JPH0717853A - Therapeutic agent for hyperlipemia - Google Patents
Therapeutic agent for hyperlipemiaInfo
- Publication number
- JPH0717853A JPH0717853A JP22038893A JP22038893A JPH0717853A JP H0717853 A JPH0717853 A JP H0717853A JP 22038893 A JP22038893 A JP 22038893A JP 22038893 A JP22038893 A JP 22038893A JP H0717853 A JPH0717853 A JP H0717853A
- Authority
- JP
- Japan
- Prior art keywords
- therapeutic agent
- synephrine
- active ingredient
- cellulose
- methyl cellulose
- 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.)
- Granted
Links
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 229940124597 therapeutic agent Drugs 0.000 title claims abstract description 14
- 201000005577 familial hyperlipidemia Diseases 0.000 title 1
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- 229960003684 oxedrine Drugs 0.000 claims abstract description 11
- 239000004480 active ingredient Substances 0.000 claims abstract description 7
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 13
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 abstract description 9
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- 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
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- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 1
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- 210000002966 serum Anatomy 0.000 description 1
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Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は高脂血症治療剤に関す
る。TECHNICAL FIELD The present invention relates to a therapeutic agent for hyperlipidemia.
【０００２】[0002]
【従来の技術】血液中の脂質濃度は動脈硬化と密接な関
係にあり、高脂血症が続くと各臓器ことに心臓、脳、お
よび肝臓の血管の硬化を起こす。血中脂質特に、コレス
テロールとトリグリセライドの増加は危険因子となって
いる。2. Description of the Related Art The lipid concentration in blood is closely related to arteriosclerosis, and if hyperlipidemia continues, hardening of blood vessels of each organ, especially the heart, brain and liver, occurs. Increased blood lipids, especially cholesterol and triglycerides, are risk factors.
【０００３】血中脂質は、カイミクロン（乳状脂粒）、
極低密度リポタンパク質（ＶＬＤＬ）、低密度タンパク
質（ＬＤＬ）、高密度タンパク質（ＨＤＬ）に分類され
ている。Blood lipids are kaimicron (milky fat granules),
It is classified into very low density lipoprotein (VLDL), low density protein (LDL) and high density protein (HDL).
【０００４】これらの血中脂質の状況により高脂血症は
６型に分類されている。Ｉ型は食事療法で対処されてい
るが、ＩＩ型以上の重篤な場合にはクロフィブレートな
どの薬剤による治療が必要とされている。[0004] Hyperlipidemia is classified into type 6 according to the status of these blood lipids. Type I is being treated with diet, but treatment with drugs such as clofibrate is required in severe cases of type II and above.
【０００５】従って、高脂血症治療剤はこれらの病態に
有効であるため、今まで種々の薬剤が開発されてきてい
る。これら従来の薬剤は副作用が少ないとされてはいた
が、種々の疑問が副作用と臨床効果の両面において出さ
れている。副作用としては、白血球減少、肝障害、筋痛
などの諸症状がある。高脂血症治療剤は長期間服用する
ためより安全な薬剤が望まれている。Therefore, since a therapeutic agent for hyperlipidemia is effective for these pathological conditions, various agents have been developed so far. Although it has been said that these conventional drugs have few side effects, various questions have been raised regarding both side effects and clinical effects. Side effects include various symptoms such as leukopenia, liver damage and myalgia. Since a hyperlipidemia therapeutic agent is taken for a long period of time, a safer drug is desired.
【０００６】また、シネフリンは化学名を４−ヒドロキ
シ−α−［（メチルアミノ）メチル］−ベンゼンメタノ
ールといい、古くから知られている公知化合物〔メルク
インデックス 第７版 〕である。Synephrine has a chemical name of 4-hydroxy-α-[(methylamino) methyl] -benzenemethanol and is a known compound [Merck Index 7th edition] which has been known for a long time.
【０００７】その薬理作用についてはアドレナリン様血
圧降下作用が知られているが、脂質代謝改善作用につい
ては知られていない。Regarding its pharmacological action, an adrenaline-like hypotensive action is known, but its lipid metabolism improving action is not known.
【０００８】[0008]
【発明が解決しようとする課題】本発明の目的は、長期
服用しても安全な高脂血症治療剤を提供することであ
る。SUMMARY OF THE INVENTION An object of the present invention is to provide a therapeutic agent for hyperlipidemia which is safe even if taken for a long time.
【０００９】[0009]
【課題を解決するための手段】本発明者らは、前記目的
の達成のために多数の化合物について種々検討した結
果、シネフリンが有意に血中コレステロール、トリグリ
セライドを低下させることを見いだし、更にその知見に
基づき本発明を完成するに至った。Means for Solving the Problems As a result of various investigations on a large number of compounds for achieving the above-mentioned object, the present inventors have found that synephrine significantly lowers blood cholesterol and triglyceride, and further findings Based on this, the present invention has been completed.
