JPH07242560A - Antimicrobial - Google Patents

Antimicrobial

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Publication number
JPH07242560A
JPH07242560A JP6052574A JP5257494A JPH07242560A JP H07242560 A JPH07242560 A JP H07242560A JP 6052574 A JP6052574 A JP 6052574A JP 5257494 A JP5257494 A JP 5257494A JP H07242560 A JPH07242560 A JP H07242560A
Authority
JP
Japan
Prior art keywords
pylori
gastritis
ulcer
treating
preventing
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
Application number
JP6052574A
Other languages
Japanese (ja)
Other versions
JP3593357B2 (en
Inventor
Tatsu Sakai
達 酒井
Shigenori Yamada
茂則 山田
Shigemitsu Osawa
重光 大沢
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eisai Co Ltd
Original Assignee
Eisai Co Ltd
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Filing date
Publication date
Application filed by Eisai Co Ltd filed Critical Eisai Co Ltd
Priority to JP05257494A priority Critical patent/JP3593357B2/en
Publication of JPH07242560A publication Critical patent/JPH07242560A/en
Application granted granted Critical
Publication of JP3593357B2 publication Critical patent/JP3593357B2/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Abstract

PURPOSE:To obtain an antimicrobial for preventing, improving and treating the diseases caused by Helicobacter pylori, a slightly aerobic, gram-negative helical bacillus, particularly recurrent digestive ulcer and gastritis. CONSTITUTION:A variety of active ingredients have ever been used for preventing, improving and treating gastric ulcer, duodenal ulcer and gastritis and recently a histamine H2-receptor antagonist is mainly used. There is a problem, however, on recurrence of these diseases in high percentages, in case that the administration is discountinued, thus no satisfactory prevention and therapy can be found. In the meantime, it has been demonstrated that Helicobacter pylori, a slight aerobic helical bacillus, lives in the gastric mucous membrane of the patients with digestive ulcers and has close relation to these diseases and it has become necessary to control H. pylori for treating gastritis and gastric ulcer. Accidentally, it has been found that the powder or extract of a herb medicine has the excellent action to control these deseases caused by the microorganism with high safety even after administration for a long period of time and is an excellent antimicrobial agent for preventing, improving and treating the diseases caused by H. pylori.

Description

【発明の詳細な説明】Detailed Description of the Invention

【0001】[0001]

【産業上の利用分野】本発明は、微好気性グラム陰性螺
旋状短桿菌であるヘリコバクター・ピロリ(Helicobacte
r pylori、以下 H.pylori)に起因する疾患、特に再発性
消化性潰瘍および胃炎を予防・改善・治療する抗菌剤に
関する。
FIELD OF THE INVENTION The present invention relates to Helicobacter pylori, which is a microaerobic gram-negative spiral bacillus.
The present invention relates to an antibacterial agent for preventing / ameliorating / treating diseases caused by r pylori (hereinafter, H. pylori), particularly recurrent peptic ulcer and gastritis.

【0002】[0002]

【発明の背景】従来、数多くの成分が胃潰瘍、十二指腸
潰瘍等の消化性潰瘍を予防・改善・治療する抗潰瘍剤と
して利用されており、最近ではそれらの中でもヒスタミ
ン H2-受容体拮抗剤が中心的に使われている。ヒスタミ
ン H2-受容体拮抗剤の登場により消化性潰瘍および胃炎
の、それも特に自覚症状の速やかな改善・治療が可能と
なった。しかしヒスタミン H2-受容体拮抗剤を含む従来
の抗潰瘍剤による消化性潰瘍治療または胃炎の治療にお
いては、治癒して薬物治療を止めた後に高率で再発する
問題があり、長らくその原因が不明であったため、有効
な予防・治療法が確立されていなかった。
BACKGROUND OF THE INVENTION A large number of components have hitherto been utilized as antiulcer agents for preventing, ameliorating and treating peptic ulcers such as gastric ulcer, duodenal ulcer, etc., and recently, histamine H 2 -receptor antagonists among them have been used. Used centrally. With the advent of histamine H 2 -receptor antagonists, it became possible to rapidly improve and treat peptic ulcer and gastritis, especially subjective symptoms. However histamine H 2 - In the treatment of conventional peptic ulcer treatment or gastritis caused by anti-ulcer agent comprising a receptor antagonist, there is a problem to recur at a high rate after stopping drug treatment and healing is long the cause Since it was unclear, effective prevention / treatment methods have not been established.

