JPH04169524A - Composition having serum lipid-improving activity - Google Patents
Composition having serum lipid-improving activityInfo
- Publication number
- JPH04169524A JPH04169524A JP2293762A JP29376290A JPH04169524A JP H04169524 A JPH04169524 A JP H04169524A JP 2293762 A JP2293762 A JP 2293762A JP 29376290 A JP29376290 A JP 29376290A JP H04169524 A JPH04169524 A JP H04169524A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- composition
- less
- tocopherol
- serum lipid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 30
- 230000000694 effects Effects 0.000 title claims abstract description 25
- 210000002966 serum Anatomy 0.000 title claims abstract description 17
- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims abstract description 18
- YYGNTYWPHWGJRM-UHFFFAOYSA-N (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene Chemical compound CC(C)=CCCC(C)=CCCC(C)=CCCC=C(C)CCC=C(C)CCC=C(C)C YYGNTYWPHWGJRM-UHFFFAOYSA-N 0.000 claims abstract description 10
- BHEOSNUKNHRBNM-UHFFFAOYSA-N Tetramethylsqualene Natural products CC(=C)C(C)CCC(=C)C(C)CCC(C)=CCCC=C(C)CCC(C)C(=C)CCC(C)C(C)=C BHEOSNUKNHRBNM-UHFFFAOYSA-N 0.000 claims abstract description 10
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N dodecahydrosqualene Natural products CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 claims abstract description 10
- 229940031439 squalene Drugs 0.000 claims abstract description 10
- TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 claims abstract description 10
- JAZBEHYOTPTENJ-JLNKQSITSA-N all-cis-5,8,11,14,17-icosapentaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O JAZBEHYOTPTENJ-JLNKQSITSA-N 0.000 claims abstract description 9
- 235000020669 docosahexaenoic acid Nutrition 0.000 claims abstract description 9
- 229940090949 docosahexaenoic acid Drugs 0.000 claims abstract description 9
- 235000020673 eicosapentaenoic acid Nutrition 0.000 claims abstract description 9
- 229960005135 eicosapentaenoic acid Drugs 0.000 claims abstract description 9
- JAZBEHYOTPTENJ-UHFFFAOYSA-N eicosapentaenoic acid Natural products CCC=CCC=CCC=CCC=CCC=CCCCC(O)=O JAZBEHYOTPTENJ-UHFFFAOYSA-N 0.000 claims abstract description 9
- 229930003799 tocopherol Natural products 0.000 claims abstract description 9
- 239000011732 tocopherol Substances 0.000 claims abstract description 9
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229960001295 tocopherol Drugs 0.000 claims abstract description 8
- 235000010384 tocopherol Nutrition 0.000 claims abstract description 8
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims abstract description 8
- VZCCETWTMQHEPK-UHFFFAOYSA-N gamma-Linolensaeure Natural products CCCCCC=CCC=CCC=CCCCCC(O)=O VZCCETWTMQHEPK-UHFFFAOYSA-N 0.000 claims abstract description 7
- VZCCETWTMQHEPK-QNEBEIHSSA-N gamma-linolenic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/CCCCC(O)=O VZCCETWTMQHEPK-QNEBEIHSSA-N 0.000 claims abstract description 7
- 235000020664 gamma-linolenic acid Nutrition 0.000 claims abstract description 7
- 229960002733 gamolenic acid Drugs 0.000 claims abstract description 7
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims abstract description 7
- JZNWSCPGTDBMEW-UHFFFAOYSA-N Glycerophosphorylethanolamin Natural products NCCOP(O)(=O)OCC(O)CO JZNWSCPGTDBMEW-UHFFFAOYSA-N 0.000 claims abstract description 6
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 6
- 229930195729 fatty acid Natural products 0.000 claims abstract description 6
- 239000000194 fatty acid Substances 0.000 claims abstract description 6
- 150000004665 fatty acids Chemical class 0.000 claims abstract description 6
- 150000008104 phosphatidylethanolamines Chemical class 0.000 claims abstract description 6
- 150000003905 phosphatidylinositols Chemical class 0.000 claims abstract description 6
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 claims abstract description 5
- 235000020778 linoleic acid Nutrition 0.000 claims abstract description 5
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 claims abstract description 5
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims abstract description 4
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims abstract description 4
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims abstract description 4
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims abstract description 4
- 239000005642 Oleic acid Substances 0.000 claims abstract description 4
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims abstract description 4