【００１０】即ち本発明は、式（Ｉ）That is, the present invention has the formula (I)
【００１１】 [0011]
【００１２】で表されるシネフリンを有効成分として含
有することを特徴とする高脂血症治療剤である。[0012] A therapeutic agent for hyperlipidemia, which comprises the synephrine represented by the following as an active ingredient.
【００１３】本発明の高脂血症治療剤の有効成分である
シネフリンは、西ドイツ特許５６６，５７８号明細書に
示される既知の化合物である。Synephrine, which is an active ingredient of the therapeutic agent for hyperlipidemia of the present invention, is a known compound shown in West German Patent No. 566,578.
【００１４】本発明の高脂血症治療剤は、下記に示すご
とく経口製剤の形態で用いられる。The therapeutic agent for hyperlipidemia of the present invention is used in the form of an oral preparation as shown below.
【００１５】すなわち、賦形剤、崩壊剤、結合剤、滑沢
剤、坑酸化剤、コーティング剤、着色剤、矯味矯臭剤、
界面活性剤、可塑剤などを混合して、顆粒剤、散剤、カ
プセル剤、錠剤として投与され得る。That is, excipients, disintegrants, binders, lubricants, antioxidants, coating agents, coloring agents, flavoring agents,
It can be administered as a granule, a powder, a capsule or a tablet by mixing a surfactant, a plasticizer and the like.
【００１６】上記製剤化するに際しては、通常の製剤化
の方法が使用できる。In formulating the above-mentioned preparation, an ordinary preparation method can be used.
【００１７】賦形剤としては、たとえばマンニトール、
キシリトール、ソルビトール、ブドウ糖、白糖、乳糖、
結晶セルロース、結晶セルロース・カルボキシメチルセ
ルロースナトリウム、りん酸水素カルシウム、コムギデ
ンプン、コメデンプン、トウモロコシデンプン、バレイ
ショデンプン、カルボキシメチルスターチナトリウム、
デキストリン、α−シクロデキストリン、β−シクロデ
キストリン、カルボキシビニルポリマー、軽質無水ケイ
酸、酸化チタン、メタケイ酸アルミン酸マグネシウム、
ポリエチレングリコール、中鎖脂肪酸トリグリセリドな
どが挙げられる。Examples of the excipient include mannitol,
Xylitol, sorbitol, glucose, sucrose, lactose,
Crystalline cellulose, crystalline cellulose / sodium carboxymethylcellulose, calcium hydrogen phosphate, wheat starch, rice starch, corn starch, potato starch, sodium carboxymethyl starch,
Dextrin, α-cyclodextrin, β-cyclodextrin, carboxyvinyl polymer, light anhydrous silicic acid, titanium oxide, magnesium aluminometasilicate,
Examples thereof include polyethylene glycol and medium chain fatty acid triglyceride.
【００１８】崩壊剤としては、低置換度ヒドロキシプロ
ピルセルロース、カルボキシメチルセルロース、カルボ
キシメチルセルロースカルシウム、カルボキシメチルセ
ルロースナトリウム、クロスカルメロースナトリウム・
Ａ型（アクチゾル）、デンプン、結晶セルロース、ヒド
ロキシプロピルスターチ、部分アルファー化デンプンな
どが挙げられる。As the disintegrant, low-substituted hydroxypropyl cellulose, carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, croscarmellose sodium.
Type A (actisol), starch, crystalline cellulose, hydroxypropyl starch, partially pregelatinized starch and the like can be mentioned.
【００１９】結合剤としては、たとえばメチルセルロー
ス、ヒドロキシプロピルセルロース、ヒドロキシプロピ
ルメチルセルロース、ポリビニールピロリドン、ゼラチ
ン、アラビアゴム、エチルセルロース、ポリビニルアル
コール、プルラン、アルファー化デンプン、寒天、タラ
ガント、アルギン酸ナトリウム、アルギン酸プロピレン
グリコールエステルなどが挙げられる。Examples of the binder include methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, gelatin, gum arabic, ethylcellulose, polyvinyl alcohol, pullulan, pregelatinized starch, agar, taragant, sodium alginate, propylene glycol alginate. And so on.
【００２０】滑沢剤としては、たとえばステアリン酸、
ステアリン酸マグネシウム、ステアリン酸カルシウム、
ステアリン酸ポリオキシル、セタノール、タルク、硬化
油、ショ糖脂肪酸エステル、ジメチルポリシロキサン、
マイクロクリスタリンワックス、ミツロウ、サラシミツ
ロウなどが挙げられる。As the lubricant, for example, stearic acid,
Magnesium stearate, calcium stearate,
Polyoxyl stearate, cetanol, talc, hydrogenated oil, sucrose fatty acid ester, dimethyl polysiloxane,
Examples include microcrystalline wax, beeswax, and beeswax.
