KR20040026872A - Sweroside as anti-inflammatory and analgesic drug - Google Patents

Sweroside as anti-inflammatory and analgesic drug Download PDF

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KR20040026872A
KR20040026872A KR1020020058494A KR20020058494A KR20040026872A KR 20040026872 A KR20040026872 A KR 20040026872A KR 1020020058494 A KR1020020058494 A KR 1020020058494A KR 20020058494 A KR20020058494 A KR 20020058494A KR 20040026872 A KR20040026872 A KR 20040026872A
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sweroside
inflammatory
analgesic
composition
active ingredient
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KR1020020058494A
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KR100796384B1 (en
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곽의종
조용백
한창균
신희재
류근호
유헌승
이해인
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에스케이케미칼주식회사
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Priority to AU2003260985A priority patent/AU2003260985B2/en
Priority to CNB03823484XA priority patent/CN100544744C/en
Priority to EP03795473A priority patent/EP1536811A4/en
Priority to PCT/KR2003/001851 priority patent/WO2004024172A1/en
Priority to US10/527,139 priority patent/US7314644B2/en
Priority to JP2004535252A priority patent/JP2006510592A/en
Publication of KR20040026872A publication Critical patent/KR20040026872A/en
Priority to HK06101294.5A priority patent/HK1081115A1/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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Abstract

PURPOSE: Provided is an anti-inflammatory drug composition which contains sweroside as an active ingredient, and exerts excellent anti-inflammatory and painkilling effects without making any toxicity. CONSTITUTION: An anti-inflammatory drug composition characteristically comprises sweroside represented by the formula(1), wherein the sweroside is extracted from Lonicera japonica, Swertia japonica, or Gentiana scabra. The composition is formulated into tablet, powder, granule, capsule, syrup, skin coating cream, or injecting solution.

Description

스웨로사이드를 유효성분으로 함유하는 소염, 진통제 조성물{Sweroside as anti-inflammatory and analgesic drug}Anti-inflammatory and analgesic composition containing sweroside as an active ingredient {Sweroside as anti-inflammatory and analgesic drug}

본 발명은 스웨로사이드(sweroside)를 유효성분으로 함유하는 소염, 진통제 조성물에 관한 것으로서, 더욱 상세하게는 소염 및 진통 효과가 매우 탁월하며, 독성 또한 거의 보이지 않아 그 유효성 및 안전성이 매우 뛰어남으로써 약제 조성물의 유효성분으로 사용될 수 있는 스웨로사이드의 새로운 용도에 관한 것이다.The present invention relates to an anti-inflammatory and analgesic composition containing sweroside as an active ingredient, and more particularly, an anti-inflammatory and analgesic effect is very excellent, and almost no toxicity is also seen, so the efficacy and safety are excellent. It relates to a new use of sweroside that can be used as an active ingredient of the composition.

옛날부터 청열이나 해독의 목적으로 인동등(Lonicera japonica), 당약 (Swertia japonica), 용담 (Gentiana scabra, Gentiana triflora, Gentiana manshurica, Gentiana rigescens, Gentiana rigescens Franch. var. stictantha Marquand) 등이 사용되어 왔으나, 어떠한 성분이 그러한 효과를 가지는지는 명확히 알려져 있지 않았다. 다만 인동등에서 주 약효성분으로서 로가닌(loganin)에 대한 활성 연구만이 주로 이루어져 왔다[J. Nat. Prod., 54(4), 1102 ~ 1104 , 1991 : Planta Med., 60, 232 ~ 234, 1994 : Phytotheraphy Res., 12, 405-408, 1998].Since ancient times, Lonicera japonica, Sugar (Swertia japonica), Gentian (Gentiana scabra, Gentiana triflora, Gentiana manshurica, Gentiana rigescens, Gentiana rigescens Franch. Var. Stictantha Marquand) It is not clear which ingredients have such effects. However, only active studies on loganin as a main active ingredient in Indong et al. Have been mainly conducted [J. Nat. Prod., 54 (4), 1102-1104, 1991: Planta Med., 60, 232-234, 1994: Phytotheraphy Res., 12, 405-408, 1998].

