JPH04154721A - Therapeutic agent of diabetes - Google Patents
Therapeutic agent of diabetesInfo
- Publication number
- JPH04154721A JPH04154721A JP2279977A JP27997790A JPH04154721A JP H04154721 A JPH04154721 A JP H04154721A JP 2279977 A JP2279977 A JP 2279977A JP 27997790 A JP27997790 A JP 27997790A JP H04154721 A JPH04154721 A JP H04154721A
- Authority
- JP
- Japan
- Prior art keywords
- therapeutic agent
- diabetes
- compound
- active ingredient
- bucillamine
- 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 abstract description 17
- 206010012601 diabetes mellitus Diseases 0.000 title abstract description 15
- 229940124597 therapeutic agent Drugs 0.000 title abstract description 12
- 150000003839 salts Chemical class 0.000 claims abstract description 7
- 239000004480 active ingredient Substances 0.000 claims abstract description 6
- VUAFHZCUKUDDBC-SCSAIBSYSA-N (2s)-2-[(2-methyl-2-sulfanylpropanoyl)amino]-3-sulfanylpropanoic acid Chemical compound CC(C)(S)C(=O)N[C@H](CS)C(O)=O VUAFHZCUKUDDBC-SCSAIBSYSA-N 0.000 claims abstract description 5
- 229960004272 bucillamine Drugs 0.000 claims abstract description 5
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000008280 blood Substances 0.000 abstract description 6
- 210000004369 blood Anatomy 0.000 abstract description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract description 5
- 239000008103 glucose Substances 0.000 abstract description 5
- 206010012689 Diabetic retinopathy Diseases 0.000 abstract description 2
- 201000010099 disease Diseases 0.000 abstract description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 2
- 238000009472 formulation Methods 0.000 abstract description 2
- 239000008187 granular material Substances 0.000 abstract description 2
- 239000007924 injection Substances 0.000 abstract description 2
- 238000002347 injection Methods 0.000 abstract description 2
- 239000000203 mixture Substances 0.000 abstract description 2
- 239000000843 powder Substances 0.000 abstract description 2
- 239000003826 tablet Substances 0.000 abstract description 2
- 238000007911 parenteral administration Methods 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 18
- 241000699670 Mus sp. Species 0.000 description 6
- 238000000034 method Methods 0.000 description 5
- 230000000144 pharmacologic effect Effects 0.000 description 5
- 229940079593 drug Drugs 0.000 description 4
- 206010067125 Liver injury Diseases 0.000 description 2
- 206010036790 Productive cough Diseases 0.000 description 2
- 229940124428 anticataract agent Drugs 0.000 description 2
- 239000003435 antirheumatic agent Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 231100000234 hepatic damage Toxicity 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 230000008818 liver damage Effects 0.000 description 2
- 208000024794 sputum Diseases 0.000 description 2
- 210000003802 sputum Anatomy 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 159000000001 potassium salts Chemical class 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
Abstract
Description
【発明の詳細な説明】
「産業上の利用分野」
本発明はブシラミンまたはその塩類を有効成分とする糖
尿病治療剤に関する。DETAILED DESCRIPTION OF THE INVENTION "Field of Industrial Application" The present invention relates to a therapeutic agent for diabetes containing bucillamine or its salts as an active ingredient.
「従来技術、発明が解決しようとする課題及び課題を解
決するための手段」
ブシラミンは抗リウマチ剤として医薬品に用いられてお
り、他にも喀痰溶解剤、肝障害抑制剤、抗白内障剤とし
て有用であることが報告されている（特公昭５６−５３
８８号、特公昭６０−１１８８８号、特公昭６２−４３
９２２号、特公昭６３−１３９６４号）。"Prior art, problems to be solved by the invention, and means for solving the problems" Bucillamine is used in medicine as an anti-rheumatic agent, and is also useful as a sputum dissolver, a liver damage inhibitor, and an anti-cataract agent. It has been reported that
No. 88, Special Publication No. 11888, Special Publication No. 60-11888, Special Publication No. 11888, Special Publication No. 62-43
No. 922, Special Publication No. 63-13964).
