JPH02174721A - Lipid lowering agent - Google Patents
Lipid lowering agentInfo
- Publication number
- JPH02174721A JPH02174721A JP63330259A JP33025988A JPH02174721A JP H02174721 A JPH02174721 A JP H02174721A JP 63330259 A JP63330259 A JP 63330259A JP 33025988 A JP33025988 A JP 33025988A JP H02174721 A JPH02174721 A JP H02174721A
- Authority
- JP
- Japan
- Prior art keywords
- chlorothricin
- lipid lowering
- lowering agent
- lipid
- active ingredient
- 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
- 239000003524 antilipemic agent Substances 0.000 title claims abstract description 11
- WUXHQHDSSKBJFH-DELKKKATSA-N chlorothricin Chemical compound COC1=CC=C(Cl)C(C)=C1C(=O)O[C@H]1[C@H](O)[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3[C@@H]4[C@H]([C@@]5(C(=O)OC=6C(=O)O[C@@]7(C=6O)C[C@@H](C)C(=C[C@H]7/C=C/CCCC[C@@H]5C=C4)C(O)=O)C)CCC3)C[C@H]2O)C)C1 WUXHQHDSSKBJFH-DELKKKATSA-N 0.000 claims abstract description 17
- 239000004480 active ingredient Substances 0.000 claims abstract description 5
- 239000001913 cellulose Substances 0.000 abstract description 5
- 229920002678 cellulose Polymers 0.000 abstract description 5
- 235000010980 cellulose Nutrition 0.000 abstract description 5
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 abstract description 4
- 239000002775 capsule Substances 0.000 abstract description 4
- 239000002552 dosage form Substances 0.000 abstract description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 abstract description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 abstract description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 abstract description 4
- 239000008187 granular material Substances 0.000 abstract description 3
- 239000000454 talc Substances 0.000 abstract description 3
- 229910052623 talc Inorganic materials 0.000 abstract description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 abstract description 2
- 229920002472 Starch Polymers 0.000 abstract description 2
- 239000011230 binding agent Substances 0.000 abstract description 2
- 239000008101 lactose Substances 0.000 abstract description 2
- 150000002632 lipids Chemical class 0.000 abstract description 2
- 239000000314 lubricant Substances 0.000 abstract description 2
- 235000019359 magnesium stearate Nutrition 0.000 abstract description 2
- 239000000546 pharmaceutical excipient Substances 0.000 abstract description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 abstract description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract description 2
- 239000008107 starch Substances 0.000 abstract description 2
- 235000019698 starch Nutrition 0.000 abstract description 2
- 239000006188 syrup Substances 0.000 abstract description 2
- 235000020357 syrup Nutrition 0.000 abstract description 2
- 239000003826 tablet Substances 0.000 abstract description 2
- 201000005577 familial hyperlipidemia Diseases 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 description 9
- 238000007796 conventional method Methods 0.000 description 5
- 208000031226 Hyperlipidaemia Diseases 0.000 description 4
- KNHUKKLJHYUCFP-UHFFFAOYSA-N clofibrate Chemical compound CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1 KNHUKKLJHYUCFP-UHFFFAOYSA-N 0.000 description 4
- 229960001214 clofibrate Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 206010003210 Arteriosclerosis Diseases 0.000 description 3
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 3
- 208000011775 arteriosclerosis disease Diseases 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 3
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 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 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 235000012239 silicon dioxide Nutrition 0.000 description 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 235000002595 Solanum tuberosum Nutrition 0.000 description 1
- 244000061456 Solanum tuberosum Species 0.000 description 1
- 241000187747 Streptomyces Species 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 235000019441 ethanol Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000002107 myocardial effect Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Landscapes
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
Description
【発明の詳細な説明】
産業上の利用分野
本発明は、脂質低下剤に関し、更に詳しくはクロロスラ
イシンを有効成分とする脂質低下剤に関する。DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to a lipid-lowering agent, and more particularly to a lipid-lowering agent containing chlorothricin as an active ingredient.
従来の技術
クロロスライシンはストレプトミセス・アンチビオティ
カス（Ｓｔｒｅｐｔｏｍｙｃｅｓ ａｎｔｉｂｉｏｔｉ
ｃｕｓ）（７）培養菌体から得られる公知の化合物であ
り、その抗菌作用及び物性がヘルベチ力・ケミ力・アク
タ（Ｈｅｌｖ、Ｃｈｉｍ、Ａｃｔａ） 、第５２巻、第
１２７〜１４２ページ（１９６９年）及び同誌第５５巻
、第２０７１〜２０９４ページ（１９７２年）に記載さ
れている。しかしながら、クロロスライシンに脂質低下
剤としての作用があることは、報告されていない。Conventional technology Chlorothricin is used for Streptomyces antibiotics
Cus) (7) It is a known compound obtained from cultured bacterial cells, and its antibacterial action and physical properties have been described in Helv, Chim, Acta, Vol. 52, pp. 127-142 (1969). ) and the same magazine, volume 55, pages 2071-2094 (1972). However, it has not been reported that chlorothricin has an action as a lipid-lowering agent.