또한, 기존의 스웨로사이드는 간보호 활성 및 항미생물 활성 정도만 알려져 왔으며[J. Ethnopharmacol., 42, 183-191, 1994 : Chem. Pharm. Bull., 45(11), 1823-1827, 1997 : Yakugaku Zasshi, 102(8), 755-759, 1982], 소염, 진통 효과에 대한 보고는 아직까지 없다.In addition, the existing spherosides have only been known for their hepatoprotective and antimicrobial activity [J. Ethnopharmacol., 42, 183-191, 1994: Chem. Pharm. Bull., 45 (11), 1823-1827, 1997: Yakugaku Zasshi, 102 (8), 755-759, 1982], anti-inflammatory, analgesic effects have not been reported yet.

이에, 본 발명자들은 인동등에 다양한 종류의 이리도이드계(iridoid) 화합물들이 함유되어 있고 이러한 물질들에 대한 연구를 진행하던 중, 이들 이리도이드계(iridoid) 화합물의 한 종류인 스웨로사이드(sweroside)가 매우 우수한 소염, 진통 작용을 가진다는 것을 밝혀냈고, 스웨로사이드(sweroside)의 반수치사율을 측정한 결과, 경구투여시 5.0 g/Kg 이상(사망개체 없음), 정맥투여시 2.0 g/Kg 이상(사망한 개체 없음)으로서 독성이 거의 없는 수준이었고 부검 결과 역시 이상이 없었던 바 이 화합물을 매우 안전하고 효과가 우수한 소염, 진통제용 조성물로 사용할 수 있음을 확인함으로써 본 발명을 완성하였다.Accordingly, the present inventors contain various kinds of iridoid compounds in phosphorus and the like, and during the study of these substances, one of these iridoid compounds is sweroside. Was found to have very good anti-inflammatory and analgesic effects. As a result of measuring the half-lethality of sweroside, 5.0 g / Kg or more (without death) and 2.0 g / Kg or more during intravenous administration The present invention was completed by confirming that the compound could be used as a very safe and effective anti-inflammatory and analgesic composition.

따라서, 본 발명은 스웨로사이드(sweroside)를 유효성분으로 함유하는 소염, 진통제용 조성물을 제공하는데 그 목적이 있다.Accordingly, an object of the present invention is to provide an anti-inflammatory, analgesic composition containing sweroside as an active ingredient.

본 발명은 스웨로사이드(sweroside)를 유효성분으로 함유하는 소염, 진통제용 조성물을 그 특징으로 한다.The present invention is characterized by an anti-inflammatory, analgesic composition containing a sweroside as an active ingredient.

이와 같은 본 발명을 더욱 상세히 설명하면 다음과 같다.Referring to the present invention in more detail as follows.

본 발명에 따른 스웨로사이드(sweroside)는 인동등(Lonicera japonica), 당약(Swertia japonica), 용담(Gentiana scabra, Gentiana triflora, Gentiana manshurica, Gentiana rigescens, Gentiana rigescens Franch. var. stictantha Marquand) 등의 식물체로부터 제조한다.The sweroside according to the present invention is a plant such as Lonera japonica, Sugar (Swertia japonica), Gentian (Gentiana scabra, Gentiana triflora, Gentiana manshurica, Gentiana rigescens, Gentiana rigescens Franch.var.stictantha Marquand) Prepared from.

