KR101713557B1 - Pharmaceutical composition comprising a pharbitidis semen or a mixture of pharbitidis semen extract and corydalis turtschaninovii extract for preventing and treating cardiovascular disease - Google Patents
Pharmaceutical composition comprising a pharbitidis semen or a mixture of pharbitidis semen extract and corydalis turtschaninovii extract for preventing and treating cardiovascular disease Download PDFInfo
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- KR101713557B1 KR101713557B1 KR1020150051766A KR20150051766A KR101713557B1 KR 101713557 B1 KR101713557 B1 KR 101713557B1 KR 1020150051766 A KR1020150051766 A KR 1020150051766A KR 20150051766 A KR20150051766 A KR 20150051766A KR 101713557 B1 KR101713557 B1 KR 101713557B1
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Abstract
본 발명은 흑축 추출물 또는 흑축과 현호색 혼합물의 추출물 또는 흑축 추출물과 현호색 추출물 혼합물을 유효성분으로 함유하는 고혈압 예방 또는 치료용 약학적 조성물에 관한 것이다. 본 발명의 여러 구현예에 따르면, 본 발명의 흑축 추출물 또는 흑축과 현호색 혼합물의 추출물 또는 흑축 추출물과 현호색 추출물 혼합물은 ACE(안지오텐신 전환효소)를 저해함으로써 안지오텐신 전환효소의 작용으로 발생하는 혈압상승을 효과적으로 억제할 뿐만 아니라, 인체에 대한 안전성이 높으므로 심혈관계 질환, 즉, 고혈압 또는 고혈압성 심장질환의 예방 및 치료용 의약품 또는 건강기능식품으로 유용하게 이용될 수 있다.
The present invention relates to a pharmaceutical composition for the prevention or treatment of hypertension, which comprises as an active ingredient an extract of black shafts or a mixture of black shafts and pristine color mixtures or a mixture of black shafts and prunus extract. According to various embodiments of the present invention, the black shark extract or the mixture of the black shark and the pale color mixture or the mixture of the black shark extract and the pale color extract of the present invention inhibits ACE (angiotensin converting enzyme), thereby effectively increasing the blood pressure caused by the action of angiotensin converting enzyme It is useful as a medicament for preventing or treating cardiovascular diseases, that is, hypertension or hypertensive heart disease, or a health functional food.
Description
본 발명은 흑축 추출물 또는 흑축 추출물과 현호색 추출물 혼합물을 유효성분으로 함유하는 심혈관계 질환 예방 또는 치료용 약학적 조성물에 관한 것이다.
The present invention relates to a pharmaceutical composition for the prevention or treatment of cardiovascular diseases, which comprises a black shark extract or a mixture of a black shark extract and a colorless extract as an active ingredient.
심혈관계 질환은 한국 성인의 사망원인 중 암 다음으로 흔한 사망원인이며, 고혈압은 심혈관질환의 주요 위험인자로서 뇌졸중, 심근경색증, 울혈성 심부전, 신장병, 말초혈관질환과 같은 치명적인 질환을 유발하는 질병이다. Cardiovascular disease is the second most common cause of death after cancer among Korean adults. Hypertension is a major risk factor for cardiovascular disease and is a disease that causes fatal diseases such as stroke, myocardial infarction, congestive heart failure, kidney disease, and peripheral vascular disease .
고혈압은 뇌졸중 발생의 약 80%를 차지하는 허혈성 뇌졸중의 교정 가능한 위험 인자들 중 가장 중요하면서 잘 알려진 인자로 수축기 혈압은 115 mmHg 이상에서 20 mmHg 증가할 때마다, 그리고 이완기 혈압은 75 mmHg 이상에서 10 mmHg 증가할 때마다 뇌졸중의 발생률이 2배씩 증가한다. 또한, 고혈압은 심근경색, 심부전 및 뇌졸중의 발생과 밀접한 관계가 있으며, 수축기 혈압이 20 mmHg씩, 이완기 혈압이 10 mmHg씩 증가할 때마다 심혈관계질환의 발병률은 2배 증가한다고 알려져 있다.
Hypertension is the most important and well-known factor among the correctable risk factors for ischemic stroke, which accounts for about 80% of strokes. Systolic blood pressure increases from 20 mmHg above 115 mmHg and diastolic blood pressure increases from 10 mmHg above 75 mmHg The incidence of stroke increases by two times with each increase. Hypertension is also closely related to the incidence of myocardial infarction, heart failure, and stroke. It is known that the incidence of cardiovascular disease is doubled every 20 mmHg of systolic blood pressure and 10 mmHg of diastolic blood pressure.
고혈압 치료를 생활습관 개선과 약물 요법으로 구분할 수 있다. 생활습관을 교정하는 생활 요법에는 식염 제한, 비만한 체중감량, 음주 제한, 운동 요법, 금연, 과일 및 채소 섭취 증대, 콜레스테롤 및 포화지방산 섭취 제한 등이 있다. 생활 요법은 혈압을 강화시킬 뿐 아니라 강압제의 작용을 증강시키고 심혈관 질환이나 위험인자의 합병을 예방하는 효과도 있어 모든 환자를 대상으로 실시한다. 생활 습관 개선이 기본적 치료이지만 목표 혈압에 도달하지 못하는 경우가 많아 대부분 약물 요법과의 병행이 필요하다.Hypertension treatment can be divided into lifestyle improvement and drug therapy. Lifestyle practices that correct lifestyle include salt restriction, obesity weight loss, alcohol restriction, exercise therapy, smoking cessation, increased fruit and vegetable intake, and restriction of cholesterol and saturated fatty acid intake. Lifestyle therapy not only strengthens blood pressure, but also enhances the action of coercive agents and prevents the complications of cardiovascular disease or risk factors. Improvement of lifestyle is a basic treatment but often does not reach the target blood pressure, and it is necessary to be concurrent with most pharmacotherapy.
고혈압의 치료를 위해 현재 많은 항고혈압제가 개발되어 사용되고 있으며 작용기전과 작용점에 따라 이뇨제, 교감신경계 작용약물(α,2-아드레날린성 길항제, β-아드레날린성 길항제), 혈관확장제, 칼슘 채널 길항제(calcium channel blockers), 안지오텐신 전환 효소(ACE, angiotensin converting enzyme) 저해제 등으로 분류된다(Mann, SJ., Neurogenic essential hypertension revisited: The case for incresed clinical and research attention, American Journal of Hypertension, 16, pp.881-888, 2003; Escobales, N., Crespo, MJ., Oxidative-nitrosative stress in hypertension, Current Vascular Pharmachology, 3, pp.231-246, 2005).Many antihypertensive agents have been developed and used for the treatment of hypertension. Depending on the mechanism of action and the point of action, diuretics, sympathomimetics (α, 2-adrenergic antagonist, β-adrenergic antagonist), vasodilator, calcium channel antagonist channel blockers and angiotensin converting enzyme (ACE) inhibitors (Mann, SJ., Neurogenic essential hypertension revisited: The case for incresed clinical and research attention, American Journal of Hypertension, 16, Escobales, N., Crespo, MJ., Oxidative-nitrosative stress in hypertension, Current Vascular Pharmacology, 3, pp. 231-246, 2005).
