experimental Example 3: Confirmation of water-dispersed emulsified particles
상기 표 26 내지 표 41에 따라 제조된 엑디스테로이드 함유 수용성 유화 조성물의 유화 압자 크기를 아래와 같이 확인하였다. 증류수 50 ml를 항온수조에서 수온 38 ℃를 유지하고, 100 rpm 속도를 유지하면서 실시예와 비교예의 유화 조성물을 1g을 투입하였다. 1시간 후 광학현미경으로 유화 입자를 관찰하고 그 결과를 도 1 및 도 2에 나타내었다. The emulsification indenter size of the ecdysteroid-containing water-soluble emulsion composition prepared according to Tables 26 to 41 was confirmed as follows. 50 ml of distilled water was maintained at a water temperature of 38 ° C in a constant temperature water bath, and 1 g of the emulsified compositions of Examples and Comparative Examples was added while maintaining a speed of 100 rpm. After 1 hour, emulsified particles were observed under an optical microscope, and the results are shown in FIGS. 1 and 2.
Zetasizer Nano ZS(Malvern Instrument, U.K.)를 사용하여 상기 증류수 중 유화입자의 크기를 측정하였다. 이때 시료에 대하여 3회 반복 측정하였고, 그 평균값을 하기 표 51에 나타내었다. The size of emulsion particles in the distilled water was measured using a Zetasizer Nano ZS (Malvern Instrument, U.K.). At this time, the sample was repeatedly measured three times, and the average value is shown in Table 51 below.
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상기 표 51, 도 1 및 도 2를 참조하면, 본 발명의 일 실시예에 해당하는 엑디스테로이드 함유 수용성 유화 조성물은 1.5 내지 2.5 μm의 유화 입자를 형성하는 반면, 비교예 33 내지 112의 엑디스테로이드 함유 수용성 유화 조성물은 유화 입자가 형성되지 않아 유화입자의 크기를 측정할 수 없었다. 이로부터 본 발명에 따른 엑디스테로이드 함유 수용성 유화 조성물은 생체에서 흡수되어 높은 생체이용률을 나타낼 수 있을 것으로 예상할 수 있다. Referring to Table 51 and FIGS. 1 and 2, the water-soluble emulsion composition containing ecdysteroids corresponding to an embodiment of the present invention forms emulsified particles of 1.5 to 2.5 μm, whereas Comparative Examples 33 to 112 containing ecdysteroids Since emulsion particles were not formed in the water-soluble emulsion composition, the size of the emulsion particles could not be measured. From this, it can be expected that the ecdysteroid-containing water-soluble emulsion composition according to the present invention can be absorbed in the living body and exhibit high bioavailability.
Claims (7)
토코페롤 1 내지 10 중량%,
카테킨 1 내지 5 중량%,
HLB 3 내지 HLB 7의 제1 계면활성제 1 내지 15 중량%,
HLB 10 내지 HLB 14의 제2 계면활성제 10 내지 50 중량%;
공계면활성제 15 내지 45 중량%, 및
식용 유지 5 내지 35 중량%,
(2) 전체 100 중량%를 만족하도록 하기 성분을 포함하는 엑디스테로이드 유화물:
엑디스테로이드 1 내지 20 중량%,
HLB 3 내지 HLB 7의 제1 계면활성제 1 내지 10 중량%,
HLB 10 내지 HLB 14의 제2 계면활성제 1 내지 20 중량%, 및
공계면활성제 50 내지 97 중량%를 포함하고,
상기 엑디스테로이드는
엑디손, 20-하이드록시엑디손(20-Hydroxyecdysone), 시아스테론(Cyasterone), 5α-20-하이드록시엑디손(5α-20-hydroxyecdysone), 20-하이드록시엑디손 22-아세테이트(20-Hydroxyecdysone 22-acetate), 20-하이드록시엑디손 2,3,22-트리아세테이트(20-Hydroxyecdysone 2,3,22-triacetate), 폴리포딘 B(Polypodine B), 포나스테론 A(Ponasterone A), 포나스테론 C(Ponasterone C), 포스트스테론(Poststerone), 루브로스테론(Rubrosterone), 튜케스테론(Turkesterone) 및 이들의 혼합물로 이루어진 군에서 선택된 1종이고,
상기 제1 계면활성제는
글리세린 지방산 에스테르, 폴리글리세린 지방산 에스테르, 솔비탄 지방 에스테르, 레시틴, 프로필렌글리콜 지방산 에스테르 및 이들의 혼합물로 이루어진 군에서 선택된 1종이고,
상기 제2 계면활성제는
폴리글리세린 지방산 에스테르, 폴리옥시에틸렌 솔비탄 지방산 에스테르, 자당 지방산 에스테르, 효소분해 레시틴 및 이들의 혼합물로 이루어진 군에서 선택된 1종이고,
상기 공계면활성제는
글리세린, 솔비톨, 폴리에틸렌글리콜, 프로필렌글리콜, 트리아세틴 및 이들의 혼합물로 이루어진 군에서 선택된 1종이고,
상기 식용 유지는
두유, 옥수수유, 채종유, 고올레산 채종유, 홍화유, 미강유, 팜유, 올리브유, 해바라기유, 야자유, 소맥 배아유, 및 중쇄중성지방(MCT Oil)으로 이루어진 군에서 선택된 1종 이상의 식용 유지이고,
상기 수용성 항산화제 유화물 1 내지 10 중량%; 및
상기 엑디스테로이드 유화물 90 내지 99 중량%를 포함하는 것인,
수용성 항산화제 유화물을 함유하는 엑디스테로이드 함유 수용성 유화 조성물.(1) A water-soluble antioxidant emulsion containing the following components to satisfy 100% by weight of the total:
1 to 10% by weight of tocopherol;
1 to 5% by weight of catechin;
1 to 15% by weight of a first surfactant of HLB 3 to HLB 7;
10 to 50% by weight of a second surfactant of HLB 10 to HLB 14;
15 to 45% by weight of a cosurfactant, and
5 to 35% by weight of edible fat and oil;
(2) Ecdysteroid emulsion containing the following components to satisfy 100% by weight of the total:
1 to 20% by weight of an ecdysteroid;
1 to 10% by weight of a first surfactant of HLB 3 to HLB 7;
1 to 20% by weight of a second surfactant of HLB 10 to HLB 14, and
50 to 97% by weight of a cosurfactant;
The ecdysteroids
Ecdysone, 20-Hydroxyecdysone, Cyasterone, 5α-20-hydroxyecdysone, 20-hydroxyecdysone 22-acetate (20- Hydroxyecdysone 22-acetate), 20-hydroxyecdysone 2,3,22-triacetate (20-Hydroxyecdysone 2,3,22-triacetate), Polypodine B, Ponasterone A, It is one selected from the group consisting of Ponasterone C, Poststerone, Rubrosterone, Turkesterone and mixtures thereof,
The first surfactant is