예를 들어, 인동등을 생약 중량 대비 약 7 ∼ 10 배량의 증류수로 2시간 내지 3시간동안 환류 추출한 후 여과하여 여액을 모으고, 다시 5 ∼ 7 배량의 증류수로 2시간 내지 3시간동안 환류 추출한 후 모은 액을 여과하여 앞의 여액과 합친 뒤 감압농축하여 그 부피가 원 생약 중량 대비 약 1 ∼ 3배량(v/w) 정도가 되도록 한 후 다시 한번 여과한다. 증류수로 추출함에 있어 물의 양이 너무 적어지게 되면 교반이 어렵게 되고 추출물의 용해도가 낮아져 추출 효율이 떨어지게 되며, 증류수의 양이 너무 많아지면 추출 효율 대비 농축할 증류수의 양이 많아져 시간과 경제적 불합리성이 발생하게 되므로 위와 같은 공정으로 진행한다. 그 후 동량의 수포화 저급 알코올을 넣어 약 10 ∼ 20 분간 30 ∼ 50 rpm 정도로 교반하고 정체시켜, 층을 분리한 뒤 수포화 저급 알코올 층을 여과, 감압 농축하여 1차 활성 정제 분획을 얻는다. 이때 사용되는 수포화 저급 알코올은 저급 알코올의 포화수용액으로서 저급 알코올에 증류수를 가하고 교반시킨 후 정체시켜 증류수로 포화된 저급 알코올 층을 취한 것으로 예를 들면, 프로필알코올, 부틸알코올 등이 사용가능하며 층분리는 2 ∼ 3회 실시한다. 만일 저급 알코올 용매 분획을 얻음에 있어 소량의 저급 알코올을 사용하게 되면 정제 효율이 떨어져 엑기스의 수율 및유효성분의 함량이 낮아지고, 과량의 저급 알코올을 사용하게 되면 정제 효율 대비 과다한 알코올 사용으로 경제성을 떨어뜨리게 된다. 따라서, 원생약 중량의 1 ∼ 3 배량(v/w)의 저급 알코올을 사용하는 것이 좋은데 상기에 기술된 양은 이 같은 정제 효율 및 경제성에 부합된다.For example, after extracting the reflux with about 7 to 10 times the distilled water in about 7 to 10 times the weight of the herbal medicine and filtered to collect the filtrate, and then reflux for 2 to 3 hours with 5 to 7 times distilled water again The collected liquid is filtered, combined with the previous filtrate, and concentrated under reduced pressure so that the volume thereof is about 1 to 3 times (v / w) relative to the weight of the original herbal medicine and filtered again. When the amount of water is too small to extract with distilled water, it becomes difficult to stir, and the solubility of the extract becomes low, so that the extraction efficiency is lowered. When the amount of distilled water is too large, the amount of distilled water to be concentrated compared to the extraction efficiency increases, resulting in unreasonable time and economic Since it occurs, proceed to the above process. Thereafter, the same amount of saturated lower alcohol is added, stirred for about 10 to 20 minutes at 30 to 50 rpm, and allowed to stand, and the layers are separated. The saturated lower alcohol layer is filtered and concentrated under reduced pressure to obtain a primary active purified fraction. The saturated lower alcohol used in this case is a saturated aqueous solution of lower alcohol, which is diluted with distilled water by adding distilled water to the lower alcohol, stirring the mixture, and taking a lower alcohol layer saturated with distilled water. Separation is performed 2-3 times. If a small amount of lower alcohol is used to obtain a lower alcohol solvent fraction, the purification efficiency is lowered, and the yield and the active ingredient content of the extract are lowered. Dropped. Therefore, it is better to use 1 to 3 times the lower alcohol (v / w) of the weight of the crude drug, and the amount described above is consistent with such purification efficiency and economy.