그러나 여전히 부작용이 적으면서, 고혈압을 치료할 수 있는 새로운 약물이 요구되고 있는 실정이다.
However, there is still a need for new drugs that can treat hypertension, with few side effects.
한편, 현호색은 양귀비과의 들현호색과 그 밖의 동속식물의 덩이줄기로, 베르베린(Berberine)과 1-카나딘(1-Canadine), 프로토핀(Protopine), 1-테트라히드로코프티신(1-Tetrahydrocoptisine)을 함유하고, 혈과 기의 순환을 모두 용이하게 하는 약재로 혈이나 기가 막힌 증상에 동반되는 통증에 대하여 기와 혈의 순환을 용이하게 하여 진통(Analgesics), 진정(Sedatives), 진경(Antispasmodics)작용을 하며 위궤양억제 등의 약리작용을 가지고 있다. On the other hand, the pale color is the tubercle of poppies and other inbred plants. Berberine, 1-Canadine, Protopine, 1-Tetrahydrocoptisine, It is a medicinal substance that facilitates the circulation of the blood and the circulation. It facilitates the circulation of the tile and blood against the pain accompanying the blood or gagged symptoms, so that the analgesics, sedatives, antispasmodics And has a pharmacological effect such as inhibition of gastric ulcer.
따라서 현호색은 한방에서 정혈약, 진통약, 진경약으로서 지혈, 항궤양 등에 사용되며, 신경 자극으로 몸이 쑤시고 아프게 느껴지는 동통 즉, 복통, 요통, 위통, 두통 등에 처방되고 있다. 몸에 혈액 순환이 잘 이루어지지 못하여 생기는 월경불순이나 월경통에도 현호색이 처방되고 있다(김대근 외, 본초생약학, 신일상사, pp.274-275, 2005).Therefore, color is used in the oriental medicine, analgesic medicine, antiepileptic medicine as antiepileptic medicine, anti-ulcer, etc. It is prescribe to the pain which the body nurses and the pain felt by the nerve stimulation, that is, abdominal pain, back pain, stomach pain and headache. The blood circulation in the body does not work well due to menstrual irregularities and dysmenorrhoea is prescribed in the color of the body (Kim Dae Keun et al., Hoko Shigakusha, Shinil Sangsaja, pp.274-275, 2005).
또한, 흑축(견우자)(黑丑, Pharbitidis Semen)은 나팔꽃(Pharbitis nil choisy)(메꽃과 convolvulaceae)의 씨를 말하는 것으로 한방과 민간에서 사하축수, 거적살충, 수종창만, 이변불통, 습열적체, 대변비결, 충적복통, 소종, 복부팽만, 변비 등에 사용하였다. 흑축에는 지방유 약 11% 및 수지성 배당체인 파비틴(pharbitin) 2%를 함유하고, 사하작용, 이뇨작용 및 살충작용을 가진다고 알려져 있다(대한약전 V 제2부 651). 또한 해수, 천식 및 변비 개선에 효과적이며, 피부의 불순물을 제거하는 마사지용 화장료 조성물로 사용되고 있다. 또한, 이뇨제-소변을 보지 못할 때 효과가 있다. 특히 고창 병에 쓰인다. 복수가 차고 몸에 부기가 있을 때 쓸 수 있다. 거담작용-가래, 기침, 천식 등에 효과를 나타낸다. 살충작용-회충, 촌충 등의 구제약으로 쓰이며 기생충에 의한 복통이나 혹은 그에 수반되어 여러 증세를 완화 시킬 목적으로 쓰인다.Pharbitidis Semen refers to the seeds of Pharbitis nil choisy (convolvulaceae), which is a subspecies in the oriental medicine and the private sector. Secretion, abdominal pain, swelling, abdominal distension, and constipation. The black shafts contain about 11% of fatty oil and 2% of pharbitin, a resinous glycoside, and are known to have subcutaneous, diuretic and insecticidal action (Korean Pharmacopoeia V, Part 2, 651). It is also effective in improving seawater, asthma and constipation, and is used as a cosmetic composition for massage which removes impurities from the skin. Also, it is effective when you do not see diuretic - urine. It is especially used for high fever disease. It can be used when revenge is cold and the body has swelling. Gadam work - effects on sputum, cough, asthma and so on. Insecticidal action - It is used as an old restriction of roundworms, tapeworms, etc. It is used for the purpose of relieving various symptoms accompanied by abdominal pain caused by parasites.
그러나 현호색과 흑축의 고혈압 관련 질환과 관련하여 상기 문헌 어디에도 개시되거나 공개된 바가 없다.
However, none of the above-mentioned documents have been disclosed or disclosed in relation to hypertension-related diseases of color and blackness.
본 발명이 해결하고자 하는 과제는 (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물을 유효성분으로 포함하는 심혈관계 질환 예방 또는 치료용 약학적 조성물을 제공하는 것이다.A problem to be solved by the present invention is to provide a pharmaceutical composition for prevention or treatment of cardiovascular diseases comprising (i) an extract of black shark or (ii) an extract of a black shade and a purple color mixture or (iii) a mixture of a black shark extract and a pale- .
본 발명이 해결하고자 하는 또 다른 과제는 (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물을 유효성분으로 포함하는 심혈관계 질환 예방 또는 개선용 건강식품 조성물을 제공하는 것이다.
Another object to be solved by the present invention is to provide a method for preventing or improving cardiovascular diseases, which comprises (i) an extract of black shark or (ii) an extract of black shade and color mixture, or (iii) To provide a food composition.
본 발명의 대표적인 일 측면에 따르면, (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물을 유효성분으로 포함하는 심혈관계 질환 예방 또는 치료용 약학적 조성물을 제공한다.According to one representative aspect of the present invention there is provided a pharmaceutical composition for the prevention or treatment of cardiovascular diseases comprising (i) an extract of a black shark or (ii) an extract of a black-and-white mixture, or (iii) a mixture of a black- Lt; / RTI >
본 발명의 대표적인 다른 측면에 따르면, (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물을 유효성분으로 포함하는 심혈관계 질환 예방 또는 개선용 건강식품 조성물을 제공한다.
According to another representative aspect of the present invention, there is provided a method for preventing or improving a cardiovascular disease comprising (i) an extract of a black shark or (ii) an extract of a black-and-white mixture, or (iii) a mixture of a black- Lt; / RTI >
본 발명의 여러 구현예에 따르면, 본 발명의 (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물은 ACE(안지오텐신 전환효소)를 저해함으로써 안지오텐신 전환효소의 작용으로 발생하는 혈압상승을 효과적으로 억제할 뿐만 아니라, 인체에 대한 안전성이 높으므로 심혈관계 질환, 즉, 고혈압 또는 고혈압성 심장질환의 예방 및 치료용 의약품 또는 건강기능식품으로 유용하게 이용될 수 있다.
