JP2710638B2 - Pancreatic disease treatment - Google Patents
Pancreatic disease treatmentInfo
- Publication number
- JP2710638B2 JP2710638B2 JP23194388A JP23194388A JP2710638B2 JP 2710638 B2 JP2710638 B2 JP 2710638B2 JP 23194388 A JP23194388 A JP 23194388A JP 23194388 A JP23194388 A JP 23194388A JP 2710638 B2 JP2710638 B2 JP 2710638B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pancreatic disease
- disease treatment
- present
- pancreatitis
- 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.)
- Expired - Fee Related
Links
Description
【発明の詳細な説明】 〈産業上の利用分野〉 本発明は２−フェニル−1,2−ベンゾイソセレナゾー
ル−３（2H）−オン（以下、化合物Ａと称す）又はその
生理学的許容塩を含有する膵臓疾患の予防又は治療剤に
関する。DETAILED DESCRIPTION OF THE INVENTION <Industrial Application Field> The present invention relates to 2-phenyl-1,2-benzisoselenazol-3 (2H) -one (hereinafter referred to as compound A) or a physiologically acceptable salt thereof. And a prophylactic or therapeutic agent for pancreatic disease.
〈従来の技術〉 従来の膵臓疾患用剤としては、エフオーワイ（メシル
酸ガベキサート）、フサン（メシル酸ナファモスタッ
ト）、ミラクリッド（ウリナスタチン）、フオイパン
（メシル酸カモスタット）等をあげることができる。し
かしながら、これらの薬剤は未だ臨床的に充分満足でき
るものではない。<Conventional technology> Examples of conventional agents for pancreatic disease include EFOY (gabexate mesilate), fusan (nafamostat mesilate), miracrid (urinastatin), fuipane (camostat mesylate) and the like. However, these drugs are not yet clinically satisfactory.
化合物Ａはグルタチオンペルオキシダーゼ様抗酸化作
用および抗炎症作用を有することが知られている（バイ
オケミカルファーマコロジーVol.33 NO.20 3235−3239
（1984）、Vol.33 NO.20 3241−3245（1984））。しか
しながら、かかる作用は膵臓疾患の治療及び予防効果と
関連性を有するものではない。Compound A is known to have a glutathione peroxidase-like antioxidant and anti-inflammatory effect (Biochemical Pharmacology Vol. 33 NO.20 3235-3239).
(1984), Vol.33 NO.20 3241-3245 (1984)). However, such action is not related to the therapeutic and preventive effects of pancreatic disease.
〈発明が解決しようとする問題点〉 本発明者らは、新規な膵臓疾患の治療剤を見いだすべ
く鋭意検討した結果、本発明を完成した。<Problems to be Solved by the Invention> The present inventors have made intensive studies to find a novel therapeutic agent for pancreatic disease, and as a result, completed the present invention.
〈発明の構成〉 本発明は、化合物Ａ又はその生理学的許容塩を有効成
分とする膵臓疾患の予防又は治療剤に関する。<Constitution of the Invention> The present invention relates to a preventive or therapeutic agent for pancreatic disease comprising Compound A or a physiologically acceptable salt thereof as an active ingredient.
本発明にかかわる膵臓疾患については、急性又は慢性
膵炎等を好ましい治療効果を期待しうるものとしてあげ
ることができる。Regarding the pancreatic disease according to the present invention, acute or chronic pancreatitis and the like can be mentioned as those which can be expected to have a favorable therapeutic effect.
本発明にかかわる化合物Ａは、賦形剤、結合剤、崩壊
剤、溶解剤等の添加剤と共に公知の製剤技術により錠
剤、カプセル剤、散剤、顆粒剤、シロップ剤、注射剤等
の剤型とすることができる。製剤の具体的処方例を下記
に示す。Compound A according to the present invention can be used in the form of tablets, capsules, powders, granules, syrups, injections and the like by known preparation techniques together with additives such as excipients, binders, disintegrants, and dissolving agents. can do. Specific examples of the formulation are shown below.
錠剤 化合物Ａ 50mg カルボキシメチルセルロース 25mg でんぷん 5mg 結晶セルロース 40mg ステアリン酸マグネシウム 2mg 計 122mg 化合物Ａは通常経口又は非経口投与される。化合物Ａ
の投与量は、経口投与の場合成人１人当たり通常100〜2
000mg/日、好ましくは200〜1000mg/日の範囲であり、患
者の症状に応じて適宜増減すればよい。Tablets Compound A 50 mg Carboxymethyl cellulose 25 mg Starch 5 mg Crystalline cellulose 40 mg Magnesium stearate 2 mg Total 122 mg Compound A is usually orally or parenterally administered. Compound A
The dose is usually 100 to 2 per adult for oral administration
It is 000 mg / day, preferably in the range of 200 to 1000 mg / day, and may be appropriately increased or decreased according to the patient's symptoms.
化合物Ａの毒性は、マウスおよびラットに経口及び腹
腔内投与で検討した結果、下記のLD50（mg/kg）値で示
されている通り極めて低毒性のものであり、又高用量投
与時の所見として、副作用的に問題となるものは何ら認
められなかった。The toxicity of Compound A was extremely low as shown by the following LD 50 (mg / kg) as a result of oral and intraperitoneal administration to mice and rats. No findings showed any adverse side effects.
〈発明の効果〉 化合物Ａは実験的急性膵炎モデルにおける血清アミラ
ーゼ、血清リパーゼ活性の上昇を有意かつ著明に抑制し
た。該二酵素活性の上昇は膵炎の診断の指標として重要
なものであることから、化合物Ａは膵臓疾患の予防又は
治療剤として優れたものである。 <Effect of the Invention> Compound A significantly and markedly suppressed the increase in serum amylase and serum lipase activities in an experimental acute pancreatitis model. Since the increase in the bienzyme activity is important as a diagnostic index for pancreatitis, Compound A is excellent as a preventive or therapeutic agent for pancreatic disease.
以下、本発明を実施例により説明するが、本発明はこ
れに限定されるものではない。Hereinafter, the present invention will be described with reference to examples, but the present invention is not limited thereto.
実施例 セルレインにより誘発される膵炎に対する化合物Ａの効
果 Sprague−Dawley系ラット（体重190−210g、雄）を24
時間絶食の後実験に供した。膵炎はセルレイン（協和発
酵株式会社）を100μg/kg1回皮下注射することによって
作製した。Example Effect of Compound A on Caerulein-Induced Pancreatitis Sprague-Dawley rats (weighing 190-210 g, male) were treated with 24
After an hour fast, they were subjected to the experiment. Pancreatitis was prepared by injecting once subcutaneous injection of 100 μg / kg of Cerulein (Kyowa Hakko Co., Ltd.).
化合物Ａは0.5％カルボオキシメチルセルロース水溶
液（以下CMC）に懸濁し、200mg/kgをセルレイン投与後6
0分前に経口投与し、また同時に化合物Ａがグルタチオ
ンペルオキシド様活性をもつことによりこの基質である
グルタチオンを生食に溶解し250mg/kgを腹腔内投与し
た。病態対照群には同量のCMCおよび生食をそれぞれ経
口および腹腔内投与した。セルレイン投与2.5時間後
に、動物をペントバルビタール麻酔下で開腹、腹大動脈
より採血し、血清アミラーゼおよびリパーゼ測定に供し
た。血清アミラーゼはCaraway変法で測定し、Somogyi u
nit（SU）で表した。血清リパーゼはBALB−DTNB法にて
測定し、国際単位（IU）で示した。結果を表２に示し
た。Compound A was suspended in an aqueous solution of 0.5% carboxymethylcellulose (hereinafter referred to as CMC), and 200 mg / kg was administered after caerulein administration.
The compound was orally administered 0 minutes before, and at the same time, since the compound A had glutathione peroxide-like activity, this substrate, glutathione, was dissolved in a saline and 250 mg / kg was intraperitoneally administered. The disease state control group was orally and intraperitoneally administered the same amounts of CMC and saline. 2.5 hours after administration of caerulein, the animals were laparotomized under pentobarbital anesthesia, blood was collected from the abdominal aorta, and subjected to serum amylase and lipase measurement. Serum amylase was measured by the modified Caraway method.
nit (SU). Serum lipase was measured by the BALB-DTNB method and expressed in international units (IU). The results are shown in Table 2.
上表から明らかなようにセルレインによるラット膵炎
モデルにおいて化合物Ａの投与により血清リパーゼ及び
血清アミラーゼの上昇が有意に抑制された。従って、化
合物Ａが膵臓疾患に対し優れた効果を有することが確認
された。 As is clear from the above table, in the rat model of pancreatitis caused by caerulein, administration of Compound A significantly suppressed the elevation of serum lipase and serum amylase. Therefore, it was confirmed that Compound A had an excellent effect on pancreatic disease.
Claims (1)
ール−３（2H）−オンまたはその生理学的許容塩を含有
する膵臓疾患の予防又は治療剤1. A preventive or therapeutic agent for pancreatic disease containing 2-phenyl-1,2-benzisoselenazol-3 (2H) -one or a physiologically acceptable salt thereof.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP23194388A JP2710638B2 (en) | 1988-09-16 | 1988-09-16 | Pancreatic disease treatment |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP23194388A JP2710638B2 (en) | 1988-09-16 | 1988-09-16 | Pancreatic disease treatment |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0283321A JPH0283321A (en) | 1990-03-23 |
| JP2710638B2 true JP2710638B2 (en) | 1998-02-10 |
Family
ID=16931493
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP23194388A Expired - Fee Related JP2710638B2 (en) | 1988-09-16 | 1988-09-16 | Pancreatic disease treatment |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2710638B2 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000058281A1 (en) | 1999-03-31 | 2000-10-05 | Daiichi Pharmaceutical Co., Ltd. | Substrates for thioredoxin reductase |
| US10058542B1 (en) | 2014-09-12 | 2018-08-28 | Thioredoxin Systems Ab | Composition comprising selenazol or thiazolone derivatives and silver and method of treatment therewith |
-
1988
- 1988-09-16 JP JP23194388A patent/JP2710638B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0283321A (en) | 1990-03-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| LAPS | Cancellation because of no payment of annual fees |