KR102172371B1 - A pharmaceutical composition comprising extract of Aloe, quince and corn silk for preventing or treating obesity - Google Patents
A pharmaceutical composition comprising extract of Aloe, quince and corn silk for preventing or treating obesity Download PDFInfo
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- KR102172371B1 KR102172371B1 KR1020190011887A KR20190011887A KR102172371B1 KR 102172371 B1 KR102172371 B1 KR 102172371B1 KR 1020190011887 A KR1020190011887 A KR 1020190011887A KR 20190011887 A KR20190011887 A KR 20190011887A KR 102172371 B1 KR102172371 B1 KR 102172371B1
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- quince
- extract
- obesity
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- pharmaceutical composition
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Abstract
본 발명은 노회, 모과 및 옥촉서예 추출물을 유효성분으로 포함하는 비만 예방 또는 치료용 약학 조성물에 관한 것이다. 상기 추출물은 노회, 모과 및 옥촉서예 단독 추출물에 비해 지방축적을 저해하는 효과가 현저히 우수하고 비만이 유도된 동물모델에서 체중 감소, 체지방 감소 및 혈중 중성지방량 감소 효과가 우수하므로, 비만 예방 또는 치료용 약학 조성물로 유용하게 사용될 수 있다.The present invention relates to a pharmaceutical composition for preventing or treating obesity, comprising an extract of presbyopia, quince, and okchok calligraphy as an active ingredient. The extract is significantly superior in the effect of inhibiting fat accumulation compared to the single extracts of nohoe, quince and okchok calligraphy, and has excellent effect of reducing weight, reducing body fat, and reducing blood triglyceride in an animal model in which obesity is induced. It can be usefully used as a pharmaceutical composition.
Description
본 발명은 노회, 모과 및 옥촉서예 추출물을 유효성분으로 포함하는 비만 예방 또는 치료용 약학 조성물에 관한 것이다.The present invention relates to a pharmaceutical composition for preventing or treating obesity, comprising an extract of presbyopia, quince, and okchok calligraphy as an active ingredient.
최근 급속한 산업화와 소득 수준의 향상, 식습관 및 식생활 등의 생활패턴이 빠르게 서구화가 진행됨에 따라 암, 당뇨병, 심혈관계 질환, 비만 등으로 대표되는 각종 성인병 환자가 급격히 증가하고 있는 추세이다. With the recent rapid industrialization, improvement of income level, and rapid westernization of lifestyle patterns such as eating habits and diet, the number of patients with various adult diseases, such as cancer, diabetes, cardiovascular disease, and obesity, is rapidly increasing.
일반적으로, 비만(obesity)은 섭취한 에너지중 소비하고 남은 것이 중성지방으로 전환되어 주로 복부와 피하지방조직의 지방세포(adipocyte)에 축적되어 지방조직이 비정상적으로 증가된 상태를 말한다. 비만은 그 자체가 일상생활의 지장을 초래하는 질병이기도 하지만, 질병 자체의 의미보다는 비만으로 인해 여러 가지 합병증을 유발하게 된다는 것에 더욱 문제의 심각성이 있다. In general, obesity refers to a state in which fat tissue is abnormally increased by being converted into triglycerides and accumulated in adipocytes of the abdominal and subcutaneous fat tissue. Obesity itself is a disease that interferes with daily life, but there is a more serious problem that obesity causes various complications rather than the meaning of the disease itself.
비만은 혈액 내의 콜레스테롤 또는 중성지방의 양이 증가되는 고지혈증을 유발하여 고혈압, 심혈관계 질환 및 뇌졸중 등의 치명적인 질병으로 발전할 수 있고, 말초조직(Kelley, D. E. et al., Diabetes, 49(5), 677-683, 2000)과 복부지방조직에서의 중성지방 축적(Kelley, D. E. et al., Am J Physiol Endocrinol Metab., 278(5), E941-948, 2000) 증가로 인슐린 저항성이 유발되어 제2형 당뇨병을 발생시킬 수도 있으므로 장기적인 관리와 치료가 절대적으로 필요하다. 또한, 동양인의 경우 서양인에 비해 체질량 지수는 적어도 복부 비만이 심하여, 고혈압, 당뇨병, 고지혈증과 같은 동맥관련 질환에 의한 합병증에 대해서 감수성이 높기 때문에 비만관리가 더욱 중요시된다.Obesity causes hyperlipidemia, which increases the amount of cholesterol or triglycerides in the blood, and can lead to fatal diseases such as high blood pressure, cardiovascular disease and stroke, and peripheral tissues (Kelley, DE et al., Diabetes, 49(5)). , 677-683, 2000) and triglyceride accumulation in abdominal adipose tissue (Kelley, DE et al., Am J Physiol Endocrinol Metab., 278(5), E941-948, 2000). It can lead to
비만을 치료하기 위해 식이요법, 운동요법, 잘못된 식습관과 생활습관을 교정해 주는 행동수정요법, 외과에서 장이나 위의 용적을 줄이는 수술요법, 식욕 억제제, 이뇨제, 설사제 혹은 포만감을 주기 위한 섬유질 등을 사용하는 약물요법 등 다양한 방법이 제공되고 있다. Diet to treat obesity, exercise therapy, behavior modification therapy to correct wrong eating and lifestyle habits, surgical therapy to reduce the volume of the intestine or stomach in surgery, appetite suppressants, diuretics, diuretics, or fiber to give a feeling of satiety Various methods, such as drug therapy using, are provided.
현재까지 개발된 비만치료제 계열은 식욕억제제, 열 대사 촉진제, 소화억제제, 호르몬조절제 등이 알려져 있다. 식욕억제제 계열들은 작용기작에 따라 중추성 아드레날린 수용체 흥분제(예. 벤즈페타민(benzphetamine), 펜터민(phentermine)), 세로토닌 재흡수 억제제(예. 펜플루라민(fenfluramine)), 아드레날린 및 세로토닌 재흡수 억제제(예. 시부트라민(sibutramine)) 등으로 나누어진다. 열 대사 촉진제(예. 에페드린/카페인 혼합제(ephedrine/caffeine combination))는 아드레날린성 β3 수용체의 효능을 증대시켜서 체내의 발열작용과 에너지 소비량을 증가시켜 비만억제 효과를 나타내므로 정상인보다 단기적인 체중감소 효능이 뛰어나게 나타난다. 그러나, 중추신경계에 작용하여 식욕을 감소시키는 작용기전 특성 상 장기간 사용 시 지속적인 효과는 떨어지는 반면 심장질환, 혈압상승, 심장마비 증가, 우울증 및 자살 증가 등 심각한 부작용을 유발한다는 문제가 있다.As for obesity treatment products developed to date, appetite suppressants, heat metabolism accelerators, digestive inhibitors, hormone regulators, etc. are known. Depending on the mechanism of action, the appetite suppressant classes include central adrenergic receptor stimulants (e.g. benzphetamine, phentermine), serotonin reuptake inhibitors (e.g. fenfluramine), adrenaline and serotonin reuptake inhibitors (e.g. Yes, it is divided into sibutramine). Heat metabolism accelerators (e.g. ephedrine/caffeine combination) increase the efficacy of adrenergic β3 receptors to increase the body's fever and energy consumption, thereby suppressing obesity. Appears outstanding. However, due to the nature of the mechanism of action of reducing appetite by acting on the central nervous system, there is a problem of causing serious side effects such as heart disease, increased blood pressure, increased heart attack, increased depression and suicide, while the lasting effect is inferior when used for a long time.