According to various embodiments of the present invention, a mixture of (i) a black shark extract of the present invention or (ii) an extract of a black-and-white mixture with a black shaft or (iii) a mixture of a black shark extract and a prickly extract may inhibit angiotensin converting enzyme It can effectively be used as a medicament for the prevention and treatment of cardiovascular diseases, i.e., hypertension or hypertensive heart disease, or a health functional food, because it not only effectively suppresses an increase in blood pressure caused by the action of enzymes but also has high safety to human body have.
이하, 본 발명에서 사용한 용어를 설명한다.
Hereinafter, terms used in the present invention will be described.
본 발명에서 사용되는 용어 "예방"은 본 발명의 조성물의 투여로 심혈관 질환을 억제시키는 모든 행위를 의미한다.As used herein, the term "prophylactic " means any action that inhibits cardiovascular disease by administration of the composition of the present invention.
본 발명에서 사용되는 용어 "치료" 및 "개선"은 본 발명의 조성물의 투여로 심혈관계 질환이 호전 또는 이롭게 변경되는 모든 행위를 의미한다.As used herein, the terms " treatment "and" improvement "refer to any action by which administration of the composition of the present invention improves or alleviates cardiovascular disease.
본 발명에서 사용되는 용어 "투여"는 임의의 적절한 방법으로 개체에 소정의 본 발명의 조성물을 제공하는 것을 의미한다.The term "administering" as used herein is meant to provide any desired composition of the invention to an individual by any suitable method.
본 발명에서 사용되는 용어 "개체"는 본 발명의 조성물을 투여하여 심혈관 질환 또는 비만에 걸린 인간, 원숭이, 개, 염소, 돼지 또는 쥐 등 모든 동물을 의미한다.The term "individual" as used herein refers to all animals, including human, monkey, dog, goat, pig or rat, suffering from cardiovascular disease or obesity by administering the composition of the present invention.
본 발명에서 사용되는 용어 "약학적으로 유효한 양"은 의학적 치료에 적용 가능한 합리적인 수혜 또는 위험 비율로 심혈관 질환을 치료하기에 충분한 양을 의미하며, 이는 개체의 비만의 중증도, 약물의 활성, 약물에 대한 민감도, 투여 시간, 투여 경로 및 배출비율, 치료기간, 동시에 사용되는 약물을 포함한 요소 및 기타 의학 분야에 잘 알려진 요소에 따라 결정될 수 있다.
As used herein, the term "pharmaceutically effective amount" means an amount sufficient to treat cardiovascular disease at a reasonable benefit or risk rate applicable to medical treatment, including the severity of the subject's obesity, the activity of the drug, The drug's sensitivity, the time of administration, the route of administration and the rate of release, the duration of the treatment, factors including simultaneously used drugs, and other factors well known in the medical arts.
이하에서, 본 발명의 여러 측면 및 다양한 구현예에 대해 더욱 구체적으로 살펴보도록 한다.
Hereinafter, various aspects and various embodiments of the present invention will be described in more detail.
본 발명의 일 측면에 따르면, (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물을 유효성분으로 포함하는 심혈관계 질환 예방 또는 치료용 약학적 조성물이 개시된다.According to one aspect of the present invention there is provided a pharmaceutical composition for the prevention or treatment of cardiovascular diseases comprising (i) an extract of black shark or (ii) an extract of a black-and-white mixture, or (iii) a mixture of a black- / RTI >
본 발명의 일 구현예에 있어서, 상기 유효성분이 상기 (ⅱ) 흑축과 현호색 혼합물의 추출물인 경우, 상기 흑측과 상기 현호색의 중량비(w/w)는 특별히 이에 한정되지 않으나, 바람직하게는 1:0.05 내지 1:20이고, 상기 흑측과 상기 현호색의 중량비(w/w)가 1:0.1 내지 1:10이면 ACE 저해활성이 55%를 초과하는 유효한 효과를 갖기 때문에 더욱 바람직하다. 상기 1: 0.1 미만이거나, 1:10을 초과하는 경우에는 혈압상승 즉, 심혈관계 질환과 관계있는 ACE(안지오텐신 전환효소)에 대한 저해 효과가 ACE 저해활성이 52% 이하로 감소하는 문제가 발생한다.In one embodiment of the present invention, the weight ratio (w / w) between the black side and the color tone is not particularly limited, but is preferably 1: 0.05 To 1:20, and the weight ratio (w / w) of the black side to the precursor color is 1: 0.1 to 1:10, which is more preferable because it has an effective effect that the ACE inhibitory activity exceeds 55%. When the ratio is less than 1: 0.1 or more than 1:10, the inhibitory effect on ACE (angiotensin converting enzyme) associated with cardiovascular diseases, ie, the blood pressure increase, causes the ACE inhibitory activity to decrease to 52% or less .
또한, 상기 유효성분이 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물인 경우, 상기 (ⅱ) 흑축과 현호색 혼합물의 추출물인 경우, 상기 흑축 추출물과 현호색 추출물의 중량비(w/w)는 특별히 이에 한정되지 않으나, 바람직하게는 1:0.05 내지 1:20이고, 상기 흑측 추출물과 상기 현호색 추출물의 중량비(w/w)가 1:0.1 내지 1:10이면 ACE 저해활성이 55%를 초과하는 유효한 효과를 갖기 때문에 더욱 바람직하다. 상기 1: 0.1 미만이거나, 1:10을 초과하는 경우에는 혈압상승 즉, 심혈관계 질환과 관계있는 ACE(안지오텐신 전환효소)에 대한 저해 효과가 ACE 저해활성이 52% 이하로 감소하는 문제가 발생한다.In addition, the weight ratio (w / w) of the black extract to the color extract is not particularly limited as long as the active ingredient is a mixture of (iii) a black shark extract and a pale color extract, and (ii) , Preferably 1: 0.05 to 1: 20, and the weight ratio (w / w) of the black extract to the colorless extract is 1: 0.1 to 1:10, the ACE inhibitory activity is effectively 55% More preferable. When the ratio is less than 1: 0.1 or more than 1:10, the inhibitory effect on ACE (angiotensin converting enzyme) associated with cardiovascular diseases, ie, the blood pressure increase, causes the ACE inhibitory activity to decrease to 52% or less .
이때, 상기 (ⅱ) 흑축과 현호색 혼합물의 추출물은 상기 흑축과 상기 현호색을 혼합한 혼합물로부터 추출물을 수득한 것으로, 상기 흑측과 상기 현호색의 혼합물을 물, 탄소수 1 내지 4의 저급 알코올, 또는 이들의 혼합용매로 추출된 것임을 특징으로 한다.(Ii) the extract of the black shade and the purple color mixture is obtained from the mixture of the black shade and the purple color, and the mixture of the black color and the purple color is mixed with water, a lower alcohol having 1 to 4 carbon atoms, And is extracted with a mixed solvent.
또한, 상기 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물은 상기 흑축으로부터 수득된 흑축 추출물과 상기 현호색으로부터 수득된 현호색의 추출물을 혼합한 것으로서, 상기 흑축 추출물과 현호색 추출물은 각각 물, 탄소수 1 내지 4의 저급 알코올, 또는 이들의 혼합용매로 추출된 것임을 특징으로 한다.(Iii) a mixture of the black shark extract and the pale color extract is a mixture of the black shark extract obtained from the above-mentioned black shrinkage and the pale-color extract obtained from said pale shade, said black shark extract and said pale- A lower alcohol, or a mixed solvent thereof.