本発明者等は優れた薬効を有する化合物であるプシラミ
ンについて、さらに新しい薬理作用を見つけるべく種々
検討した結果、糖尿病治療剤として有用であることを見
い出した。The present inventors conducted various studies to discover new pharmacological effects on psillamine, which is a compound with excellent medicinal efficacy, and found that it is useful as a therapeutic agent for diabetes.
「発明の構成」
本発明は下記式で示されるプシラミンまたはその塩類（
以下本化合物という）を有効成分とする糖尿病治療剤に
関する。"Structure of the Invention" The present invention relates to psilamine or a salt thereof represented by the following formula (
The present invention relates to a therapeutic agent for diabetes containing a compound (hereinafter referred to as the present compound) as an active ingredient.
Ｈｓ
ＣＩ（３−Ｃ−ＣＯＮ ＨＣＨＣＯＯＨ晶 ＣＨ２５
Ｈ
本発明における塩類とは、医薬として許容される塩であ
ればよく、ナトリウム塩、カリウム塩等が例として挙げ
られる。Hs CI (3-C-CON HCHCOOH crystal CH25
H The salts in the present invention may be any pharmaceutically acceptable salts, and examples thereof include sodium salts, potassium salts, and the like.
本化合物が抗リウマチ剤、喀痰溶解剤、肝障害抑制剤、
抗白内障剤として有用であることが報告されている。This compound is an anti-rheumatic agent, a sputum solubilizer, a liver damage inhibitor,
It has been reported to be useful as an anti-cataract agent.
本発明者等は、このように医薬として優れた性質を有す
る本化合物のさらに新しい薬理作用を見つけるべく種々
検討した結果、糖尿病治療剤として有用であることを見
い出した。The present inventors conducted various studies to discover new pharmacological effects of the present compound, which has such excellent properties as a medicinal agent, and found that the compound is useful as a therapeutic agent for diabetes.
糖尿病に対する薬物の有用性を調べる方法として、スト
レプトシト７ンで惹起した糖尿病マウスに薬物を投与す
る方法が知られている Ｉ’Ｆｕｊｉｉａｔ ａｌ、、
Ｊｐｎ、 Ｊ、 Ｐｈａｒｍａｅｏｌ、＋ ３４ 、
１１３（１９８４））。そこで、このモデルを用いて
本化合物の有用性を調べた。As a method to examine the usefulness of drugs for diabetes, there is a known method of administering drugs to diabetic mice induced with streptocytone.
Jpn, J, Pharmaeol, +34,
113 (1984)). Therefore, we investigated the usefulness of this compound using this model.
詳細な結果については薬理試験の項で述べるが、本化合
物をマウスに投与したものは、コントロールと比較して
明らかに血液中のグルコース量が減少しており、本化合
物が糖尿病の治療剤として有用であることが実証された
。Detailed results will be discussed in the pharmacological test section, but when this compound was administered to mice, the amount of glucose in the blood clearly decreased compared to controls, making this compound useful as a therapeutic agent for diabetes. It has been proven that
尚、本発明における糖尿病治療剤とは、糖尿病性網膜症
のように糖尿病に起因するいろいろな疾患の治療剤をも
包含するものである。Note that the therapeutic agent for diabetes in the present invention includes therapeutic agents for various diseases caused by diabetes, such as diabetic retinopathy.
本化合物は経口投与、非経口投与のいずれでも投与する
ことができ、公知の製剤技術により錠剤、顆粒剤、散剤
、注射剤等の製剤とすることができる。The present compound can be administered either orally or parenterally, and can be formulated into tablets, granules, powders, injections, and the like using known formulation techniques.