한편, 지방분해 저해제 계열 비만치료제인 오를리스타트(orlistat)는 중성지방을 분해하는 췌장의 지방분해효소인 리파아제(pancreatic lipase)에 비가역적인 결합을 하여 불활성화 시킴으로써, 중성지방 및 콜레스테롤의 흡수를 감소시킴과 동시에 배설을 촉진시키는 기작으로 항비만 작용을 하였다. 그러나 오를리스타트 또한 복통, 설사, 지용성 비타민 흡수 억제 등의 부작용들이 있으며, 장기 복용 시 심각한 간 손상 유발 등이 알려져 있어, 현재는 이에 대한 안전성 재검토가 진행 중에 있다.On the other hand, orlistat, a lipolysis inhibitor-based obesity treatment drug, reduces the absorption of triglycerides and cholesterol by irreversibly binding to and inactivating lipase, a lipolytic enzyme of the pancreas that degrades triglycerides. At the same time, it acted as an anti-obesity mechanism as a mechanism to promote excretion. However, Orlistat also has side effects such as abdominal pain, diarrhea, and inhibition of absorption of fat-soluble vitamins, and it is known to cause serious liver damage when taken for a long time, and safety review is currently underway.
따라서 시판 중인 합성 비만치료제의 대부분은 심각한 부작용이 있는 것으로 알려져 있기 때문에, 부작용이 없으면서도 비만을 효과적으로 치료할 수 있는 비만치료제의 개발이 절실한 실정이다.Therefore, since most of the synthetic anti-obesity drugs on the market are known to have serious side effects, there is an urgent need to develop an obesity treatment agent that can effectively treat obesity without any side effects.
노회(Aloe)는 나리과(Liliaceae)에 속하는 다년생 초본으로 알로에라고도 한다. 노회는 장에 자극을 가하는 성질이 있고 차가운 성질이 있어서, 열로 인한 건조 변비증 등에 사용되며, 기생충이나 해충 따위를 제거하는 데에 사용되는 것으로 알려져 있다. 또한, 노회는 위장병, 천식 등을 치유하는 효능이 있고, 베인 상처, 화상, 튼 상처 등을 치유하는 효능이 있어 내복용뿐만 아니라 외용으로도 사용되어 왔다. 노회로부터 분리된 화합물로는 알로에신(Aloesin), 알로에레신(Aloeresin) 등 크로몬(Chromone) 계열의 화합물들이 알려져 있다.Aloe is a perennial herb belonging to the Liliaceae family, also known as aloe. Presbytery is known to be used for dry constipation due to heat and to remove parasites and pests because of its cold and cold properties. In addition, the presbytery has the effect of curing gastrointestinal diseases and asthma, and has the effect of healing cuts, burns, and sprained wounds, so it has been used not only for internal use but also for external use. As a compound isolated from the presbytery, chromone-based compounds such as aloesin and aloeresin are known.
모과(quince)는 장미과에 속하는 낙엽교목의 열매로 당분, 칼슘, 인, 철, 칼륨, β-카로틴 및 비타민 C 등이 풍부하고 약 2% 사포닌, 2~3% 유기산, 플라보노이드 및 탄닌 등이 함유되어 있으며, 이외에도 다양한 영양 성분이 함유되어 있다. Quince is the fruit of a deciduous tree belonging to the Rosaceae family. It is rich in sugar, calcium, phosphorus, iron, potassium, β-carotene and vitamin C, and contains about 2% saponin, 2~3% organic acids, flavonoids and tannins. In addition, it contains various nutrients.
또한 모과는 오래전부터 식용 및 약용으로 이용되어 왔으며, 특히 기침, 감기, 기관지염 완화 효능이 있는 것으로 알려져 있다. 그러나, 일반 과실에 비해 수분함량이 적고 떫은맛이 강하며 석세포 및 목질이 발달하여 육질이 거친 편으로, 가공화하는데 어려움이 있어 대부분의 모과는 폐기되고 있는 실정이다. 따라서 모과의 새로운 기능적 가치를 평가하고 다양한 산업에 접목시켜 폐기되는 자원을 재활용할 필요성이 있다. In addition, quince has long been used for edible and medicinal purposes, and is known to be particularly effective in relieving cough, cold, and bronchitis. However, compared to general fruits, most of the quinces are discarded due to the fact that the moisture content is low, the astringency is strong, and the flesh is rough due to the development of stone cells and wood. Therefore, there is a need to recycle waste resources by evaluating the new functional value of quince and grafting it into various industries.
옥촉서예(corn silk)는 옥수수의 열매 부분을 싸고 있는 황색 또는 담갈색을 띄는 실 같은 부분으로 옥수수수염, 옥발 또는 옥미발로도 불린다. 옥촉서예에는 지방유, 정유, 식물 고무 물질, 지방, 쓴맛 배당체, 레진(resin), 사포닌(saponin), 알칼로이드(alkaloid), 메이신(maysin) 이외에 이노시톨(inositol), 크립토산틴(cryptoxanthin), 비타민 C, 비타민 K, 시토스테롤(sitosterol), 스티그마스테롤(stigmasterol), 말릭산, 타타릭산(tartaric acid), 글루코오스, 자일란, 갈락탄, 카테콜 등이 함유되어 있으며, 특히 비타민 K가 다량으로 포함되어 있다. Corn silk is a yellow or light brown thread-like part that surrounds the fruit part of corn, and is also called corn beard, jade bal or jade mibal. In addition to fatty oils, essential oils, plant rubber substances, fats, bitter glycosides, resins, saponins, alkaloids, and maysin, inositol, cryptoxanthin, vitamin C , Vitamin K, sitosterol, stigmasterol, malic acid, tartaric acid, glucose, xylan, galactan, catechol, etc., and especially vitamin K is contained in large amounts.
현재까지 밝혀진 약리작용으로는 방사선유발 산화스트레스 억제, 당뇨병과 노화의 합병증과 관련된 최종당화산물 생성 억제, 당뇨병성 신장변증 억제, 항산화, 이뇨효과 등이 보고되었다. 또한 식품, 향료 및 식품첨가물로도 활용되고 있는데 FEMA(Flavor and Extract Manufacturers Association), FDA(Food and Drug Administration)에 의해 GRAS(Generally recognized As Safe) 물질로 등재되어 있으며, 주로 음료, 빙과류, 사탕, 제빵 등에 이용되는 것으로 알려져 있다.The pharmacological action revealed so far has been reported to suppress radiation-induced oxidative stress, suppress the production of final glycosylated products related to complications of diabetes and aging, suppress diabetic nephropathy, antioxidant, and diuretic effects. It is also used as a food, flavoring, and food additive, and is listed as a GRAS (Generally Recognized As Safe) substance by FEMA (Flavor and Extract Manufacturers Association) and FDA (Food and Drug Administration). It is known to be used in baking.