상기 흑축 추출물과 현호색 추출물의 혼합물은 흑축과 현호색을 상기 중량비로 혼합하여 추출한 추출물 또는 각각의 추출물을 상기 중량비로 혼합하여 혼합한 혼합물이 사용될 수 있다. The mixture of the black and white extracts may be a mixture of the extracts obtained by mixing the black shales and the pale colors at the above weight ratios, or the extracts or the respective extracts at the above weight ratios.
보다 구체적으로, 본 발명의 추출물은 하기와 같이 수득될 수 있다. 먼저, 본 발명의 흑축 또는 현호색 또는 흑축과 현호색의 혼합물을 각각 세척 및 건조한 후, 건조 생약 또는 분쇄기로 분쇄하여 분쇄 생약을 얻고, 분쇄 생약을 그라인더로 갈아 분말화한 다음 상기 건조 생약 또는 분쇄 생약 중의 약 1 내지 25 배, 바람직하게는 5 배 내지 15 배 분량의 물, 탄소수 1 내지 4의 저급 알코올, 또는 이들의 혼합용매, 바람직하게는 에탄올로 20 내지 100 ℃, 바람직하게는 45 내지 75 ℃의 추출온도에서 약 1 내지 100 시간 동안, 바람직하게는 65 내지 80 시간 동안 열수 추출, 냉침 추출, 환류 냉각 추출 또는 초음파 추출 등의 추출방법으로 1 회 내지 5 회 추출하여 감압여과하고 동결건조하여 수득될 수 있다. More specifically, the extract of the present invention can be obtained as follows. First, the mixture of the black shade or the pale color of the present invention or the mixture of the black color and the pale color is washed and dried, respectively, and then pulverized with a dry herb or a pulverizer to obtain a pulverized herb. The pulverized herb is pulverized with a grinder to be pulverized, Preferably 1 to 25 times, and preferably 5 to 15 times, water, a lower alcohol having 1 to 4 carbon atoms, or a mixed solvent thereof, preferably ethanol, at 20 to 100 占 폚, preferably 45 to 75 占 폚 Extraction is carried out once to five times with an extraction method such as hot water extraction, cold extraction, reflux cooling extraction or ultrasonic extraction for about 1 to 100 hours, preferably 65 to 80 hours at the extraction temperature, followed by filtration under reduced pressure and lyophilization .
본 발명에 따른 약학적 조성물은 심혈관계 질환, 바람직하게는 고혈압 또는 고혈압성 심장질환 예방 또는 치료용 약학적 조성물임을 특징으로 한다. The pharmaceutical composition according to the present invention is a pharmaceutical composition for preventing or treating cardiovascular diseases, preferably hypertension or hypertensive heart disease.
일반적으로 고혈압이란 안정 상태에서 수축기 혈압, 확장기 혈압 또는 평균 동맥압 등이 정상에 비해 지속적으로 높게 유지되는 상태를 말한다. 사람의 경우, 성인의 정상적인 수축기 혈압과 확장기 혈압은 각각 120 mmHg와 80 mmHg, 평균 동맥압은 100 mmHg 그리고 맥압은 40 mmHg 정도 된다. 그러나 사람마다 다소 차이가 있기 때문에 수축기 혈압이 140 mmHg 확장기 혈압이 90 mmHg 이하의 범위 내에 있으면 흔히 정상으로 간주한다. 따라서 고혈압이란 수축기 혈압이 140 mmHg 이상, 확장기 혈압이 90 mmHg 이상으로 지속적으로 유지될 때를 말한다.
Generally, hypertension refers to a state in which the systolic blood pressure, diastolic blood pressure, or mean arterial pressure is kept higher than the normal level in a stable state. In humans, adult normal systolic and diastolic blood pressures are 120 mmHg and 80 mmHg, mean arterial pressure is 100 mmHg, and pulse pressure is 40 mmHg. However, it is often considered normal if the systolic blood pressure is within 140 mmHg and the diastolic blood pressure is within 90 mmHg, because there is a slight difference between individuals. Therefore, hypertension refers to when the systolic blood pressure is more than 140 mmHg and the diastolic blood pressure is more than 90 mmHg.
고혈압성 심장질환은 혈압이 비정상적으로 상승된 상태로 유지되는 것으로 인해 발생하는 질병을 말한다. 예를 들면, 이에 한정되지는 않으나 관상 동맥 질환, 뇌혈관 질환, 말초혈관질환, 대동맥질환, 신장 기능장애, 심부전증 및 시력 장애가 포함된다. 상기 관상 동맥 질환의 예로는 협심증 및 심근 경색증을 들 수 있으며, 뇌혈관 질환의 예로는 중풍, 뇌출혈, 뇌경색을 들 수 있다. 이외에도 본 발명에 따른 약학적 조성물은 또한 당뇨병, 고지혈증, 동맥경화증 및 천식, 만성폐질환 등의 합병증의 치료 또는 예방에 적용될 수 있다.Hypertensive heart disease is a disease caused by an abnormally elevated blood pressure. Examples include, but are not limited to, coronary artery disease, cerebrovascular disease, peripheral vascular disease, aortic disease, renal dysfunction, heart failure, and visual disturbance. Examples of the coronary artery disease include angina pectoris and myocardial infarction. Examples of cerebrovascular diseases include stroke, cerebral hemorrhage, and cerebral infarction. In addition, the pharmaceutical composition according to the present invention can also be applied to the treatment or prevention of complications such as diabetes, hyperlipidemia, arteriosclerosis and asthma, chronic lung disease and the like.
본 발명의 약학적 조성물은 개별적으로 또는 다른 종류의 혈압 강하용 조성물과의 혼합하여 투여할 수 있다. 본 발명의 약학적 조성물은 단독으로 투여할 수 있지만, 일반적으로 선택된 투여 경로 및 표준 약제 입자를 기본으로 하여 선택된 약학적 담체와 함께 투여할 수 있다.The pharmaceutical compositions of the present invention may be administered individually or in combination with other types of hypotensive agents. The pharmaceutical compositions of the present invention may be administered alone, but may be administered with a pharmaceutical carrier selected on the basis of the generally chosen route of administration and standard pharmaceutical particles.
본 발명의 약학적 조성물은 포유동물에 어떠한 방법으로도 투여할 수 있다. 예를 들면, 경구 또는 비경구적으로 투여할 수 있다. 비경구적인 투여방법으로는 이에 한정되지는 않으나, 피하 내, 정맥 내, 근육 내 또는 복강 내 투여할 수 있다.The pharmaceutical composition of the present invention can be administered to mammals by any method. For example, it can be administered orally or parenterally. Parenteral administration methods include, but are not limited to, subcutaneous, intravenous, intramuscular or intraperitoneal administration.