【0003】一方1979年以降になって、消化性潰瘍患者
の胃粘膜内に、微好気性グラム陰性螺旋状短桿菌である
H.pylori が存在し、細菌が胃炎や胃潰瘍と密接な関連
を持つことが示された。なお H.pylori は、1989年以前
にはキャンピロバクター・ピロリ(Campylobacter pylor
i)と呼ばれていたが、細菌分類学上の再考察から、同年
以降は H.pyloriと改名されており、中には C.pylori
と表記する文献もあるが、両者は基本的に同一のもので
ある。
On the other hand, since 1979, it is a microaerobic Gram-negative spiral bacillus in the gastric mucosa of patients with peptic ulcer.
The presence of H. pylori has been shown to indicate that bacteria are closely associated with gastritis and gastric ulcers. Before 1989, H. pylori was Campylobacter pylor
Although it was called i), it was renamed H.pylori after the same year due to a review of bacterial taxonomy, and in some cases C.pylori
There is a document described as, but both are basically the same.

【0004】例えば、メディカル・ジャーナル・オブ・
オーストラリア(Med.J.Aust.) 第142巻,436-439頁,1985
年およびアメリカン・ジャーナル・オブ・ガストロエン
テロロジー(Am.J.Gastroentel.) 第82巻,192-199頁,198
7年には、健常人ボランティアに H.pylori を経口投与
すると、急性胃炎が発症したとの報告がなされている。
For example, Medical Journal of
Australia (Med.J.Aust.) Vol. 142, pp. 436-439, 1985
Year and American Journal of Gastroentelology (Am. J. Gastroentel.) Vol. 82, 192-199, 198.
In 7 years, it was reported that oral administration of H. pylori to healthy volunteers caused acute gastritis.

【0005】またガストロエンテロロジー(Gastroente
l.)第94巻,33-40頁,1988年には、消化性潰瘍患者に抗生
物質を投与して H.pylori を除菌すると、胃組織像の改
善が認められたことも報告されており、 H.pylori と胃
炎や消化性潰瘍との関連性が注目されている。
In addition, Gastroente
l.) 94, 33-40, 1988, it was also reported that the administration of antibiotics to patients with peptic ulcer to eradicate H. pylori resulted in the improvement of gastric histology. However, the relationship between H. pylori and gastritis and peptic ulcer is drawing attention.

【0006】さらにランセット(Lancet),1437-1442頁,1
988年には、 H.pylori 陽性の消化性潰瘍患者は、陰性
の患者と比較して消化性潰瘍の再発率が高いことが報告
され、再発性消化性潰瘍を予防・治療するには、H.pylo
ri の除菌が必須であることが明らかになった。
Lancet, pp. 1437-1442, 1
In 988, patients with peptic ulcer positive for H. pylori were reported to have a higher recurrence rate of peptic ulcer than those with negative H. pylori. .pylo
It became clear that the sterilization of ri is essential.

【0007】[0007]

【従来技術】H.pylori を除菌することが可能な薬剤と
しては、ペニシリン系やセファロスポリン系、テトラサ
イクリン系、ニューキノロン系、マクロライド系などの
抗生物質、あるいはプラウトノールやソファルコン、塩
酸ベネキサート、ビスマス製剤、オメプラゾールランソ
プラゾールなどのベンズイミダゾール系化合物などの抗
潰瘍剤がある。
[Background Art] As agents capable of erasing H. pylori, antibiotics such as penicillins, cephalosporins, tetracyclines, new quinolones, macrolides, proutonol, sofalcone, and benexate hydrochloride are used. , Bismuth preparations, and ulcer agents such as benzimidazole compounds such as omeprazole and lansoprazole.

【0008】[0008]

【本発明が解決しようとする問題点】従来の H.pylori
を除菌することが可能な薬剤の中でも、ベンズイミダゾ
ール系化合物以外の上記抗潰瘍剤に属する薬剤は除菌作
用が非常に弱く、常用量では十分な除菌が期待できない
問題があった。一方抗生物質に属する薬剤は、除菌作用
は非常に強力ではあるが、過敏症や下痢等の副作用が多
く、また長期間使用すると臓器・血液障害等の非回復性
の重篤な副作用や耐性菌が出現するなどの問題が多く、
臨床上、 H.pylori に起因する再発性消化性潰瘍および
胃炎を確実かつ長期間安全に予防・治療できる薬剤が望
まれていた。
[Problems to be Solved by the Present Invention] Conventional H. pylori
Among the drugs capable of sterilizing bacillus, the drugs belonging to the above-mentioned anti-ulcer agents other than the benzimidazole compounds have a very weak bactericidal action, and there is a problem that sufficient bactericidal action cannot be expected at a regular dose. On the other hand, drugs belonging to antibiotics have very strong bactericidal action, but have many side effects such as hypersensitivity and diarrhea, and when used for a long period of time, non-recoverable serious side effects such as organ and blood disorders and resistance. There are many problems such as the appearance of bacteria,
Clinically, a drug that can reliably and safely prevent and treat recurrent peptic ulcer and gastritis caused by H. pylori has been desired.

