JPS58216119A - Antiulcer agent - Google Patents
Antiulcer agentInfo
- Publication number
- JPS58216119A JPS58216119A JP10006782A JP10006782A JPS58216119A JP S58216119 A JPS58216119 A JP S58216119A JP 10006782 A JP10006782 A JP 10006782A JP 10006782 A JP10006782 A JP 10006782A JP S58216119 A JPS58216119 A JP S58216119A
- Authority
- JP
- Japan
- Prior art keywords
- antiulcer agent
- ulcer
- capsimycin
- active component
- agent
- 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
Landscapes
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
本発明はカゾシマイシンを有効成分とする新規な抗潰瘍
剤に関する。カブシマイシンは、従来キゅうりの灰色疫
病、立枯病に有効な抗生物質として知られ【いたのみで
、薬理作用については、全く知られていなかった化合物
である。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a novel anti-ulcer agent containing casocimycin as an active ingredient. Kabushimycin is a compound that has only been known as an antibiotic effective against gray late blight and damping-off of cucumbers, but its pharmacological effects were completely unknown.
本発明者らは、このカブシマイシンの薬理活性について
鋭意検討をおこなっていたところ、該化合物が極めて優
れた抗潰瘍作用を示す事を見い出し本発明を完成した。The present inventors have conducted extensive studies on the pharmacological activity of this kabushimycin, and have discovered that this compound exhibits an extremely excellent anti-ulcer effect, and have completed the present invention.
すなわち、本発明は次の式(1)、
で表わされるカブシマイシンを有効成分とする抗潰瘍剤
を提供するものである。That is, the present invention provides an anti-ulcer agent containing kabushimycin represented by the following formula (1) as an active ingredient.
本発明のカブシマイシンは分子式C,oH,,N20゜
分子量524.64、融点186℃(分ps)の無色針
状の結晶で、クロロホルム、ピリジンに可溶、エーテル
、ベンゼン、n−へキサン、水に不溶の酸性化合物であ
り、例えば特開昭55−310号に開示のN1#法によ
り賽易に製造される。Kabushimycin of the present invention is a colorless needle-like crystal with a molecular formula of C, oH,, N20°, a molecular weight of 524.64, and a melting point of 186°C (min ps), and is soluble in chloroform, pyridine, ether, benzene, n-hexane, and water. It is an acidic compound that is insoluble in, and can be easily produced, for example, by the N1# method disclosed in JP-A No. 55-310.
以下にカブシマイレンの抗潰瘍効果を示す。The anti-ulcer effect of Kabushimaren is shown below.
(1) インドメタシン潰瘍に対する効果体重180
〜200yの7週令のドンリュウ系雄性ラット1群6匹
を使用し、48時間絶食後、カブシマイレンをジメチル
スルホキシドを5チ加えた生理食塩液に溶解して検体と
し、その所定量を経口投与した。(1) Effect of indomethacin on ulcer weight 180
A group of 6 male Donryu rats, aged ~200 y and 7 weeks old, were used, and after fasting for 48 hours, Kabushima Ren was dissolved in physiological saline containing 5 g of dimethyl sulfoxide to prepare a sample, and a predetermined amount of the sample was orally administered. .
1時間後、インドメタシンを25号勺経口投与し、5時
間後に2チブリリアントプルー溶液を静脈内に投与して
胃を摘出した。冑を切開し、生成した潰瘍部位の長径を
測り、合計して得た数値(in)を潰瘍係数とした。One hour later, indomethacin was orally administered using a No. 25 tube, and 5 hours later, a 2-tibrilliant blue solution was administered intravenously, and the stomach was removed. The helmet was incised, the long axis of the generated ulcer site was measured, and the total value (in) was taken as the ulcer coefficient.
結果を第1表に示す。The results are shown in Table 1.
(2) ストレス潰瘍に対する効果
体重23〜26gの5週令ddY系雄性マウス1群8匹
を使用し、カブシマイレンな、ジメチルスルホキシドな
5%加えた生理食塩液に溶解して検体とし、その所定量
を経口投与した。マウスを垂直に保持し、首部まで水温
26℃の水槽中に沈め8時間放置した。2チプIJ 1
7アントプルー溶液を静脈内に投与した後、胃な摘出し
潰瘍生成の有無を調べた。結果を石2表に示す。(2) Effect on stress ulcers A group of eight 5-week-old ddY male mice weighing 23 to 26 g were used as a sample by dissolving them in a physiological saline solution containing 5% dimethyl sulfoxide and a predetermined amount of the sample. was administered orally. The mice were held vertically and submerged up to their necks in a water bath with a water temperature of 26°C for 8 hours. 2 chips IJ 1
After intravenously administering the 7antoplue solution, the stomachs were removed and examined for the presence or absence of ulcer formation. The results are shown in Table 2.