본 발명의 약학적 조성물의 경구투여를 위해서는 캡슐, 정제 및 산제와 같은 고체 형태 또는 엘릭시스 시럽 및 현탁제와 같은 액체 형태로 제형화 할 수 있다. 또한, 비경구적으로 투여하기 위해서는 무균적인 액체 형태로 제형화 할 수 있다.For oral administration, the pharmaceutical compositions of the present invention may be formulated in solid form such as capsules, tablets and powders or in liquid form such as elixir syrups and suspensions. For parenteral administration, it may be formulated in an aseptic liquid form.
캡슐은 유당, 전분, 셀룰로오즈 유도체, 마그네슘 스테아레이트, 스테아르산 등과 같은 활성성분 및 분말화된 담체를 함유할 수 있다. 또한, 희석제를 사용하여 압착된 정제를 제조할 수 있다. 정제와 캡슐은 모두 서방성 생성물로서 제조하여 수 시간에 걸쳐 약제가 연속 방출되도록 할 수 있다. 압착된 정제는 당 피복 또는 필름 피복시킬 수 있다.Capsules may contain active ingredients such as lactose, starch, cellulose derivatives, magnesium stearate, stearic acid, and the like, and powdered carriers. In addition, compressed tablets can be prepared using a diluent. Both tablets and capsules can be manufactured as sustained release products to allow continuous release of the drug over a period of several hours. Compressed tablets may be coated with sugar or film.
경구 투여용 액체 형태의 약학적 조성물은 환자의 기호를 증진시키기 위하여 색소 및 향료를 함유할 수 있다.Pharmaceutical compositions in liquid form for oral administration may contain pigments and flavors to enhance patient preference.
비경구 투여용 액체 형태의 약학적 조성물은 적합한 담체로서 물, 적합한 오일, 염수, 수성 덱스트로즈(포도당) 및 프로필렌 글리콜 또는 폴리에틸렌 글리콜과 같은 글리콜을 함유할 수 있다. 바람직하게는, 수용성 활성 성분 염, 적합한 안정화제, 및 완충물질을 포함할 수 있다. 적합한 안정화제로는 나트륨 비설파이트, 나트륨 설파이트 또는 아스코르브산과 같은 산화방지제가 포함된다. 또한, 상기 비경구 투여용 액체 형태의 약학적 조성물은 염화벤즈알코늄, 메틸-또는 프로필-파라벤, 및 클로로부탄올과 같은 보존제를 함유할 수 있다.Pharmaceutical formulations in liquid form for parenteral administration may contain water as a suitable carrier, suitable oils, saline, aqueous dextrose (glucose) and glycols such as propylene glycol or polyethylene glycol. Preferably, it may comprise a water soluble active ingredient salt, a suitable stabilizing agent, and a buffering material. Suitable stabilizers include antioxidants such as sodium bisulfite, sodium sulfite or ascorbic acid. In addition, the pharmaceutical composition in liquid form for parenteral administration may contain a preservative such as benzalkonium chloride, methyl- or propyl-paraben, and chlorobutanol.
본 발명에 따른 심혈관계 질환용 약학적 조성물의 투여량은 연령, 건강정도, 체중, 질병 중증도, 치료횟수에 따라 조절될 수 있다. 일반적으로, 본 발명의 혈압 강하용 조성물의 1 일 투여량은 체중 1 kg당약 1 내지 500 mg 이 바람직하다. 1회 이상 적용시 1 내지 500 mg/kg/일, 바람직하게는 50 내지 300 mg/kg/일이 되도록 투여할 수 있다.
The dosage of the pharmaceutical composition for cardiovascular diseases according to the present invention can be adjusted according to age, health, weight, disease severity, and the number of treatments. Generally, the daily dose of the hypotensive composition of the present invention is preferably 1 to 500 mg per 1 kg of body weight. 1 to 500 mg / kg / day, preferably 50 to 300 mg / kg / day when applied at least once.
또한, 본 발명의 (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물은 혈압을 강하시켜 심혈관계 질환, 즉, 고혈압 또는 고혈압성 심장질환을 예방하기 위한 목적으로 식품에 첨가될 수 있다. In addition, a mixture of (i) a black shark extract or (ii) an extract of a black-and-white mixture of the present invention, or (iii) a mixture of a black shark extract and a pale extract of the present invention lower blood pressure to prevent a cardiovascular disease, i.e., hypertension or hypertensive heart disease May be added to the food for the purpose of.
본 발명의 식품 조성물에 포함되는 (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물은 컬럼 크로마토그래피를 통해 정제된 것이 바람직하나, 단순히 용매 추출법에 의해 수득된 추출물도 포함될 수 있다. (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물을 첨가할 수 있는 식품으로는 예를 들어, 이에 한정되지는 않으나 각종 식품류, 육류, 음료수, 스넥류, 과자류, 면류, 껌류, 아이스크림류, 알콜 음료류, 티백차, 인스탄트차, 과립, 향료, 정제 및 캡슐 등이 있다.It is preferable that the mixture of (i) the black shark extract or (ii) the black shrink and the mixture of the color mixture contained in the food composition of the present invention or (iii) the mixture of the black shark extract and the pale color extract is purified through column chromatography, May also be included. Foods to which (i) an extract of black shark or (ii) an extract of a black-and-white mixture, or (iii) a mixture of a black shark extract and a prickly extract may be mentioned, including but not limited to various foods, meats, Snacks, snacks, noodles, gums, ice cream, alcoholic beverages, tea bags, instant tea, granules, spices, tablets and capsules.
본 발명의 (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물은 식품에 그대로 첨가하거나 다른 식품 또는 식품 성분과 함께 사용될 수 있고, 통상적인 방법에 따라 적절하게 사용될 수 있다. 유효 성분의 혼합량은 그의 사용 목적(예방 또는 개선용)에 따라 적합하게 결정될 수 있다. 일반적으로, 건강식품 중의 상기 화합물의 양은 전체 식품 중량의 0.1 내지 90 중량부로 가할 수 있다. 그러나 건강 및 위생을 목적으로 하거나 또는 건강 조절을 목적으로 하는 장기간의 섭취의 경우에는 상기 양은 상기 범위 이하일 수 있으며, 안전성 면에서 아무런 문제가 없기 때문에 유효성분은 상기 범위 이상의 양으로도 사용될 수 있다.A mixture of the (i) black shark extract of the present invention or (ii) an extract of a black-and-white mixture with black shrink or (iii) a black shark extract and a pale extract may be added to the food as they are or may be used together with other food or food ingredients, Can be appropriately used. The amount of the active ingredient to be mixed can be suitably determined according to the intended use (for prevention or improvement). Generally, the amount of the compound in the health food may be 0.1 to 90 parts by weight of the total food. However, in the case of long-term ingestion intended for health and hygiene purposes or health control purposes, the amount may be less than the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount in the above range.