It is one selected from the group consisting of glycerin fatty acid esters, polyglycerin fatty acid esters, sorbitan fatty esters, lecithin, propylene glycol fatty acid esters, and mixtures thereof;
The second surfactant is
It is one selected from the group consisting of polyglycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, sucrose fatty acid esters, enzymatically degraded lecithin, and mixtures thereof;
The cosurfactant is
It is one selected from the group consisting of glycerin, sorbitol, polyethylene glycol, propylene glycol, triacetin, and mixtures thereof,
The edible fats and oils
At least one edible oil selected from the group consisting of soybean oil, corn oil, rapeseed oil, high oleic acid rapeseed oil, safflower oil, rice bran oil, palm oil, olive oil, sunflower oil, palm oil, wheat germ oil, and medium chain triglycerides (MCT Oil),
1 to 10% by weight of the water-soluble antioxidant emulsion; and
Which comprises 90 to 99% by weight of the ecdysteroid emulsion,
An ecdysteroid-containing water-soluble emulsion composition containing a water-soluble antioxidant emulsion.
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020200174987A KR102524312B1 (en) | 2020-12-15 | 2020-12-15 | Water-soluble emulsion composition comprising ecdysteroid |
PCT/KR2021/018429 WO2022131654A1 (en) | 2020-12-15 | 2021-12-07 | Water-soluble emulsion composition containing ecdysteroid |
PCT/KR2021/018428 WO2022131653A1 (en) | 2020-12-15 | 2021-12-07 | Water-soluble emulsion composition containing natural polyphenol compound |
EP21906957.2A EP4265127A1 (en) | 2020-12-15 | 2021-12-07 | Water-soluble emulsion composition containing natural polyphenol compound |
PCT/KR2021/018432 WO2022131656A1 (en) | 2020-12-15 | 2021-12-07 | Alkaloid-containing, water-soluble emulsified composition |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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KR1020200174987A KR102524312B1 (en) | 2020-12-15 | 2020-12-15 | Water-soluble emulsion composition comprising ecdysteroid |
Publications (2)
Publication Number | Publication Date |
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KR20220085855A KR20220085855A (en) | 2022-06-23 |
KR102524312B1 true KR102524312B1 (en) | 2023-04-21 |
Family
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KR1020200174987A KR102524312B1 (en) | 2020-12-15 | 2020-12-15 | Water-soluble emulsion composition comprising ecdysteroid |
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KR (1) | KR102524312B1 (en) |
WO (1) | WO2022131654A1 (en) |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100359044B1 (en) * | 1993-07-08 | 2003-02-05 | 노파르티스 아게 | Pharmaceutical Compositions for Hardly Soluble Active Substances |
JP2005179367A (en) | 2003-12-22 | 2005-07-07 | L'oreal Sa | Use of ecdysteroid for preparing dermatological or cosmetological composition preventing hair loss |
US20060018937A1 (en) * | 2002-10-25 | 2006-01-26 | Foamix Ltd. | Steroid kit and foamable composition and uses thereof |
JP2011252015A (en) | 2003-05-22 | 2011-12-15 | Lipocine Inc | Pharmaceutical composition and dosage form for administration of hydrophobic drug |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6027749B2 (en) * | 2012-02-07 | 2016-11-16 | 小川香料株式会社 | Oil-soluble antioxidant and method for producing the same |
CA2930505C (en) * | 2013-12-20 | 2019-06-18 | F. Hoffman-La Roche Ag | Compounds comprising one or more hydrophobic domains and a hydrophilic domain comprising peg moieties, useful for binding cells |
-
2020
- 2020-12-15 KR KR1020200174987A patent/KR102524312B1/en active IP Right Grant
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2021
- 2021-12-07 WO PCT/KR2021/018429 patent/WO2022131654A1/en unknown
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100359044B1 (en) * | 1993-07-08 | 2003-02-05 | 노파르티스 아게 | Pharmaceutical Compositions for Hardly Soluble Active Substances |
US20060018937A1 (en) * | 2002-10-25 | 2006-01-26 | Foamix Ltd. | Steroid kit and foamable composition and uses thereof |
JP2011252015A (en) | 2003-05-22 | 2011-12-15 | Lipocine Inc | Pharmaceutical composition and dosage form for administration of hydrophobic drug |
JP2005179367A (en) | 2003-12-22 | 2005-07-07 | L'oreal Sa | Use of ecdysteroid for preparing dermatological or cosmetological composition preventing hair loss |
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WO2022131654A1 (en) | 2022-06-23 |
KR20220085855A (en) | 2022-06-23 |
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