JPH0518810B2 - - Google Patents
Info
- Publication number
- JPH0518810B2 JPH0518810B2 JP4429884A JP4429884A JPH0518810B2 JP H0518810 B2 JPH0518810 B2 JP H0518810B2 JP 4429884 A JP4429884 A JP 4429884A JP 4429884 A JP4429884 A JP 4429884A JP H0518810 B2 JPH0518810 B2 JP H0518810B2
- Authority
- JP
- Japan
- Prior art keywords
- nifedipine
- present
- ulcer agent
- gastric
- dimethyl
- 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 - Lifetime
Links
Landscapes
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】
本発明は、ニフエジピン（nifedipine）の一般
名称で知られいている１，４−ジヒドロ−２，６
−ジメチル−４−（２−ニトロフエニル）−３，５
−ピリジンジカルボキシリツクアシドジメチルエ
ステルの新規医薬用途に関するものである。
ニフエジピンは、化学式（Ｉ）によつて示され
る結晶性の化合物であつて、現在、血圧降下剤と
して広く使用されている薬剤である。
ニフエジピンは、その作用機序から、カルシウ
ムイオン結抗剤といわれているものであり
血管平滑筋を弛緩することにより、血圧低下作
用を発現するものと一般に認められておりその他
の薬効については、未だ殆んど知られていないの
が現状である。本願発明者は、ニフエジピンの薬
効を追求していた際、驚くべきことに、この化合
物が、著しい胃酸分泌抑制作用を示すことを見い
だし、本発明を完成したものである。
ニフエジピンの胃酸分泌抑制作用は、現在消化
性潰瘍剤として広く使用されているシメチジン
（cimetidine）の有する胃酸分泌抑制作用よりも
強力であることが本発明者らによつて確認されて
いる。ニフエジピンを、抗潰瘍剤として投与する
場合の投与量は、成人一日当り10〜100mgの範囲
で、その効果を期待できるが、症状、年齢、性別
その他の要因によつて適宜増減することは勿論の
ことである。本願抗潰瘍剤は、経口投与により用
いられるが、剤形としては、錠剤、顆粒剤、カプ
セル剤等一般の経口剤において採用されるいづれ
の剤形でも可能である。以下に、ニフエジピンの
胃酸分泌抑制作用を示す薬理試験例を掲げる。
〔薬理試験例〕
本願化合物の胃液分泌抑制作用の検定のため、
Shayの方法（Gastroenterology26，ｐ，906）に
したがつて、24時間絶食したラツトを用い、ニフ
エジピンを遮光下で１％カルボキシメチルセルロ
ース液に懸濁させて、50mg／Kgの割合で十二指腸
内に投与し、４時間後に開腹して、胃を取り出
し、胃液の量及びPH値、胃液酸度抑制率（％）、
総酸度抑制率（％）を測定した。結果を次表に示
す。
【表】DETAILED DESCRIPTION OF THE INVENTION The present invention describes the use of 1,4-dihydro-2,6
-dimethyl-4-(2-nitrophenyl)-3,5
- A novel pharmaceutical use of pyridine dicarboxylic acid dimethyl ester. Nifedipine is a crystalline compound represented by the chemical formula (I), and is currently a drug widely used as an antihypertensive agent. Nifedipine is said to be a calcium ion binder due to its mechanism of action. It is generally accepted that it exerts a blood pressure lowering effect by relaxing vascular smooth muscles, and little is currently known about its other medicinal effects. When the inventor of the present application was pursuing the medicinal efficacy of nifedipine, he surprisingly discovered that this compound exhibits a remarkable effect of suppressing gastric acid secretion, thereby completing the present invention. The present inventors have confirmed that the gastric acid secretion suppressing effect of nifedipine is stronger than that of cimetidine, which is currently widely used as a peptic ulcer agent. When administering nifedipine as an anti-ulcer agent, the dosage range is 10 to 100 mg per day for adults, and its effectiveness can be expected; however, the dose may be adjusted as appropriate depending on symptoms, age, gender, and other factors. That's true. The anti-ulcer agent of the present invention is used by oral administration, and the dosage form may be any dosage form employed in general oral preparations such as tablets, granules, and capsules. Examples of pharmacological tests demonstrating the gastric acid secretion suppressing effect of nifedipine are listed below. [Pharmacological test example] To test the gastric juice secretion suppressing effect of the compound of the present application,
According to the method of Shay (Gastroenterology 26, p. 906), using rats fasted for 24 hours, nifedipine was suspended in 1% carboxymethyl cellulose solution and administered into the duodenum at a rate of 50 mg/Kg under light protection. After 4 hours, the abdomen was opened, the stomach was removed, and the amount of gastric juice and PH value, gastric juice acidity suppression rate (%),
The total acidity suppression rate (%) was measured. The results are shown in the table below. 【table】
Claims (1)
（２−ニトロフエニル）−３，５−ピリジンジカル
ボキシリツクアシドジメチルエステル（ニフエジ
ピン）を有効成分として含有することを特徴とす
る抗潰瘍剤。1 1,4-dihydro-2,6-dimethyl-4-
An anti-ulcer agent comprising (2-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester (nifedipine) as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP4429884A JPS60188319A (en) | 1984-03-07 | 1984-03-07 | Antiulcerative agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP4429884A JPS60188319A (en) | 1984-03-07 | 1984-03-07 | Antiulcerative agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS60188319A JPS60188319A (en) | 1985-09-25 |
| JPH0518810B2 true JPH0518810B2 (en) | 1993-03-15 |
Family
ID=12687596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP4429884A Granted JPS60188319A (en) | 1984-03-07 | 1984-03-07 | Antiulcerative agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS60188319A (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1180400A (en) * | 1998-11-16 | 2000-06-05 | Hokuriku Seiyaku Co. Ltd | Remedies for digestive tract functional disorder |
-
1984
- 1984-03-07 JP JP4429884A patent/JPS60188319A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS60188319A (en) | 1985-09-25 |
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