본 발명의 건강 기능성 음료 조성물은 지시된 비율로 필수 성분으로서 상기 화합물을 함유하는 외에는 다른 성분에는 특별한 제한이 없으며 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상술한 천연 탄수화물의 예는 모노사카라이드, 예를 들어, 포도당, 과당 등; 디사카라이드, 예를 들어 말토스, 슈크로스 등; 및 폴리사카라이드, 예를 들어 덱스트린, 시클로덱스트린 등과 같은 통상적인 당, 및 자일리톨, 소르비톨, 에리트리톨 등의 당알콜이다. 상술한 것 이외의 향미제로서 천연 향미제(타우마틴, 스테비아 추출물(예를 들어 레바우디오시드 A, 글리시르히진등) 및 합성 향미제(사카린, 아스파르탐 등)를 유리하게 사용할 수 있다. 상기 천연 탄수화물의 비율은 본 발명의 조성물 100 당 일반적으로 약 1 내지 20 g, 바람직하게는 약 5 내지 12 g이다.The health functional beverage composition of the present invention is not particularly limited to the other ingredients other than the above-mentioned compounds as essential ingredients in the indicated ratios and may contain various flavors or natural carbohydrates as additional ingredients such as ordinary beverages. Examples of the above-mentioned natural carbohydrates include monosaccharides such as glucose, fructose and the like; Disaccharides such as maltose, sucrose and the like; And polysaccharides, for example, conventional sugars such as dextrin, cyclodextrin and the like, and sugar alcohols such as xylitol, sorbitol and erythritol. Natural flavors (tau martin, stevia extracts (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavors (saccharin, aspartame, etc.) can be advantageously used as flavors other than those described above The ratio of the natural carbohydrate is generally about 1 to 20 g, preferably about 5 to 12 g per 100 of the composition of the present invention.
상기 외에 본 발명의 (ⅰ) 흑축 추출물 또는 (ⅱ) 흑축과 현호색 혼합물의 추출물 또는 (ⅲ) 흑축 추출물과 현호색 추출물의 혼합물은 여러 가지 영양제, 비타민, 광물(전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 중진제(치즈, 초콜릿 등), 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제 등을 함유할 수 있다. 그 밖에 본 발명의 혼합 추출물은 천연 과일 쥬스 및 과일 쥬스 음료 및 야채 음료의 제조를 위한 과육을 함유할 수 있다. 이러한 성분은 독립적으로 또는 조합하여 사용할 수 있다. 이러한 첨가제의 비율은 그렇게 중요하진 않지만 본 발명의 혼합 추출물 100 중량부 당 0.1 내지 약 20 중량부의 범위에서 선택되는 것이 일반적이다.
In addition to the above, a mixture of (i) a black shark extract or (ii) an extract of a black-and-white mixture with a black shark or (iii) a black-shark extract and a pale yellowish extract according to the present invention may contain various nutrients, vitamins, minerals (electrolytes) Used in flavors such as flavorings, coloring agents and thickening agents (cheese, chocolate etc.), pectic acid and its salts, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, And the like. In addition, the mixed extract of the present invention may contain natural fruit juice and pulp for the production of fruit juice drinks and vegetable drinks. These components may be used independently or in combination. The ratio of such additives is not so important, but is generally selected in the range of 0.1 to about 20 parts by weight per 100 parts by weight of the mixed extract of the present invention.
이하에서 실시예 등을 통해 본 발명을 더욱 상세히 설명하고자 하며, 다만 이하에 실시예 등에 의해 본 발명의 범위와 내용이 축소되거나 제한되어 해석될 수 없다. 또한, 이하의 실시예를 포함한 본 발명의 개시 내용에 기초한다면, 구체적으로 실험 결과가 제시되지 않은 본 발명을 통상의 기술자가 용이하게 실시할 수 있음은 명백한 것이며, 이러한 변형 및 수정이 첨부된 특허청구범위에 속하는 것도 당연하다.
Hereinafter, the present invention will be described in more detail with reference to Examples and the like, but the scope and content of the present invention can not be construed to be limited or limited by the following Examples. It will be apparent to those skilled in the art that various modifications and variations can be made in the present invention without departing from the spirit and scope of the present invention as set forth in the following claims. It is natural that it belongs to the claims.
실시예 1 내지 21: 흑축과 현호색 혼합물의 추출물 제조.EXAMPLES 1 to 21: Preparation of extracts of black shrubs and color mixtures.
경동시장의 한약재상에서 건조된 현호색(Corydalis Tuber)과 흑축(Pharbitis seed)을 구입하여 협잡물을 제거한 뒤 사용하였다. 건조한 현호색과 흑축은 분쇄하였다. 상기 분쇄된 흑축과 현호색을 각각 표 1의 중량으로 혼합한 뒤 8배의 (v/w) 50 %의 에탄올 수용액을 가해 상온에서 48 시간 동안 냉침 후 여과하였다. 상기 여과액을 45-65 ℃에서 감압농축한 후, 동결건조시켜 흑축 및 현호색 혼합물의 추출 연조 엑스를 수득하였다.Corydalis Tuber and Pharbitis seed, which were dried on the herb medicinal materials of Kyungdong market, were purchased and used to remove the contaminants. The dry color and black shafts were crushed. The pulverized black shafts and pre-existing colors were mixed by the weights shown in Table 1, followed by 8 times (v / w) 50% aqueous ethanol solution, followed by cold-pressing at room temperature for 48 hours. The filtrate was concentrated under reduced pressure at 45-65 占 폚 and then lyophilized to obtain an extractive soft X-ray of a black-and-white mixture.
실시예 22: 흑축 추출물의 제조Example 22: Preparation of black shrimp extract
상기 분쇄된 흑축 20 g을 사용한 점을 제외하고는 실시예 1과 실질적으로 동일한 방법을 사용하여 흑축 추출물을 수득하였다.
A black shroud extract was obtained using substantially the same method as in Example 1, except that 20 g of the crushed black shafts were used.
비교예 1: 현호색 추출물의 제조COMPARATIVE EXAMPLE 1: Preparation of color-proof extract
상기 분쇄된 현호색 20 g을 사용한 점을 제외하고는 실시예 1과 실질적으로 동일한 방법을 사용하여 현호색 추출물을 수득하였다.
A precursor extract was obtained using substantially the same method as in Example 1, except that 20 g of the crushed pale color was used.
실험예 1: ACE(안지오텐신 전환효소) 저해 확인Experimental Example 1: Confirmation of ACE (angiotensin converting enzyme) inhibition
흑축 추출물, 현호색 추출물과 흑축 및 현호색의 혼합 추출물의 ACE 저해 효과는 쿠스만 등의 방법(Cushman D.W. et al., Biochem. Pharm., 20, pp 1637-1647, 1971)을 일부 변경한 ACE 측정 kit(Dojindo)를 이용해 in vitro cell free system으로 측정하였다. 시료군에는 시료, 완충액 및 효소를 첨가하여 측정하였으며, blank 1에는 시료 대신 탈이온수를, blank 2에는 시료 및 효소 대신 탈이온수를 첨가하여 측정하였다. 양성 대조군으로는 시판되고 있는 ACE 저해제인 에날라프릴ⓡ 10 mg(Enalapril Tablets 10 mg LGCI, 엘지생명과학)을 사용하였다.The ACE inhibitory effect of the extracts of black shark, purple color extract and black shale and pale yellow color was evaluated by ACE measurement kit (Kushman DW et al., Biochem. Pharm., 20, pp 1637-1647, 1971) (Dojindo) in vitro cell free system. Buffer 1 was prepared by adding deionized water instead of the sample, and blank 2 was added by adding deionized water instead of the sample and enzyme. As a positive control, 10 mg (Enalapril Tablets 10 mg LGCI, LG Life Science), a commercially available ACE inhibitor, was used.