한편, 노회, 모과 및 옥촉서예 추출물을 포함하는 비만 치료용 조성물과 관련된 종래기술로서, 한국등록특허 제10-0510239호에는 옥수수수염, 알로에를 포함하는 혼합물의 항비만 효과가 개시되었으며, 한국등록특허 제10-1851639호에는 모과 추출물의 항비만 효과가 개시되었고, 한국등록특허 제10-1732146호에는 옥수수수염 및 탱자 복합 추출물의 항비만 효과가 개시되었으며, 선행논문 [Pothuraju, R. et al., Phytother Res., 30(2), 200-207, 2016]에는 알로에 추출물의 항비만 효과가 개시된 바 있으나, 본 발명과 같이 노회, 모과 및 옥촉서예를 모두 포함하는 혼합 추출물의 항비만 효과에 대해서는 언급된 바가 없다.On the other hand, as a prior art related to a composition for treating obesity comprising an extract of presbytery, quince and oyster calligraphy, Korean Patent No. 10-0510239 discloses the anti-obesity effect of a mixture containing corn beard and aloe, and Korean registered patent No. 10-1851639 discloses the anti-obesity effect of the Chinese quince extract, and Korean Patent No. 10-1732146 discloses the anti-obesity effect of the corn beard and tanja complex extract, and previous papers [Pothuraju, R. et al., Phytother Res., 30(2), 200-207, 2016] discloses the anti-obesity effect of the aloe extract, but mentions the anti-obesity effect of the mixed extract including all of the presbytery, quince and oyster calligraphy as in the present invention. Nothing happened.
본 발명자들은 항비만용 조성물을 연구하는 과정에서, 노회, 모과 및 옥촉서예를 특정 배합비로 혼합한 추출물이 단독 추출물에 비해 항비만 효과가 특히 우수함을 확인함으로써 본 발명을 완성할 수 있었다.In the course of researching a composition for anti-obesity, the present inventors were able to complete the present invention by confirming that the extract obtained by mixing presbytery, quince and oyster calligraphy at a specific mixing ratio has particularly excellent anti-obesity effect compared to the single extract.
본 발명의 목적은 노회, 모과 및 옥촉서예 추출물을 유효성분으로 포함하는 비만 예방 또는 치료용 약학 조성물을 제공하는데 있다. It is an object of the present invention to provide a pharmaceutical composition for preventing or treating obesity comprising an extract of presbytery, quince and oyster calligraphy as an active ingredient.
본 발명은 노회, 모과 및 옥촉서예 추출물을 유효성분으로 포함하는 비만 예방 또는 치료용 약학 조성물에 관한 것이다.The present invention relates to a pharmaceutical composition for preventing or treating obesity, comprising an extract of presbyopia, quince, and okchok calligraphy as an active ingredient.
상기 노회, 모과 및 옥촉서예는 1~3:0.5~2:2.5~5의 중량비로 혼합한 후 추출하며, 노회 추출물, 모과 추출물 및 옥촉서예 추출물을 1~3:0.5~2:2.5~5의 중량비로 혼합하는 것도 가능하다. 그러나, 상기 혼합 중량비 조건을 벗어나서 노회, 모과 및 옥촉서예를 혼합하는 경우 항비만 활성이 현저하게 낮아지므로 바람직하지 않다.The presbytery, quince, and okchok calligraphy examples are extracted after mixing in a weight ratio of 1 to 3: 0.5 to 2: 2.5 to 5, and the presbytery extract, quince extract, and okchok calligraphy extract of 1 to 3: 0.5 to 2: 2.5 to 5 It is also possible to mix by weight ratio. However, it is not preferable because the anti-obesity activity is remarkably lowered in the case of mixing noshoe, quince, and okchok calligraphy outside the mixing weight ratio condition.
상기 추출물은 노회, 모과 및 옥촉서예 혼합물 또는 각각의 노회, 모과 및 옥촉서예를 물, C1 내지 C4 알코올 또는 이들의 혼합용액을 용매로 하여 추출한 것이며, 상기 C1 내지 C4의 알코올은 메탄올, 에탄올, 프로판올, 이소프로판올, 부탄올 및 이소부탄올로 이루어진 군에서 선택될 수 있다. 추출시 사용되는 물, C1 내지 C4의 알코올 또는 이들의 혼합용액은 사용되는 노회, 모과 및 옥촉서예 단독 또는 혼합물 중량 대비 2~50배 부피를 사용할 수 있으며 상기 과정을 1~5회 반복하는 것도 가능하다. The extract is a mixture of presbyopia, quince and oyster calligraphy, or each presbytery, quince and oyster calligraphy extracted using water, C1 to C4 alcohol or a mixed solution thereof as a solvent, and the alcohols of C1 to C4 are methanol, ethanol, and propanol. , It may be selected from the group consisting of isopropanol, butanol and isobutanol. Water used for extraction, C1 to C4 alcohol, or a mixed solution thereof may be used alone or in a volume of 2 to 50 times the weight of a mixture of presbyopia, quince, and oyster calligraphy used, and the above process may be repeated 1 to 5 times. Do.
상기 추출물의 추출시간은 특별히 제한되는 것은 아니나, 10분 내지 1일 이내에 추출하는 것이 바람직하고, 추출방법은 통상적으로 사용되는 모든 추출방법, 예컨대, 가압 추출, 침지(냉침, 온침), 초음파 추출, 환류 추출법 등을 사용할 수 있으며, 추출용 기기로는 통상의 추출기기, 초음파분쇄추출기 또는 분획기를 이용할 수 있다. The extraction time of the extract is not particularly limited, but it is preferable to extract within 10 minutes to 1 day, and the extraction method includes all commonly used extraction methods, such as pressure extraction, immersion (cold immersion, warm needle), ultrasonic extraction, A reflux extraction method, etc. may be used, and a conventional extraction device, an ultrasonic grinding extractor, or a fractionator may be used as an extraction device.
상기 추출물은 부유하는 고체 입자를 제거하기 위하여 여과시키는 단계를 추가로 포함할 수 있다. 면, 나일론 등을 이용하여 입자를 걸러 내거나 한외여과, 냉동여과법, 원심분리법 등을 사용할 수 있으며, 식물체 분리 추출에 이용되는 공지의 방법을 단독 또는 적합하게 조합한 방법을 이용할 수 있다. The extract may further include filtering to remove suspended solid particles. Cotton, nylon, or the like may be used to filter particles, or ultrafiltration, freeze filtration, centrifugation, etc. may be used, and a method in which a known method used for separation and extraction of plants may be used alone or in an appropriate combination.
또한, 상기 추출물은 상기 추출 과정으로부터 얻은 추출액, 상기 추출액의 희석액이나 농축액, 상기 추출액을 건조하여 얻어지는 건조물, 상기 추출액의 조정제물이나 정제물, 또는 이들의 혼합물 등, 추출액 자체 및 추출액을 이용하여 형성 가능한 모든 제형의 추출물을 포함한다.In addition, the extract is formed using the extract itself and the extract, such as an extract obtained from the extraction process, a dilute or concentrate of the extract, a dried product obtained by drying the extract, a preparation or purified product of the extract, or a mixture thereof. Includes extracts of all possible formulations.