【0009】このような背景のもとに、常用量で十分な
H.pylori 除菌作用を有し、かつ長期間使用しても安全
性の高い薬剤の開発が続けられてきた。
Against this background, the usual dose is sufficient.
Development of a drug that has a bactericidal action against H. pylori and is highly safe even after long-term use has been continued.

【0010】例えば特開平2-209809号公報には、胃酸分
泌抑制作用を有する抗潰瘍剤である5−メトキシ−2−
(4−メトキシ−3,5−ジメチルピリジン−2−イ
ル)メチルスルフィニル−1H−ベンズイミダゾール
(一般名、オメプラゾール)またはその塩が、 H.pylor
i の臨床分離株の1つであるH.pylori8005に対して抗菌
作用を有することが記載されている。
For example, Japanese Patent Laid-Open No. 2-209809 discloses 5-methoxy-2-, an antiulcer agent having a gastric acid secretion inhibitory action.
(4-Methoxy-3,5-dimethylpyridin-2-yl) methylsulfinyl-1H-benzimidazole (generic name, omeprazole) or a salt thereof is H.pylor
It has been described that it has an antibacterial activity against H. pylori 8005, which is one of the clinical isolates of i.

【0011】また特開平3-173817号公報にはランソプラ
ゾールを始めとするベンズイミダゾール系化合物が、
H.pylori の標準菌株であるH.pylori NCTC-11916,NCTC-
11637および臨床分離株であるH.pylori PCL-56,CPY-001
1-1,KS-13,CLO-1,CLO-6に対して抗菌作用を有すること
が記載されている。
Further, Japanese Patent Laid-Open No. 3-173817 discloses benzimidazole compounds such as lansoprazole,
H.pylori NCTC-11916, NCTC- which is a standard strain of H.pylori
11637 and clinical isolates H. pylori PCL-56, CPY-001
It is described that it has an antibacterial action against 1-1, KS-13, CLO-1, and CLO-6.

【0012】臨床において、抗生物質と同等の H.pylor
i 除菌作用を発揮するためには、 H.pylori 標準菌株お
よび臨床分離株に対して幅広い抗菌作用を有することが
必要である。前記の H.pylori に有効な抗生物質の抗菌
活性は、最小発育阻止濃度(以下、MIC)が高くても約 1
μg/ml以下であり、同等の作用を期待するにはこの数値
以下の抗菌活性を有することが、再発性潰瘍に対する臨
床的有用性を判断する基準となる。
Clinically, H.pylor equivalent to antibiotics
In order to exert the bactericidal action, it is necessary to have a wide range of antibacterial action against H. pylori standard strains and clinical isolates. The antibacterial activity of the above-mentioned antibiotics effective against H. pylori is about 1 even if the minimum inhibitory concentration (MIC) is high.
It is μg / ml or less, and antibacterial activity equal to or less than this value is expected to be expected to be equivalent, and it is a standard for judging clinical usefulness for recurrent ulcer.

【0013】かかる観点から前記の発明化合物群を評価
すると、特開平2-209809号公報および特開平3-173817号
公報に記載されているオメプラゾールは十分な抗菌活性
を有しているとは言えず、また特開平3-173817号公報に
記載されているオメプラゾール以外の発明化合物群にお
いても、すべての試験菌株に対して比較的抗生物質に近
い抗菌活性を有しているものは、14化合物中3化合物の
みであった。
When the above-mentioned invention compounds are evaluated from such a viewpoint, it cannot be said that the omeprazoles described in JP-A-2-209809 and JP-A-3-173817 have sufficient antibacterial activity. In addition, among the compounds of the invention other than omeprazole described in Japanese Patent Laid-Open No. 3-173817, those having antibacterial activity relatively close to antibiotics against all test strains are 3 out of 14 compounds. Only the compound.