효소 활성 저해율의 계산은 하기 수학식 1로 계산하였다.
The enzyme activity inhibition rate was calculated by the following equation (1).
[수학식 1][Equation 1]
ACE inhibitory activity (inhibition rate %) = [(Ablank1-Asample)/(Ablank1-Ablank2)] X 100
ACE inhibitory activity = [(A blank1 -A sample ) / (A blank1 -A blank2 )] X 100
그 결과, 하기 표 2에서 나타난 바와 같이 흑축 추출물 단독 처리에 의한 ACE 저해활성은 0.5 μg/ml에서 10.0 μg/ml 처리시까지 농도 의존적으로 ACE 저해 활성이 증가하여 10.0 μg/ml 처리시 약 58 %의 ACE 저해활성을 나타내는 것을 확인하였다. As a result, as shown in Table 2, ACE inhibitory activity by the single treatment of black shrimp extract increased ACE inhibitory activity in a concentration-dependent manner from 0.5 μg / ml to 10.0 μg / ml, and was about 58% at 10.0 μg / ACE < / RTI >
현호색 추출물 단독 처리에 의해서는 0.5 μg/ml에서 10.0 μg/ml 처리시까지 농도 의존적으로 ACE 저해 활성이 증가하여 10.0 μg/ml 처리시 약 63 %의 ACE 저해활성을 나타내는 것을 확인하였다. 흑축 및 현호색의 혼합 비율에 따른 ACE 저해활성을 비교하기 위해서 다양한 혼합 비율의 혼합 추출물을 처리하였다. 각 생약을 1.0 μg/ml로 단독 처리하였을 경우 흑축 추출물은 약 37 %, 현호색 추출물은 약 46 %의 저해활성을 보였다. The ACE inhibitory activity was increased in a concentration-dependent manner from 0.5 μg / ml to 10.0 μg / ml by ACE inhibitor alone, indicating that ACE inhibition activity was about 63% at 10.0 μg / ml treatment. In order to compare ACE inhibitory activities according to the blending ratio of black shade and pale shade, mixed extracts of various mixing ratios were treated. When each herbal medicine was treated with 1.0 μg / ml alone, about 37% of black extract and 46% of colorectal extract were inhibited.
실시예 1 내지 21에서와 같이 각각의 생약을 1:0.05에서 1:20의 혼합비율로 혼합한 혼합물의 추출물을 1.0 μg/ml로 처리하였을 경우 50-91 %의 저해활성을 보여 생약 단독 추출물 처리 대비 저해활성이 증가되었음을 확인하였다. 특히, 흑축 및 현호색의 1:5 혼합 추출물에서 약 91 %로 가장 큰 효과를 나타내는 것을 확인하였다(표 2).As in Examples 1 to 21, when the mixture of each herbal medicine was mixed at a mixing ratio of 1: 0.05 to 1:20, the inhibitory activity was 50-91% when treated with 1.0 μg / ml of extract, Inhibitory activity was increased. In particular, it was confirmed that the highest effect was obtained in the 1: 5 mixed extract of black shale and pale color, at about 91% (Table 2).
상기 흑축과 현호색 혼합물의 추출물에서 각각의 생약의 혼합비율이 ACE 저해활성에 미치는 영향을 확인한 결과, 상기 흑축과 현호색을 20:1(1:0.05) 및 1:20의 혼합비율로 혼합한 혼합물의 추출물을 제조하고, 이를 1.0 μg/ml로 처리하였을 경우, 생약 단독 추출물 1 μg/ml 처리한 거보다 저해활성은 우수하다는 것이 확인되어 심혈관계 질환 예방 또는 치료용 조성물 및 심혈관계 질환예방 또는 개선용 건강식품 조성물로 사용할 수 있다. 다만, 상기 흑축과 현호색 혼합 추출물에서 각각의 생약의 혼합비율이 20:1 및 1:20인 경우 50% 내지 52%로 ACE 저해활성의 절반정도에 불과하므로, 이보다 최대 1.8 배 더 우수한 10:1 내지 1:10의 혼합비율로 혼합한 흑축과 현호색 혼합물의 추출물이 바람직하다.As a result of examining the effect of the mixing ratio of each herbal medicine on the ACE inhibitory activity in the extracts of the black shrub and the pale yellow mixture, it was found that the mixture of the above black shrunken and pale yellow was mixed at a mixing ratio of 20: 1 (1: 0.05) Extracts were prepared and treated with 1.0 μg / ml, the inhibitory activities were superior to those obtained by treatment with 1 μg / ml of herbal medicine extract alone. Thus, compositions for prevention or treatment of cardiovascular diseases and prevention or improvement of cardiovascular diseases Can be used as a health food composition. However, in the case of mixing the herbal medicines in the black shrinkage and pale yellow color mixed extracts at a ratio of 20: 1 and 1:20, it is 50% to 52%, which is about half of the ACE inhibitory activity. To 1:10 are preferable.
특히, 상기 흑축과 현호색 혼합물의 추출물에서 각각의 생약의 혼합비율(w/w)이 1:5인 경우에는 90% 이상의 ACE 저해활성을 가지므로, 상기 혼합비율(w/w)인 것이 가장 바람직하다. 아울러 상기 1:5 혼합비율 조건에서의 흑축과 현호색 혼합물의 추출물은 단독으로 사용한 10 배 농도의 흑축 추출액, 현호색 추출액보다 30 % 이상 우수할뿐더러 에닐라프릴보다도 13% 높은 ACE 저해활성을 갖는다.In particular, when the mixing ratio (w / w) of each herbal medicine is 1: 5 in the extract of the black shade and the color mixture, the mixture has the ACE inhibitory activity of 90% or more, Do. In addition, the extracts of the black-and-white mixture at the above 1: 5 mixing ratio have an ACE inhibitory activity that is more than 30% higher than that of the black extract and ascorbic acid extract of 10-fold concentration alone and 13% higher than that of nilapril.
즉, 본 발명에 따른 흑축 및 현호색 혼합물의 추출물이 1:1의 혼합비율 조건으로 제조된 1 μg/ml의 ACE 저해활성과, 생약을 단독으로 사용한 흑축 추출물 0.5 μg/ml(20.09 %)와 현호색 추출물 0.5 μg/ml(24.58 %)를 1:1로 합하여 계산된 ACE 저해활성보다 저해활성이 12 % 이상 더 우수하다는 것을 확인하였으므로 본 발명은 흑축 또는 현호색 추출물을 각각 사용한 것보다 현저히 우수한 효과를 갖는다는 것을 알 수 있다.That is, the ACE inhibitory activity of 1 μg / ml prepared by mixing the black-and-white mixture according to the present invention at a mixing ratio of 1: 1, the black extract of 0.5 μg / ml (20.09%) using herbal medicine alone, It was confirmed that the inhibitory activity was more than 12% higher than the ACE inhibitory activity calculated by adding 1: 1 of the extract (0.5 μg / ml (24.58%)). Therefore, the present invention has remarkably excellent effects .
