JPH0539218A - Therapeutic agent for radiation injury - Google Patents

Therapeutic agent for radiation injury

Info

Publication number
JPH0539218A
JPH0539218A JP3195342A JP19534291A JPH0539218A JP H0539218 A JPH0539218 A JP H0539218A JP 3195342 A JP3195342 A JP 3195342A JP 19534291 A JP19534291 A JP 19534291A JP H0539218 A JPH0539218 A JP H0539218A
Authority
JP
Japan
Prior art keywords
injuries
therapeutic agent
melting point
acid polymer
agent
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.)
Pending
Application number
JP3195342A
Other languages
Japanese (ja)
Inventor
Kiichi Sawai
井 喜 一 澤
Masatsune Kurono
野 昌 庸 黒
Yasuaki Kondo
藤 保 昭 近
Takahiko Mitani
谷 隆 彦 三
Shoji Yokochi
地 祥 司 横
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.)
Sanwa Kagaku Kenkyusho Co Ltd
Original Assignee
Sanwa Kagaku Kenkyusho Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Sanwa Kagaku Kenkyusho Co Ltd filed Critical Sanwa Kagaku Kenkyusho Co Ltd
Priority to JP3195342A priority Critical patent/JPH0539218A/en
Publication of JPH0539218A publication Critical patent/JPH0539218A/en
Pending legal-status Critical Current

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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

PURPOSE:To obtain the subject therapeutic agent, containing 3- oxygermylpropionic acid polymer having high safety and physico-chemical properties of a specified specific gravity, solubility in water and melting point as an active ingredient, and having protective action or radiation injuries, especially injuries to hematopoietic function. CONSTITUTION:A therapeutic agent for radiation injuries containing an organogermanium compound (i.e., 3-oxygermylpropionic acid polymer), expressed by the formula ((n) is 1 or a larger integer than that) and physico-chemical properties, i.e., appearance of white needlelike crystals, melting point at 230 deg.C, (aggregation near the melting point), especially specific gravity of 2.23 and solubility of 1.57 (in water at 20 deg.C) as an active ingredient. This agent is a therepeutic medicine having high lifesaving effects on injuries to hematopoietic function occurring at a high frequency in accidental exposure, radiotherapy of cancer, etc. The aforementioned agent can be used as dosage forms of a tablet, a capsule, a powder, a granule, a troche, a pill, a suppository, etc. The dose is preferably about 150mg/day for an adult (50kg) by oral administration.

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 式 [(O1/2
eCHCHCOOH]n (式中nは1又はそれ以上の整数を意味する)にて示さ
る3−オキシゲルミルプロピオン酸からなる放射線障害
治療剤に係る。
The present invention relates to the formula [(O 1/2 ) 3 G
eCH 2 CH 2 COOH] n (wherein n represents an integer of 1 or more) according to the radiation injury therapeutic agent comprising Shimesaru 3 oxygermylpropionic acid at.

【0002】[0002]

【従来技術】放射線医療、原発、放射性物質保管施設等
の取扱従業者や事故発生時の近郊住民の被爆は最近地球
的環境破壊問題として注目されている。また放射線医療
特に悪性腫瘍に対する放射線療法は照射に伴う急性障害
の発生が有効な治療の妨げとなっている。
2. Description of the Related Art Radiation medical treatment, nuclear power plants, radioactive materials storage facilities, and the like, and the exposure of workers in the suburbs at the time of an accident have received attention as a global environmental destruction problem. Radiation therapy, especially for radiation therapy for malignant tumors, is hindering effective treatment due to the occurrence of acute damage associated with irradiation.

【0003】被爆100 〜500 rem では造血臓器の障害
が、500 〜2000rem では消化管症状が、それ以上の被爆
では中枢神経系の症状が支配的とされ、LD
100/30日は約700 rem、LD50/30日は約400
remである。
At 100 to 500 rem, hematopoietic organ disorders are predominant, at 500 to 2000 rem, gastrointestinal symptoms are predominant, and at more than 100 rem, central nervous system symptoms are predominant.
100/30 days is about 700 rem, LD 50/30 days is about 400
rem.

【0004】急性被爆では25rem程度でも造血機能障害
が発生し増悪期より回復期を経ずに短時間の間に死亡す
る例も報告されており、急性被爆に対する延命効果の高
い薬剤の出現が望まれていた。
[0004] In acute exposure, it has been reported that hematopoietic dysfunction occurs even at about 25 rem and death occurs within a short period of time from the exacerbation period to the recovery period, and the emergence of a drug with a long life-prolonging effect on acute exposure is desired. It was rare.