一方、脳梗空、心筋校本などの循環器系疾患の原因とな
る動脈硬化性疾患は、近年益々増加する傾向を示し、動
脈硬化の予防と治療は社会的な急務と考えられる。動脈
硬化性疾患の最も有力な危険因子は高脂質血症であるこ
とは周知の事実であり、高脂質血症の治療により動脈硬
化を改善することが期待される。On the other hand, arteriosclerosis, which causes circulatory system diseases such as cerebral infarction and myocardial stroke, has been on the rise in recent years, and the prevention and treatment of arteriosclerosis is considered an urgent social need. It is a well-known fact that the most important risk factor for arteriosclerotic disease is hyperlipidemia, and treatment of hyperlipidemia is expected to improve arteriosclerosis.
このような高脂質血症に用いられる脂質低下剤としては
、クロフィブレート、クロフィブレートなどが知られて
いる。Clofibrate, clofibrate, and the like are known as lipid-lowering agents used for such hyperlipidemia.
発明が解決しようとする課題
しかしながら、重篤な高脂質血症患者の病態改善を目的
としたより強力な脂質低下剤がなお必要とされている。Problems to be Solved by the Invention However, there is still a need for more potent lipid-lowering agents aimed at improving the pathological condition of patients with severe hyperlipidemia.
課題を解決するだめの手段
本発明者らは、前記課題を解決すべく鋭意努力した結果
、クロロスライシンが従来の詣質低下剤より強力な脂質
低下作用を有することを見いだし、本発明を完成した。Means to Solve the Problems As a result of our earnest efforts to solve the above-mentioned problems, the present inventors discovered that chlorothricin has a more powerful lipid-lowering effect than conventional hypoxia-lowering agents, and completed the present invention. did.
すなわち、本発明はクロロスライシンを有効成分とする
脂質低下剤である。That is, the present invention is a lipid-lowering agent containing chlorothricin as an active ingredient.
クロロスライシンの投与量は、投与ルート、投与対象と
なる年齢、症状などによって適宜選定されるが、一般に
成人に対して１日に１００〜２０００ｍｇを１〜３回に
分けて経口投与する。The dosage of chlorothricin is appropriately selected depending on the administration route, the age of the subject, symptoms, etc., but in general, 100 to 2000 mg is orally administered to adults in 1 to 3 divided doses per day.
投与剤形としては、常法によりカプセル剤、錠剤、顆粒
剤、シロップ剤などの任意の剤形に加工して使用するこ
とができる。製剤化に用いることができるものとしては
、結合剤として結晶セルロース、ポリビニルピロリドン
、ヒドロキシプロピルセルロースなどであり、賦形剤と
してデンプン、乳糖などの糖類、結晶セルロース、カル
ボキシメチルセルロース、タルク、軽質無水ケイ酸など
であり、滑沢剤としてステアリン酸マグネシウム、タル
ク、ラウリル硫酸ナトリウム、流動パラフィンなどであ
る。この他、崩壊剤、安定剤、湿潤剤、界面活性剤、溶
媒なども添加することができる。As for the dosage form, it can be processed into any dosage form such as capsules, tablets, granules, syrups, etc. by conventional methods. Examples of substances that can be used for formulation include crystalline cellulose, polyvinylpyrrolidone, hydroxypropyl cellulose, etc. as binders, and starch, sugars such as lactose, crystalline cellulose, carboxymethylcellulose, talc, and light anhydrous silicic acid as excipients. Examples of lubricants include magnesium stearate, talc, sodium lauryl sulfate, and liquid paraffin. In addition, disintegrants, stabilizers, wetting agents, surfactants, solvents, etc. can also be added.
実施例 以下、本発明の実施例を示す。Example Examples of the present invention will be shown below.
（実施例１）
下記の組成でクロロスライシンを含有する錠剤を常法に
より製造した。(Example 1) Tablets containing chlorothricin with the following composition were manufactured by a conventional method.
組成 ５クロロスライシ
ン ５００低ｆｉｆｆｉ 換度ヒド
ロキシプロピルセルロース ８０結晶セルロース
１００軽質無水ケイ酸
２０１錠あたり
２０ｍｇ
（実施例２）
下記の組成でクロロスライシンを含有するカプセル剤を
常法により製造した。Composition 5 Chloroslicin 500 Low fiffi Converted hydroxypropylcellulose 80 Crystalline cellulose
100 light silicic anhydride
20mg per 201 tablets (Example 2) Capsules containing chlorothricin with the following composition were manufactured by a conventional method.