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims abstract description 4
- 150000002632 lipids Chemical class 0.000 claims description 20
- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 claims 2
- 210000004369 blood Anatomy 0.000 abstract description 8
- 239000008280 blood Substances 0.000 abstract description 8
- 208000007536 Thrombosis Diseases 0.000 abstract description 3
- 239000003795 chemical substances by application Substances 0.000 abstract description 2
- 206010008132 Cerebral thrombosis Diseases 0.000 abstract 1
- 201000001429 Intracranial Thrombosis Diseases 0.000 abstract 1
- 230000002411 adverse Effects 0.000 abstract 1
- 230000000747 cardiac effect Effects 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 229960004232 linoleic acid Drugs 0.000 abstract 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 28
- 235000012000 cholesterol Nutrition 0.000 description 13
- 208000031226 Hyperlipidaemia Diseases 0.000 description 8
- 238000012360 testing method Methods 0.000 description 7
- 231100000517 death Toxicity 0.000 description 6
- 230000034994 death Effects 0.000 description 6
- 208000006011 Stroke Diseases 0.000 description 5
- 201000010099 disease Diseases 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
- 208000019622 heart disease Diseases 0.000 description 5
- 239000003814 drug Substances 0.000 description 4
- 206010003210 Arteriosclerosis Diseases 0.000 description 3
- 208000011775 arteriosclerosis disease Diseases 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 231100000957 no side effect Toxicity 0.000 description 3
- 150000003904 phospholipids Chemical class 0.000 description 3
- 206010020772 Hypertension Diseases 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- DTOSIQBPPRVQHS-PDBXOOCHSA-N alpha-linolenic acid Chemical compound CC\C=C/C\C=C/C\C=C/CCCCCCCC(O)=O DTOSIQBPPRVQHS-PDBXOOCHSA-N 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 206010008118 cerebral infarction Diseases 0.000 description 2
- 208000026106 cerebrovascular disease Diseases 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 208000010125 myocardial infarction Diseases 0.000 description 2
- 231100000956 nontoxicity Toxicity 0.000 description 2
- SECPZKHBENQXJG-FPLPWBNLSA-N palmitoleic acid Chemical compound CCCCCC\C=C/CCCCCCCC(O)=O SECPZKHBENQXJG-FPLPWBNLSA-N 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 150000003626 triacylglycerols Chemical class 0.000 description 2
- 208000000668 Chronic Pancreatitis Diseases 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 235000021319 Palmitoleic acid Nutrition 0.000 description 1
- 206010033649 Pancreatitis chronic Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000007059 acute toxicity Effects 0.000 description 1
- 231100000403 acute toxicity Toxicity 0.000 description 1
- 235000020661 alpha-linolenic acid Nutrition 0.000 description 1
- 210000002565 arteriole Anatomy 0.000 description 1
- SECPZKHBENQXJG-UHFFFAOYSA-N cis-palmitoleic acid Natural products CCCCCCC=CCCCCCCCC(O)=O SECPZKHBENQXJG-UHFFFAOYSA-N 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 230000002354 daily effect Effects 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 208000010706 fatty liver disease Diseases 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 208000023589 ischemic disease Diseases 0.000 description 1
- 230000000302 ischemic effect Effects 0.000 description 1
- 229960004488 linolenic acid Drugs 0.000 description 1
- 230000037356 lipid metabolism Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 235000019149 tocopherols Nutrition 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 235000021122 unsaturated fatty acids Nutrition 0.000 description 1
- 150000004670 unsaturated fatty acids Chemical class 0.000 description 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- QUEDXNHFTDJVIY-UHFFFAOYSA-N γ-tocopherol Chemical class OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1 QUEDXNHFTDJVIY-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【発明の詳細な説明】 〈産業上の利用分野〉 この発明は血清脂質改善作用を有する組成物に関する。[Detailed description of the invention] <Industrial application field> The present invention relates to a composition having a serum lipid improving effect.
〈発明の背景〉
近年癌や心臓病或は脳卒中等の成人病が著しく増加しつ
つあり、数年前よりこの３つの疾患による死亡者数が３
大死因として年間死亡者総数の上位３位を占めるに至っ
ている。ちなみに昭和６３年には癌と心臓病及び脳卒中
による死亡者数が年間死亡者総数の６２％を占めた。<Background of the invention> In recent years, adult diseases such as cancer, heart disease, and stroke have been increasing significantly, and since several years ago, the number of deaths from these three diseases has increased by 3.
