JPH0528704B2 - - Google Patents
Info
- Publication number
- JPH0528704B2 JPH0528704B2 JP25128984A JP25128984A JPH0528704B2 JP H0528704 B2 JPH0528704 B2 JP H0528704B2 JP 25128984 A JP25128984 A JP 25128984A JP 25128984 A JP25128984 A JP 25128984A JP H0528704 B2 JPH0528704 B2 JP H0528704B2
- Authority
- JP
- Japan
- Prior art keywords
- substance
- weight
- formula
- antitumor
- administration
- 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
- 239000002246 antineoplastic agent Substances 0.000 claims description 7
- 239000000126 substance Substances 0.000 description 17
- 206010028980 Neoplasm Diseases 0.000 description 6
- 241001465754 Metazoa Species 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 3
- 230000000259 anti-tumor effect Effects 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 241000282412 Homo Species 0.000 description 2
- 208000006268 Sarcoma 180 Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 238000002054 transplantation Methods 0.000 description 2
- PWMWNFMRSKOCEY-UHFFFAOYSA-N 1-Phenyl-1,2-ethanediol Chemical compound OCC(O)C1=CC=CC=C1 PWMWNFMRSKOCEY-UHFFFAOYSA-N 0.000 description 1
- RMMXTBMQSGEXHJ-UHFFFAOYSA-N Aminophenazone Chemical compound O=C1C(N(C)C)=C(C)N(C)N1C1=CC=CC=C1 RMMXTBMQSGEXHJ-UHFFFAOYSA-N 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000009036 growth inhibition Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 235000020374 simple syrup Nutrition 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000012439 solid excipient Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000723 toxicological property Toxicity 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
本願は抗腫瘍剤、詳しくは一般式（）で示さ
れる物質を含有する抗腫瘍剤に関する。
本発明者らは、抗腫瘍剤の開発における研究に
おいて、腫瘍に対し一般式（）式で示される物
質を用いると抗腫瘍作用がある事を見い出し本願
完成した。
本願は下記一般式（）：
（式中、R1はCH3又はCH2＝CHを、
R2はＨ又はClを、
R3はＨ，CH3、又はCH2SO3Naを表わす）
で表される化学物質（以下本物質と称す）および
該化学物質を活性成分として含有する抗腫瘍剤に
関する。
本物質中には医療薬日本医薬品集、第７版、35
−36頁、404〜405頁、1983年、薬業時報社、新開
発医薬品便覧、第２版、55−56頁、1981年、薬業
時報社等に記載されている公知の抗炎症作用を有
する物質も含まれる。その安全性も十分確認され
ている。
本物質の物理学的並びに毒物学的特性を次の表
１に示す。
The present application relates to an antitumor agent, specifically an antitumor agent containing a substance represented by the general formula (). The present inventors, in their research for the development of antitumor agents, discovered that a substance represented by the general formula (2) has an antitumor effect on tumors, and completed the present application. This application is based on the following general formula (): (In the formula, R 1 represents CH 3 or CH 2 =CH, R 2 represents H or Cl, and R 3 represents H, CH 3 or CH 2 SO 3 Na.) (referred to as a chemical substance) and an antitumor agent containing the chemical substance as an active ingredient. This substance contains medical drugs, Japanese Pharmaceutical Collection, 7th edition, 35
-Page 36, pp. 404-405, 1983, Yakugyo Jihosha, Newly developed drug handbook, 2nd edition, pp. 55-56, 1981, Yakugyo Jihosha, etc. This also includes substances that have. Its safety has also been fully confirmed. The physical and toxicological properties of this substance are shown in Table 1 below.
【表】
本物質は動物又は人腫瘍に有効である。本物質
は腫瘍細胞数の減少、延命率、腫瘍増殖抑制率等
においてその効果を確認し有効性を判断した。
本物質を抗腫瘍剤として用いる場合、症状に応
じて薬効を得るのに十分な量の有効成分が含有さ
れた投薬単位形で提供することができる。その形
態としては経口用として散剤、細粒剤、顆粒剤、
錠剤、緩衝錠剤、糖衣錠剤、カプセル剤、シロツ
プ剤、丸剤、懸濁剤、液剤、乳剤などの形態をと
り得る。非経口用としては注射液としてのアンプ
ル、ビンなどの形態をとり得る。座剤、軟膏の形
態でもよい。
本物質は単独又は製薬上許容し得る希釈剤及び
他の薬剤と混合して用いてもよく、希釈剤として
固体、液体、半固体の賦形剤、増量剤、結合剤、
湿潤化剤、崩壊剤、表面活性剤、滑沢剤、分散
剤、緩衝剤、香料、保存料、補助剤、溶剤等が使
用され得る。
本物質を製剤の形で用いる場合、製剤中に活性
成分は一般に0.01〜100重量％、好ましくは0.05
〜80重量％含まれる。
本物質は人間及び動物に経口的または非経口的
に投与される。経口的投与は舌下投与を包含す
る。非経口的投与は注射投与（例えば皮下、筋
肉、静脈注射、点滴）、直腸投与などを含む。塗
布してもよい。
本物質の投与量は投与対象が動物か人間かによ
り、また年齢、個人差、病状などに影響されるの
で場合によつては下記範囲外量を投与する場合も
あるが、一般に人間を対象とする場合、本物質の
投与量は１日当り0.1〜1500mg／Kg、好ましくは
１〜500mg／Kgである。１日２〜４回に分けて投
与してもよい。
以下、実施例により本発明をさらに説明する。
実施例 １
Sarcoma−180に対する抗腫瘍効果
Sarcoma−180細胞１×106個をICR−JCL系マ
ウスの腋下部皮下に移植し、移植24時間後より隔
日に10回、0.5％CMC溶液中に溶解もしくは懸濁
させた本物質の所定量を経口投与した。移植後25
日目に腫瘍結節を摘出し、次式により増殖抑制率
（I.R.％）を算出した。
（１−Ｔ／Ｃ）×100＝1.R.（％）
Ｔ：投与群平均腫瘍重量
Ｃ：対照群平均腫瘍重量
結果は表２に示す。尚１群10匹ずつ用いてその
平均値を用いた。
表２から明らかな如く、本物質に腫瘍縮小効果
がみられ、抗腫瘍効果が認められた。[Table] This substance is effective against animal or human tumors. The effectiveness of this substance was determined by confirming its effectiveness in reducing the number of tumor cells, prolonging survival, suppressing tumor growth, etc. When the present substance is used as an antitumor agent, it can be provided in a dosage unit form containing a sufficient amount of the active ingredient to obtain a medicinal effect depending on the symptom. Its forms include powder, fine granules, and granules for oral use.