이 1차 정제 분획물에 대하여 다시 ODS(Octadecylsilane) 레진을 이용해 컬럼 크로마토그래피를 실시하는데 10%(v/v) 메탄올 수용액부터 10%(v/v)씩 메탄올 양을 늘려가며 레진 부피의 2 ∼ 3배량의 용매를 스텝-그래디언트 방식으로 용출시키고 레진의 양은 상기의 1차 정제 분획물 중량의 50 ∼ 100배 중량을 사용한다. 이때, 20 ∼ 30%(v/v) 메탄올 수용액을 용출시킨 분획에서 스웨로사이드(sweroside)의 함량이 가장 높으며, 이 분획물을 다시 컬럼크로마토그래피를 수행하여 스웨로사이드를 분리한다.The first purified fraction was subjected to column chromatography using Octadecylsilane (ODS) resin again. The amount of methanol was increased from 10% (v / v) aqueous solution to 10% (v / v) by 2 ~ 3 of the resin volume. The amount of solvent is eluted in a step-gradient manner and the amount of resin is 50 to 100 times the weight of the above primary purified fraction. In this case, the content of sweroside is the highest in the fraction eluted with 20-30% (v / v) methanol aqueous solution, and the fraction is subjected to column chromatography again to separate the sworoside.

당약 및 용담 역시 상기의 인동등과 같은 방법으로 추출 정제 후 ODS 컬럼 크로마토그래피를 실시하여 스웨로사이드를 분리한다.Glucose and gentian are also extracted and purified by the same method as the above phosphorus, and then subjected to ODS column chromatography to separate sworosides.

본 발명에 따른 스웨로사이드는 다음 화학식 1로 표시되는 화합물을 말한다.Sweroside according to the present invention refers to a compound represented by the following formula (1).

이렇게 하여 얻어진 스웨로사이드에 대해 아라키돈산 유도성 귀 부종법(Arachidonic acid induced ear edema test)과 크로톤 오일 유도성 귀 부종법(Croton oil induced ear edema test)을 통하여 소염 효과를 측정하고, 아세트산 유도성 라이딩법(Acetic acid induced writhing test)을 통해 진통 효과를 측정한 결과 매우 뛰어난 소염, 진통 활성이 있음을 확인하였다.The anti-inflammatory effect of the sweroside thus obtained was measured through the Arachidonic acid induced ear edema test and the Croton oil induced ear edema test. Analyzing the analgesic effect through the riding (Acetic acid induced writhing test) was confirmed that the very excellent anti-inflammatory, analgesic activity.

따라서, 스웨로사이드는 소염, 진통제로 유용하게 사용될 수 있다.Therefore, sweroside can be usefully used as an anti-inflammatory and analgesic agent.

한편, 본 발명에 따른 스웨로사이드가 치료용 약제로 이용되기 위해서는 약제학적 분야에서 공지의 방법에 의하여 제조될 수 있으며, 그 자체 또는 약학적으로 허용되는 담체(carrier), 부형제(forming agent), 희석제(diluent) 등과 혼합하여 경구 투여하거나 비경구 투여할 수 있으며, 특히 분말제, 과립제, 정제, 캡슐제, 시럽제, 피부도포제 또는 주사제의 제형으로 제조되어 사용될 수 있다.Meanwhile, in order to use the sweroside according to the present invention as a therapeutic agent, it may be prepared by a known method in the pharmaceutical field, and may be a carrier, an excipient, a carrier, a pharmaceutically acceptable agent, or the like. It may be administered orally or parenterally in combination with a diluent or the like, and may be prepared and used in the form of powder, granule, tablet, capsule, syrup, skin coating or injection.