組成 弘クロロスライシ
ン ５００結晶セルロース
３００軽質無水ケイ酸
１カプセルあたり ８４０ｍｇ（実
施例３）
下記の組成でクロロスライシンを含有する顆粒剤を常法
により製造した。Composition Hirochloroslicin 500 crystalline cellulose
840 mg per capsule of 300 light anhydrous silicic acid (Example 3) Granules containing chlorothricin having the following composition were produced by a conventional method.
組成 。Composition.
クロロスライシン １０００バレイ
シヨデンブン １ｏ００ヒドロキシプ
ロピルセルロース ４゜１包あたり
０５０ｍｇ
（実施例４）
下記の組成でクロロスライシンを含有する液剤を常法に
より製造した。Chlorothricin 1000 Potato Denbun 1000 Hydroxypropyl Cellulose 4° 050 mg per package (Example 4) A liquid preparation containing Chlorothricin with the following composition was produced by a conventional method.
組成
りロロスライシン ２０００ｍｇエ
チルアルコール ２０ｒＢｌ硬化
エチレンヒマシ油
（商品名、ニラコール社製） １００ｍｇ精製水
を加えて
１００ａｔ！
発明の効果
本発明により、優れた脂質低下剤を提供することが可能
となった。Composition Rorothricin 2000mg Ethyl alcohol 20rBl Hardened ethylene castor oil (trade name, manufactured by Niracol) 100mg Add purified water to 100at! Effects of the Invention The present invention has made it possible to provide an excellent lipid-lowering agent.
試験例 次に、試験例により本発明の効果を具体的に説明する。Test example Next, the effects of the present invention will be specifically explained using test examples.
（試験例１） 脂質低下作用試験 ウィスター系ラットＳＬＣＲ−５０８（５週齢。(Test Example 1) Lipid lowering effect test Wistar rat SLCR-508 (5 weeks old).
雄性９体重１２１±７ｇ）を１群５匹として試験動物に
供した。試験薬剤はクロロスライシン並びに比較として
クロフィブレート及びクロフィブレートを使用した。Nine males weighing 121±7 g were used as test animals in groups of five. The test drugs used were chlorothricin and clofibrate and clofibrate for comparison.
上記試験薬剤を０゜２％カルボキシメチルセルロース溶
液に懸濁して体重１ｋｇあたり１００ｍｇを１日１１３
日間経口投与した。コントロールとして薬剤を含まない
０．２％カルボキシメチルセルロース溶液を用いて同様
に試験した。The above test drug was suspended in a 0.2% carboxymethyl cellulose solution and administered at a dose of 100 mg per kg of body weight per day.
Orally administered for 1 day. A similar test was conducted using a 0.2% carboxymethylcellulose solution containing no drug as a control.
投与終了後、１日絶食した後、血清中のコレステロール
量を自動分析装置（日立社製７１５０型）にて測定した
。After the administration, the subjects fasted for one day, and then the amount of cholesterol in the serum was measured using an automatic analyzer (Model 7150, manufactured by Hitachi).
その結果を第１表に示す。The results are shown in Table 1.
ｔｃｈｆｉｅｌｄ＆ １Ｊｉｌｃｏｘｏｎ）法によりＬ
Ｄ、、値を算出した。L by the tchfield & 1Jilcoxon) method.
D, value was calculated.
この結果、クロロスライシンのＬＤ、値は３１５ｍｇ／
ｋｇであった。As a result, the LD value of chlorothricin was 315 mg/
It was kg.
第 １ 表Table 1
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63330259A JPH02174721A (en) | 1988-12-27 | 1988-12-27 | Lipid lowering agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63330259A JPH02174721A (en) | 1988-12-27 | 1988-12-27 | Lipid lowering agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH02174721A true JPH02174721A (en) | 1990-07-06 |
Family
ID=18230640
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP63330259A Pending JPH02174721A (en) | 1988-12-27 | 1988-12-27 | Lipid lowering agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH02174721A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6548536B2 (en) | 1998-08-31 | 2003-04-15 | Kyowa Hakko Kogyo Co., Ltd. | Agent for inducing apoptosis |
-
1988
- 1988-12-27 JP JP63330259A patent/JPH02174721A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6548536B2 (en) | 1998-08-31 | 2003-04-15 | Kyowa Hakko Kogyo Co., Ltd. | Agent for inducing apoptosis |
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