본 발명에 따른 약학 조성물은 일반적으로 사용되는 약학적으로 허용 가능한 담체와 함께 적합한 형태로 제형화될 수 있다. "약학적으로 허용 가능"이란 생리학적으로 허용되고 인간에게 투여될 때, 통상적으로 위장 장애, 현기증 등과 같은 알레르기 반응 또는 이와 유사한 반응을 일으키지 않는 조성물을 말한다. 또한, 상기 조성물은 각각 통상의 방법에 따라 산제, 과립제, 정제, 캡슐제, 현탁액, 에멀젼, 시럽, 에어로졸 등의 경구형 제형, 외용제, 좌제 및 멸균 주사용액의 형태로 제형화하여 사용될 수 있다. The pharmaceutical composition according to the present invention may be formulated in a suitable form together with a generally used pharmaceutically acceptable carrier. "Pharmaceutically acceptable" refers to a composition that is physiologically acceptable and, when administered to a human, does not usually cause an allergic reaction or similar reaction such as gastrointestinal disorders, dizziness, and the like. In addition, the compositions may be formulated and used in the form of oral dosage forms such as powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, etc., external preparations, suppositories, and sterile injectable solutions according to a conventional method.
상기 조성물에 포함될 수 있는 담체, 부형제 및 희석제로는 락토오스, 덱스트로즈, 수크로스, 소르비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 전분, 아라비아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로오스, 메틸 셀룰로오스, 미결정셀룰로오스, 폴리비닐 피롤리돈, 물, 파라옥시벤조산메틸, 파라옥시벤조산프로필, 탈크, 스테아르산마그네슘 및 광물유를 포함할 수 있으나, 이에 한정되는 것은 아니다. 제제화할 경우에는 보통 사용하는 충진제, 안정화제, 결합제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 조제된다. 경구투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형제제는 본 발명의 추출물에 적어도 하나 이상의 부형제, 예를 들면, 전분, 미결정셀룰로오스, 수크로스 또는 락토오스, 저치환도히드록시프로필셀룰로오스, 히프로멜로오스 등을 섞어 조제된다. 또한 단순한 부형제 이외에 스테아르산마그네슘, 탈크 같은 활택제들도 사용된다. 경구를 위한 액상 제제로는 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데 흔히 사용되는 단순희석제인 물, 유동파라핀 이외에 여러 가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다. 비경구 투여를 위한 제제에는 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조제제, 좌제가 포함된다. 비수성용제, 현탁용제로는 프로필렌글리콜, 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다. 좌제의 기제로는 위텝솔(witepsol), 마크로골, 트윈(tween) 61, 카카오지, 라우린지, 글리세롤, 젤라틴 등이 사용될 수 있다. 비경구 투여용 제형으로 제제화하기 위하여 상기 추출물 또는 이의 약학적으로 허용되는 염을 멸균되고/되거나 방부제, 안정화제, 수화제 또는 유화 촉진제, 삼투압 조절을 위한 염 및/또는 완충제 등의 보조제, 및 기타 치료적으로 유용한 물질과 함께 물에 혼합하여 용액 또는 현탁액으로 제조하고, 이를 앰플 또는 바이알 단위 투여형으로 제조할 수 있다.Carriers, excipients, and diluents that can be included in the composition include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum arabic, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl Cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methyl paraoxybenzoate, propyl paraoxybenzoate, talc, magnesium stearate, and mineral oil may be included, but are not limited thereto. In the case of formulation, it is prepared using diluents or excipients such as commonly used fillers, stabilizers, binders, disintegrants, and surfactants. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, and such solid preparations include at least one excipient, for example, starch, microcrystalline cellulose, sucrose or lactose, in the extract of the present invention, It is prepared by mixing low-substituted hydroxypropyl cellulose and hypromellose. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid preparations for oral use include suspensions, liquid solutions, emulsions, syrups, etc. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweetening agents, fragrances, and preservatives may be included. . Preparations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, lyophilized preparations, and suppositories. Propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate may be used as the non-aqueous solvent and the suspension. As a base for suppositories, witepsol, macrogol, tween 61, cacao butter, laurin, glycerol, gelatin, and the like may be used. In order to formulate a formulation for parenteral administration, the extract or a pharmaceutically acceptable salt thereof is sterilized and/or an adjuvant such as a preservative, a stabilizer, a hydrating agent or an emulsifying agent, a salt and/or a buffer for controlling the osmotic pressure, and other treatments It can be prepared as a solution or suspension by mixing in water with a useful substance, and it can be prepared in ampoules or vials unit dosage form.
본 발명에 개시된 추출물을 유효성분으로 포함하는 약학 조성물은 쥐, 가축, 인간 등의 포유동물에 다양한 경로로 투여될 수 있다. 투여의 모든 방식은 예상될 수 있는데, 예를 들면, 경구, 직장 또는 정맥, 근육, 피하, 자궁내 경막 또는 뇌혈관내 주사에 의해 투여될 수 있다. 투여량은 치료받을 대상의 연령, 성별, 체중, 치료할 특정 질환 또는 병리 상태, 질환 또는 병리 상태의 심각도, 투여시간, 투여경로, 약물의 흡수, 분포 및 배설률, 사용되는 다른 약물의 종류 및 처방자의 판단 등에 따라 달라질 것이다. 이러한 인자에 기초한 투여량 결정은 당업자의 수준 내에 있으며, 일반적으로 투여량은 0.01㎎/㎏/일 내지 대략 2000㎎/㎏/일의 범위이다. 더 바람직한 투여량은 1㎎/㎏/일 내지 500㎎/㎏/일이다. 투여는 하루에 한번 투여할 수도 있고, 수회 나누어 투여할 수 있다. 상기 투여량은 어떠한 면으로든 본 발명의 범위를 한정하는 것은 아니다. The pharmaceutical composition comprising the extract disclosed in the present invention as an active ingredient can be administered to mammals such as mice, livestock, and humans by various routes. All modes of administration can be expected and can be administered, for example, by oral, rectal or intravenous, intramuscular, subcutaneous, intrauterine dural or cerebrovascular injection. The dosage is the age, sex, weight of the subject to be treated, the specific disease or pathology to be treated, the severity of the disease or pathology, the time of administration, the route of administration, the absorption, distribution and excretion rate of the drug, the types of other drugs used, and the prescriber's It will depend on your judgment, etc. Dosage determination based on these factors is within the level of one of ordinary skill in the art, and dosages generally range from 0.01 mg/kg/day to approximately 2000 mg/kg/day. A more preferred dosage is from 1 mg/kg/day to 500 mg/kg/day. Administration may be administered once a day, or may be divided several times. The above dosage does not in any way limit the scope of the present invention.
또 다른 일면에 있어서, 본 발명은 노회, 모과 및 옥촉서예 추출물을 유효성분으로 포함하는 비만 예방 또는 개선용 건강기능식품에 관한 것이다. 상기 건강기능식품은 유용한 기능성을 가진 원료나 성분을 사용하여 제조 또는 가공한 식품을 지칭하는 것으로, 예를 들어 건강보조식품, 기능성 식품, 영양제, 보조제 등을 모두 포함한다. In yet another aspect, the present invention relates to a health functional food for preventing or improving obesity, comprising an extract of presbytery, quince and okchok calligraphy as an active ingredient. The health functional food refers to a food manufactured or processed using raw materials or ingredients having useful functionality, and includes, for example, health supplements, functional foods, nutritional supplements, and supplements.