또한, 본 발명에 따른 유효성분인 스웨로사이드의 인체 투여량은 체내에서 활성성분의 흡수도, 물활성화율 및 배설 속도, 환자의 연령, 성별 및, 상태, 치료할 질병의 중증정도 등에 따라 적절히 선택되나 일반적으로 성인에게 1일 1 ∼ 200 mg 정도의 사용량에서 투여하는 것이 바람직하다. 따라서, 인동등, 당약, 용담을 정제한 엑기스의 단위투여형 제제는 전술한 스웨로사이드의 유효량 범위를 고려하여 본 발명의 활성 물질을 1 ∼ 200 mg을 함유하도록 제형화 하는 것이 좋다. 이렇게 제형화된 단위투여형 제제는 필요에 따라 약제의 투여를 감시하거나 관찰하는 전문가의 판단과 개인의 요구에 따라 전문화된 투약법을 사용하거나 일정시간 간격으로 수회 투여할 수 있으며, 바람직하게는 하루에 1 ~ 3회 투여할 수 있다. 또한, 상기 약제 조성물은 경구 또는 비경구로 투여될 수 있으며, 비경구 투여는 정맥내, 근육내, 직장내 투여, 피부도포 등이 가능하다.In addition, the human dose of sweroside, the active ingredient according to the present invention, is appropriately selected according to the absorbency of the active ingredient in the body, the rate of water activation and excretion, the age, sex and condition of the patient, and the severity of the disease to be treated. However, in general, it is preferable to administer to adults in an amount of about 1 to 200 mg per day. Therefore, it is preferable to formulate a unit dosage form of extract, such as phosphorus, sugar, and gentian, containing 1 to 200 mg of the active substance of the present invention in consideration of the effective amount range of sweroside described above. The formulated unit dosage form may be administered several times at regular intervals or by using a specialized dosing method according to the judgment of an expert who monitors or observes the administration of the drug as necessary and the needs of the individual. May be administered 1-3 times. In addition, the pharmaceutical composition may be administered orally or parenterally, parenteral administration may be intravenous, intramuscular, rectal administration, skin coating and the like.

더구나, 본 발명에 따른 스웨로사이드의 급성독성 시험에서 경구투여시 5.0 g/Kg에서도 사망한 개체가 없었고 정맥주사시 2.0 g/Kg에서도 사망한 개체가 없었으며 부검 결과 역시 이상 소견이 없었으므로 매우 안전한 소염, 진통제로 사용할 수 있음을 확인하였다.Moreover, in the acute toxicity test of sweroside according to the present invention, there was no death in 5.0 g / Kg at oral administration and no death at 2.0 g / Kg at intravenous injection, and the autopsy showed no abnormal findings. It was confirmed that it can be used as a safe anti-inflammatory and analgesic agent.

이하, 본 발명은 다음 실시예에 의거하여 더욱 상세히 설명하겠는바, 본 발명이 이에 한정되는 것은 아니다.Hereinafter, the present invention will be described in more detail based on the following examples, but the present invention is not limited thereto.

실시예 1 : 스웨로사이드(sweroside)의 소염 효과 측정Example 1 Determination of the anti-inflammatory effect of sweroside

크로톤 오일 유도성 귀부종법(Croton oil induced ear edema test)은 실험 실시 4시간 전에 절식시킨 6주령 ICR 마우스(body weight : 20 ∼ 30 g , n=6, SLC, Japan)에 대해 꼬리 정맥을 통해 스웨로사이드를 투여하고 15분 후 2.5 % 크로톤 오일(croton oil)로 발염시킨 뒤 4시간 후에 두께측정기(dial thickness gauge)를 사용하여 왼쪽 귀와 오른쪽 귀의 두께를 각각 측정하여 다음 수학식 1에 의해 발염율을 계산하였고, 다음 표 1에 약효를 나타내었다. 상기와 같은 방법으로 실험하되 경구로 투여하여 얻어진 약효는 다음 표 2에 나타내었다.Croton oil induced ear edema test was performed through the tail vein on 6-week-old ICR mice (body weight: 20-30 g, n = 6, SLC, Japan) fasted 4 hours before the experiment. After 15 minutes of roside administration, after 4 minutes of dyeing with 2.5% croton oil, the thickness of the left and right ears was measured using a dial thickness gauge, respectively. Was calculated and shown in Table 1 below. Experiments in the same manner as described above but obtained by oral administration is shown in Table 2 below.