As a major cause of death, it ranks in the top three in the total number of deaths each year. By the way, in 1988, the number of deaths due to cancer, heart disease, and stroke accounted for 62% of the total annual deaths.
これらの疾患のうち心臓病と脳卒中は血中のコレステロ
ールや燐脂質や中性脂肪等が正常値の範囲を大きく上回
る所謂高脂血症が最大の引金になっている。即ち高脂血
症は動脈硬化の大きな原因となり、動脈硬化は心臓病や
脳卒中をはじめ細動脈に富む各臓器に重大な虚血性の障
害を引き起こす、また動脈硬化は高血圧の一因ともなり
、高血圧も心臓病や脳卒中の発症の危険度を高くする。Among these diseases, the main trigger for heart disease and stroke is so-called hyperlipidemia, in which blood cholesterol, phospholipids, triglycerides, etc. greatly exceed the normal range. In other words, hyperlipidemia is a major cause of arteriosclerosis, and arteriosclerosis causes serious ischemic damage to various organs rich in arterioles, including heart disease and stroke. Arteriosclerosis also contributes to high blood pressure. It also increases the risk of developing heart disease and stroke.
〈発明が解決しようとする課題〉
従来このような高脂血症を予防或は治療するために種々
の治療剤が医家により臨床に用いられているが、その多
くは十分な効果がなく、また効果を得られるまでに長期
間を要する問題がある。また効果があったとしても特定
の血中脂質にのみ効果があり他の脂質には効果がない等
全ての血中脂質に効果があるものは少なかった。更に副
作用が大きい等の問題があった。そのため従来より効果
が大きく、全ての血中脂質に効果があり、また効果を得
るのに長期間を要せず、更に副作用のない予防又は治療
剤が求められていた。<Problem to be solved by the invention> Various therapeutic agents have been used clinically by doctors to prevent or treat hyperlipidemia, but many of them are not sufficiently effective or There is a problem in that it takes a long time to obtain an effect. Furthermore, even if they were effective, there were few that were effective against all blood lipids, such as those that were effective only against specific blood lipids and not other lipids. Furthermore, there were other problems such as severe side effects. Therefore, there has been a need for a prophylactic or therapeutic agent that is more effective than ever, is effective against all blood lipids, does not require a long period of time to achieve its effects, and has no side effects.
本発明は上記した要望に応えるためになされたもので、
血清脂質改善に有効な組成物を提供することを目的とす
る。The present invention was made in response to the above-mentioned demands, and
The purpose of the present invention is to provide a composition effective for improving serum lipids.
〈発明の概要〉
上記目的を達成するために、本発明者らは、生体内にお
ける各種不飽和脂肪酸や不飽和炭化水素の作用に着目し
、α−リノレン酸なども含めた種々の物質についても対
象として、効果的な配合材料の種類と配合比率について
実験研究を重ねた結果、経口投与が容易でしかも優れた
血清脂質改善効果を示す組成物を開発するにいたった。<Summary of the Invention> In order to achieve the above object, the present inventors focused on the effects of various unsaturated fatty acids and unsaturated hydrocarbons in vivo, and also investigated various substances including α-linolenic acid. As a result of repeated experimental research on the types and ratios of effective compounding materials, we were able to develop a composition that is easy to administer orally and exhibits excellent serum lipid-improving effects.
即ち本発明の血清脂質改善作用を有する組成物は、スク
アレン、エイコサペンタエン酸、ドコサヘキサエン酸及
びトコフェロールを含有することを基本的な主成分とす
る。That is, the composition having a serum lipid improving effect according to the present invention basically contains squalene, eicosapentaenoic acid, docosahexaenoic acid, and tocopherol as main components.
またこれらに加えてホスファチジルコリン、ホスファチ
ジルエタノールアミン、ホスファチジルイノシトール、
リノール酸、γ−リノレン酸を含有することが望ましい
。In addition to these, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol,
It is desirable to contain linoleic acid and γ-linolenic acid.
更に上記各成分に加えてオレイン酸等の脂肪酸を含有す
ることも可能である。Furthermore, it is also possible to contain fatty acids such as oleic acid in addition to the above-mentioned components.