상기 추출물은 전체 건강기능식품 총 중량에 대하여 바람직하게는 0.001중량% 내지 50중량%, 더 바람직하게는 0.001중량% 내지 30중량%, 가장 바람직하게는 0.001중량% 내지 10중량%로 하여 첨가될 수 있다. The extract may be added in an amount of preferably 0.001% to 50% by weight, more preferably 0.001% to 30% by weight, and most preferably 0.001% to 10% by weight based on the total weight of the health functional food. have.
본 발명의 건강기능식품은 정제, 캡슐제, 환제 또는 액제 등의 형태를 포함하며, 본 발명 추출물을 첨가할 수 있는 식품으로는, 예를 들어, 각종 식품류, 음료, 껌, 차, 비타민 복합제 등이 있다.The health functional food of the present invention includes the form of tablets, capsules, pills or liquids, and foods to which the extract of the present invention can be added include, for example, various foods, beverages, gums, teas, vitamin complexes, etc. There is this.
본 발명은 노회, 모과 및 옥촉서예 추출물을 유효성분으로 포함하는 비만 예방 또는 치료용 약학 조성물에 관한 것이다. 상기 추출물은 노회, 모과 및 옥촉서예 단독 추출물에 비해 지방축적을 저해하는 효과가 현저히 우수하고 비만이 유도된 동물모델에서 체중 감소, 체지방 감소 및 혈중 중성지방량 감소 효과가 우수하므로, 비만 예방 또는 치료용 약학 조성물로 유용하게 사용될 수 있다.The present invention relates to a pharmaceutical composition for preventing or treating obesity, comprising an extract of presbyopia, quince, and okchok calligraphy as an active ingredient. The extract is significantly superior in the effect of inhibiting fat accumulation compared to the single extracts of nohoe, quince and okchok calligraphy, and has excellent effect of reducing weight, reducing body fat, and reducing blood triglyceride in an animal model in which obesity is induced. It can be usefully used as a pharmaceutical composition.
도 1은 3T3-L1 세포에서 본 발명 실시예 및 비교예의 처리에 따른 지방구 축적 변화를 Oil red O 염색법으로 확인한 결과이다.
도 2는 HepG2 세포에서 본 발명 실시예 및 비교예의 처리에 따른 중성지방량 변화를 확인한 결과이다.
도 3은 비만이 유도된 동물모델에서 본 발명 실시예 및 비교예의 처리에 따른 내장 지방 및 복부 지방량 변화를 확인한 결과이다.
도 4는 비만이 유도된 동물모델에서 본 발명 실시예 및 비교예의 처리에 따른 혈중 중성지방량 변화를 확인한 결과이다.1 is a result of confirming the change in fat cell accumulation according to the treatment of Examples and Comparative Examples of the present invention in 3T3-L1 cells by Oil red O staining.
2 is a result of confirming the change in triglyceride mass according to the treatment of Examples and Comparative Examples of the present invention in HepG2 cells.
3 is a result of confirming the change in the amount of visceral fat and abdominal fat according to the treatment of Examples and Comparative Examples of the present invention in an obesity-induced animal model.
4 is a result of confirming the change in the amount of triglyceride in blood according to the treatment of Examples and Comparative Examples of the present invention in an animal model in which obesity is induced.
이하 본 발명의 바람직한 실시예를 상세히 설명하기로 하였다. 그러나 본 발명은 여기서 설명되는 실시예에 한정되지 않고 다른 형태로 구체화될 수도 있다. 오히려, 여기서 소개되는 내용이 철저하고 완전해지고, 당업자에게 본 발명의 사상을 충분히 전달하기 위해 제공하는 것이다.Hereinafter, a preferred embodiment of the present invention will be described in detail. However, the present invention is not limited to the embodiments described herein and may be embodied in other forms. Rather, the content introduced herein becomes thorough and complete, and is provided to sufficiently convey the spirit of the present invention to those skilled in the art.
<실시예 1. 노회, 모과 및 옥촉서예를 포함하는 추출물의 제조><Example 1. Preparation of extracts containing presbytery, quince and oyster calligraphy>
노회(경동시장) 200g, 모과(경동시장) 100g 및 옥촉서예(경동시장) 350g을 혼합한 다음 95% 에탄올 수용액 13ℓ를 더하여, 20℃에서 200rpm으로 72시간 동안 교반 추출하였다. 상기 과정으로부터 얻은 추출액을 여과하여 여과액 얻고, 이를 회전진공농축기로 40℃에서 감압 농축한 다음 동결 건조하여 분말 형태의 노회, 모과 및 옥촉서예 추출물 약 93g(14.3% 수율)을 얻었다. 상기 과정으로부터 얻은 동결건조 분말은 사용전까지 -80℃에서 보관하였다.200 g of nohoe (Gyeongdong market), 100 g of Chinese quince (Gyeongdong market), and 350 g of Okchok calligraphy (Gyeongdong market) were mixed, and then 13ℓ of 95% ethanol aqueous solution was added, followed by stirring and extraction at 20°C at 200 rpm for 72 hours. The extract obtained from the above process was filtered to obtain a filtrate, which was concentrated under reduced pressure at 40° C. with a rotary vacuum concentrator, and then freeze-dried to obtain about 93 g (14.3% yield) of powdery extracts of Noshoe, Chinese quince and Okchok Calligraphy. The freeze-dried powder obtained from the above process was stored at -80°C until use.
<비교예 1. 노회 추출물의 제조><Comparative Example 1. Preparation of noshoe extract>
상기 실시예 1과 동일하게 제조하되 노회 200g, 모과 100g 및 옥촉서예 350g을 혼합하는 대신 노회 650g을 단독으로 사용하여 비교대상 노회 추출물을 얻었다.In the same manner as in Example 1, but instead of mixing 200 g of noshoe, 100 g of quince, and 350 g of Okcheok calligraphy, 650 g of noshoe was used alone to obtain a comparison target noshoe extract.
<비교예 2. 모과 추출물의 제조><Comparative Example 2. Preparation of quince extract>
상기 실시예 1과 동일하게 제조하되 노회 200g, 모과 100g 및 옥촉서예 350g을 혼합하는 대신 모과 650g을 단독으로 사용하여 비교대상 모과 추출물을 얻었다.It was prepared in the same manner as in Example 1, but instead of mixing 200 g of noshoe, 100 g of quince, and 350 g of quince, 650 g of quince was used alone to obtain a quince extract for comparison.
<비교예 3. 옥촉서예 추출물의 제조><Comparative Example 3. Preparation of extract of Okchok calligraphy>
상기 실시예 1과 동일하게 제조하되 노회 200g, 모과 100g 및 옥촉서예 350g을 혼합하는 대신 옥촉서예 650g을 단독으로 사용하여 비교대상 옥촉서예 추출물을 얻었다.It was prepared in the same manner as in Example 1, but instead of mixing 200 g of noshoe, 100 g of quince, and 350 g of Okchok calligraphy, 650g of Okchok calligraphy was used alone to obtain an extract of Okchok calligraphy for comparison.