【0014】そこで本発明者らは、優れた H.pylori 除
菌作用を有し、かつ長期間投与した際も安全性が高いと
いう要件を備えている薬剤について鋭意研究を行ってき
た。その結果、生薬粉末または生薬抽出物が抗菌剤とし
て所期の目的を達することを見い出し本発明を完成し
た。したがって、本発明の目的は臨床的有用性の高い抗
菌剤、ヘリコバクター・ピロリ除菌剤、胃炎または胃潰
瘍予防・治療・改善剤を提供することにある。
Therefore, the inventors of the present invention have conducted extensive studies on a drug having an excellent H. pylori bactericidal action and having a requirement that it is highly safe even after long-term administration. As a result, they have found that a crude drug powder or a crude drug extract achieves the intended purpose as an antibacterial agent, and completed the present invention. Therefore, an object of the present invention is to provide an antibacterial agent, a Helicobacter pylori bactericidal agent, a gastritis-or gastric ulcer-preventing / treating / ameliorating agent having high clinical utility.

【0015】本発明にかかる生薬粉末または生薬抽出物
は、日本薬局方に収載されている健胃・止瀉・鎮痛・鎮
痙作用等を有している成分であるが、本発明者らはその
後の研究により、意外にも抗生物質と同等の H.pylori
除菌作用を有していることを見い出し、本発明を完成し
たものである。
The crude drug powder or crude drug extract according to the present invention is a component listed in the Japanese Pharmacopoeia, which has stomachic, antidiarrheal, analgesic, antispasmodic effects, etc. Research shows that H. pylori is surprisingly equivalent to antibiotics
The present invention has been completed by discovering that it has a bactericidal action.

【0016】[0016]

【課題を解決するための手段】本発明にかかる生薬粉末
または生薬抽出物は、オウバク(黄柏)、コウボク(和
厚朴)、ケイヒ(桂皮)、チョウジ(丁子)、ハッカ
(薄荷)、ウイキョウ(茴香)またはショウキョウ(生
姜)から選ばれた1種以上であり、すべて医薬原料等と
して入手できるものである。本発明はこれらの生薬成分
を有効成分とする抗菌剤であり、 H.pylori 除菌剤であ
り、胃炎または胃潰瘍予防・治療・改善剤である。
[Means for Solving the Problems] A crude drug powder or a crude drug extract according to the present invention is Owakaku (yellow oak), Koboku (Japanese koboku), Keihi (cinnamon skin), clove (clove), peppermint (light load), fennel (wikkou). It is one or more kinds selected from (incense) or ginger (ginger), all of which can be obtained as a medicinal raw material. The present invention is an antibacterial agent containing these crude drug components as active ingredients, a H. pylori bactericidal agent, and a preventive, therapeutic, and ameliorating agent for gastritis or gastric ulcer.

【0017】したがって本発明の目的は、抗生物質と同
等の H.pylori 除菌作用を有し、かつ長期間投与した際
にも安全性が高く、特に胃炎または潰瘍に対して優れた
臨床的有用性を有する抗菌剤、 H.pylori 除菌剤を提供
することにある。
Therefore, an object of the present invention is to have a H. pylori bactericidal action equivalent to that of antibiotics, and to be highly safe even after long-term administration, and especially to have excellent clinical usefulness against gastritis or ulcer. An object is to provide an antibacterial agent, H. pylori bactericidal agent, which has a property.

【0018】なお本発明にかかる生薬抽出物は、水ある
いはアルコール・アセトン等の有機溶媒で抽出した成分
であれば限定されない。
The crude drug extract according to the present invention is not limited as long as it is a component extracted with water or an organic solvent such as alcohol / acetone.

【0019】次に本発明の効果を示すため、抗菌力試験
例を掲げる。
Next, in order to show the effect of the present invention, an example of antibacterial activity test is given.

【発明の効果】抗菌力試験 (方法)H.pylori、細菌、酵母、カビは、標準株を用い
た。また H.pylori は日本化学療法学会標準法のペーパ
ー・ディスク法に、細菌、酵母、カビは同じく寒天平板
希釈法に、それぞれ準じて下記生薬抽出物の in vitro
抗菌力を測定した。
EFFECT OF THE INVENTION Antibacterial Test (Method) Standard strains were used for H. pylori, bacteria, yeast and mold. In addition, H. pylori is in accordance with the Japanese Society of Chemotherapy standard method of paper disk method, and bacteria, yeast, and mold are also in accordance with the agar plate dilution method.
Antibacterial activity was measured.