含有比率としては、スクアレンをスクアレン液として３
０ｗｔ％以上８５ ｗ ｔ％以下、エイコサペンタエン
酸を１ｗｔ％以上１０ｗｔ％以下、ドコサヘキサエン酸
を０．５ｗｔ％以上５ｗｔ％以下、ホスファチジルコリ
ンを１ｗｔ％以上Ｌｏｗｔ％以下、ホスファチジルエタ
ノールアミンを０゜５ｗｔ％以上５ｗｔ％以下、ホスフ
ァチジルイノシトールを０．４ｗｔ％以上４ｗｔ％以下
、γ−リノレン酸を０．３ｗｔ％以上４ｗｔ％以下、リ
ノール酸を２．５ｗｔ％以上２５ｗｔ％以下、その他の
脂肪酸を１０ｗｔ％以上５０ｗｔ％以下。The content ratio is 3 squalene as squalene liquid.
0 wt% or more and 85 wt% or less, eicosapentaenoic acid 1 wt% or more and 10 wt% or less, docosahexaenoic acid 0.5 wt% or more and 5 wt% or less, phosphatidylcholine 1 wt% or more and Lowt% or less, phosphatidylethanolamine 0°5 wt% or more 5 wt% or less, phosphatidylinositol from 0.4 wt% to 4 wt%, γ-linolenic acid from 0.3 wt% to 4 wt%, linoleic acid from 2.5 wt% to 25 wt%, other fatty acids from 10 wt% to 50 wt%. %below.
トコフェロールを０．０６ｗｔ％以上６ｗｔ％以下とす
るのが最も効果的であることが明かとなった。It has become clear that it is most effective to limit tocopherol to 0.06 wt% or more and 6 wt% or less.
上記組成物は液剤そのままで用いることも出来るが、軟
質ゼラチン製カプセル等に封入して用いてもよい。The above-mentioned composition can be used as a liquid formulation, but it may also be used after being enclosed in a soft gelatin capsule or the like.
〈実施例〉 上記組成物につきその効果を臨床試験により確認した。<Example> The effectiveness of the above composition was confirmed through clinical trials.
その実施例を以下説明する。An example thereof will be described below.
実施例１：
すでに高脂血症の診断をうけている者５名について、つ
ぎのような臨床試験を試みた。すなわち下記成分の本発
明に係る組成物を１回９００ｍｇずつ１日３回、４か月
間投与して１か月ごとに血中の総コレステロール、燐脂
質、中性脂肪、β−リボ蛋白、遊離コレステロール、Ｈ
ＤＬコレステロールのそれぞれの値を検査した。Example 1: The following clinical test was conducted on five people who had already been diagnosed with hyperlipidemia. That is, the composition according to the present invention containing the following ingredients was administered at a dose of 900 mg three times a day for 4 months, and blood total cholesterol, phospholipids, triglycerides, β-riboproteins, and free cholesterol, H
The respective values of DL cholesterol were tested.
その結果を、５名の平均値で第１図に示す。The results are shown in FIG. 1 as the average values of five people.
なお、それぞれの検査項目の正常値または基準値の範囲
は、総コレステロール：１２０ｍｇ以上２５０ｍｇ／ｄ
ｌ以下、燐脂質：１５０ｍｇ以上２８０ｍｇ／ｃｌｌ以
下、中性脂肪：４０ｍｇ以上１７０ｍｇ／ｄｉ以下、β
−リボ蛋白：２００ｍ２以上５５０ｍｇ／ｄｉ以下、遊
離コレステロール：３０ｍｇ以上６０ ｍ ｇ ／ ｄ
１以下、ＨＤＬコレステロールは男性で４０ｍｇ以上
７０ ｍ ｇ ／ ｄｌ以下、女性で４５ｍｇ以上７５
ｍｇ／ｄｌ以下とされている。The range of normal or standard values for each test item is total cholesterol: 120mg or more, 250mg/d.
1 or less, phospholipid: 150 mg or more and 280 mg/cll or less, neutral fat: 40 mg or more and 170 mg/di or less, β
-Riboprotein: 200 m2 or more and 550 mg/di or less, free cholesterol: 30 mg or more and 60 mg/d
1 or less, HDL cholesterol is 40 mg or more and 70 mg/dl or less for men, and 45 mg or more and 75 for women.
mg/dl or less.