【００２１】抗酸化剤としては、たとえばジブチルヒド
ロキシトルエン（ＢＨＴ）、没食子酸プロピル、ブチル
ヒドロキシアニソール（ＢＨＡ）、α−トコフェロー
ル、クエン酸などが挙げられる。Examples of the antioxidant include dibutylhydroxytoluene (BHT), propyl gallate, butylhydroxyanisole (BHA), α-tocopherol and citric acid.
【００２２】コーティング剤としては、たとえばヒドロ
キシプロピルメチルセルロース、ヒドロキシプロピルセ
ルロース、メチルセルロース、エチルセルロース、ヒド
ロキシプロピルメチルセルロースフタレート、ヒドロキ
シプロピルメチルセルロースアセテートサクシネート、
カルボキシメチルエチルセルロース、酢酸フタル酸セル
ロース、ポリビニルアセタールジエチルアミノアセテー
ト、アミノアルキルメタアクリレートコポリマー、ヒド
ロキシプロピルメチルセルロースアセテートサクシネー
ト、メタアクリル酸コポリマー、セルロースアセテート
トリメリテート（ＣＡＴ）、ポリビニルアセテートフタ
レート、セラックなどが挙げられる。As the coating agent, for example, hydroxypropylmethylcellulose, hydroxypropylcellulose, methylcellulose, ethylcellulose, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate,
Carboxymethyl ethyl cellulose, cellulose acetate phthalate, polyvinyl acetal diethylaminoacetate, aminoalkylmethacrylate copolymer, hydroxypropylmethylcellulose acetate succinate, methacrylic acid copolymer, cellulose acetate trimellitate (CAT), polyvinyl acetate phthalate, shellac and the like. .
【００２３】着色剤としては、たとえばタール色素、酸
化チタンなどが挙げられる。Examples of colorants include tar dyes and titanium oxide.
【００２４】矯味矯臭剤としては、クエン酸、アジピン
酸、アスコルビン酸、メントールなどが挙げられる。Examples of the corrigent include citric acid, adipic acid, ascorbic acid, menthol and the like.
【００２５】界面活性剤としては、たとえばポリオキシ
エチレン硬化ヒマシ油、モノステアリン酸グリセリン、
モノステアリン酸ソルビタン、モノパルミチン酸ソルビ
タン、モノラウリン酸ソルビタン、ポリオキシエチレン
ポリオキシプロピレンブロックコポリマー、ポリソルベ
ート類、ラウリル硫酸ナトリウム、マクロゴール類、シ
ョ糖脂肪酸エステルなどが挙げられる。Examples of the surfactant include polyoxyethylene hydrogenated castor oil, glyceryl monostearate,
Examples thereof include sorbitan monostearate, sorbitan monopalmitate, sorbitan monolaurate, polyoxyethylene polyoxypropylene block copolymer, polysorbates, sodium lauryl sulfate, macrogols and sucrose fatty acid ester.
【００２６】可塑剤としては、クエン酸トリエチル、ト
リアセチン、セタノールなどが挙げられる。Examples of the plasticizer include triethyl citrate, triacetin, cetanol and the like.
【００２７】本発明の高脂血症治療剤の有効成分である
シネフリンは、成人に対し１日当り１ｍｇ〜１０００ｍ
ｇ、好ましくは１０ｍｇ〜６００ｍｇ投与する。Synephrine, the active ingredient of the therapeutic agent for hyperlipidemia of the present invention, is 1 mg to 1000 m per day for an adult.
g, preferably 10 mg to 600 mg.
【発明の効果】本発明の高脂血症治療剤の有効成分であ
るシネフリンは、血中の中性脂肪、トリグリセライド、
およびコレステロールを低下させる作用を示すので高脂
血症治療剤として有用である。EFFECTS OF THE INVENTION Synephrine, which is an active ingredient of the therapeutic agent for hyperlipidemia of the present invention, comprises neutral fat in blood, triglyceride,
It also has the effect of lowering cholesterol and is useful as a therapeutic agent for hyperlipidemia.
【００２８】[0028]
【００２９】試験例１Test Example 1
【００３０】（試験食） 検体１；表１に示す餌にシネフリン０．１％含有させた
試験食 検体２；表１に示す餌にシネフリン０．５％含有させた
試験食 対照検体；表１に示す試験食(Test food) Specimen 1; Test food containing 0.1% synephrine in the diet shown in Table 1; Sample 2; Test food containing 0.5% synephrine in the diet shown in Table 1 Control sample; Table 1 Test meal shown in
【００３１】[0031]
【表１】 [Table 1]
【００３２】（試験動物）ウイスター系雄性ラット（４
週齢、体重６０〜７０ｇ） ３群１８匹 （試験方法）ラットを金網飼育ケージに１匹ずつ飼育し
た（室温２３度）。(Test animal) Wistar male rat (4
(Age, week weight, 60-70 g) 18 animals in 3 groups (Test method) Rats were bred one by one in a wire mesh cage (room temperature 23 ° C).
【００３３】１群６匹づつ３群に分け、各群のラットに
試験食（検体１，２，対照検体）および水を１４日間自
由に摂取させた。摂取量は、毎日、体重は１日おきに測
定した。飼育終了後、臓器重量を測定し、肝臓および血
清中の脂質濃度を測定した。Each group was divided into 3 groups of 6 animals, and the rats in each group were allowed to freely ingest the test diet (samples 1, 2 and control sample) and water for 14 days. Intake was measured daily and body weight was measured every other day. After the rearing, the organ weight was measured and the lipid concentrations in the liver and serum were measured.
【００３４】（結果）結果を表２〜９に示す。(Results) The results are shown in Tables 2-9.
【００３５】[0035]
【表２】 [Table 2]
【００３６】[0036]
【表３】 [Table 3]
【００３７】[0037]
【表４】 [Table 4]
【００３８】[0038]
Claims (1)
特徴とする高脂血症治療剤。1. A formula A therapeutic agent for hyperlipidemia, which comprises a synephrine represented by the following as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP22038893A JP3502951B2 (en) | 1993-07-06 | 1993-07-06 | Hyperlipidemia treatment |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP22038893A JP3502951B2 (en) | 1993-07-06 | 1993-07-06 | Hyperlipidemia treatment |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0717853A true JPH0717853A (en) | 1995-01-20 |
| JP3502951B2 JP3502951B2 (en) | 2004-03-02 |
Family
ID=16750342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP22038893A Expired - Fee Related JP3502951B2 (en) | 1993-07-06 | 1993-07-06 | Hyperlipidemia treatment |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3502951B2 (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998053798A1 (en) * | 1997-05-27 | 1998-12-03 | Takeda Chemical Industries, Ltd. | Solid pharmaceutical preparation |
| US7070805B2 (en) | 1998-07-28 | 2006-07-04 | Takeda Pharmaceutical Company Limited | Rapidly disintegrable solid preparation |
| US7431942B2 (en) | 1998-05-18 | 2008-10-07 | Takeda Pharmaceutical Company Limited | Orally disintegrable tablets |
| CN100440991C (en) * | 1997-04-10 | 2008-12-03 | 高通股份有限公司 | Method and system for handling telephone communications to or from a subscriber unit |
| US7670624B2 (en) | 2004-01-29 | 2010-03-02 | Astella Pharma Inc. | Gastrointestinal-specific multiple drug release system |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1587638A (en) | 1977-06-03 | 1981-04-08 | Berema Sa | Iodophenoxyphenylalkenoic acid derivatives and pharmaceutical preparations containing them |
-
1993
- 1993-07-06 JP JP22038893A patent/JP3502951B2/en not_active Expired - Fee Related
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100440991C (en) * | 1997-04-10 | 2008-12-03 | 高通股份有限公司 | Method and system for handling telephone communications to or from a subscriber unit |
| WO1998053798A1 (en) * | 1997-05-27 | 1998-12-03 | Takeda Chemical Industries, Ltd. | Solid pharmaceutical preparation |
| US6299904B1 (en) | 1997-05-27 | 2001-10-09 | Takeda Chemical Industries, Ltd. | Solid pharmaceutical preparation |
| US6586004B2 (en) | 1997-05-27 | 2003-07-01 | Takeda Chemical Industries, Ltd. | Solid preparation |
| US7431942B2 (en) | 1998-05-18 | 2008-10-07 | Takeda Pharmaceutical Company Limited | Orally disintegrable tablets |
| US7875292B2 (en) | 1998-05-18 | 2011-01-25 | Takeda Pharmaceutical Company Limited | Orally disintegrable tablets |
| US9901546B2 (en) | 1998-05-18 | 2018-02-27 | Takeda Pharmaceutical Company Limited | Orally disintegrable tablets |
| US7070805B2 (en) | 1998-07-28 | 2006-07-04 | Takeda Pharmaceutical Company Limited | Rapidly disintegrable solid preparation |
| US7670624B2 (en) | 2004-01-29 | 2010-03-02 | Astella Pharma Inc. | Gastrointestinal-specific multiple drug release system |
Also Published As
| Publication number | Publication date |
|---|---|
| JP3502951B2 (en) | 2004-03-02 |
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