【0020】(1) オウバク(黄柏)水抽出エキス (2) コウボク(和厚朴)水抽出エキス (3) ケイヒ(桂皮)油 (4) チョウジ(丁子)油 (5) ハッカ(薄荷)油 (6) ウイキョウ(茴香)油 (7) ショウキョウ(生姜)油(1) Water extract of yellow oak (2) Water extract of koboku (3) Cayhi oil (4) Clove oil (5) Mint oil ( 6) Fennel oil (7) Ginger oil

【0021】なお寒天平板法においては、各被験物質を
2%、1%、0.5%となるように培地に加え、最小発育阻止濃度
(%)を求めた。またペーパー・ディスク法においては、
各被験物質の2%、1%、0.5%溶液を調製した後、紙にしみこ
ませ、この紙を培地の上に乗せて最小発育阻止濃度(%)
を求めた。また、 H.pylori 以外の細菌は、トリプチケ
ースソイアガー(ベクター・ディクソン・アンド・カン
パニー社製)を用い、37℃で、3日間培養した。酵母・
カビはグルコース・ペプトンアガー(ベクター・ディク
ソン・アンド・カンパニー社製)を用い、25℃で、5日
間培養した。
In the agar plate method, each test substance was
Add 2%, 1%, 0.5% to the medium to obtain the minimum inhibitory concentration
(%) Was calculated. In the paper-disc method,
After preparing 2%, 1%, and 0.5% solutions of each test substance, soak it in a paper and put this paper on the medium to obtain the minimum inhibitory concentration (%).
I asked. For bacteria other than H. pylori, trypticase soy agar (manufactured by Vector Dixon and Company) was used and cultured at 37 ° C for 3 days. yeast·
As the mold, glucose peptone agar (manufactured by Vector Dixon and Company) was used and cultured at 25 ° C. for 5 days.

【0022】試験平板培地には、Brucella agar(ベクタ
ー・ディクソン・アンド・カンパニー社製、商品名: BB
L Microbiology Systems)に馬脱繊維血液を7%添加した
ものを用いた。37℃、pH7.0にて3日間、微好気的条件
下に(ベクター・ディクソン・アンド・カンパニー社
製、商品名: キャンピパック)培養し、最小発育阻止濃
度(以下MIC、単位[%])を求めた。
Brucella agar (manufactured by Vector Dixon and Company, trade name: BB
L Microbiology Systems) to which 7% horse defibrinated blood was added was used. Cultured at 37 ° C, pH 7.0 for 3 days under microaerobic conditions (Vector Dixon and Company, trade name: Campipack) to obtain the minimum inhibitory concentration (MIC, unit [%] below). ) Was asked.

【0023】(結果)結果を表1に示す。(Results) The results are shown in Table 1.

【0024】[0024]

【表1】 [Table 1]

【0025】上記の表1から、本発明にかかる生薬粉末
または生薬抽出物は、優れた H.pylori除菌作用を有す
ることが明らかである。また本発明化合物は抗生物質で
はないので、耐性菌に対する有効性も期待できる。なお
本発明にかかる生薬成分は、生薬として安全性は広く認
められているところであり、長期間の投与も可能であ
る。さらに他のグラム陽性菌およびグラム陰性菌や酵
母、カビに対しては発育を阻止せず、 H.pylori に選択
的な除菌作用を示した。したがって抗生物質投与時に起
きる、腸内細菌叢の交代などの、臨床上の問題も生じな
い。
From Table 1 above, it is apparent that the crude drug powder or crude drug extract according to the present invention has an excellent H. pylori bactericidal action. Since the compound of the present invention is not an antibiotic, it can be expected to be effective against resistant bacteria. The crude drug component according to the present invention is widely recognized as safe as a crude drug, and can be administered for a long period of time. Furthermore, it did not inhibit the growth of other Gram-positive and Gram-negative bacteria, yeast and mold, and showed a selective eradication effect on H. pylori. Therefore, clinical problems such as alternation of intestinal flora that occur when antibiotics are administered do not occur.