It can take the form of tablets, buffered tablets, sugar-coated tablets, capsules, syrups, pills, suspensions, solutions, emulsions and the like. For parenteral use, it can be in the form of ampoules, bottles, etc. as injection solutions. It may also be in the form of suppositories or ointments. The substance may be used alone or in admixture with pharmaceutically acceptable diluents and other agents, including solid, liquid, or semi-solid excipients, fillers, binders,
Wetting agents, disintegrants, surfactants, lubricants, dispersants, buffers, fragrances, preservatives, adjuvants, solvents, etc. may be used. When the substance is used in the form of a formulation, the active ingredient in the formulation is generally 0.01 to 100% by weight, preferably 0.05%.
Contains ~80% by weight. The substance is administered orally or parenterally to humans and animals. Oral administration includes sublingual administration. Parenteral administration includes injection administration (eg, subcutaneous, intramuscular, intravenous injection, infusion), rectal administration, and the like. May be applied. The dose of this substance 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 range shown below may be administered, but in general, it is not recommended for humans. In this case, the dosage of the substance is 0.1 to 1500 mg/Kg, preferably 1 to 500 mg/Kg per day. It may be administered in divided doses 2 to 4 times a day. The present invention will be further explained below with reference to Examples. Example 1 Antitumor effect on Sarcoma-180 1 x 10 6 Sarcoma-180 cells were subcutaneously transplanted into the lower armpit of ICR-JCL mice and dissolved in 0.5% CMC solution 10 times every other day starting 24 hours after transplantation. Alternatively, a predetermined amount of the suspended substance was orally administered. 25 days after transplantation
On day 1, tumor nodules were excised, and the growth inhibition rate (IR%) was calculated using the following formula. (1-T/C)×100=1.R. (%) T: Average tumor weight of administration group C: Average tumor weight of control group The results are shown in Table 2. In addition, 10 animals were used for each group, and the average value was used. As is clear from Table 2, this substance had a tumor shrinking effect and an antitumor effect.
【表】
製剤化例 １
４−ジメチルアミノ−１−フエニル−２，３−
ジメチル−５−ピラゾロン又は１−フエニル−
２，３−ジメチル−５−ピラゾロン−４−メチル
−アミノメタンスルホン酸ナトリウム1.5重量部、
単シロツプ8.0重量部に精製水100重量部を加えて
経口剤とした。[Table] Formulation example 1 4-dimethylamino-1-phenyl-2,3-
Dimethyl-5-pyrazolone or 1-phenyl-
1.5 parts by weight of sodium 2,3-dimethyl-5-pyrazolone-4-methyl-aminomethanesulfonate,
An oral preparation was prepared by adding 100 parts by weight of purified water to 8.0 parts by weight of simple syrup.
Claims (1)
剤。 ３ 式： で示される特許請求の範囲第１項に記載の抗腫瘍
剤。[Claims] 1 General formula (): (In the formula, R 1 represents CH 3 or CH 2 =CH, R 2 represents H or Cl, and R 3 represents H, CH 3 or CH 2 SO 3 Na). 2 formula: The antitumor agent according to claim 1, which is represented by: 3 formula: The antitumor agent according to claim 1, which is represented by:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP25128984A JPS61129125A (en) | 1984-11-28 | 1984-11-28 | Antitumor agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP25128984A JPS61129125A (en) | 1984-11-28 | 1984-11-28 | Antitumor agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS61129125A JPS61129125A (en) | 1986-06-17 |
| JPH0528704B2 true JPH0528704B2 (en) | 1993-04-27 |
Family
ID=17220589
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP25128984A Granted JPS61129125A (en) | 1984-11-28 | 1984-11-28 | Antitumor agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS61129125A (en) |
-
1984
- 1984-11-28 JP JP25128984A patent/JPS61129125A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS61129125A (en) | 1986-06-17 |
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