JPH0615476B2 - Anti-infective agent - Google Patents
Anti-infective agentInfo
- Publication number
- JPH0615476B2 JPH0615476B2 JP60109854A JP10985485A JPH0615476B2 JP H0615476 B2 JPH0615476 B2 JP H0615476B2 JP 60109854 A JP60109854 A JP 60109854A JP 10985485 A JP10985485 A JP 10985485A JP H0615476 B2 JPH0615476 B2 JP H0615476B2
- Authority
- JP
- Japan
- Prior art keywords
- infective agent
- injection
- chitin
- present
- infective
- 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
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】 （産業上の利用分野） 本発明は、新期な抗感染症剤に関するものである。TECHNICAL FIELD The present invention relates to a novel anti-infective agent.
（従来の技術） 従来、抗感染症剤として抗生物質等種々のものが知られ
ているが、耐性菌の出現や患者への強い副作用を示す等
の欠点を有するために新規な抗感染症剤の出現が望まれ
ていた。また、免疫機能が低下した者たとえばガン患者
や臓器移植等のために免疫抑制処置を受けた患者等は真
菌類の日知見感染を受け易く、免疫機能亢進作用を示す
安全な抗感染症剤の出現が望まれていた。このような新
規な抗感染症剤として、本発明者は先に天然界に多量に
存在するキチンまたはキトサンを有効成分とする抗感染
症剤を提供した（特開昭59-27827号公報）。(Prior Art) Conventionally, various anti-infective agents such as antibiotics have been known, but they are novel anti-infective agents because they have drawbacks such as emergence of resistant bacteria and strong side effects to patients. Was expected. In addition, a person with a weakened immune function, such as a cancer patient or a patient who has been subjected to immunosuppressive treatment for organ transplantation, etc., is vulnerable to daily infection with fungi, and is a safe anti-infective agent that exhibits an immune function-enhancing action. Appearance was desired. As such a novel anti-infective agent, the present inventor previously provided an anti-infective agent containing chitin or chitosan, which is present in large amounts in the natural world, as an active ingredient (Japanese Patent Laid-Open No. 59-27827).
（発明が解決しようとする問題点） しかしながら、キチンまたはキトサンを有効成分とする
抗感染症剤はすぐれた抗感染活性を有するが、キチンお
よびキトサンが水不溶性の高分子物質であるために、注
射剤等の製剤化および投与において問題点を有し、抗感
染症剤として未だ充分満足できるものではなかった。(Problems to be Solved by the Invention) However, an anti-infective agent containing chitin or chitosan as an active ingredient has excellent anti-infective activity, but since chitin and chitosan are water-insoluble polymer substances, injection is difficult. It has problems in formulation and administration of agents and the like, and it has not been sufficiently satisfactory as an anti-infective agent.
（問題点を解決するための手段、作用） 本発明者らは、キチンおよびキトサンの有する問題点を
解決し、更にすぐれた活性を有する薬剤を提供すべく鋭
意研究を重ねた結果、キチンを分解して得られる水溶性
のキトサンオリゴマー（キトオリゴ糖ともいう）が意外
にも抗感染症剤としてすぐれた特性を有することを見出
し、本発明を完成するに至った。(Means and Actions for Solving Problems) The inventors of the present invention have solved the problems of chitin and chitosan and, as a result of earnest studies to provide a drug having excellent activity, decomposed chitin. It was found that the water-soluble chitosan oligomer (also referred to as chitooligosaccharide) thus obtained surprisingly has excellent properties as an anti-infective agent, and completed the present invention.
本発明の抗感染症剤はキトサンオリゴマーを有効成分と
するものであり、具体的にはキトビオース、キトトリオ
ース、キトテトラオース、キトペンタオース、キトヘキ
サオース等があげられる。The anti-infective agent of the present invention contains chitosan oligomer as an active ingredient, and specific examples thereof include chitobiose, chitotriose, chitotetraose, chitopentaose, chitohexaose and the like.
本発明の抗感染症剤は有効成分のキトサンオリゴマーが
水溶性であるので、これらを常法により注射剤、錠剤、
粉剤等の形に製剤し、静脈注射、経口投与等によって使
用される。Since the active ingredient of the anti-infective agent of the present invention is a chitosan oligomer which is water-soluble, an injection, tablet,
It is used by intravenous injection, oral administration, etc. after it is prepared in the form of powder or the like.
本発明の抗感染症剤はカンジダ、アルビカンス（Candid
a albicans）等の真菌、黄色ブドウ球菌、その他のグ
ラム陽性菌ならびにグラム陰性菌等の各種の菌に対しす
ぐれた抗感染効果を示し、その有効薬量は体重kg当り10
〜200mgである。The anti-infective agent of the present invention includes Candida and Albicans (Candid).
albicans), Staphylococcus aureus, other Gram-positive and Gram-negative bacteria, and an excellent anti-infection effect. The effective dose is 10 kg / kg of body weight.
~ 200 mg.
（本発明の効果） 本発明の抗感染症剤はカニの甲羅等に存在する天然のキ
チンを分解して得られるキトサンオリゴマーを有効成分
とするので人体に対する毒性、副作用がほとんどなく、
またキトサンオリゴマーが水溶性であるために注射剤等
の製剤化および投与が簡便であり、かつ薬効の発現が早
い、免疫機能亢進作用を示す等のすぐれた効果を示す。(Effect of the present invention) Since the anti-infective agent of the present invention contains chitosan oligomer obtained by decomposing natural chitin existing in the shell of crab etc. as an active ingredient, it has almost no toxicity to human body and side effects,
In addition, since the chitosan oligomer is water-soluble, it is easy to formulate and administer an injection and the like, and exhibits excellent effects such as rapid onset of drug effect and an effect of enhancing immune function.