（組成物）
スクアレン ： ５５．０ｗｔ％エイコサペ
ンタエン酸： ４．０ｗｔ％ドコサヘキサエン酸
： ２．０ｗｔ％ホスファチジルコリン： ２
．Ｏｗｔ％ネスファチジルエタノールアミン
・ １． ５ｗｔ ％ネスフ１チジルイノ
シトール ° １． Ｏｗｔ
％リノール酸 ８．Ｏｗｔ％γ−リ
ノレン酸 ・ １．Ｏｗｔ％総トコフェロール
： ２．５ｗｔ％オレイン酸
４．０ｗｔ％パルミチン酸 ・ ３．０ｗｔ％
パルミトレイン酸 ： １．０ｗｔ％その他
： １４．５ｗｔ％第１図で示した臨床試
験結果かられかるように本発明に係わる組成物は極めて
優れた効果を有している。即ち本発明による組成物によ
れば、投与開始１か月後の検査の時点で既に充分な効果
がみられ、血中脂質の種類の全てについてバランスの取
れた効果が得られている。しかも副作用は全く見られな
かった。(Composition) Squalene: 55.0wt% eicosapentaenoic acid: 4.0wt% docosahexaenoic acid
: 2.0wt% phosphatidylcholine: 2
．． Owt% nesphatidylethanolamine
・1. 5wt% Nesph 1 Tidylinositol °1. Owt
% linoleic acid 8. Owt% γ-linolenic acid ・1. Owt% total tocopherols
: 2.5wt% oleic acid
4.0wt% palmitic acid 3.0wt%
Palmitoleic acid: 1.0wt% others
: 14.5wt% As can be seen from the clinical test results shown in Figure 1, the composition according to the present invention has extremely excellent effects. That is, according to the composition according to the present invention, sufficient effects were already observed at the time of testing one month after the start of administration, and well-balanced effects were obtained for all types of blood lipids. Moreover, no side effects were observed.
実施例２：
さらに、高脂血症に加えて［非Ａ非Ｂウィルス性慢性肝
臓疾患Ｊに罹患している患者３人を対象に選んで、実施
例１と同一の組成物、同一の方法により臨床試験を実施
したところ、平均値において第２図に示すような成績を
得た。Example 2: Furthermore, three patients suffering from non-A, non-B viral chronic liver disease J in addition to hyperlipidemia were treated with the same composition and method as in Example 1. When a clinical test was carried out, the results shown in Figure 2 were obtained in terms of average values.
実施例３：
さらに、高脂血症に加えて［脂肪肝ｊならびに「慢性膵
臓炎」を併発している患者２名を対象に選んで、実施例
１と同一の組成物、同一の方法により臨床試験を実施し
たところ、平均値において第３図に示すような成績を得
た。Example 3: In addition to hyperlipidemia, two patients with fatty liver disease and chronic pancreatitis were treated with the same composition and method as in Example 1. When a clinical test was conducted, the results shown in Figure 3 were obtained in terms of average values.
実施例４：
さらに、高脂血症に加えて高血圧症を併発している患者
２名を対象に、実施例１と同一の組成物、同一の方法に
より臨床試験を実施したところ、平均値において第４図
に示すような成績を得た。Example 4: Furthermore, a clinical trial was conducted using the same composition and method as in Example 1 on two patients who had hypertension in addition to hyperlipidemia. The results shown in Figure 4 were obtained.
上記実施例２と実施例３及び実施例４の成績を実施例１
と比較すると１本組成物の投与開始の初期にはコレステ
ロールの数値が投与前よりやや上昇する傾向が認められ
たがこれは短期間の現象で。Example 1 shows the results of Example 2, Example 3, and Example 4 above.
In comparison, there was a tendency for cholesterol values to rise slightly from before administration at the beginning of administration of this composition, but this was a short-term phenomenon.
時間の経過とともに全て正常値の範囲に落ち着いてくる
という結果が得られた。The results showed that all values settled down to normal values over time.
このことは、単に高脂血症のみを発症している例におけ
る効果に限らず、他の疾患にともなって脂質代謝に異状
を来している場合にも効果があることを証明したものと
判断することができる。This is considered to be evidence that it is effective not only in cases with only hyperlipidemia, but also in cases where lipid metabolism is abnormal due to other diseases. can do.
なお、むしろ低いことが問題とされる善玉コレステロー
ルの別名を持つＨＤＬコレステロールは。In addition, HDL cholesterol, which has another name for good cholesterol, is considered to be a problem because of its low level.