以上の如くカブシマイレンは、実験潰瘍に対し、極めて
優れた防止効果を示−1”、 Lかも、カブシマイレン
の毒性は、LD50 : 600〜700 Ill/に
9(マウス、経口投与)であり、安全な薬物である。As mentioned above, Kabushima Ren has an extremely excellent preventive effect on experimental ulcers. It's a drug.
次に本発明抗潰瘍剤の投与方法及び投与量を示す。Next, the administration method and dosage of the anti-ulcer agent of the present invention will be shown.
投与方法は、錠剤、カプセル剤、顆粒剤、シロップ剤等
による経口投与が好ましい。As for the administration method, oral administration using tablets, capsules, granules, syrups, etc. is preferred.
投与量は、通常、成人において、経口投与量としてo、
o i〜100η/匈が適当である。・これを1日1回
ないし数回に分けて服用する。The dosage is usually o, as an oral dose in adults.
o i~100η/匈 is suitable.・Take this once a day or in divided doses.
経口用剤とするには、通常の製造方法に従って製造し得
る。即ち、デンプン、乳糖、マンニトール等の試製剤、
カルボキシメチルセルロースナトリウム、ヒドロキシプ
ロピルセルロース等ノ結合剤、結晶セルロース、カルざ
キシメチルセルロースカルシウム等の崩壊剤、メルク、
ステアリン酸マグネシウム等の滑沢剤、軽質無水ケイ酸
等の流動性向上剤等を適宜組み仕せて処方することによ
り、錠剤、カプセル剤、顆粒剤等な製造し得る。Oral preparations can be manufactured according to conventional manufacturing methods. That is, test preparations of starch, lactose, mannitol, etc.
Binders such as carboxymethyl cellulose sodium and hydroxypropyl cellulose, disintegrants such as crystalline cellulose and carboxymethyl cellulose calcium, Merck,
Tablets, capsules, granules, etc. can be manufactured by appropriately combining and formulating a lubricant such as magnesium stearate, a fluidity improver such as light anhydrous silicic acid, and the like.
次に実施例を挙げ本発明の抗潰瘍剤を説明する。Next, the antiulcer agent of the present invention will be explained with reference to Examples.
実施例1 錠剤 常法により、下記成分・分量の錠剤1個を製造した。Example 1 Tablet One tablet with the following ingredients and quantities was manufactured by a conventional method.
カブシマイレン 1009D−マ/二1
・−ル 150結晶セルロース
50デ/デフ28
カルボキシメチルセルロース 16カルシウム
タルク 4
全 ml 350■実施例2
カプセル剤
常法により、下記成分・分量の顆粒を製造し、これな3
号カプセル1個に充填してカプセル剤な製造した。Kabushimiren 1009D-Ma/21
・-Rule 150 crystalline cellulose
50 de/def 28 carboxymethylcellulose 16 calcium talc 4 total ml 350■Example 2
CapsulesProduce granules with the following ingredients and amounts using a conventional method.
A capsule was manufactured by filling one No. 1 capsule.
カブシマイレン 259 結晶セルロース 17呼 軽質無水ケイM 79Kabushimiren 259 Crystalline cellulose 17 types Light anhydrous silicone M 79
Claims (1)
潰瘍剤。An anti-ulcer agent whose active ingredient is kabushimycin represented by the following formula.
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP10006782A JPS58216119A (en) | 1982-06-11 | 1982-06-11 | Antiulcer agent |
GB08310454A GB2120098A (en) | 1982-04-30 | 1983-04-18 | Antiulcer drugs comprising ikarugamycin or capsimycin |
IT48172/83A IT1167631B (en) | 1982-04-30 | 1983-04-28 | IKARUGAMYCIN AND CAPSIMYCIN-BASED ANTI-ULCER DRUG |
DE19833315674 DE3315674A1 (en) | 1982-04-30 | 1983-04-29 | ANTIULCUS AGENT |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP10006782A JPS58216119A (en) | 1982-06-11 | 1982-06-11 | Antiulcer agent |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS58216119A true JPS58216119A (en) | 1983-12-15 |
Family
ID=14264114
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP10006782A Pending JPS58216119A (en) | 1982-04-30 | 1982-06-11 | Antiulcer agent |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS58216119A (en) |
-
1982
- 1982-06-11 JP JP10006782A patent/JPS58216119A/en active Pending
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