<실험예 1. 지방세포에서의 항비만 효과 확인><Experimental Example 1. Confirmation of anti-obesity effect in adipocytes>
실험예 1-1. 지방 축적 억제 효과 확인Experimental Example 1-1. Confirmation of fat accumulation inhibitory effect
지방세포인 3T3-L1 세포에서 본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물의 처리에 따른 지방 축적 억제 효과를 Oil red O 염색법으로 확인하였다.In the adipocyte 3T3-L1 cells, the effect of inhibiting fat accumulation according to the treatment of the extracts of Presbyopia, Chinese quince and Okchokseoye of Example 1 of the present invention was confirmed by Oil red O staining.
3T3-L1 세포(한국세포주은행, Korean cell line bank, KCLB)는 DMEM(Dulbecco's modified eagle medium)에 10% FCS(Fetal calf serum) 및 1% 페니실린-스트렙토마이신(Penicillin-Streptomycin)이 첨가된 배지를 사용하여 37℃ 및 5% CO2 조건의 배양기에서 배양하였다. 3T3-L1 cells (Korean cell line bank, KCLB) are DMEM (Dulbecco's modified eagle medium) in a medium containing 10% FCS (Fetal calf serum) and 1% Penicillin-Streptomycin (Penicillin-Streptomycin). And cultured in an incubator under conditions of 37° C. and 5% CO 2 .
지방세포로의 분화를 위해 3T3-L1 세포를 6웰 플레이트에 5×105세포/웰로 분주하고, 세포가 100% 컨플루언트(confluent) 상태가 될 때까지 이틀에 한번씩 배지를 교체해 주면서 배양하였다. 100% 컨플루언트 상태가 확인된 2일 후 0.5mM IBMX(3-isobutyl-1-methylxanthine), 1μM 덱사메타손(dexamethasone), 1㎍/㎖ 인슐린 및 10% FBS(Fetal bovine serum)를 포함하는 DMEM 배지에서 2일 동안 배양함으로써 지방세포 분화를 개시하였다.For differentiation into adipocytes, 3T3-L1 cells were dispensed into a 6-well plate at 5×10 5 cells/well, and cultured while changing the medium once every two days until the cells became 100% confluent. DMEM medium containing 0.5mM IBMX (3-isobutyl-1-methylxanthine), 1 μM dexamethasone, 1 μM/mL insulin and 10% Fetal bovine serum (FBS) 2 days after the 100% confluent state was confirmed Adipocyte differentiation was initiated by culturing at for 2 days.
분화 유도를 위해 1㎍/㎖ 인슐린 및 10% FBS를 포함하는 DMEM 배지로 교환하면서 진행하였으며, 육안으로 분화가 완료되면 50% 에탄올 수용액에 100㎍/㎖의 농도로 용해된 실시예 또는 비교예의 추출물을 세포에 처리하여 48시간 동안 배양하였다.In order to induce differentiation, an extract of Example or Comparative Example dissolved in a concentration of 100 µg/ml in 50% ethanol aqueous solution when differentiation was completed with the naked eye when the differentiation was completed with DMEM medium containing 1µg/ml insulin and 10% FBS. Was treated on the cells and cultured for 48 hours.
48시간 후 3T3-L1 세포의 배양액을 제거하고 인산완충용액(phosphate buffered saline)으로 세척한 후 10% 포르말린 용액을 이용하여 37℃ 배양기에서 1시간 동안 세포를 고정시켰다. 이후, 포르말린 용액을 제거하고 1차 증류수로 세척한 다음 Oil red O 염색용액을 넣고 상온에서 2시간 동안 염색하였다. 염색 후 증류수로 세척하고 60% 이소프로판올에 녹인 다음 500㎚ 파장에서 흡광도를 분석하였으며, 흡광도 분석 결과로부터 지방구 축적률을 계산하여 도 1에 나타내었다. After 48 hours, the culture medium of 3T3-L1 cells was removed, washed with phosphate buffered saline, and then the cells were fixed in an incubator at 37° C. for 1 hour using 10% formalin solution. Thereafter, the formalin solution was removed, washed with primary distilled water, and then oil red O dyeing solution was added and dyed at room temperature for 2 hours. After dyeing, washing with distilled water and dissolving in 60% isopropanol, the absorbance was analyzed at a wavelength of 500 nm, and the fat globule accumulation rate was calculated from the absorbance analysis result and shown in FIG. 1.
도 1을 참고하면, 본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물(100㎍/㎖ 처리)은 비교예 1 내지 3과 같이 단독 추출물(100㎍/㎖ 처리)을 지방세포에 처리하는 것에 비해 지방구 축적 억제 효과가 우수하였다. Referring to FIG. 1, the extracts (100 µg/ml treatment) of Nohoe, Chinese quince and Okchok-seoye of Example 1 of the present invention were applied to the adipocytes with a single extract (100µg/ml treatment) as in Comparative Examples 1 to 3. In comparison, the effect of inhibiting fat cell accumulation was excellent.
특히 본 발명자들은 상기 실험을 수행하기 전 다양한 배합비로 노회, 모과 및 옥촉서예를 혼합 추출하고 지방구 축적률을 확인하였으며, 그 결과 상기 실시예 1과는 다르게 노회, 모과 및 옥촉서예 중 1종 이상의 성분이 포함되지 않는 추출물이거나 또는 노회, 모과 및 옥촉서예의 혼합비가 1~3:0.5~2:2.5~5를 벗어나서 옥촉서예 기준으로 노회 및 모과가 4배 이상 더 포함되거나 또는 덜 포함되는 경우, 혼합에 의한 상승효과가 낮았음을 확인하였다.Particularly, the present inventors mixed and extracted presbytery, quince, and okchok calligraphy at various mixing ratios before carrying out the above experiment, and confirmed the fat globule accumulation rate.As a result, unlike in Example 1, at least one of presbytery, quince and okchok calligraphy If the extract does not contain any ingredients or the mixing ratio of presbytery, quince and quince is out of 1~3:0.5~2:2.5~5 and contains more than 4 times more or less presbytery and quince based on quince It was confirmed that the synergistic effect by was low.
이로부터, 비만 예방 또는 치료시 노회, 모과 및 옥촉서예 단독 추출물을 사용하는 것보다는 본 발명과 같이 특정 혼합비로 노회, 모과 및 옥촉서예를 혼합하여 사용하는 것이 항비만 효과를 나타내는데 가장 효과적임을 알 수 있었다.From this, it can be seen that the use of a mixture of presbytery, quince and oyster calligraphy at a specific mixing ratio as in the present invention is the most effective in showing the anti-obesity effect, rather than using the single extract of presbytery, quince and quince calligraphy when obesity prevention or treatment. there was.
실험예 1-2. 중성지방 축적 억제 효과 확인Experimental Example 1-2. Checking the effect of inhibiting the accumulation of triglycerides
본 발명 노회, 모과 및 옥촉서예 추출물의 처리에 따른 중성지방 축적 억제 효과를 확인하기 위해, HepG2 세포에서 중성지방량을 측정하였다.In order to confirm the effect of inhibiting the accumulation of triglycerides according to the treatment of the present invention presbytery, Chinese quince, and Okchokseoye extract, the amount of triglyceride in HepG2 cells was measured.