【0026】上記の実験例から明らかなように、本発明
にかかる生薬成分は抗生物質と同等の優れたH.pylori除
菌作用を有し、従って H.pylori に起因する胃炎または
胃潰瘍を予防・改善・治療する抗菌剤として有用であ
る。
As is clear from the above experimental examples, the crude drug component according to the present invention has an excellent H. pylori bactericidal action equivalent to that of antibiotics, and therefore prevents gastritis or gastric ulcer caused by H. pylori. It is useful as an antibacterial agent for improving and treating.

【0027】具体的には、健胃・止瀉・鎮痛・鎮痙作用
等を有しつつ、胃炎または胃潰瘍を予防・改善・治療
し、かつ H.pylori に起因する再発性潰瘍・胃炎をも予
防・改善・治療できる安全性の高い抗菌剤として、抗生
剤を併用することなく長期間投与することが可能であ
る。
[0027] Specifically, while having good stomach, antidiarrheal, analgesic, antispasmodic action, etc., it prevents / ameliorates / treats gastritis or gastric ulcer, and also prevents recurrent ulcer / gastritis caused by H. pylori. -As a highly safe antibacterial agent that can be improved and treated, it can be administered for a long period of time without concomitant use of antibiotics.

【0028】本発明化合物を、抗菌剤として患者に投与
する際の投与経路、投与量は、患者の症状、潰瘍・胃炎
の種類・程度、年齢、心・肝・腎機能などにより異なり
限定されないが、通常成人では、 1日 0.1〜1500mgを、
好ましくは 1〜1000mgを、より好ましくは 10〜750mg
を、さらに好ましくは 50〜500mgを経口投与する。
The administration route and dose for administering the compound of the present invention to a patient as an antibacterial agent vary depending on the patient's symptoms, the type and degree of ulcer / gastritis, age, heart / liver / kidney function, etc., but are not limited thereto. , Usually for adults, 0.1-1500mg daily,
Preferably 1 to 1000 mg, more preferably 10 to 750 mg
Is more preferably orally administered in an amount of 50 to 500 mg.

【0029】投与剤型としては、例えば散剤、細粒剤、
顆粒剤、錠剤、カプセル剤、液剤などが挙げられる。製
剤化の際は、通常の製剤担体を用いて常法により製造す
ることができる。
The dosage form includes, for example, powders, fine granules,
Granules, tablets, capsules, liquids and the like can be mentioned. In the case of formulation, it can be produced by a conventional method using an ordinary formulation carrier.

【0030】常法により経口用固形製剤を調製する場合
は、主薬に賦形剤、さらに必要に応じて結合剤、崩壊
剤、滑沢剤、着色剤、矯味矯臭剤などを加えた後、常法
により錠剤、被覆錠剤、顆粒剤、散剤、カプセル剤等と
する。
When an oral solid preparation is prepared by a conventional method, an excipient and, if necessary, a binder, a disintegrating agent, a lubricant, a coloring agent, a flavoring agent and the like are added to By the method, tablets, coated tablets, granules, powders, capsules and the like are prepared.

【0031】賦形剤としては、例えば乳糖、コーンスタ
ーチ、白糖、ブドウ糖、マンニトール、ソルビット、結
晶セルロース、二酸化ケイ素などが、結合剤としては、
例えばポリビニルアルコール、ポリビニルエーテル、エ
チルセルロース、メチルセルロース、アラビアゴム、ト
ラガント、ゼラチン、シェラック、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
リビニルピロリドンなどが、崩壊剤としては、例えば澱
粉、寒天、ゼラチン末、結晶セルロース、炭酸カルシウ
ム、炭酸水素ナトリウム、クエン酸カルシウム、デキス
トリン、ペクチン、カルボキシメチルセルロース・カル
シウム等が、滑沢剤としては、例えばステアリン酸マグ
ネシウム、タルク、ポリエチレングリコール、シリカ、
硬化植物油等が、着色剤としては医薬品に添加すること
が許可されているものが、矯味矯臭剤としては、ココア
末、ハッカ脳、芳香散、ハッカ油、竜脳、桂皮末等が用
いられる。これらの錠剤、顆粒剤には糖衣、その他必要
により適宜コーティングすることは勿論差し支えない。
As the excipient, for example, lactose, corn starch, sucrose, glucose, mannitol, sorbitol, crystalline cellulose, silicon dioxide, etc., and as the binder,
For example, polyvinyl alcohol, polyvinyl ether, ethyl cellulose, methyl cellulose, gum arabic, tragacanth, gelatin, shellac, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone and the like, and as disintegrating agents, for example, starch, agar, gelatin powder, crystalline cellulose, carbonic acid. Calcium, sodium hydrogencarbonate, calcium citrate, dextrin, pectin, carboxymethylcellulose / calcium, etc., as the lubricant, for example, magnesium stearate, talc, polyethylene glycol, silica,
Although hardened vegetable oils and the like are permitted to be added to pharmaceuticals as coloring agents, cocoa powder, mint brain, aroma powder, peppermint oil, dragon brain, cinnamon powder and the like are used as flavoring agents. Needless to say, these tablets and granules may be sugar-coated or may be appropriately coated if necessary.