【0005】また、3−オキシゲルミルプロピオン酸は
複雑な重合性を有し、多用な用途を有するため薬理活性
の面から近年極めて注目されている化合物であり、抗ウ
イルス作用など古くから注目されていたが、被爆障害の
治療効果については知られていない。(特公昭57-53800
号等)
Further, 3-oxygermylpropionic acid is a compound which has received a great deal of attention in recent years from the viewpoint of pharmacological activity because it has complex polymerizability and has various uses. However, it is not known about the therapeutic effect on A-bomb injury. (Japanese Patent Publication Sho 57-53800
No.)

【発明が解決しようとする問題点】[Problems to be Solved by the Invention]

【0006】被爆が予測される場合はラジカル消去剤が
一般的に利用されているが、偶発的に放射性物質を摂取
したり、被爆してしまったような場合は排泄促進剤やア
デニン、レシチン、パロチン等の代謝性薬剤いわゆる栄
養剤的なものしかなく、決定的な治療方法がないのが現
状である。
Radical scavengers are generally used when exposure is predicted, but in the case of accidental intake of radioactive substances or exposure, excretion enhancers, adenine, lecithin, The current situation is that there is no definitive treatment method because there are only metabolic drugs such as parotin, which are so-called nutritional drugs.

【0007】本発明者は上記の実情に鑑み、被爆障害を
有効に軽減、回復する事の出来る物質を得るために検索
し、本発明を完成するに至った。すなわち本発明は偶発
的被爆や癌の放射線療法等にあって、高頻度で発生する
造血機能障害に対する救命効果の高い薬剤を提供するも
のである。
In view of the above situation, the present inventor has completed the present invention by searching for a substance capable of effectively reducing and recovering radiation damage. That is, the present invention provides a drug having a high life-saving effect against frequently occurring hematopoietic dysfunction in accidental exposure, radiation therapy for cancer, and the like.

【0008】[0008]

【問題点を解決するための手段及び作用】本発明は安全
性の高い、比重(密度)2.23、溶解度(水)1.5
7(20°C)、融点約230°C(付近凝集)の物理
化学的性質を有する3−オキシゲルミルプロピオン酸重
合体を放射線被爆障害の治療剤として利用するものであ
る。
[Means and Actions for Solving Problems] The present invention is highly safe and has a specific gravity (density) of 2.23 and a solubility (water) of 1.5.
A 3-oxygermylpropionic acid polymer having a physicochemical property of 7 (20 ° C) and a melting point of about 230 ° C (aggregation in the vicinity) is used as a therapeutic agent for radiation exposure damage.

【0009】なお、製剤加工にあっては3−オキシゲル
ミルプロピオン酸重合体の活性を維持するため圧縮製剤
の場合は水溶解性の高い低分子性物質ことに白糖、ソル
ビトール、果糖、ショ糖、ブドウ糖、乳糖、マンニトー
ルによる組成物が、顆粒剤、カプセル剤、散剤の場合は
ヒドロキシプロピルセルロース(HPC)、アルブミ
ン、ペプシン等の高分子性物質によって安定化された組
成物形態の利用が好ましい。
In order to maintain the activity of the 3-oxygermylpropionic acid polymer during processing of the preparation, in the case of the compressed preparation, a low molecular weight substance having high water solubility, particularly sucrose, sorbitol, fructose and sucrose. In the case of granules, capsules, and powders, the composition of glucose, lactose, and mannitol is preferably used in the form of a composition stabilized by a polymeric substance such as hydroxypropyl cellulose (HPC), albumin, and pepsin.

【0010】[0010]

【剤型及び投与量】本発明による固形製剤の剤型として
は、通常は経口用に圧縮加工された錠剤、カプセル剤、
散剤、顆粒剤の形態で使用されるが、トロ−チ剤、丸
剤、坐剤等としても使用可能である。
[Dosage Form and Dosage] The dosage form of the solid preparation according to the present invention is usually orally compressed tablets, capsules,
It is used in the form of powder or granules, but can also be used as troches, pills, suppositories and the like.