또한, 아라키돈산 유도성 귀 부종법(Arachidonic acid induced ear edema test)은 실험 실시 4시간 전에 절식시킨 6주령 ICR 마우스(body weight : 20 ∼ 30g, n=6, SLC, Japan)에 대해 꼬리 정맥을 통해 스웨로사이드를 투여하고 15분 후 0.05 % 아라키돈산으로 발염시킨 뒤 1시간 후에 두꼐측정기를 사용하여 왼쪽 귀와 오른쪽 귀의 두께를 각각 측정하여 상기 수학식 1로 계산한 후 억제율을 다음 표 3에 나타내었다. 상기와 같은 방법으로 실험하되 경구로 투여하여 얻어진 약효는 다음 표 4에 나타내었다.In addition, the Arachidonic acid induced ear edema test was performed in 6-week-old ICR mice (body weight: 20-30 g, n = 6, SLC, Japan) fasted 4 hours before the experiment. 15 minutes after administration of sweroside through the inflamed with 0.05% arachidonic acid after 1 hour after measuring the thickness of the left ear and the right ear using a cephalometer respectively calculated by Equation 1 shown in Table 3 below It was. Experiments in the same manner as described above, but obtained by oral administration is shown in Table 4 below.

실시예 2 : 스웨로사이드(sweroside)의 진통 효과 측정Example 2 Measurement of Analgesic Effect of Sweroside

아세트산 유도성 라이딩법(Acetic acid induced writhing test)은 실험 실시 전날에 절식시킨 ICR 마우스(body weight : 20 ∼ 30 g , n=8, SLC, Japan)에 대해 꼬리 정맥을 통해 스웨로사이드를 투여하고 20분 후 0.7 % 아세트산을 복강 주사한 뒤 15분 후에 10분간의 라이딩(writhing) 횟수를 측정하여 염증 억제율을 다음 표5에 나타내었다. 상기와 같은 방법으로 실험하되 경구로 투여하여 얻어진 약효는 다음 표 6에 나타내었다.The acetic acid induced writhing test was administered through the tail vein to the fasted ICR mice (body weight: 20-30 g, n = 8, SLC, Japan) on the day before the experiment. Inflammation inhibition rate is shown in Table 5 after measuring the number of riding for 10 minutes after intraperitoneal injection of 0.7% acetic acid after 20 minutes after 15 minutes. Experimental method as described above, but obtained by oral administration is shown in Table 6 below.

실시예 3 : 독성시험Example 3 Toxicity Test

실험 실시 4시간 전에 절식시킨 SD 래트(body weight : 120 ∼ 170 g, 단위 용량 당 암수 각각 5마리, SLC, Japan)에 대해 꼬리 정맥을 통해 스웨로사이드를 1.0 g/Kg, 1.5 g/Kg, 2.0 g/Kg 단위로 투여하고 30분간 육안으로 관찰한 뒤 30분 간격으로 육안 관찰하였다. 또한, 약물 투여 후 2주간의 사망률 관찰, 일반증상 관찰, 체중측정을 하였고 부검하여 각 장기의 이상 유무를 확인하였다.For SD rats (body weight: 120-170 g, 5 males per unit dose, SLC, Japan) 4 hours before the experiment, 1.0 g / Kg, 1.5 g / Kg, 2.0 g / Kg was administered and visually observed for 30 minutes and then visually observed at 30 minute intervals. In addition, two weeks after the drug administration, mortality, general symptoms, and body weight were measured, and autopsy confirmed abnormalities of each organ.

최종 정제물의 치사량은 경구투여시 5.0 g/Kg 이상(사망개체 없음), 정맥주사시 2.0 g/Kg 이상(사망개체 없음)으로 나타났으며 정맥주사시 2.0 g/Kg의 용량에서 투여 후 약 10분간 호흡 증가 및 활동력 감소가 나타났으나 곧 회복되었고 다른 증상은 보이지 않았으며 체중 변화 또한 시험 물질의 투여에 의한 증감은 나타나지 않았다. 부검 결과 역시 대조군과 변화가 없었다.The final dose of the final tablets was 5.0 g / Kg or more (no death) upon oral administration, 2.0 g / Kg or more (no death) during intravenous injection, and about 10 g after administration at a dose of 2.0 g / Kg during intravenous injection. Increased breathing and decreased activity occurred for a minute, but soon recovered, no other symptoms, and no change in body weight. Autopsy results were also unchanged from the control group.