【0032】また液剤を調製する場合にも、通常の製剤
担体を用いて常法により製造することができる。
Also, when preparing a liquid preparation, it can be produced by a conventional method using a usual pharmaceutical carrier.

【0033】次に本発明にかかる抗菌剤の製剤例の代表
例として、ケイヒの製剤例を実施例として示す。下記の
処方例によりそれぞれの製剤とするが、本発明の実施例
がこれらに限定されないことは言うまでもない。
Next, as a typical example of the formulation example of the antibacterial agent according to the present invention, a formulation example of Keihi is shown as an example. Each formulation is prepared according to the following formulation examples, but it goes without saying that the examples of the present invention are not limited thereto.

【0034】[0034]

【実施例】実施例1 ケイヒ倍散の調製 下記処方に従い、常法によりケイヒ倍散を得た。 Example 1 Preparation of Keihi-Hokusan According to the following formulation, Keihi-Hyosan was obtained by a conventional method.

【0035】[0035]

【表2】 [Table 2]

【0036】実施例2 ケイヒの散剤 下記処方に従い、常法によりケイヒの散剤を得た。 Example 2 Keihi powder A keihi powder was obtained by a conventional method according to the following formulation.

【0037】[0037]

【表3】 [Table 3]

【0038】実施例3 ケイヒの顆粒剤 下記処方に従い、常法によりケイヒの顆粒剤を得た。 Example 3 Keihi Granules According to the following formulation, Keihi granules were obtained by a conventional method.

【0039】[0039]

【表4】 [Table 4]

【0040】実施例4 ケイヒの錠剤 下記処方に従い、湿式によりケイヒの錠剤を得た。 Example 4 Keihi Tablets Keihi tablets were obtained by a wet method according to the following formulation.

【0041】[0041]

【表5】 [Table 5]

【0042】実施例5 ケイヒのドリンク剤 下記処方に従い、以下の方法によりケイヒのドリンク剤
を得た。 ケイヒ油、プロピルパラベン、香料をアルコールに溶解
した−(1) 別に、その他の成分を精製水約70mlに溶解し、(1)を少
しづつ加えて均一にした後、100mlにメスアップした。
通常の濾過(0.45mm)した後、容器に充填し、必要により
殺菌した。
Example 5 Keihi Drink Agent According to the following formulation, a Keihi drink agent was obtained by the following method. Cayhi oil, propylparaben, and fragrance were dissolved in alcohol- (1) Separately, other components were dissolved in about 70 ml of purified water, and (1) was added little by little to make uniform, and then the volume was raised to 100 ml.
After normal filtration (0.45 mm), it was filled in a container and sterilized if necessary.

【0043】[0043]

【表6】 [Table 6]

【0044】なお、ケイヒ以外のオウバク、コウボク、
チョウジ、ハッカ、ウイキョウ、ショウキョウ等の製剤
についても、同様にして製造することができる。また、
2種類以上の生薬成分を配合してもよい。
It should be noted that, other than Keihi,
Formulations such as clove, peppermint, fennel, and ginger can be manufactured in the same manner. Also,
You may mix 2 or more types of crude drug components.

Claims (4)

【特許請求の範囲】[Claims] 【請求項1】 生薬粉末または生薬抽出物を有効成分と
する抗菌剤。
1. An antibacterial agent containing a crude drug powder or a crude drug extract as an active ingredient.
【請求項2】 ヘリコバクター・ピロリ除菌剤である請
求項1記載の抗菌剤。
2. The antibacterial agent according to claim 1, which is a Helicobacter pylori bactericidal agent.
【請求項3】 胃炎または胃潰瘍予防・治療・改善剤で
ある請求項1ないし2記載の抗菌剤。
3. The antibacterial agent according to claim 1, which is an agent for preventing, treating, and improving gastritis or gastric ulcer.
【請求項4】 生薬がオウバク、コウボク、ケイヒ、チ
ョウジ、ハッカ、ウイキョウまたはショウキョウから選
ばれた1種以上である請求項1ないし3記載の抗菌剤。
4. The antibacterial agent according to claim 1, wherein the crude drug is one or more selected from Oataku, Koboku, Keihi, Clove, mint, fennel and ginger.
JP05257494A 1994-02-28 1994-02-28 Antibacterial agent Expired - Fee Related JP3593357B2 (en)