実施例１乃至実施例４のいずれにおいても本発明に係わ
る組成物の投与によって数値が上昇すると言う成績を得
ており、この点でもその優れた作用が示されている。In all of Examples 1 to 4, the results were obtained in which the numerical values increased by administration of the composition according to the present invention, demonstrating its excellent effect in this respect as well.
実施例５：
本発明に係る組成物の毒性を検査した結果、毒性は全く
見られなかった。すなわち２０匹のラッチに１か月間連
続して毎日８ｇ／ｋｇずつ実施例１と同一の組成物を経
口投与した。また該組成物を４２ ｇ ／ ｋ ｇを１
か月間毎日２０匹のマウスに経口投与した。その後１０
日間状態をｖＲ察したが死亡はゼロであり、全く毒性は
なかった。Example 5: As a result of testing the toxicity of the composition according to the present invention, no toxicity was found. That is, the same composition as in Example 1 was orally administered to 20 rats at a dose of 8 g/kg every day for one month continuously. In addition, 42 g/kg of the composition was added to 1
Twenty mice were orally administered daily for a period of months. then 10
VR was used to monitor the condition for days, but there were no deaths and no toxicity at all.
即ち急性毒性はＬ Ｄ、、が３５ ｇ ／ ｋ ｇ以上
であることを確認した。That is, it was confirmed that the acute toxicity was 35 g/kg or more.
以上の各実施例に示すように本発明の組成物は極めてす
ぐれた血清脂質改善作用を有する。また、脳梗塞・心筋
梗塞に代表される虚血性疾患の治療は血清脂質の改善が
必須とされることから、これらの疾患の治療促進作用を
も合わせた効果が期待でき、上記疾患の予防および治療
促進のための医薬品および医薬品材料としての本発明の
組成物の有用性は極めて高いと云える。As shown in the above Examples, the composition of the present invention has an extremely excellent serum lipid improving effect. In addition, since improvement of serum lipids is essential for the treatment of ischemic diseases such as cerebral infarction and myocardial infarction, it is expected that it will have an effect that also promotes the treatment of these diseases. It can be said that the composition of the present invention is extremely useful as a drug and a drug material for promoting treatment.
〈発明の効果〉
以上説明したように本発明の組成物によれば、短期間で
血中脂質の改善効果がありしかも副作用がない。そのた
め血栓形成防止作用及び血栓症治療効果があり、脳梗塞
や心筋梗塞の予防及び治療薬として用いることが可能で
ある。<Effects of the Invention> As explained above, the composition of the present invention has the effect of improving blood lipids in a short period of time and has no side effects. Therefore, it has an effect of preventing thrombosis and treating thrombosis, and can be used as a preventive and therapeutic drug for cerebral infarction and myocardial infarction.
第１図は実施例１のコレステロール等血清脂質量の変化
を示すグラフ、第２図は実施例２のコレステロール等血
清脂質量の変化を示すグラフ、第３図は実施例３のコレ
ステロール等血清脂質量の変化を示すグラフ、第４図は
実施例４のコレステロール等血清脂質量の変化を示すグ
ラフである。
特許出願人 日誠マリン工業株式会社代理人
弁理士 高 橋 清Figure 1 is a graph showing changes in the amount of serum lipids such as cholesterol in Example 1, Figure 2 is a graph showing changes in serum lipids such as cholesterol in Example 2, and Figure 3 is a graph showing changes in serum lipids such as cholesterol in Example 3. FIG. 4 is a graph showing changes in the amount of serum lipids such as cholesterol in Example 4. Patent applicant Nissei Marine Industry Co., Ltd. Agent
Patent attorney Kiyoshi Takahashi
Claims (1)
エン酸及びトコフェロールを含有する血清脂質改善作用
を有する組成物。 ２）スクアレン、エイコサペンタエン酸、ドコサヘキサ
エン酸、ホスファチジルコリン、ホスファチジルエタノ
ールアミン、ホスファチジルイノシトール、リノール酸
、γ−リノレン酸及びトコフェロールを含有する血清脂
質改善作用を有する組成物。 ３）スクアレン、エイコサペンタエン酸、ドコサヘキサ
エン酸、ホスファチジルコリン、ホスファチジルエタノ
ールアミン、ホスファチジルイノシトール、トコフェロ
ール及びリノール酸、γ−リノレン酸、その他の脂肪酸
を含有する血清脂質改善作用を有する組成物。 ４）スクアレン：３０ｗｔ％以上８５ｗｔ％以下、エイ
コサペンタエン酸：１ｗｔ％以上１０ｗｔ％以下、ドコ
サヘキサエン酸：０．５ｗｔ％以上５ｗｔ％以下、ホス
ファチジルコリン：１ｗｔ％以上１０ｗｔ％以下、ホス
ファチジルエタノールアミン：０．５ｗｔ％以上５ｗｔ
％以下、ホスファチジルイノシトール：０．４ｗｔ％以
上４ｗｔ％以下、γ−リノレン酸：０．３ｗｔ％以上４