먼저, HepG2 세포를 4×105세포/웰로 분주하고 24시간 배양한 다음 2mM 팔미트산을 처리하여 24시간 추가 배양하였다. 이후, 100㎍/㎖ 농도로 실시예 또는 비교예가 포함된 배지로 교환한 다음 24시간 배양하였다. 배양 후 배양액을 제거하고 세포를 수거하여 5% Triton X-100으로 세포를 용해하였다. 세포 용해물을 원심분리하여 상등액을 얻은 다음, 중성지방측정 키트(Sigma-aldrich, MO, USA)를 사용하여 중성지방량을 정량하고 그 결과를 도 2에 나타내었다.First, HepG2 cells were aliquoted into 4×10 5 cells/well, cultured for 24 hours, and then treated with 2mM palmitic acid and cultured for additional 24 hours. Thereafter, it was exchanged with a medium containing Examples or Comparative Examples at a concentration of 100 μg/ml and cultured for 24 hours. After incubation, the culture medium was removed, the cells were collected, and the cells were lysed with 5% Triton X-100. The cell lysate was centrifuged to obtain a supernatant, and then the amount of triglyceride was quantified using a triglyceride measurement kit (Sigma-aldrich, MO, USA), and the results are shown in FIG. 2.
도 2를 살펴보면, 본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물은 비교예 1 내지 3과 같이 단독 추출물을 처리하는 것에 비해 2배 이상으로 중성지방량이 감소함을 알 수 있었다. Referring to FIG. 2, it was found that the amount of triglycerides was reduced by two or more times compared to treatment with a single extract as in Comparative Examples 1 to 3 in the Nohoe, Chinese quince, and Okchokseoye extract of Example 1 of the present invention.
따라서, 상기 결과로부터 본 발명 노회, 모과 및 옥촉서예 추출물은 지방 축적 억제 효과 및 중성지방량 억제 효과가 우수하므로, 비만 예방 또는 치료용 조성물로 유용하게 사용할 수 있음을 알 수 있었다.Therefore, from the above results, it was found that the extracts of the present invention presbytery, quince and oyster seeds have excellent effects of inhibiting fat accumulation and suppressing triglycerides, and thus can be usefully used as a composition for preventing or treating obesity.
<< 실험예Experimental example 2. 동물모델에서의 2. In animal models 항비만Anti-obesity 효과 확인> Check the effect>
실험예 2-1. 비만 동물의 체중, 내장 지방 및 복부 지방량 변화 확인 Experimental Example 2-1. Check changes in weight, visceral fat and abdominal fat in obese animals
비만 동물 구축을 위해 5주령 수컷 C57BL/6J 마우스(오리엔트바이오, Korea)를 온도 22~25℃, 상대습도 50~60%, 명암주기 12시간, 조도 200~300 LUX가 유지되는 동물시험시설에서 일주일간 순화시켰다. 마우스용 폴리카보네이트 상자에 2마리씩 사육하고, 순화기간인 1주일 동안 일반사료((주)퓨리나, Korea)와 음수는 자유식이 하였다.To build obese animals, 5-week-old male C57BL/6J mice (Orient Bio, Korea) work in an animal testing facility that maintains a temperature of 22~25℃, a relative humidity of 50~60%, a light and dark cycle of 12 hours, and an illuminance of 200~300 LUX. Purified for a week. Two animals were reared in polycarbonate boxes for mice, and normal feed (Purina Co., Korea) and drinking water were freely fed for one week during the acclimatization period.
순화 후 평균 체중이 유사하도록 군당 16마리씩 군 분리하였으며 정상군은 일반식이(10% kcal fat diet, Research Diets Inc. NJ, USA)를 실시하였고, 대조군, 실시예 1 및 비교예 3은 고지방식이(60% kcal fat diet(Research Diets Inc. NJ, USA)를 8주간 자유식이 하였다. After acclimatization, 16 animals were separated per group so that the average weight was similar, and the normal group was subjected to a general diet (10% kcal fat diet, Research Diets Inc. NJ, USA), and the control group, Example 1, and Comparative Example 3 were fed a high fat diet. (60% kcal fat diet (Research Diets Inc. NJ, USA) was freely fed for 8 weeks.
정상군은 일반식이를 섭취시킨 날부터 0.5% CMC(carboxymethylcellulose) 용액을 56일간 매일 1회씩 총 56회 경구 투여하였고, 대조군은 고지방식이를 섭취시킨 날부터 0.5% CMC 용액을 56일간 매일 1회씩 총 56회 경구 투여하였으며, 실시예 1 또는 비교예 3은 고지방식이를 섭취시킨 날부터 0.5% CMC 용액에 상기 실시예 1 또는 비교예 3 추출물을 각각 투여농도 500㎎/㎏가 되도록 매일 조제하여 56일간 매일 1회씩 총 56회 경구 투여하였다. In the normal group, 0.5% CMC (carboxymethylcellulose) solution was administered orally once a day for 56 days for a total of 56 times from the day of ingestion, and the control group received 0.5% CMC solution once daily for 56 days from the day of ingestion of the high fat diet. A total of 56 times were administered orally, and in Example 1 or Comparative Example 3, the extract of Example 1 or Comparative Example 3 was prepared daily in a 0.5% CMC solution from the day of ingesting a high fat diet so that the concentration of each of the extracts was 500 mg/kg. A total of 56 times were administered orally once daily for 56 days.
비만 동물의 체중은 매주 2회 측정하였으며, 내장 지방 및 복부 지방의 무게는 실험 마지막날 투여 후 저녁부터 15시간 절식한 다음 동물을 희생시켜 내장지방 및 복부지방을 분리하고 그 무게를 측정하였다. 비만 동물의 체중 변화량은 표 1에 나타내었으며, 내장지방 및 복부지방 변화는 도 3에 나타내었다.The weight of obese animals was measured twice a week, and the weight of visceral fat and abdominal fat was measured after fasting for 15 hours from the evening after administration on the last day of the experiment, and the animals were sacrificed to separate visceral fat and abdominal fat, and their weights were measured. Changes in weight of obese animals are shown in Table 1, and changes in visceral fat and abdominal fat are shown in FIG. 3.
+500㎎/㎏ 실시예 1High fat diet +0.5% CMC
+500 mg/kg Example 1
+500㎎/㎏ 비교예 3High fat diet +0.5% CMC
+500mg/kg Comparative Example 3
표 1 및 도 3을 살펴보면, 비만이 유도된 동물모델에 본 발명 실시예 1을 투여하는 경우, 대조군 또는 비교예 3을 투여하는 경우에 비해 체중, 내장 지방 및 복부 지방량이 유의적으로 감소하였다. Looking at Tables 1 and 3, when administering Example 1 of the present invention to an animal model in which obesity was induced, the amount of body weight, visceral fat, and abdominal fat was significantly reduced compared to the case of administering the control or Comparative Example 3.
이러한 결과로부터, 본 발명과 같이 특정 혼합비로 혼합한 노회, 모과 및 옥촉서예 추출물은 개별 생약 중 가장 효과가 우수했던 옥촉서예 추출물을 단독으로 투여하는 것 보다 항비만 효과가 훨씬 더 우수한 조성물임을 알 수 있었다. From these results, it can be seen that the presbytery, quince, and okchok calligraphy extracts mixed at a specific mixing ratio as in the present invention have a much better anti-obesity effect than the single administration of the extract of Okchokseoye, which was the most effective among individual herbal medicines. there was.