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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998009652A1 (en) * 1996-09-06 1998-03-12 Otsuka Pharmaceutical Co., Ltd. COMPOSITION, ANTIMICROBIAL AGENT, INFECTION PREVENTIVE, AND FOOD AGAINST $i(HELICOBACTER PYLORI)
US6187313B1 (en) * 1996-03-26 2001-02-13 Nature's Sunshine Products, Inc. Composition and method for treating and preventing helicobactor-pylori-associated stomach gastritis, ulcers and cancer
JP2001072599A (en) * 1999-09-03 2001-03-21 Kagome Co Ltd Novel hepatic disturbance inhibitor
JP2002205939A (en) * 2001-01-05 2002-07-23 Sankyo Co Ltd Antiulcer agent composition
GB2453728A (en) * 2007-10-16 2009-04-22 Medical & Pharmaceutical Indus Use of a potent extract from the rhizomes of Zingiber officinale to treat gastric ulcers
CN103127262A (en) * 2013-02-19 2013-06-05 青岛正大海尔制药有限公司 Chinese medicine composition capable of curing chronic gastritis
CN104288749A (en) * 2014-11-10 2015-01-21 天农大(天津)生物科技有限公司 Traditional Chinese medicine composition for treating pig gastric ulcer and preparation method thereof
CN109646664A (en) * 2019-02-15 2019-04-19 王捷虹 Three fragrant dispelling cold Yao Bingjius
JP2020504144A (en) * 2017-01-11 2020-02-06 チョン クン ダン ファーマシューティカル コーポレーション Composition for preventing or treating gastritis or peptic ulcer
CN114128727A (en) * 2020-09-04 2022-03-04 艾沐外株式会社 Preparation method of natural antibacterial substance and antibacterial agent containing natural antibacterial substance

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6187313B1 (en) * 1996-03-26 2001-02-13 Nature's Sunshine Products, Inc. Composition and method for treating and preventing helicobactor-pylori-associated stomach gastritis, ulcers and cancer
WO1998009652A1 (en) * 1996-09-06 1998-03-12 Otsuka Pharmaceutical Co., Ltd. COMPOSITION, ANTIMICROBIAL AGENT, INFECTION PREVENTIVE, AND FOOD AGAINST $i(HELICOBACTER PYLORI)
JP2001072599A (en) * 1999-09-03 2001-03-21 Kagome Co Ltd Novel hepatic disturbance inhibitor
JP2002205939A (en) * 2001-01-05 2002-07-23 Sankyo Co Ltd Antiulcer agent composition
GB2453728A (en) * 2007-10-16 2009-04-22 Medical & Pharmaceutical Indus Use of a potent extract from the rhizomes of Zingiber officinale to treat gastric ulcers
GB2453728B (en) * 2007-10-16 2009-11-04 Medical & Pharmaceutical Indus Use of a potent product extracted from rhizomes of zingiber offcinale in preparation of a medicament for treatment gastritis, gastric ulcer and duodenal ulcer
CN103127262A (en) * 2013-02-19 2013-06-05 青岛正大海尔制药有限公司 Chinese medicine composition capable of curing chronic gastritis
CN104288749A (en) * 2014-11-10 2015-01-21 天农大(天津)生物科技有限公司 Traditional Chinese medicine composition for treating pig gastric ulcer and preparation method thereof
JP2020504144A (en) * 2017-01-11 2020-02-06 チョン クン ダン ファーマシューティカル コーポレーション Composition for preventing or treating gastritis or peptic ulcer
CN109646664A (en) * 2019-02-15 2019-04-19 王捷虹 Three fragrant dispelling cold Yao Bingjius
CN114128727A (en) * 2020-09-04 2022-03-04 艾沐外株式会社 Preparation method of natural antibacterial substance and antibacterial agent containing natural antibacterial substance
JP2022043964A (en) * 2020-09-04 2022-03-16 エムワイ カンパニー,リミテッド Method for producing natural antimicrobial substance, and antimicrobial agent comprising natural antimicrobial substance produced by the production method

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