50, 100 및 150 mg/Kg의 용량으로 국소 독성 실험시에도 주사용 생리식염수 투여군과의 차이는 발견할 수 없었고 조직괴사나 염증반응 등의 독성 또한 보이지 않았다.At the doses of 50, 100 and 150 mg / Kg, no differences were observed between the physiological saline-administered groups and no toxicity, such as tissue necrosis and inflammatory reactions.

제조예 1 : 정제의 제조Preparation Example 1 Preparation of Tablet

스웨로사이드(sweroside)를 이용하여 다음과 같은 조성으로 경구 투여용 정제를 제조하였다.Using sweroside, a tablet for oral administration was prepared in the following composition.

<조 성〉<Composition>

스웨로사이드 160㎎Sweroside 160mg

경질무수규산 20㎎Light anhydrous silicic acid 20mg

옥수수전분 87㎎Corn starch 87mg

결정셀룰로오스 72㎎Crystalline Cellulose 72mg

글리콘산전분나트륨 60㎎Sodium Glyconate 60mg

스테아린산마그네슘 6㎎Magnesium Stearate 6mg

총 672 ㎎672 mg total

제조예 2 : 시럽제의 제조Preparation Example 2 Preparation of Syrup

스웨로사이드(sweroside)를 이용하여 다음과 같은 조성으로 시럽제를 제조하였다.Syrup was prepared in the following composition using a sweroside (sweroside).

〈조 성〉<Furtherance>

스웨로사이드4,000 ㎎Swallowside4,000 mg

파라옥시안식향산메틸 5% 에탄올용액 60 ㎎Methyl paraoxybenzoate 5% ethanol solution 60 mg

파라옥시안식향산프로필 5% 에탄올용액 40 ㎎Paraoxybenzoate 5% ethanol solution 40 mg

안식향산나트륨 5% 수용액 100 ㎎Sodium benzoate 5% aqueous solution 100 mg

바나나분말 10% 수용액 600 ㎎Banana powder 10% aqueous solution 600 mg

D-솔비톨 140,000 ㎎D-sorbitol 140,000 mg

증류수 196 ㎖196 ml of distilled water

제조예 3 : 주사제의 제조Preparation Example 3 Preparation of Injection

스웨로사이드(sweroside)를 이용하여 다음과 같은 조성으로 주사제를 제조하였다.Injection was prepared using the sweroside with the following composition.

주사용앰플:스웨로사이드 20 mgInjectable Ampoule: 20 mg of sweroside

만니톨 60 mgMannitol 60 mg

대응하는 용매샘플 : 주사용 생리식염수 2000 mgCorresponding solvent sample: 2000 mg of saline for injection

총 2080 mg2080 mg total

제조예 4 : 주사제의 제조Preparation Example 4 Preparation of Injection

스웨로사이드(sweroside)를 이용하여 다음과 같은 조성으로 주사제를 제조하였다.Injection was prepared using the sweroside with the following composition.

주사용앰플: 스웨로사이드 50 mgInjectable Ampoule: Sweroside 50 mg

KH2(PO4) 8.5 mgKH 2 (PO 4 ) 8.5 mg

주사용 생리식염수 3000 mgPhysiological saline for injection 3000 mg

총 3058.5 mgTotal 3058.5 mg

제조예 5 : 주사제의 제조Preparation Example 5 Preparation of Injection

스웨로사이드(sweroside)를 이용하여 다음과 같은 조성으로 주사제를 제조하였다.Injection was prepared using the sweroside with the following composition.

주사용앰플:스웨로사이드 100 mgInjectable Ampoule: Swooroside 100 mg

만니톨 300 mgMannitol 300 mg

KH2(PO4) 17 mgK H2 (PO 4 ) 17 mg

주사용 생리식염수 3000 mgPhysiological saline for injection 3000 mg

총 3417 mg3417 mg total

제조예 6 : 연고제의 제조Preparation Example 6 Preparation of Ointment

스웨로사이드(sweroside)를 이용하여 다음과 같은 조성으로 연고제를 제조하였다.An ointment was prepared using a sweroside with the following composition.

