JPS6040411B2 - Antitumor agent containing ethyl piperidyl acetylaminobenzoate - Google Patents
Antitumor agent containing ethyl piperidyl acetylaminobenzoateInfo
- Publication number
- JPS6040411B2 JPS6040411B2 JP54151625A JP15162579A JPS6040411B2 JP S6040411 B2 JPS6040411 B2 JP S6040411B2 JP 54151625 A JP54151625 A JP 54151625A JP 15162579 A JP15162579 A JP 15162579A JP S6040411 B2 JPS6040411 B2 JP S6040411B2
- Authority
- JP
- Japan
- Prior art keywords
- substance
- acetylaminobenzoate
- antitumor agent
- containing ethyl
- agent containing
- 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
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】
本発明は、下記一般式（１）で示されるピベリジルアセ
チルァミノ安息香酸エチルを含有する抗腫濠剤に関する
。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an antitumor agent containing ethyl piberidyl acetylaminobenzoate represented by the following general formula (1).
本発明者は上記一股式で示されるピベリジルアセチルァ
ミノ安息香酸エチル（以下本物質と略称する。The present inventor has developed ethyl piberidyl acetylaminobenzoate (hereinafter abbreviated as the present substance) represented by the above-mentioned single-pronged formula.
）が抗腫傷作用を有することを見出し、一方、本物質は
毒性が低く、長期の投与が可能であつて医薬品として有
用であることを立証し、本発明をなすに至った。したが
って本発明は長期にわたって投与、特に経口投与が可能
な抗腫場剤を提供することを目的とする。) was found to have an anti-tumor effect, and on the other hand, it was demonstrated that this substance has low toxicity, can be administered for a long period of time, and is useful as a pharmaceutical, leading to the present invention. Therefore, an object of the present invention is to provide an anti-tumor agent that can be administered over a long period of time, especially orally.
以下本発明について詳しく説明する。The present invention will be explained in detail below.
一般式（１）で示されるピベリジルアセチルアミノ安息
香酸エチルは、既知物質であり、局所麻酔作用、鎮屋作
用、制吐作用を有する薬剤として実用に供されているが
、本発明者はさらに研究を重ねた結果、本物質が抗腫場
剤としての薬効をもち経口投与の形態において使用でき
ることを見出した。Ethyl piberidyl acetylaminobenzoate represented by the general formula (1) is a known substance and has been put to practical use as a drug having local anesthetic, sedative, and antiemetic effects. As a result of further research, it was discovered that this substance has medicinal efficacy as an anti-tumor agent and can be used in the form of oral administration.
次に本物質の毒物学的特性および薬理学的特性について
順を追って説明する。Next, the toxicological and pharmacological properties of this substance will be explained step by step.
｛１） 急性毒性
すでに知られている如く、本物質のマウスに対する急性
毒性は文献によれば次の通りである。{1) Acute toxicity As is already known, the acute toxicity of this substance to mice is as follows according to literature.
表１ 本物質のＬＤ５ｏ値 上記に示されるように、本物質が高いＬＤ５。Table 1 LD5o value of this substance As shown above, this substance has a high LD5.
を示し、医薬として安全に適用できることが確認される
。【２ー 抗腫蕩作用
Ｓａｒｃｏｍａ−１８脇細胞１×１ぴ個をＩＣＲ−ＪＣ
Ｌマウスの膝下部皮下に移植、移植２４ｒ後より隔日に
１０回、ＣＭＣ−Ｎａ２％含有の水または懸濁させた本
物質１００雌′ｋｇ経口投与（ｐ．ｏ．）した。It is confirmed that the drug can be safely applied as a medicine. [2- Anti-tumor effect Sarcoma-18 armpit cells 1 x 1 cells were added to ICR-JC
The substance was implanted subcutaneously below the knee of L mice, and 100 kg of this substance suspended in water or containing 2% CMC-Na was orally administered (p.o.) 10 times every other day from 24 hours after implantation.
移植後２５日目１こ瞳傷結節を摘出し、次式により増殖
抑制率（１．Ｒ．％）を算出した。（１−Ｔ／Ｃ）ｘｌ
ｏｏ−１．Ｒ．（％）Ｔ：投与群平均腫湯重量
Ｃ：対照群平均種場重量
結果は表２に示す。On the 25th day after transplantation, one pupil wound nodule was removed, and the growth inhibition rate (1.R.%) was calculated using the following formula. (1-T/C)xl
oo-1. R. (%) T: Administration group average seed field weight C: Control group average seed field weight The results are shown in Table 2.
表２ 本物質のＳａｒｃｏｍａ−１８０
に対する抗腫蕩作用
投与量：１００紛れ夕×ｌＯＰ．０．投与上記試験結果
から本物質結果から本物質は明らかに抗腫傷作用があり
、各種の腹湯に対し有効であることが判る。Table 2 Antitumor effect of this substance against Sarcoma-180 Dose: 100 ml x 1 OP. 0. Administration The above test results show that this substance clearly has an anti-tumor effect and is effective against various types of abdominal pain.
次に、本物質を上記抗鷹揚性袷療剤として適用するため
の製剤化について説明する。Next, the preparation of a formulation for applying this substance as the above-mentioned anti-falconry agent will be explained.
本物質は抗腫傷剤として使用する場合種々の形態で適用
できる。The substance can be applied in various forms when used as an anti-tumor agent.