（実施例） 製剤例 注射剤の製造 キトヘキサオース 10ｇ、注射用生理食塩水適量をとり
全量１０００mlとし、第十日本薬局方注射剤の製法によ
って注射剤を得た。(Examples) Formulation Example Production of Injection An injection was obtained by the manufacturing method of the 10th Japanese Pharmacopoeia injection, taking 10 g of chitohexaose and an appropriate amount of physiological saline for injection to make a total volume of 1000 ml.
実験例１ 抗感染効果試験１ SPR−ddY雄性マウス（１群８匹）にリステリア・モノシ
トゲネス(Listeriamonocytogenes)菌感染の５日前、３
日前および１日前に、製剤例に準じて調製したキトヘキ
サオースの注射液50mg／kg（キトヘキサオース基準）、
及びキチン（特開昭59-27827の実施例１と同様に製造し
たもの）を用いて上記製剤例と同様にして得た注射液50
mg／kg（キチン基準）をマウスの腹腔内に投与し、次い
でこれに、あらかじめ Ｌ．monocytogens Serotype 4b株をブレインハートイ
ンフュージョンのスラントに移植し37℃で培養後Trypti
cal Soy Brothに移植37℃で２４時間振盪培養を行
い、培養停止後生理食塩水で菌を洗浄し菌数６×１０８
個／mlに調製しておいたその０．１ml（感染菌数６×1
0.７個）をマウス腹腔内に接種感染させ感染後１５日目
の生存率を求めた。Experimental Example 1 Anti-infection effect test 1 5 days before infection of Listeria monocytogenes bacteria in SPR-ddY male mice (8 mice per group), 3
Injection solution of chitohexaose 50 mg / kg (based on chitohexaose) prepared according to the formulation example one day before and one day before,
And an injection solution obtained by using chitin (produced in the same manner as in Example 1 of JP-A-59-27827) in the same manner as in the above-mentioned formulation example.
mg / kg (based on chitin) was intraperitoneally administered to mice, which was then pre-treated with L. Monocytogens Serotype 4b strain was transplanted to Brain Heart Infusion slant and incubated at 37 ° C, then Trypti
Transfer to cal soy broth, cultivate with shaking at 37 ° C for 24 hours, and after stopping the culturing, wash the bacteria with physiological saline, and count the number of bacteria 6 × 10 8.
0.1 ml that was prepared to the number of cells / ml
The 0.7 cells) was determined inoculum viability of 15 days after infection were infected intraperitoneally into mice.
その結果、キトヘキサオースを投与したマウスの生存率
は87.5％、キチンを投与したマウスの生存率は66.7％、
未投与のマウス（対照）の生存率は37.5％であった。As a result, the survival rate of mice administered with chitohexaose was 87.5%, the survival rate of mice administered with chitin was 66.7%,
The survival rate of untreated mice (control) was 37.5%.
Claims (1)
染症剤1. An anti-infective agent containing chitosan oligomer as an active ingredient.
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP60109854A JPH0615476B2 (en) | 1985-05-22 | 1985-05-22 | Anti-infective agent |
| CA000496106A CA1261264A (en) | 1984-11-29 | 1985-11-25 | Immunopotentiating agents and method |
| DE8585308687T DE3583217D1 (en) | 1984-11-29 | 1985-11-28 | USE OF CHITIN OR CHITOSAN OLIGOMERS FOR PRODUCING A MEDICINAL PRODUCT FOR STRENGTHENING THE DEFENSE FORCES AGAINST BACTERIA AND MUSHROOM INFECTIONS AND AGAINST TUMOR GROWTH. |
| DK550685A DK165731C (en) | 1984-11-29 | 1985-11-28 | USE OF CHITIN OR CHITOSANOL OIGOMERS FOR THE PREPARATION OF IMMUNOPOTENSIVE AGENTS |
| EP85308687A EP0183556B1 (en) | 1984-11-29 | 1985-11-28 | Use of chitin- or chitosan-oligomers for the manufacture of a immunopotentiating agent for enhancing the immune response against bacterial and fungal infections and against the growth of tumours |
| US07/363,307 US4971956A (en) | 1984-11-29 | 1989-06-07 | Immunopotentiating agents and method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP60109854A JPH0615476B2 (en) | 1985-05-22 | 1985-05-22 | Anti-infective agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS61268626A JPS61268626A (en) | 1986-11-28 |
| JPH0615476B2 true JPH0615476B2 (en) | 1994-03-02 |
Family
ID=14520870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP60109854A Expired - Fee Related JPH0615476B2 (en) | 1984-11-29 | 1985-05-22 | Anti-infective agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0615476B2 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10207022B2 (en) * | 2009-09-01 | 2019-02-19 | Medoderm Gmbh | Chitosan tissue dressing |
| JP2019513137A (en) * | 2016-03-30 | 2019-05-23 | アユヴィス リサーチ インク．Ａｙｕｖｉｓ Ｒｅｓｅａｒｃｈ， Ｉｎｃ． | Novel composition and method of treatment |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5927827A (en) * | 1982-08-10 | 1984-02-14 | Shigeo Suzuki | Anti-infective agent |
-
1985
- 1985-05-22 JP JP60109854A patent/JPH0615476B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPS61268626A (en) | 1986-11-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| LAPS | Cancellation because of no payment of annual fees |