실험예 2-2. 비만 동물의 혈중 중성지방량 변화 확인Experimental Example 2-2. Confirmation of changes in blood triglycerides in obese animals
상기 실험예 2-1과 같이 동물모델에 정상군, 대조군, 실시예 1 또는 비교예 3을 56일간 매일 1회씩 총 56회 경구 투여하고, 마지막 시험물질 투여일 저녁부터 15시간 절식 후 0.4㎖/head 용량으로 콘 오일(corn oil)을 경구 투여하였다. 콘 오일 투여 전(0시간), 투여 후 2, 4, 6시간 후에 동물모델 꼬리에서 채혈하여 중성지방측정기(Accutrend plus, Roche, Switzerland)로 중성지방을 측정하고 이를 도 4에 나타내었다. As in Experimental Example 2-1, the normal group, the control group, Example 1 or Comparative Example 3 were orally administered once a day for 56 days for 56 days for a total of 56 times, and after fasting for 15 hours from the evening of the last test substance administration, 0.4 ml/ Corn oil was orally administered as a head dose. Before corn oil administration (0 hour), 2, 4, 6 hours after administration, blood was collected from the tail of an animal model, and triglycerides were measured with a triglyceride meter (Accutrend plus, Roche, Switzerland), and this is shown in FIG. 4.
도 4를 참고하면, 비만이 유도된 동물모델에 본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물을 투여하는 경우, 대조군을 투여하는 경우에 비해 혈중 중성지방량이 100㎎/㎗ 이상 유의적으로 감소한 것을 확인할 수 있었다. 그러나 비교예 3의 옥촉서예 단독 추출물을 비만이 유도된 동물모델에 투여하는 경우 본 발명 실시예 1과는 다르게 대조군 대비 유의적인 혈중 중성지방량 감소 효과가 없었다.Referring to Figure 4, when administering the presbytery, Chinese quince, and Okchokseoye extract of Example 1 of the present invention to an animal model in which obesity is induced, the amount of triglyceride in blood was significantly greater than 100 mg/dL compared to the case of administering the control group. It was confirmed that it decreased. However, in the case of administering the extract of Okchokseo Example of Comparative Example 3 to an animal model in which obesity was induced, unlike Example 1 of the present invention, there was no significant blood triglyceride reduction effect compared to the control group.
따라서 본 발명과 같이 노회, 모과 및 옥촉서예를 특정 혼합비로 혼합하여 사용하는 것이 비만 치료 효과가 가장 우수한 조성물임을 알 수 있었다. Therefore, it was found that the use of presbyopia, quince, and okchok calligraphy at a specific mixing ratio, as in the present invention, has the most excellent effect on treating obesity.
<제제예 1. 정제의 제조><Formulation Example 1. Preparation of tablets>
본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물 20g을 각각 락토오스 175.9g, 감자전분 180g 및 콜로이드성 규산 32g과 혼합하였다. 이 혼합물에 10% 젤라틴 용액을 첨가시킨 후, 분쇄해서 14 메쉬체를 통과시켰다. 이것을 건조시키고 여기에 감자전분 160g, 활석 50g 및 스테아린산 마그네슘 5g을 첨가해서 얻은 혼합물을 정제로 만들었다. 20 g of the extracts of Noshoe, Chinese quince and Okchok calligraphy of Example 1 of the present invention were mixed with 175.9 g of lactose, 180 g of potato starch, and 32 g of colloidal silicic acid, respectively. After adding a 10% gelatin solution to this mixture, it was pulverized and passed through a 14 mesh sieve. This was dried, and 160 g of potato starch, 50 g of talc and 5 g of magnesium stearate were added thereto, and the resulting mixture was made into tablets.
<제제예 2. 캡슐제의 제조><Formulation Example 2. Preparation of capsules>
본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물 100㎎, 옥수수전분 100㎎, 유당 100㎎ 및 스테아린산 마그네슘 2㎎을 혼합한 후 통상의 캡슐제 제조방법에 따라 상기의 성분을 혼합하고 젤라틴 캡슐에 충전하여 캡슐제를 제조하였다.After mixing 100 mg of presbyopia, quince and oyster calligraphy extract of Example 1 of the present invention, 100 mg of corn starch, 100 mg of lactose and 2 mg of magnesium stearate, the above ingredients were mixed according to a conventional capsule preparation method, and then in a gelatin capsule. Filled to prepare a capsule.
<제제예 3. 주사제의 제조><Formulation Example 3. Preparation of injection>
본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물 1g, 염화나트륨 0.6g 및 아스코르브산 0.1g을 증류수에 용해시켜서 100㎖를 만들었다. 이 용액을 병에 넣고 20℃에서 30분간 가열하여 멸균시켰다.1 g of the extract of Noshoe, Chinese quince, and Okchok calligraphy of Example 1, 0.6 g of sodium chloride and 0.1 g of ascorbic acid were dissolved in distilled water to make 100 ml. This solution was put in a bottle and sterilized by heating at 20° C. for 30 minutes.
<제제예 4. 건강기능식품의 제조><Formulation Example 4. Preparation of health functional food>
본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물 20g, 비타민 혼합물 적량, 비타민 A 아세테이트 70㎍, 비타민 E 1.0㎎, 비타민 B1 0.13㎎, 비타민 B2 0.15㎎, 비타민 B6 0.5㎎, 비타민 B12 0.2㎍, 비타민 C 10㎎, 비오틴 10㎍, 니코틴산아미드 1.7㎎, 엽산 50㎍, 판토텐산 칼슘 0.5㎎, 무기질 혼합물 적량, 황산제1철 1.75㎎, 산화아연 0.82㎎, 탄산 마그네슘 25.3㎎, 제1인산칼륨 15㎎, 제2인산칼슘 55㎎, 구연산칼륨 90㎎, 탄산칼슘 100㎎, 염화마그네슘 24.8㎎을 섞어 과립으로 제조하였으나, 용도에 따라 다양한 제형으로 변형시켜 제조할 수 있다. 또한, 상기의 비타민 및 미네랄 혼합물의 조성비를 임의로 변형 실시하여도 무방하며, 통상의 건강기능식품 제조방법에 따라 상기의 성분을 혼합하여 제조할 수 있다.Presbytery of the present invention Example 1, quince and oyster extract 20g, vitamin mixture appropriate amount, vitamin A acetate 70 ㎍, vitamin E 1.0 mg, vitamin B1 0.13 mg, vitamin B2 0.15 mg, vitamin B6 0.5 mg, vitamin B12 0.2 ㎍,
<< 제제예Formulation example 5. 건강기능성 음료의 제조> 5. Manufacturing of health functional beverages>
본 발명 실시예 1의 노회, 모과 및 옥촉서예 추출물 1g, 구연산 0.1g, 프락토올리고당 100g, 정제수 900g을 섞어 통상의 음료 제조방법에 따라 교반, 가열, 여과, 살균, 냉장하여 음료를 제조하였다.A beverage was prepared by mixing 1 g of an extract of Noshoe, Chinese quince and oyster Calligraphy Example 1 of the present invention, 0.1 g of citric acid, 100 g of fructooligosaccharide, and 900 g of purified water, followed by stirring, heating, filtering, sterilization, and refrigeration according to a conventional beverage preparation method.
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