【0011】なお、3−オキシゲルミルプロピオン酸重
合体を人に投与する場合の投与量としては、剤型、患者
の年齢等に依存するが、一般には1〜1500mg/kg 範
囲内であり、成人(体重50kg)に対する経口投与では
150mg/日程度が好ましい。
The dose of the 3-oxygermylpropionic acid polymer administered to a human depends on the dosage form, the age of the patient, etc., but is generally in the range of 1 to 1500 mg / kg. Oral administration to an adult (body weight 50 kg) is preferably about 150 mg / day.

【0012】以下には本発明の効果を、実施例により更
に詳細に説明する。
The effects of the present invention will be described in more detail below with reference to examples.

【0013】[0013]

【実施例】【Example】

【0014】製剤例1(散 剤) ヒドロキシプロピルセルロース、3−オキシゲルミルプ
ロピオン酸重合体2:1をエタノールを湿潤剤として練
合し、50゜C以下の温度で乾燥後粉末又は粒状の組成物
を得た。
Formulation Example 1 (Powder) Hydroxypropyl cellulose and 3-oxygermylpropionic acid polymer 2: 1 were kneaded with ethanol as a wetting agent, dried at a temperature of 50 ° C. or lower, and then powdered or granular composition. I got a thing.

【0015】製剤例2(カプセル剤) 以下処方でカプセル剤を調整した。 本発明による3−オキシゲルミルプロピオン酸重合体 10mg 乳 糖 165.5mg HPC(ヒドロキシプロピルセルロース) 2.7mg ステアリン酸マグネシウム 1.8mg 1カプセルあたり 180mg Formulation Example 2 (Capsule) A capsule was prepared according to the following formulation. 3-Oxygermylpropionic acid polymer according to the present invention 10 mg Lactose 165.5 mg HPC (hydroxypropyl cellulose) 2.7 mg Magnesium stearate 1.8 mg 180 mg per capsule

【0016】製剤例3(錠 剤) 以下処方で圧縮錠剤を調整した。 3−オキシゲルミルプロピオン酸重合体 10.0 ソルビトール 41.7 果 糖 1.2 HPCーL 3.0 ステアリン酸マグネシウム 1.8 白 糖 適 量 180.0mg Formulation Example 3 (tablets) Compressed tablets were prepared according to the following formulation. 3-Oxygermylpropionic acid polymer 10.0 Sorbitol 41.7 Fructose 1.2 HPC-L 3.0 Magnesium stearate 1.8 White sugar Suitable amount 180.0 mg

【0017】薬効薬理試験例 1)放射線障害防護作用 (a)被験薬物 製造例3の薬剤Pharmacological and Pharmacological Test Example 1) Radiation Damage Protective Action (a) Test Drug Drug of Production Example 3

【0018】(b)試験方法 試験動物としてはddY系雄性マウス(5週齢)を一群
10匹で使用した。なお、すべてのマウスは腸内細菌の
感染を抑制するために抗生物質を投与した。軟X線照射
装置にて等電圧140kv、照射量650レントゲン
(R)をマウスに照射して30日後の生存率および平均
生存日数を調べた。
(B) Test method As test animals, male ddY mice (5 weeks old) were used in groups of 10. All mice were administered with antibiotics in order to suppress the infection of intestinal bacteria. Mice were irradiated with an equal voltage of 140 kv and an irradiation dose of 650 roentgen (R) using a soft X-ray irradiation device, and the survival rate and the average survival time after 30 days were examined.

【0019】被験薬物は0.5%ゼラチン溶液に溶解し
て照射直後に単回経口投与、または照射直後から3日間
3回連続経口投与を行った。
The test drug was dissolved in a 0.5% gelatin solution and orally administered once immediately after irradiation, or continuously 3 times for 3 days immediately after irradiation.

【0020】(c)結果 結果は以下の表 1に記載のごとく、本発明組成物は非
投与群に比べて生存率および平均生存日数を有意に延長
し明らかな放射線障害防護並びに救命作用を示した。
(C) Results As shown in Table 1 below, the composition of the present invention significantly prolongs the survival rate and the average survival time as compared with the non-administered group, and shows a clear radiation damage protection and life-saving effect. It was

【0021】[0021]