本化合物の投与量は症状、剤型、年令等によって決めら
れるが、経口投与の場合、通常１日１０〜ｌｏ００ｍｇ
を１回または数回に分けて投与すればよい。The dosage of this compound is determined depending on symptoms, dosage form, age, etc., but in the case of oral administration, it is usually 10 to 100 mg per day.
may be administered once or in several doses.
糖呆病九対する薬物の有用性を調ベア已方法として、ス
トレプトシトシンで惹起した糖尿病マウスに薬物を投与
する方法が知られている（Ｆｕｊｉｉｅｔ ａｌ、、
Ｊｐｎ、 Ｊ、 Ｐｈａｒｍａｅｏｌ、＋ ３４．
１１３（１９８４））。そこで、このモデルを用いて本
化合物の有用性を調べた。As a method to test the effectiveness of drugs against diabetes mellitus, a method is known in which drugs are administered to diabetic mice induced with streptocytosine (Fujiie et al.
Jpn, J, Pharmaeol, +34.
113 (1984)). Therefore, we investigated the usefulness of this compound using this model.
（実験方法）
上記の文献に準じ、本化合物の投与量が１０ｍｇ／ｋｇ
となるように餌に混ぜてＩＣＲ系マウス（１群６匹）Ｋ
投与し、ストレプトシトシンは生理食塩液に溶解したも
のを投与開始より５日間４０ｍｇ／ｋｇ腹腔内投与した
。本化合物投与８日および１５日後にマウスより採血を
行ない、血液中のグルコース量を定量した。なお、コン
トロールとしては本化合物を投与せず、ストレプトシト
シンのみを投与したものを用いた。(Experimental method) According to the above literature, the dose of this compound was 10 mg/kg.
ICR mice (6 mice per group) were mixed with food so that
Streptocytosine was dissolved in physiological saline and administered intraperitoneally at a dose of 40 mg/kg for 5 days from the start of administration. Blood was collected from the mice 8 and 15 days after administration of the present compound, and the amount of glucose in the blood was determined. As a control, the present compound was not administered, and only streptocytosine was administered.
（結果） 得られた結果を表に示す。(result) The results obtained are shown in the table.
１コントロ一ル群１ １９９ １ ４１０ １表に
示すように、本化合物を投与したものはコントロールと
比較して明らかに血液中のグルコース量が減少した。1 Control Group 1 199 1 410 1 As shown in Table 1, the amount of glucose in the blood of those administered with this compound was clearly reduced compared to the control.
「発明の効果」
薬理試験の結果で示されるように、本化合物は血液中の
グルコース量を減少させる作用を有すること〃菖ら、本
化合物が糖尿病治療剤として有用であることが明らかと
なった。"Effect of the Invention" As shown by the results of pharmacological tests, this compound has the effect of reducing the amount of glucose in the blood.It has become clear that this compound is useful as a therapeutic agent for diabetes. .
Claims (1)
剤。A antidiabetic agent containing bucillamine or its salts as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP27997790A JP2816499B2 (en) | 1990-10-17 | 1990-10-17 | Diabetes treatment |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP27997790A JP2816499B2 (en) | 1990-10-17 | 1990-10-17 | Diabetes treatment |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH04154721A true JPH04154721A (en) | 1992-05-27 |
| JP2816499B2 JP2816499B2 (en) | 1998-10-27 |
Family
ID=17618586
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP27997790A Expired - Fee Related JP2816499B2 (en) | 1990-10-17 | 1990-10-17 | Diabetes treatment |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2816499B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6576668B1 (en) | 1999-06-21 | 2003-06-10 | Santen Pharmaceutical Co., Ltd. | Remedies for arthrosis deformans |
-
1990
- 1990-10-17 JP JP27997790A patent/JP2816499B2/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6576668B1 (en) | 1999-06-21 | 2003-06-10 | Santen Pharmaceutical Co., Ltd. | Remedies for arthrosis deformans |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2816499B2 (en) | 1998-10-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |