JPS60322B2 - Antitumor agent containing procainamide hydrochloride - Google Patents
Antitumor agent containing procainamide hydrochlorideInfo
- Publication number
- JPS60322B2 JPS60322B2 JP15162679A JP15162679A JPS60322B2 JP S60322 B2 JPS60322 B2 JP S60322B2 JP 15162679 A JP15162679 A JP 15162679A JP 15162679 A JP15162679 A JP 15162679A JP S60322 B2 JPS60322 B2 JP S60322B2
- Authority
- JP
- Japan
- Prior art keywords
- substance
- procainamide hydrochloride
- antitumor agent
- agent containing
- present
- 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
- 229960003253 procainamide hydrochloride Drugs 0.000 title claims description 8
- ABTXGJFUQRCPNH-UHFFFAOYSA-N procainamide hydrochloride Chemical compound [H+].[Cl-].CCN(CC)CCNC(=O)C1=CC=C(N)C=C1 ABTXGJFUQRCPNH-UHFFFAOYSA-N 0.000 title claims description 8
- 239000002246 antineoplastic agent Substances 0.000 title claims description 6
- 239000000126 substance Substances 0.000 claims description 20
- 239000003814 drug Substances 0.000 description 8
- 230000000259 anti-tumor effect Effects 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 239000000203 mixture Substances 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 208000006268 Sarcoma 180 Diseases 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 230000007059 acute toxicity Effects 0.000 description 2
- 231100000403 acute toxicity Toxicity 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 239000002504 physiological saline solution Substances 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 230000002110 toxicologic effect Effects 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N Magnesium oxide Chemical compound [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- -1 ampoules Substances 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 230000009036 growth inhibition Effects 0.000 description 1
- 238000002513 implantation Methods 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 210000003127 knee Anatomy 0.000 description 1
- 231100000053 low toxicity Toxicity 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229940088417 precipitated calcium carbonate Drugs 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000003860 topical agent Substances 0.000 description 1
- 231100000723 toxicological property Toxicity 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Description
【発明の詳細な説明】
本発明は一般式（１）で表わされる塩酸プロカィンアミ
ドを含有する抗腫場剤に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an antitumor topical agent containing procainamide hydrochloride represented by general formula (1).
本発明は下記一般式で示される塩酸プロカィンアミド（
以下、本物質と略称）が抗腫場作用を有し、一方、本物
質は毒性が低く、長期の投与が可能であって医薬品とし
て有用であることの知見を得て、本発明をなすに至った
。The present invention relates to procainamide hydrochloride (
The present invention was based on the knowledge that this substance (hereinafter abbreviated as "this substance") has an anti-tumor effect, has low toxicity, can be administered for a long period of time, and is useful as a pharmaceutical. It's arrived.
したがって、本発明は長期にわたって投与、特に経口投
与が可能な抗腫蕩剤を提供することを目的とする。Therefore, an object of the present invention is to provide an antitumor 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.
本発明の抗腫場剤の有効成分である上記一般式（１）で
示される本物質は公知物質であり、不整脈治療剤として
実用に供されているが、それが抗腫場作用を有すること
についての報告は未だみられない。The substance represented by the above general formula (1), which is the active ingredient of the anti-tumor agent of the present invention, is a known substance and has been put to practical use as a therapeutic agent for arrhythmia; however, it has no anti-tumor effect. There are no reports yet.
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、本物質の各種動物に対する急
性毒性は下記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 various animals is as follows, according to the following literature.
【１｝ 日本医薬品集 第５集 ｐ私０（１９７９）薬
業時報社【２｝ Ｔｏｘに Ｓｕ戊ｔａｎｃｅ ＬＳ
ｔｌ９７４Ｅｄｉｔｉｏｎ ｐ９５（１９７４）Ｕ．Ｓ
．Ｄｅｐｔ．ｏｆ Ｈｅａｌｔｈ，Ｅｄｕｃａｔｉｏｎ
ａｎｄ Ｗｅｌｆａｒｅ表１ 本物質のＬＤ５ｏ値
上記毒物学的特性にかんがみ本物質の薬剤適性が理解し
得る。[1] Japanese Pharmaceutical Collection Vol. 5 p 0 (1979) Yakugyo Jihosha [2] Tox Sutance LS
tl974Edition p95 (1974) U. S
．． Dept. of Health, Education
and Welfare Table 1 LD5o value of this substance In view of the above toxicological properties, the drug suitability of this substance can be understood.
‘２１ 抗腫場作用
Ｓａｒｃｏｍａ−１８０細胞１×１び個をＩＣＲ一ＪＣ
Ｌマウスの膝下部皮下に移植し、移植２岬時間後より隔
日にＩＭ団、滅菌生理食塩水に溶解させた本物質を６０
雌／ｋｇ経口投与（ｐ．ｏ．）した。'21 Anti-tumor effect Sarcoma-180 cells 1 x 1 cells were added to ICR-JC.
The substance was implanted subcutaneously below the knee of L mice, and from 2 hours after implantation, the substance was dissolved in sterile physiological saline in an IM group every other day.
Female/kg was administered orally (p.o.).
移植後２５日目に腫傷結節を摘出し、次式により増殖抑
制率（１．Ｒ．％）を算出した。（１−Ｔ／Ｃ）×１０
０＝１．Ｒ．（％）Ｔ：投与群平均腫湯重量
Ｃ：対照群平均腫場重量
結果は表２に示す。On the 25th day after transplantation, the tumor nodules were excised, and the growth inhibition rate (1.R.%) was calculated using the following formula. (1-T/C)×10
0=1. R. (%) T: Administration group average tumor weight C: Control group average tumor weight The results are shown in Table 2.
表２ 本物質のＳａｒｃｏｍａ−１８０に対する杭種傷
作用
投与量 ６０の身／Ｋ夕×ｌＯＰ．○
表２より明らかのように本物質は抗腫場効果がある。Table 2 Dosage of this substance to cause damage to Sarcoma-180 60 bodies/K evening x 1 OP. ○ As is clear from Table 2, this substance has an anti-tumor effect.
次に、本物質を上記治療剤として適用するための製剤化
について説明する。Next, formulation for applying this substance as the above-mentioned therapeutic agent will be explained.
本物質は抗腫場剤として使用する場合種々の形態で適用
できる。This 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、それらの投与に通
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、額粒、錠剤、糖衣錠、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整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, so they can take any form suitable for their administration. Additionally, the substance can be presented in dosage unit form, including powders, pellets, tablets, dragees, capsules, suppositories, suspensions, etc., provided they contain an effective dosage.
It can take various forms such as solutions, emulsions, ampoules, and injections. It should therefore be understood that the medicaments of the present invention can be prepared by the application of 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。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.
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ｌｋ９、１日当り２〜１２０の９、好ましくは１０
〜６０雌であり、非経口的投与量は体重ｌｋ９、１日当
り０．１〜ｌｏｗｐ、好ましくは１〜５のｐを１回〜４
回に分けて投与する。In this case, oral administration also includes sublingual administration,
Parenteral administration includes subcutaneous, intramuscular, intravenous, etc. injections and infusions. The dosage 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, but in general, when administering to humans, the oral dosage of this substance is 2 to 120 9, preferably 10
~60 females, parenteral dosage is lk9 body weight, 0.1 to low p per day, preferably 1 to 5 p once to 4
Administer in 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。Specific examples of formulation of the drug of the present invention are shown below as examples.
実施例中の部は特記しない限り重量を示す。実施例 １
塩酸プロカィンアミド １礎部重質酸化マ
グネシウム １５〃乳 糖
７５〃を均一に混合して粉末、又は細粒状と
して散剤とする、又この散剤をカプセル容器に入れてカ
プセルとする。Parts in the examples indicate weight unless otherwise specified. Example 1 Procainamide hydrochloride 1 Base heavy magnesium oxide 15 Lactose
75 is uniformly mixed to form a powder or fine granules, and this powder is placed in a capsule container to form a capsule.
実施例 ２
塩酸プロカィンアミド ４５部デンプン
１５〃乳糖
１６〃結晶セルロース ２１〃
ポリビニルアルコール ３〃水
３０〃を均一に混合して操和後、
破砕造粒し、乾燥し、筋別して顎粒剤とする。Example 2 Procainamide hydrochloride 45 parts starch
15. Lactose
16〃Crystalline cellulose 21〃Polyvinyl alcohol 3〃Water
After uniformly mixing and stirring 30〃,
It is crushed, granulated, dried, and divided into strips to make jaw granules.
実施例 ３
実施例２で得られた額粒剤９６部にステアリン酸カルシ
ウム４部を加え圧縮成形して直径１仇舷の錠剤とする。Example 3 4 parts of calcium stearate was added to 96 parts of the tablets obtained in Example 2, and the mixture was compressed to form tablets with a diameter of 1 m.
実施例 ４塩酸プロカィンアミド 班部ポ
リビニルアルコール ６″水
３０〃を用いて実施例２と同様に
して顎粒剤とする。Example 4 Procainamide hydrochloride Malabe polyvinyl alcohol 6″ water
A jaw granule was prepared in the same manner as in Example 2 using No. 30.
得られた額粒の９礎部‘こ結晶セルロース１碇都を加え
て圧縮成形して直径８側の錠剤とし、これにシロップゼ
ラチン沈降性炭酸カルシウムを加え糠衣錠とする。実施
例 ５
塩酸プロカィンアミド １碇部ペンジル
アルコール ３〃生理食塩水
８７〃を加え加温混合後滅菌して注射剤と
する。Nine parts of the obtained grains are added with one part of crystalline cellulose and compressed to form tablets with a diameter of 8 sides.Syrup gelatin and precipitated calcium carbonate are added to the tablets to make bran-coated tablets. Example 5 Procainamide hydrochloride 1. Penzyl alcohol 3. Physiological saline
87〃 is added, heated and mixed, and then sterilized to prepare an injection.
Claims (1)
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。[Claims] 1. An antitumor agent characterized by containing procainamide hydrochloride represented by the general formula ▲ Numerical formula, chemical formula, table, etc. ▼. 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 |
|---|---|---|---|
| JP15162679A JPS60322B2 (en) | 1979-11-21 | 1979-11-21 | Antitumor agent containing procainamide hydrochloride |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP15162679A JPS60322B2 (en) | 1979-11-21 | 1979-11-21 | Antitumor agent containing procainamide hydrochloride |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5675425A JPS5675425A (en) | 1981-06-22 |
| JPS60322B2 true JPS60322B2 (en) | 1985-01-07 |
Family
ID=15522648
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP15162679A Expired JPS60322B2 (en) | 1979-11-21 | 1979-11-21 | Antitumor agent containing procainamide hydrochloride |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS60322B2 (en) |
-
1979
- 1979-11-21 JP JP15162679A patent/JPS60322B2/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5675425A (en) | 1981-06-22 |
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