【表 1】 生存率および平均生存日数 群設定 生存率(%) 平均生存日数(日) 非投与 10 12.0 1 mg/Kg 単回 20 15.3 10 mg/Kg 単回 40 19.8 * 100 mg/Kg 単回 50 20.8 * 1 mg/Kg 3回 30 19.1 * 10 mg/Kg 3回 40 19.9 * 100 mg/Kg 3回 50 21.6 * *:有意水準p<0.05で非投与群と有意差あり[Table 1] Survival rate and average survival days Group setting Survival rate (%) Average survival time (days) Non-administration 10 12.0 1 mg / Kg Single dose 20 15.3 10 mg / Kg Single dose 40 19.8 * 100 mg / Kg Single 50 20.8 * 1 mg / Kg 3 times 30 19.1 * 10 mg / Kg 3 times 40 19.9 * 100 mg / Kg 3 times 50 21.6 * *: Significance level p < 0.05 is significantly different from non-administered group

【0022】[0022]

【発明の効果】本発明は3−オキシゲルミルプロピオン
酸の放射線障害防護並びに救命作用の発見によるもので
あり被爆に対して増悪期より回復期を経ずに死に至る重
篤症例に対しても救命効果の高い薬剤を提供するもので
ある。
INDUSTRIAL APPLICABILITY The present invention is based on the discovery of protection against radiation damage and life-saving action of 3-oxygermylpropionic acid, and even in serious cases of exposure to death without a recovery period from an exacerbation period to a death. It provides a drug with a high life-saving effect.

───────────────────────────────────────────────────── フロントページの続き (72)発明者 三 谷 隆 彦 名古屋市東区東外堀町35番地 株式会社三 和化学研究所内 (72)発明者 横 地 祥 司 名古屋市東区東外堀町35番地 株式会社三 和化学研究所内 ─────────────────────────────────────────────────── ─── Continuation of front page (72) Inventor Takahiko Mitani 35 Higashi Sotobori-cho, Higashi-ku, Nagoya City Sanwa Chemical Research Institute Co., Ltd. Sanwa Institute of Chemistry

Claims (2)

【特許請求の範囲】[Claims] 【請求項1】式 [(O1/2 GeCHCHCO
OH]n (式中nは1又はそれ以上の整数を意味する)にて示さ
れ、白色針状結晶を有し融点が230°C(付近凝集)
である有機ゲルマニウム化合物を有効成分として含有す
る放射線障害治療剤
1. The formula [(O 1/2 ) 3 GeCH 2 CH 2 CO
OH] n (wherein n represents an integer of 1 or more) and has white needle crystals and a melting point of 230 ° C. (aggregation in the vicinity).
Radiation Damage Remedy Containing an Organic Germanium Compound of
【請求項2】放射線照射による造血機能障害防御作用を
有する請求項1記載の放射線障害治療剤
2. The therapeutic agent for radiological disorders according to claim 1, which has a protective effect on hematopoietic dysfunction due to radiation irradiation.
JP3195342A 1991-08-05 1991-08-05 Therapeutic agent for radiation injury Pending JPH0539218A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP3195342A JPH0539218A (en) 1991-08-05 1991-08-05 Therapeutic agent for radiation injury

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP3195342A JPH0539218A (en) 1991-08-05 1991-08-05 Therapeutic agent for radiation injury

Publications (1)

Publication Number Publication Date
JPH0539218A true JPH0539218A (en) 1993-02-19

Family

ID=16339577

Family Applications (1)

Application Number Title Priority Date Filing Date
JP3195342A Pending JPH0539218A (en) 1991-08-05 1991-08-05 Therapeutic agent for radiation injury

Country Status (1)

Country Link
JP (1) JPH0539218A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014017046A1 (en) 2012-07-23 2014-01-30 国立大学法人東京大学 Prophylactic and/or therapeutic agent for radiation damage
US11782344B2 (en) 2015-04-21 2023-10-10 Fujifilm Electronic Materials U.S.A., Inc. Photosensitive polyimide compositions

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014017046A1 (en) 2012-07-23 2014-01-30 国立大学法人東京大学 Prophylactic and/or therapeutic agent for radiation damage
US9895331B2 (en) 2012-07-23 2018-02-20 The University Of Tokyo Prophylactic and/or therapeutic agent for radiation damage
US11782344B2 (en) 2015-04-21 2023-10-10 Fujifilm Electronic Materials U.S.A., Inc. Photosensitive polyimide compositions
US11899364B2 (en) 2015-04-21 2024-02-13 Fujifilm Electronic Materials U.S.A., Inc. Photosensitive polyimide compositions

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