また、本物質は単独又は製薬上許容しうる希釈剤および
他の薬剤との混合物形態でも使用できる。本物質は経口
的又は非経口的にも適用できるので、それらの投与に適
した任意の形態をとり得る。さらに、本物質は投薬単位
形で提供することができ、有効薬量が含有されていれば
散剤、顎粒、錠剤、糠衣錠、カプセル、座薬、懸濁剤、
液剤、乳剤、アンプル、注射液などの種々の形態をとり
得る。したがって、本発明の薬剤は従来公知のいかなる
製剤化手段の適用によっても調製可能であると理解すべ
きである。The substances can also be used alone or in admixture with pharmaceutically acceptable diluents and other agents. The substances can also be applied orally or parenterally and may take any form suitable for their administration. Additionally, the substance can be provided in dosage unit form, including powders, jaws, tablets, bran-coated tablets, capsules, suppositories, suspensions, etc., provided they contain an effective dosage.
It can take various forms such as solutions, emulsions, ampoules, and injections. Therefore, it should be understood that the medicament of the present invention can be prepared by applying any conventionally known formulation means.
なお、本発明の薬剤における本物質（有効成分）の含量
は０．０１〜１００％好ましくは０．１〜７０％（重量
）の広範囲に調整できる。本発明の薬剤は前述したよう
にヒトおよび動物に対して経口的もしくは非経口的に投
与されるが、特に経口投与が好ましい。この場合、経口
投与は舌下投与も包含するものであり、非経口投与は、
皮下、筋肉、静脈などの注射ならびに点滴を包含する。
本発明薬剤の投与量は対象が動物かヒトにより、又年令
、個人差、病状などに影響されるので、場合によっては
下記範囲外量を投与する場合も生ずるが、一般にヒトを
対象する場合、本物質の経口的投与量は体重ｌｋｇ、１
日当り１〜２００の９、好ましくは１０〜１００の９で
あり、非経口的投与量は体重ｌｋ９、１日当り０．１〜
１０の９、好ましくは、０．５〜２の９を１回〜４回に
分けて投与する。The content of the substance (active ingredient) in the drug of the present invention can be adjusted within a wide range of 0.01 to 100%, preferably 0.1 to 70% (by weight). As mentioned above, the drug of the present invention is administered orally or parenterally to humans and animals, with oral administration being particularly preferred. In this case, oral administration includes sublingual administration, and parenteral administration includes
This includes subcutaneous, intramuscular, intravenous injections, and infusions.
The dose of the drug of the present invention depends on whether the subject is an animal or a human, and is influenced by age, individual differences, medical conditions, etc. In some cases, doses outside the following range may be administered; however, in general, when administering to humans, , the oral dosage of this substance is 1 kg body weight, 1
9 of 1 to 200 per day, preferably 9 of 10 to 100, and the parenteral dosage is 0.1 to 9 of body weight per day.
9 in 10, preferably 0.5 to 2 in 9, is administered in 1 to 4 divided doses.
以下に実施例として本発明の薬剤の製剤化の具体例を示
す。実施例中の部は特記しない限り重量を示す。実施例
１
ピベリジルアセチルアミノ安息香酸エチル ２碇部沈降
炭酸カルシウム ２０〃マグネシ
アーアルミナハイドレイト ３５〃デンプン
２５″を均一に混合
して控和後、破砕、造粒し乾燥し、筋別して、額粒剤と
する。Specific examples of formulation of the drug of the present invention are shown below as examples. Parts in the examples indicate weight unless otherwise specified. Example 1 Ethyl piberidyl acetylaminobenzoate 2 Precipitated calcium carbonate 20 Magnesia alumina hydrate 35 Starch
After homogeneously mixing and diluting, the mixture is crushed, granulated, dried, and divided into stripes to form granules.
Claims (1)
有効成分とすることを特徴とする抗腫瘍剤。 ２ 経口投与形態にある特許請求の範囲第１項記載の抗
腫瘍剤。[Scope of Claims] 1. An antitumor agent characterized by containing ethyl piperidylacetylaminobenzoate represented by the general formula ▲ mathematical formula, chemical formula, table, etc. ▼ as an active ingredient. 2. The antitumor agent according to claim 1, which is in an oral administration form.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP54151625A JPS6040411B2 (en) | 1979-11-21 | 1979-11-21 | Antitumor agent containing ethyl piperidyl acetylaminobenzoate |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP54151625A JPS6040411B2 (en) | 1979-11-21 | 1979-11-21 | Antitumor agent containing ethyl piperidyl acetylaminobenzoate |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5675432A JPS5675432A (en) | 1981-06-22 |
| JPS6040411B2 true JPS6040411B2 (en) | 1985-09-11 |
Family
ID=15522626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP54151625A Expired JPS6040411B2 (en) | 1979-11-21 | 1979-11-21 | Antitumor agent containing ethyl piperidyl acetylaminobenzoate |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6040411B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01168513U (en) * | 1988-05-13 | 1989-11-28 |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU7847800A (en) * | 1999-10-15 | 2001-04-30 | Mayo Foundation For Medical Education And Research | Topical anesthetics useful for treating cancer, autoimmune diseases and ischemia |
-
1979
- 1979-11-21 JP JP54151625A patent/JPS6040411B2/en not_active Expired
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01168513U (en) * | 1988-05-13 | 1989-11-28 |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5675432A (en) | 1981-06-22 |
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