<조성><Composition>

스웨로사이드 5 g5 g of sweroside

유동파라핀 10 g10 g of liquid paraffin

경납 9 g9 g of light solder

에탄올 8 g8 g of ethanol

모노올레인산 소르비탄 2 g2 g of monooleic acid sorbitan

폴리소르베이트 4 g4 g of polysorbates

파라옥시안식향산 프로필 0.05 g0.05 g of paraoxybenzoic acid profile

파라옥시안식향산 메틸 0.1 g0.1 g of methyl paraoxybenzoate

농글리세린 10 g10 g of concentrated glycerin

정제수 적량Purified water

이상에서 설명한 바와 같이, 본 발명에 따른 스웨로사이드(sweroside)는 약효가 매우 우수하고 독성 거의 보이지 않아 그 유효성 및 안전성이 뛰어난 소염, 진통제로 사용하는데 적합하다.As described above, the sweroside according to the present invention is very good in efficacy and hardly toxic, and thus is suitable for use as an anti-inflammatory and analgesic agent having excellent efficacy and safety.

Claims (2)

다음 화학식 1로 표시되는 스웨로사이드(sweroside)를 유효성분으로 함유하는 소염, 진통제용 조성물.The anti-inflammatory and analgesic composition comprising a sweroside represented by the following formula (1) as an active ingredient. [화학식 1][Formula 1] 제 1 항에 있어서, 상기 조성물은 정제, 분말제, 과립제, 캡슐제, 시럽제, 피부도포제 또는 주사제의 제형으로 사용되는 것을 특징으로 하는 소염, 진통제용 조성물.According to claim 1, wherein the composition is an anti-inflammatory, analgesic composition, characterized in that used in the formulation of tablets, powders, granules, capsules, syrups, skin coatings or injections.
KR1020020058494A 2002-09-11 2002-09-26 Sweroside as anti-inflammatory and analgesic drug KR100796384B1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
KR1020020058494A KR100796384B1 (en) 2002-09-26 2002-09-26 Sweroside as anti-inflammatory and analgesic drug
CNB03823484XA CN100544744C (en) 2002-09-11 2003-09-08 Method, its application in antiinflammatory and analgesic of extraction and purification active component from stem of Caulis Lonicerae
EP03795473A EP1536811A4 (en) 2002-09-11 2003-09-08 EXTRACTION AND PURIFICATION METHOD OF ACTIVE CONSTITUENTS FROM STEM OF i LONICERA JAPONICA /i THUNB., ITS USAGE FOR ANTI-INFLAMMATORY AND ANALGESIC DRUG
PCT/KR2003/001851 WO2004024172A1 (en) 2002-09-11 2003-09-08 Extraction and purification method of active constituents from stem of lonicera japonica thunb., its usage for anti-inflammatory and analgesic drug
AU2003260985A AU2003260985B2 (en) 2002-09-11 2003-09-08 Extraction and purification method of active constituents from stem of Lonicera japonica Thunb., its usage for anti-inflammatory and analgesic drug
US10/527,139 US7314644B2 (en) 2002-09-11 2003-09-08 Extraction and purification method of active constituents from stem of Lonicera japonica thunb., its usage for anti-inflammatory and analgesic drug
JP2004535252A JP2006510592A (en) 2002-09-11 2003-09-08 Extraction and purification method of active component of honeysuckle (LonicerajaponicaThumb.) Stem, its use for anti-inflammatory analgesic
HK06101294.5A HK1081115A1 (en) 2002-09-11 2006-01-27 Extraction and purification method of active constituents from stem of lonicera japonica thunb., its usage for anti-inflammatory and analgesic drug
US11/652,360 US20070111955A1 (en) 2002-09-11 2007-01-11 Extraction and purification method of active constituents from stem of Lonicera japonica Thunb., its usage for anti-inflammatory and analgesic drug

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