ｗｔ％以下、リノール酸：２．５ｗｔ％以上２５ｗｔ％
以下、その他の脂肪酸：１０ｗｔ％以上５０ｗｔ％以下
、トコフェロール：０．０６ｗｔ％以上６ｗｔ％以下を
含有する血清脂質改善作用を有する組成物。 ５）前記その他の脂肪酸がオレイン酸を主成分とする請
求項第４項の血清脂質改善作用を有する組成物。[Scope of Claims] 1) A composition containing squalene, eicosapentaenoic acid, docosahexaenoic acid, and tocopherol and having a serum lipid improving effect. 2) A composition having a serum lipid improving effect containing squalene, eicosapentaenoic acid, docosahexaenoic acid, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, linoleic acid, γ-linolenic acid, and tocopherol. 3) A composition having a serum lipid improving effect containing squalene, eicosapentaenoic acid, docosahexaenoic acid, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, tocopherol, and linoleic acid, γ-linolenic acid, and other fatty acids. 4) Squalene: 30 wt% or more and 85 wt% or less, eicosapentaenoic acid: 1 wt% or more and 10 wt% or less, docosahexaenoic acid: 0.5 wt% or more and 5 wt% or less, phosphatidylcholine: 1 wt% or more and 10 wt% or less, phosphatidylethanolamine: 0.5 wt % or more 5wt
% or less, phosphatidylinositol: 0.4 wt% or more and 4 wt% or less, γ-linolenic acid: 0.3 wt% or more 4
wt% or less, linoleic acid: 2.5 wt% or more 25 wt%
Hereinafter, a composition having a serum lipid improving effect containing other fatty acids: 10 wt% or more and 50 wt% or less and tocopherol: 0.06 wt% or more and 6 wt% or less. 5) The composition having a serum lipid improving effect according to claim 4, wherein said other fatty acid has oleic acid as a main component.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2293762A JPH04169524A (en) | 1990-11-01 | 1990-11-01 | Composition having serum lipid-improving activity |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2293762A JPH04169524A (en) | 1990-11-01 | 1990-11-01 | Composition having serum lipid-improving activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH04169524A true JPH04169524A (en) | 1992-06-17 |
Family
ID=17798892
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2293762A Pending JPH04169524A (en) | 1990-11-01 | 1990-11-01 | Composition having serum lipid-improving activity |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH04169524A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002002105A1 (en) * | 2000-06-29 | 2002-01-10 | Laxdale Limited | Therapeutic combinations of fatty acids |
| KR20020069539A (en) * | 2001-02-26 | 2002-09-05 | 주식회사 두산 | Composition for healthy brain |
| WO2003056939A1 (en) * | 2002-01-10 | 2003-07-17 | Puleva Biotech, S.A. | Oil blends |
| WO2007057090A1 (en) * | 2005-11-18 | 2007-05-24 | Farmaleis, S.L. | A combination comprising squalene, a phospholipid and an omega 3 fatty acid for the treatment of cancer |
-
1990
- 1990-11-01 JP JP2293762A patent/JPH04169524A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002002105A1 (en) * | 2000-06-29 | 2002-01-10 | Laxdale Limited | Therapeutic combinations of fatty acids |
| KR20020069539A (en) * | 2001-02-26 | 2002-09-05 | 주식회사 두산 | Composition for healthy brain |
| WO2003056939A1 (en) * | 2002-01-10 | 2003-07-17 | Puleva Biotech, S.A. | Oil blends |
| WO2007057090A1 (en) * | 2005-11-18 | 2007-05-24 | Farmaleis, S.L. | A combination comprising squalene, a phospholipid and an omega 3 fatty acid for the treatment of cancer |
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