혼합 추출액Black and cyan
Mixed extract
Claims (15)
A pharmaceutical composition for the prevention or treatment of hypertension or hypertensive heart disease, comprising (i) an extract of black shark or (ii) an extract of a black shade mixture and (iii) a mixture of black shark extract and pale yellow extract.
상기 흑축과 상기 현호색의 중량비(w/w)는 1:0.05 내지 1:20인 것을 특징으로 하는 고혈압 또는 고혈압성 심장질환 예방 또는 치료용 약학적 조성물.
2. The method according to claim 1, wherein when the effective component is the extract of (ii)
Wherein the weight ratio (w / w) of the black shade to the precursor color is 1: 0.05 to 1:20.
상기 흑축 추출물과 현호색 추출물의 중량비(w/w)는 1:0.05 내지 1:20인 것을 특징으로 하는 고혈압 또는 고혈압성 심장질환 예방 또는 치료용 약학적 조성물.
The method according to claim 1, wherein said effective component is (iii) a mixture of a black shark extract and a pale yellow extract,
Wherein the weight ratio (w / w) of the black extract to the colorectal extract is 1: 0.05 to 1:20.
상기 흑축과 현호색 또는 흑축 추출물과 현호색 추출물의 중량비(w/w)가 1:5 인 것을 특징으로 하는 고혈압 또는 고혈압성 심장질환 예방 또는 치료용 약학적 조성물.
The method according to claim 1, wherein the effective component is (i) an extract of a mixture of a black shade and a purple color, or (iii) a mixture of a black shade extract and a pale-
The weight ratio (w / w) of the above-mentioned black shafts and purple or black shampoos and pale yellow extracts was 1: 5 Or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the manufacture of a medicament for preventing or treating hypertension or hypertensive heart disease.
The pharmaceutical composition for preventing or treating hypertension or hypertensive heart disease according to claim 1, wherein the extract is extracted with water, a lower alcohol having 1 to 4 carbon atoms, or a mixed solvent thereof.
The pharmaceutical composition for preventing or treating hypertension or hypertensive heart disease according to claim 1, wherein the composition has an inhibitory activity (%) of 36 to 92% with respect to an angiotensin converting enzyme (ACE) Composition.
The composition for preventing or treating hypertension or hypertensive heart disease according to claim 1, wherein the composition further comprises at least one additive selected from the group consisting of pharmaceutically acceptable excipients, disintegrants, binders and glidants. .
The composition for preventing or treating hypertension or hypertensive heart disease according to claim 1, wherein the composition is an oral composition having a formulation of a tablet, a capsule, a solution, a suspension, or a syrup.
A health food composition for preventing or ameliorating hypertension or hypertensive heart disease, which comprises (i) an extract of black shark or (ii) an extract of black shade and purple color mixture or (iii) a mixture of black shark extract and purple color extract.
상기 흑축과 상기 현호색의 중량비(w/w)는 1:0.05 내지 1:20인 것을 특징으로 하는 고혈압 또는 고혈압성 심장질환 예방 또는 개선용 건강식품 조성물.
11. The method according to claim 10, wherein when the effective component is the extract of (ii)
Wherein the weight ratio (w / w) of the black shade to the color tone is 1: 0.05 to 1:20.
상기 흑축 추출물과 현호색 추출물의 중량비(w/w)는 1:0.05 내지 1:20인 것을 특징으로 하는 고혈압 또는 고혈압성 심장질환 예방 또는 개선용 건강식품 조성물.
11. The method of claim 10, wherein said effective component is (iii) a mixture of a black shark extract and a pale yellow extract,
Wherein the weight ratio (w / w) of the black extract to the color extract is 1: 0.05 to 1:20.
상기 흑축과 현호색 또는 흑축 추출물과 현호색 추출물의 중량비(w/w)가 1:5 인 것을 특징으로 하는 고혈압 또는 고혈압성 심장질환 예방 또는 개선용 건강식품 조성물.
11. The method according to claim 10, wherein said effective component is (ii) an extract of a mixture of black shade and purple color, or (iii)
The weight ratio (w / w) of the above-mentioned black shafts and purple or black shampoos and pale yellow extracts was 1: 5 Or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the prevention or amelioration of hypertension or hypertensive heart disease.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020150051766A KR101713557B1 (en) | 2015-04-13 | 2015-04-13 | Pharmaceutical composition comprising a pharbitidis semen or a mixture of pharbitidis semen extract and corydalis turtschaninovii extract for preventing and treating cardiovascular disease |
| PCT/KR2016/003137 WO2016167493A2 (en) | 2015-04-13 | 2016-03-28 | Pharmaceutical composition for preventing or treating cardiovascular diseases, containing pharbitis seed extract or mixture of pharbitis seed extract and corydalis extract as active ingredient |
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| Application Number | Priority Date | Filing Date | Title |
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| KR1020150051766A KR101713557B1 (en) | 2015-04-13 | 2015-04-13 | Pharmaceutical composition comprising a pharbitidis semen or a mixture of pharbitidis semen extract and corydalis turtschaninovii extract for preventing and treating cardiovascular disease |
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| KR20160121912A KR20160121912A (en) | 2016-10-21 |
| KR101713557B1 true KR101713557B1 (en) | 2017-03-22 |
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| WO (1) | WO2016167493A2 (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005320323A (en) | 2004-04-09 | 2005-11-17 | Taisho Pharmaceut Co Ltd | Lipase inhibitor |
| JP2011519368A (en) | 2008-05-01 | 2011-07-07 | アフェクサ ライフ サイエンシーズ インコーポレイテッド | Pharmaceutical composition comprising an extract of yellow ream and bitter tea useful for reducing blood lipid concentration |
| US20130045987A1 (en) | 2010-05-03 | 2013-02-21 | Dignity Health | Novel methods of use of tetrahydroberberine (thb) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN100554270C (en) * | 2004-12-29 | 2009-10-28 | 中国人民解放军第二军医大学 | Deydrokaividing, dehydrogenation apocavidine and preparation of compositions method thereof |
| EP2206508B1 (en) * | 2006-02-28 | 2013-08-21 | Dong-A ST Co., Ltd. | Extract of herbal and the composition containing the same |
| WO2014000119A1 (en) * | 2012-06-25 | 2014-01-03 | 佛山市顺德区合生源医药研发有限公司 | Anti-tachyarrhythmia formulation and preparation method thereof |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005320323A (en) | 2004-04-09 | 2005-11-17 | Taisho Pharmaceut Co Ltd | Lipase inhibitor |
| JP2011519368A (en) | 2008-05-01 | 2011-07-07 | アフェクサ ライフ サイエンシーズ インコーポレイテッド | Pharmaceutical composition comprising an extract of yellow ream and bitter tea useful for reducing blood lipid concentration |
| US20130045987A1 (en) | 2010-05-03 | 2013-02-21 | Dignity Health | Novel methods of use of tetrahydroberberine (thb) |
Also Published As
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| KR20160121912A (en) | 2016-10-21 |
| WO2016167493A3 (en) | 2016-12-08 |
| WO2016167493A2 (en) | 2016-10-20 |
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